Fused tricyclic KRAS inhibitors
Patent Information
- Application Number
- JP2025165118
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2021-02-08
- Filing Date
- 2025-10-01
- Publication Date
- 2026-03-02
AI Technical Summary
KRAS mutations are prevalent in various cancers, particularly pancreatic, colorectal, and lung cancers, and current treatments lack effective inhibitors to target mutant KRAS, which is crucial for cancer cell growth and survival.
Development of compounds that modulate KRAS activity, including specific inhibitors to inhibit KRAS activity in cancer cells, administered as pharmaceutical compositions.
The compounds effectively inhibit KRAS activity, providing a therapeutic approach for treating diseases characterized by KRAS mutations, such as pancreatic, colorectal, and lung cancers.
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Abstract
Description
[Technical Field]
[0001] Related Applications This application is related to U.S. Provisional Patent Application No. 63 / 011,089, filed April 16, 2020, and U.S. Provisional Patent Application No. 63 / 146,899, filed February 8, 2021, the contents of each of which are incorporated by reference in their entirety.
[0002] The present disclosure provides compounds, as well as compositions and methods of use thereof, that modulate KRAS activity and are useful in the treatment of various diseases, including cancer. [Background technology]
[0003] Ras proteins are part of a family of small GTPases that are activated by growth factors and various extracellular stimuli. The Ras family regulates intracellular signaling pathways that are involved in cell growth, migration, survival, and differentiation. When RAS proteins are activated at the cell membrane, key effectors bind and initiate a cascade of intracellular signaling pathways, including the RAF and PI3K kinase pathways. Somatic mutations in RAS can lead to uncontrolled cell growth and malignant transformation, while RAS protein activation is tightly regulated in normal cells (Simanshu, D. et al. Cell 170.1(2017):17-33).
[0004] The Ras family consists of three members: KRAS, NRAS, and HRAS. RAS-mutated cancers account for approximately 25% of human cancers. KRAS is the most commonly mutated isoform, accounting for 85% of all RAS mutations, while NRAS and HRAS are mutated in 12% and 3% of all RAS-mutated cancers, respectively (Simanshu, D. et al. Cell 170.1 (2017): 17-33). KRAS mutations are prevalent in the top three most lethal types of cancer: pancreatic (97%), colorectal (44%), and lung (30%) (Cox, AD et al. Nat Rev Drug Discov (2014) 13:828-51). The majority of RAS mutations occur at amino acid residues 12, 13, and 61. The frequency of specific mutations varies between RAS gene isoforms, with G12 and Q61 mutations predominating in KRAS and NRAS, respectively, and G12, G13, and Q61 mutations occurring most frequently in HRAS. Furthermore, the spectrum of mutations in RAS isoforms differs between cancer types. For example, KRAS G12D mutations predominate in pancreatic cancer (51%), followed by colorectal adenocarcinoma (45%) and lung cancer (17%), while KRAS G12V mutations are associated with pancreatic cancer (30%), followed by colorectal adenocarcinoma (27%) and lung adenocarcinoma (23%) (Cox, AD et al. Nat Rev Drug Discov (2014) 13:828-51). In contrast, KRAS G12C mutations predominate in non-small cell lung cancer (NSCLC), accounting for 11-16% of lung adenocarcinomas and 11-16% of pancreatic adenocarcinomas. KRAS accounts for 2-5% of all cancers, including colorectal adenocarcinomas (Cox, AD et al. Nat. Rev. Drug Discov. (2014) 13:828-51). Genomic studies across hundreds of cancer cell lines have demonstrated that cancer cells containing KRAS mutations are highly dependent on KRAS function for cell growth and survival (McDonald, R. et al. Cell 170 (2017):577-592). The role of mutant KRAS as an oncogenic driver is further supported by extensive in vivo experimental evidence showing that mutant KRAS is required for the development and maintenance of initial tumors in animal models (Cox, AD et al. Nat. Rev. Drug Discov. (2014) 13:828-51).
[0005] Taken together, these findings suggest that KRAS mutations play an important role in human cancer; therefore, the development of inhibitors targeting mutant KRAS may be useful in the clinical treatment of diseases characterized by KRAS mutations. Summary of the Invention
[0006] The present disclosure relates, inter alia, to compounds of formula I: [ka] or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein.
[0007] The present disclosure further provides pharmaceutical compositions comprising a compound of the present disclosure, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.
[0008] The present disclosure further provides a method for inhibiting KRAS activity, comprising administering to an individual the compound of the present disclosure or its pharmaceutically acceptable salt.The present disclosure also provides the use of the compound described herein in the manufacture of a medicament for use in therapy.The present disclosure also provides the compound described herein for use in therapy.
[0009] The present disclosure further provides a method of treating a disease or disorder in a patient, comprising administering to the patient a therapeutically effective amount of a compound of the present disclosure, or a pharmaceutically acceptable salt thereof. DETAILED DESCRIPTION OF THE INVENTION
[0010] compound In one aspect, the present disclosure provides a compound of formula I: [ka] or a pharmaceutically acceptable salt thereof (In the formula, each [ka] independently represent a single bond or a double bond; X is N or CR 7 and; Y is N or C; R 1 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, CN, OR a1 , S.R. a1 , C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 ,OC(O)R b1 , OC(O)NR c1 R d1 , N.R. c1 R d1 , N.R. c1 C(O)R b1 , N.R. c1 C(O)OR a1 , N.R. c1 C(O)NR c1 R d1 , N.R. c1S(O)R b1 , N.R. c1 S(O)2R b1 , N.R. c1 S(O)NR c1 R d1 , S(O)R b1 , S(O)NR c1 R d1 , S(O)2R b1 , S(O)NR c1 R d1 , and B.R. h1 R i1 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a2 , S.R. a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 ,OC(O)R b2 , OC(O)NR c2 R d2 , N.R. c2 R d2 , N.R. c2 C(O)Rb2 , N.R. c2 C(O)OR a2 , N.R. c2 C(O)NR c2 R d2 , C(=NR e2 )R b2 , C(=NOR a2 )R b2 , C(=NR e2 )NR c2 R d2 , N.R. c2 C(=NR e2 )NR c2 R d2 , N.R. c2 C(=NR e2 )R b2 , N.R. c2 S(O)R b2 , N.R. c2 S(O)2R b2 , N.R. c2 S(O)NR c2 R d2 , S(O)R b2 , S(O)NR c2 R d2 , S(O)2R b2 , S(O)NR c2 R d2 , and B.R. h2 R i2 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 22 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 1 is C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and the 5-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 5-10 membered heteroaryl and the 4-10 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 10 substituted with 1, 2, 3, or 4 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR f3 , S.R. a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 ,OC(O)R b3 , OC(O)NR c3 R d3 , N.R. c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , N.R. c3C(O)NR c3 R d3 , C(=NR e3 )R b3 , C(=NOR a3 )R b3 , C(=NR e3 )NR c3 R d3 , N.R. c3 C(=NR e3 )NR c3 R d3 , N.R. c3 C(=NR e3 )R b3 , N.R. c3 S(O)R b3 , N.R. c3 S(O)2R b3 , N.R. c3 S(O)NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O)2R b3 , S(O)NR c3 R d3 , and B.R. h3 R i3 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 30 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a single bond and Y is C, then YR 6 is selected from C=O and C=S; R 4 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, halo, CN, OR a4 , S.R. a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 ,OC(O)R b4 , OC(O)NR c4 R d4 , N.R. c4 R d4 , N.R. c4 C(O)R b4 , N.R. c4 C(O)OR a4 , N.R. c4 C(O)NR c4 R d4 , N.R. c4 S(O)R b4 , N.R. c4 S(O)2R b4 , N.R. c4 S(O)NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O)2R b4 , S(O)NR c4 R d4 , and B.R. h4 R i4 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, 4- to 6-membered heterocycloalkyl, phenyl, and 5- to 6-membered heteroaryl are each optionally selected from R g substituted with 1, 2, 3, or 4 substituents independently selected from R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 ,OC(O)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , N.R. c5 C(O)NR c5 R d5 , C(=NR e5 )R b5 , C(=NOR a5 )R b5 , C(=NR e5 )NR c5 R d5 , N.R. c5 C(=NR e5 )NR c5 R d5 , N.R. c5 C(=NR e5 )R b5 , N.R. c5 S(O)R b5 , N.R. c5 S(O)2R b5 , N.R. c5 S(O)NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O)2Rb5 , S(O)NR c5 R d5 , and B.R. h5 R i5 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 50 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R 4 does not exist; R 6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3Alkylene, Halo, D, CN, NO2, OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 ,OC(O)R b6 , OC(O)NR c6 R d6 , N.R. c6 R d6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , C(=NR e6 )R b6 , C(=NOR a6 )R b6 , C(=NR e6 )NR c6 R d6 , N.R. c6 C(=NR e6 )NR c6 R d6 , N.R. c6 C(=NR e6 )R b6 , N.R. c6 S(O)R b6 , N.R. c6 S(O)2R b6 , N.R. c6 S(O)NR c6 R d6 , S(O)R b6 , S(O)NR c6 R d6 , S(O)2R b6 , S(O)NR c6 R d6 , and B.R. h6 R i6 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 60 substituted with 1, 2, 3, or 4 substituents independently selected from R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7 ,OC(O)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , C(=NR e7 )R b7 , C(=NOR a7 )R b7 , C(=NR e7 )NR c7 R d7 , N.R. c7 C(=NR e7 )NR c7 Rd7 , N.R. c7 C(=NR e7 )R b7 , N.R. c7 S(O)R b7 , N.R. c7 S(O)2R b7 , N.R. c7 S(O)NR c7 R d7 , S(O)R b7 , S(O)NR c7 R d7 , S(O)2R b7 , S(O)NR c7 R d7 , and B.R. h7 R i7 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 70 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 2 is C 3~10 Cycloalkyl, 4-14 membered heterocycloalkyl, C 6~10 aryl, and 5-10 membered heteroaryl, wherein the 4-14 membered heterocycloalkyl and the 5-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 5-10 membered heteroaryl and the 4-14 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10Cycloalkyl, 4-14 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 20 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a10 , S.R. a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 ,OC(O)R b10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R. c10 C(O)R b10 , N.R. c10 C(O)OR a10 , N.R. c10 C(O)NR c10 R d10 , C(=NR e10 )R b10 , C(=NOR a10 )R b10 , C(=NR e10 )NR c10 R d10 , N.R. c10 C(=NR e10 )NR c10 R d10 , N.R. c10 S(O)R b10 , N.R. c10S(O)2R b10 , N.R. c10 S(O)NR c10 R d10 , S(O)R b10 , S(O)NR c10 R d10 , S(O)2R b10 , S(O)NR c10 R d10 , and B.R. h10 R i10 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 11 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 11 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a11 , S.R. a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)ORa11 ,OC(O)R b11 , OC(O)NR c11 R d11 , N.R. c11 R d11 , N.R. c11 C(O)R b11 , N.R. c11 C(O)OR a11 , N.R. c11 C(O)NR c11 R d11 , N.R. c11 S(O)R b11 , N.R. c11 S(O)2R b11 , N.R. c11 S(O)NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O)2R b11 , S(O)NR c11 R d11 , and B.R. h11 R i11 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 12 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 12 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a12 , S.R. a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 ,OC(O)R b12 , OC(O)NR c12 R d12 , N.R. c12 R d12 , N.R. c12 C(O)R b12 , N.R. c12 C(O)OR a12 , N.R. c12 C(O)NR c12 R d12 , N.R. c12 S(O)R b12 , N.R. c12 S(O)2R b12 , N.R. c12 S(O)NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 , S(O)2R b12 , S(O)NR c12 R d12 , and B.R. h12 R i12 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a20 , S.R. a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 ,OC(O)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , C(=NR e20 )R b20 , C(=NOR a20 )R b20 , C(=NR e20 )NR c20 R d20 , N.R. c20 C(=NR e20 )NR c20 R d20 , N.R. c20 S(O)R b20 , N.R. c20 S(O)2R b20 , N.R. c20 S(O)NR c20 R d20 , S(O)R b20 , S(O)NR c20 R d20 , S(O)2R b20 , S(O)NR c20 R d20 , and B.R. h20 R i20 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 21 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 21 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a21 , S.R. a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , N.R. c21 R d21 , N.R. c21 C(O)R b21 , N.R. c21 C(O)OR a21 , N.R. c21 C(O)NR c21 R d21 , N.R. c21 S(O)R b21 , N.R. c21 S(O)2R b21 , N.R. c21S(O)NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 , S(O)2R b21 , S(O)NR c21 R d21 , and B.R. h21 R i21 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 22 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a22 , S.R. a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 ,OC(O)R b22, OC(O)NR c22 R d22 , N.R. c22 R d22 , N.R. c22 C(O)R b22 , N.R. c22 C(O)OR a22 , N.R. c22 C(O)NR c22 R d22 , N.R. c22 S(O)R b22 , N.R. c22 S(O)2R b22 , N.R. c22 S(O)NR c22 R d22 , S(O)R b22 , S(O)NR c22 R d22 , S(O)2R b22 , S(O)NR c22 R d22 , and B.R. h22 R i22 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 23 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 23 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a23 , S.R. a23 , C(O)R b23 , C(O)NR c23 R d23 , C(O)OR a23 ,OC(O)R b23 , OC(O)NR c23 R d23 , N.R. c23 R d23 , N.R. c23 C(O)R b23 , N.R. c23 C(O)OR a23 , N.R. c23 C(O)NR c23 R d23 , N.R. c23 S(O)R b23 , N.R. c23 S(O)2R b23 , N.R. c23 S(O)NR c23 R d23 , S(O)R b23 , S(O)NR c23 R d23 , S(O)2R b23 , S(O)NR c23 R d23 , and B.R. h23 R i23 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C1~3 Each alkylene is optionally represented by R 24 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 24 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a24 , S.R. a24 , C(O)R b24 , C(O)NR c24 R d24 , C(O)OR a24 ,OC(O)R b24 , OC(O)NR c24 R d24 , N.R. c24 R d24 , N.R. c24 C(O)R b24 , N.R. c24 C(O)OR a24 , N.R. c24 C(O)NR c24 R d24 , N.R. c24 S(O)R b24 , N.R. c24 S(O)2R b24 , N.R. c24 S(O)NR c24 R d24 , S(O)R b24 , S(O)NR c24 R d24 , S(O)2R b24 , S(O)NR c24 R d24 , and B.R. h24 R i24 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 30 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a30 , S.R. a30 , C(O)R b30 , C(O)NR c30 R d30 , C(O)OR a30 ,OC(O)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , N.R. c30 C(O)NR c30 R d30 , N.R. c30 S(O)R b30 , N.R. c30 S(O)2R b30 , N.R. c30 S(O)NR c30 R d30 , S(O)R b30 , S(O)NR c30 R d30 , S(O)2R b30 , S(O)NR c30 R d30 , and B.R. h30 R i30 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 31 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a31 , S.R. a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , N.R. c31 R d31 , N.R. c31 C(O)R b31 , N.R. c31 C(O)OR a31 , N.R. c31 C(O)NR c31 R d31 , N.R. c31 S(O)R b31 , N.R. c31 S(O)2R b31 , N.R. c31S(O)NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 , S(O)2R b31 , S(O)NR c31 R d31 , and B.R. h31 R i31 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 32 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 32 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a32 , S.R. a32 , C(O)R b32 , C(O)NR c32 R d32 , C(O)OR a32 ,OC(O)R b32 , OC(O)NR c32 R d32 , N.R. c32 R d32 , N.R. c32 C(O)R b32 , N.R. c32 C(O)OR a32 , N.R. c32 C(O)NR c32 Rd32 , N.R. c32 S(O)R b32 , N.R. c32 S(O)2R b32 , N.R. c32 S(O)NR c32 R d32 , S(O)R b32 , S(O)NR c32 R d32 , S(O)2R b32 , S(O)NR c32 R d32 , and B.R. h32 R i32 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 50 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a50 , S.R. a50 , C(O)R b50 , C(O)NR c50 R d50 , C(O)OR a50 ,OC(O)R b50 , OC(O)NR c50 R d50 , N.R. c50 R d50 , N.R.c50 C(O)R b50 , N.R. c50 C(O)OR a50 , N.R. c50 C(O)NR c50 R d50 , N.R. c50 S(O)R b50 , N.R. c50 S(O)2R b50 , N.R. c50 S(O)NR c50 R d50 , S(O)R b50 , S(O)NR c50 R d50 , S(O)2R b50 , S(O)NR c50 R d50 , and B.R. h50 R i50 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 51 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 51 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 6~10 Aryl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a51 , S.R. a51 , C(O)R b51 , C(O)NR c51 R d51, C(O)OR a51 ,OC(O)R b51 , OC(O)NR c51 R d51 , N.R. c51 R d51 , N.R. c51 C(O)R b51 , N.R. c51 C(O)OR a51 , N.R. c51 C(O)NR c51 R d51 , N.R. c51 S(O)R b51 , N.R. c51 S(O)2R b51 , N.R. c51 S(O)NR c51 R d51 , S(O)R b51 , S(O)NR c51 R d51 , S(O)2R b51 , S(O)NR c51 R d51 , and B.R. h51 R i51 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, C 6~10 The aryl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 52 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 52 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a52 , S.R. a52 , C(O)R b52 , C(O)NR c52 R d52 , C(O)OR a52 ,OC(O)R b52 , OC(O)NR c52R d52 , N.R. c52 R d52 , N.R. c52 C(O)R b52 , N.R. c52 C(O)OR a52 , N.R. c52 C(O)NR c52 R d52 , N.R. c52 S(O)R b52 , N.R. c52 S(O)2R b52 , N.R. c52 S(O)NR c52 R d52 , S(O)R b52 , S(O)NR c52 R d52 , S(O)2R b52 , S(O)NR c52 R d52 , and B.R. h52 R i52 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 60 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a60 , S.R. a60 , C(O)Rb60 , C(O)NR c60 R d60 , C(O)OR a60 ,OC(O)R b60 , OC(O)NR c60 R d60 , N.R. c60 R d60 , N.R. c60 C(O)R b60 , N.R. c60 C(O)OR a60 , N.R. c60 C(O)NR c60 R d60 , N.R. c60 S(O)R b60 , N.R. c60 S(O)2R b60 , N.R. c60 S(O)NR c60 R d60 , S(O)R b60 , S(O)NR c60 R d60 , S(O)2R b60 , S(O)NR c60 R d60 , and B.R. h60 R i60 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 70 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a70 , S.R. a70 , C(O)R b70 , C(O)NR c70 R d70 , C(O)OR a70 ,OC(O)R b70 , OC(O)NR c70 R d70 , N.R. c70 R d70 , N.R. c70 C(O)R b70 , N.R. c70 C(O)OR a70 , N.R. c70 C(O)NR c70 R d70 , N.R. c70 S(O)R b70 , N.R. c70 S(O)2R b70 , N.R. c70 S(O)NR c70 R d70 , S(O)R b70 , S(O)NR c70 R d70 , S(O)2R b70 , S(O)NR c70 R d70 , and B.R. h70 R i70 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 71 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 71 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a71 , S.R. a71 , C(O)R b71 , C(O)NR c71 R d71 , C(O)OR a71 ,OC(O)R b71 , OC(O)NR c71 R d71 , N.R. c71 R d71 , N.R. c71 C(O)R b71 , N.R. c71 C(O)OR a71 , N.R. c71 C(O)NR c71 R d71 , N.R. c71 S(O)R b71 , N.R. c71 S(O)2R b71 , N.R. c71 S(O)NR c71 R d71 , S(O)R b71 , S(O)NR c71 R d71, S(O)2R b71 , S(O)NR c71 R d71 , and B.R. h71 R i71 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 72 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 72 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a72 , S.R. a72 , C(O)R b72 , C(O)NR c72 R d72 , C(O)OR a72 ,OC(O)R b72 , OC(O)NR c72 R d72 , N.R. c72 R d72 , N.R. c72 C(O)R b72 , N.R. c72 C(O)OR a72 , N.R. c72 C(O)NR c72 R d72 , N.R. c72 S(O)R b72 , N.R. c72 S(O)2R b72 , N.R.c72 S(O)NR c72 R d72 , S(O)R b72 , S(O)NR c72 R d72 , S(O)2R b72 , S(O)NR c72 R d72 , and B.R. h72 R i72 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R a1 , R b1 , R c1 , and R d1 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c1 and R d1 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: Rh1 and R i1 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h1 and R i1 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a2 , R b2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 22 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c2 and R d2 together with the N atom to which they are attached, R 22 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e2 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h2 and R i2 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h2 and R i2 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e3 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R f3 and R j3 are respectively, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h3 and R i3 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h3 and R i3 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a4 , R b4 , R c4 , and R d4 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c4 and R d4 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h4 and R i4are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h4 and R i4 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a5 , R b5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e5 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h5 and R i5 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h5 and R i5 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a6 , R b6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 60 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c6 and R d6together with the N atom to which they are attached, R 60 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e6 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h6 and R i6 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h6 and R i6 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a7 , R b7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 70 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c7 and R d7 together with the N atom to which they are attached, R 70 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e7 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h7 and R i7 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h7 and R i7 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a10, R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 11 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c10 and R d10 together with the N atom to which they are attached, R 11 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e10 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h10 and R i10 are OH and C, respectively. 1~6Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h10 and R i10 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a11 , R b11 , R c11 , and R d11 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 12 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c11 and R d11 together with the N atom to which they are attached, R 12 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h11 and R i11 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h11 and R i11 together with the B atoms to which they are bonded, 1~6 Alkyl and C1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a12 , R b12 , R c12 , and R d12 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h12 and R i12 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h12 and R i12 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 21 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c20 and R d20 together with the N atom to which they are attached, R 21 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e20 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h20 and R i20 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h20 and R i20 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a21 , R b21 , R c21 , and R d21 are H and C, respectively.1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c21 and R d21 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h21 and R i21 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h21 and R i21 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a22 , R b22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 23 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c22 and R d22 together with the N atom to which they are attached, R 23 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h22 and R i22 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h22 and R i22 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a23 , R b23 , R c23 , and R d23 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 24 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c23 and R d23 together with the N atom to which they are attached, R 24 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h23 and R i23 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h23 and R i23 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a24 , R b24 , R c24 , and R d24 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h24 and R i24 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h24 and Ri24 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h30 and R i30 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h30 and R i30 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 32 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c31 and R d31 together with the N atom to which they are attached, R 32 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h31 and R i31 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h31 and R i31 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a32 , R b32 , R c32 , and R d32are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h32 and R i32 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h32 and R i32 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a50 , R b50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 51 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c50 and Rd50 together with the N atom to which they are attached, R 51 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h50 and R i50 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h50 and R i50 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a51 , R b51 , R c51 , and R d51 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 52 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c51 and R d51 together with the N atom to which they are attached, R 52 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h51and R i51 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h51 and R i51 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a52 , R b52 , R c52 , and R d52 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h52 and R i52 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h52 and R i52 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c60 and R d60 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h60 and R i60 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h60 and R i60 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a70 , R b70 , R c70 , and R d70 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 71 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c70 and R d70 together with the N atom to which they are attached, R 71 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h70 and R i70 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h70 and R i70 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a71 , R b71 , R c71 , and R d71 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 72or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c71 and R d71 together with the N atom to which they are attached, R 72 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h71 and R i71 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h71 and R i71 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a72 , R b72 , R c72 , and R d72 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h72 and R i72 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h72 and R i72 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; Each R g D, OH, NO2, CN, halo, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 3~6 Cycloalkyl-C 1~2 Alkylene, C 1~6 Alkoxy, C 1~6 Haloalkoxy, C 1~3 Alkoxy-C 1~3 Alkyl, C 1~3 Alkoxy-C 1~3 Alkoxy, HO-C 1~3 Alkoxy, HO-C 1~3 Alkyl, Cyano-C 1~3 Alkyl, H2N-C 1~3 Alkyl, Amino, C 1~6 Alkylamino, di(C 1~6 Alkyl)amino, thio, C 1~6 Alkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkyl sulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl) carbamyl, carboxy, C 1~6 Alkyl carbonyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkylcarbonylamino, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonyloxy, aminocarbonyloxy, C 1~6 Alkylaminocarbonyloxy, di(C 1~6 alkyl)aminocarbonyloxy, C 1~6 Alkyl sulfonyl amino, amino sulfonyl, C 1~6 Alkylaminosulfonyl, di(C 1~6 Alkyl)aminosulfonyl, aminosulfonylamino, C 1~6 Alkylaminosulfonylamino, di(C1~6 Alkyl)aminosulfonylamino, aminocarbonylamino, C 1~6 Alkylaminocarbonylamino, and di(C 1~6 alkyl)aminocarbonylamino; however, [ka] is a double bond and Y is N, Cy 1 is other than 3,5-dimethylisoxazol-4-yl).
[0011] In another aspect, the present disclosure provides a compound of formula I: [ka] or a pharmaceutically acceptable salt thereof (In the formula, each [ka] independently represent a single bond or a double bond; X is N or CR 7 and; Y is N or C; R 1 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, CN, OR a1 , S.R. a1 , C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 ,OC(O)R b1 , OC(O)NR c1 R d1 , N.R. c1 R d1 , N.R. c1 C(O)Rb1 , N.R. c1 C(O)OR a1 , N.R. c1 C(O)NR c1 R d1 , N.R. c1 S(O)R b1 , N.R. c1 S(O)2R b1 , N.R. c1 S(O)NR c1 R d1 , S(O)R b1 , S(O)NR c1 R d1 , S(O)2R b1 , S(O)NR c1 R d1 , and B.R. h1 R i1 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a2 , S.R. a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)ORa2 ,OC(O)R b2 , OC(O)NR c2 R d2 , N.R. c2 R d2 , N.R. c2 C(O)R b2 , N.R. c2 C(O)OR a2 , N.R. c2 C(O)NR c2 R d2 , C(=NR e2 )R b2 , C(=NOR a2 )R b2 , C(=NR e2 )NR c2 R d2 , N.R. c2 C(=NR e2 )NR c2 R d2 , N.R. c2 C(=NR e2 )R b2 , N.R. c2 S(O)R b2 , N.R. c2 S(O)2R b2 , N.R. c2 S(O)NR c2 R d2 , S(O)R b2 , S(O)NR c2 R d2 , S(O)2R b2 , S(O)NR c2 R d2 , and B.R. h2 R i2 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3Each alkylene is optionally represented by R 22 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 1 is C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and the 5-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 5-10 membered heteroaryl and the 4-10 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 10 substituted with 1, 2, 3, or 4 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR f3 , S.R. a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 ,OC(O)R b3 , OC(O)NR c3 R d3 , N.R.c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , N.R. c3 C(O)NR c3 R d3 , C(=NR e3 )R b3 , C(=NOR a3 )R b3 , C(=NR e3 )NR c3 R d3 , N.R. c3 C(=NR e3 )NR c3 R d3 , N.R. c3 C(=NR e3 )R b3 , N.R. c3 S(O)R b3 , N.R. c3 S(O)2R b3 , N.R. c3 S(O)NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O)2R b3 , S(O)NR c3 R d3 , and B.R. h3 R i3 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 30 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a single bond and Y is C, then YR 6 is selected from C=O and C=S; R 4 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, halo, CN, OR a4 , S.R. a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 ,OC(O)R b4 , OC(O)NR c4 R d4 , N.R. c4 R d4 , N.R. c4 C(O)R b4 , N.R. c4 C(O)OR a4 , N.R. c4 C(O)NR c4 R d4 , N.R. c4 S(O)R b4 , N.R. c4 S(O)2R b4 , N.R. c4 S(O)NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O)2R b4 , S(O)NR c4 R d4 , and B.R. h4 R i4 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, 4- to 6-membered heterocycloalkyl, phenyl, and 5- to 6-membered heteroaryl are each optionally selected from R gsubstituted with 1, 2, 3, or 4 substituents independently selected from R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 ,OC(O)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , N.R. c5 C(O)NR c5 R d5 , C(=NR e5 )R b5 , C(=NOR a5 )R b5 , C(=NR e5 )NR c5 R d5 , N.R. c5 C(=NR e5 )NR c5 R d5 , N.R. c5 C(=NR e5 )R b5 , N.R. c5 S(O)R b5 , N.R. c5 S(O)2R b5 , N.R. c5S(O)NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O)2R b5 , S(O)NR c5 R d5 , and B.R. h5 R i5 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 50 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R 4 does not exist; R 6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 ,OC(O)R b6 , OC(O)NR c6 R d6 , N.R. c6 R d6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , C(=NR e6 )R b6 , C(=NOR a6 )R b6 , C(=NR e6 )NR c6 R d6 , N.R. c6 C(=NR e6 )NR c6 R d6 , N.R. c6 C(=NR e6 )R b6 , N.R. c6 S(O)R b6 , N.R. c6 S(O)2R b6 , N.R. c6 S(O)NR c6 R d6 , S(O)R b6 , S(O)NR c6 R d6 , S(O)2R b6 , S(O)NR c6 R d6 , and B.R. h6 R i6 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 60 substituted with 1, 2, 3, or 4 substituents independently selected from R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7 ,OC(O)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , C(=NR e7 )R b7 , C(=NOR a7 )R b7 , C(=NRe7 )NR c7 R d7 , N.R. c7 C(=NR e7 )NR c7 R d7 , N.R. c7 C(=NR e7 )R b7 , N.R. c7 S(O)R b7 , N.R. c7 S(O)2R b7 , N.R. c7 S(O)NR c7 R d7 , S(O)R b7 , S(O)NR c7 R d7 , S(O)2R b7 , S(O)NR c7 R d7 , and B.R. h7 R i7 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 70 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 2 is C 3~10 Cycloalkyl, 4-14 membered heterocycloalkyl, C 6~10aryl, and 5-10 membered heteroaryl, wherein the 4-14 membered heterocycloalkyl and the 5-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 5-10 membered heteroaryl and the 4-14 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10 Cycloalkyl, 4-14 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 20 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a10 , S.R. a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 ,OC(O)R b10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R. c10 C(O)R b10 , N.R. c10 C(O)OR a10 , N.R. c10 C(O)NR c10 R d10 , C(=NRe10 )R b10 , C(=NOR a10 )R b10 , C(=NR e10 )NR c10 R d10 , N.R. c10 C(=NR e10 )NR c10 R d10 , N.R. c10 S(O)R b10 , N.R. c10 S(O)2R b10 , N.R. c10 S(O)NR c10 R d10 , S(O)R b10 , S(O)NR c10 R d10 , S(O)2R b10 , S(O)NR c10 R d10 , and B.R. h10 R i10 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 11 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 11 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a11 , S.R. a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , N.R. c11 R d11 , N.R. c11 C(O)R b11 , N.R. c11 C(O)OR a11 , N.R. c11 C(O)NR c11 R d11 , N.R. c11 S(O)R b11 , N.R. c11 S(O)2R b11 , N.R. c11 S(O)NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O)2R b11 , S(O)NR c11 R d11 , and B.R. h11 R i11 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3Each alkylene is optionally represented by R 12 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 12 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a12 , S.R. a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 ,OC(O)R b12 , OC(O)NR c12 R d12 , N.R. c12 R d12 , N.R. c12 C(O)R b12 , N.R. c12 C(O)OR a12 , N.R. c12 C(O)NR c12 R d12 , N.R. c12 S(O)R b12 , N.R. c12 S(O)2R b12 , N.R. c12 S(O)NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 , S(O)2R b12 , S(O)NR c12 R d12 , and B.R. h12 R i12 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a20 , S.R. a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 ,OC(O)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , C(=NR e20 )R b20 , C(=NOR a20 )R b20 , C(=NR e20 )NR c20 R d20 , N.R. c20 C(=NR e20 )NR c20 R d20 , N.R. c20 S(O)R b20 , N.R. c20 S(O)2R b20 , N.R. c20 S(O)NR c20 R d20 , S(O)R b20 , S(O)NR c20 R d20 , S(O)2Rb20 , S(O)NR c20 R d20 , and B.R. h20 R i20 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 21 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 21 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a21 , S.R. a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , N.R. c21 R d21 , N.R. c21 C(O)R b21 , N.R.c21 C(O)OR a21 , N.R. c21 C(O)NR c21 R d21 , N.R. c21 S(O)R b21 , N.R. c21 S(O)2R b21 , N.R. c21 S(O)NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 , S(O)2R b21 , S(O)NR c21 R d21 , and B.R. h21 R i21 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 22 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a22 , S.R. a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 ,OC(O)R b22 , OC(O)NR c22 R d22 , N.R. c22 R d22 , N.R. c22 C(O)R b22 , N.R. c22 C(O)OR a22 , N.R. c22 C(O)NR c22 R d22 , N.R. c22 S(O)R b22 , N.R. c22 S(O)2R b22 , N.R. c22 S(O)NR c22 R d22 , S(O)R b22 , S(O)NR c22 R d22 , S(O)2R b22 , S(O)NR c22 R d22 , and B.R. h22 R i22 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 23 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 23is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a23 , S.R. a23 , C(O)R b23 , C(O)NR c23 R d23 , C(O)OR a23 ,OC(O)R b23 , OC(O)NR c23 R d23 , N.R. c23 R d23 , N.R. c23 C(O)R b23 , N.R. c23 C(O)OR a23 , N.R. c23 C(O)NR c23 R d23 , N.R. c23 S(O)R b23 , N.R. c23 S(O)2R b23 , N.R. c23 S(O)NR c23 R d23 , S(O)R b23 , S(O)NR c23 R d23 , S(O)2R b23 , S(O)NR c23 R d23 , and B.R. h23 R i23 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 24 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 24 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a24 , S.R. a24 , C(O)R b24 , C(O)NR c24 R d24 , C(O)OR a24 ,OC(O)R b24 , OC(O)NR c24 R d24 , N.R. c24 R d24 , N.R. c24 C(O)R b24 , N.R. c24 C(O)OR a24 , N.R. c24 C(O)NR c24 R d24 , N.R. c24 S(O)R b24 , N.R. c24 S(O)2R b24 , N.R. c24 S(O)NR c24 R d24 , S(O)R b24 , S(O)NR c24 R d24 , S(O)2R b24 , S(O)NR c24 R d24 , and B.R. h24 R i24 C1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 30 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a30 , S.R. a30 , C(O)R b30 , C(O)NR c30 R d30 , C(O)OR a30 ,OC(O)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , N.R. c30 C(O)NR c30 R d30 , N.R. c30 S(O)R b30 , N.R. c30 S(O)2R b30 , N.R. c30 S(O)NR c30 R d30 , S(O)R b30 , S(O)NR c30 R d30, S(O)2R b30 , S(O)NR c30 R d30 , and B.R. h30 R i30 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 31 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a31 , S.R. a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , N.R. c31 R d31 , N.R. c31 C(O)Rb31 , N.R. c31 C(O)OR a31 , N.R. c31 C(O)NR c31 R d31 , N.R. c31 S(O)R b31 , N.R. c31 S(O)2R b31 , N.R. c31 S(O)NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 , S(O)2R b31 , S(O)NR c31 R d31 , and B.R. h31 R i31 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 32 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 32 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a32 , S.R. a32 , C(O)R b32 , C(O)NR c32 R d32 , C(O)OR a32 ,OC(O)Rb32 , OC(O)NR c32 R d32 , N.R. c32 R d32 , N.R. c32 C(O)R b32 , N.R. c32 C(O)OR a32 , N.R. c32 C(O)NR c32 R d32 , N.R. c32 S(O)R b32 , N.R. c32 S(O)2R b32 , N.R. c32 S(O)NR c32 R d32 , S(O)R b32 , S(O)NR c32 R d32 , S(O)2R b32 , S(O)NR c32 R d32 , and B.R. h32 R i32 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 50 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a50 , S.R.a50 , C(O)R b50 , C(O)NR c50 R d50 , C(O)OR a50 ,OC(O)R b50 , OC(O)NR c50 R d50 , N.R. c50 R d50 , N.R. c50 C(O)R b50 , N.R. c50 C(O)OR a50 , N.R. c50 C(O)NR c50 R d50 , N.R. c50 S(O)R b50 , N.R. c50 S(O)2R b50 , N.R. c50 S(O)NR c50 R d50 , S(O)R b50 , S(O)NR c50 R d50 , S(O)2R b50 , S(O)NR c50 R d50 , and B.R. h50 R i50 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 51 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 51 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C1~6 Haloalkyl, C 3~6 Cycloalkyl, C 6~10 Aryl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a51 , S.R. a51 , C(O)R b51 , C(O)NR c51 R d51 , C(O)OR a51 ,OC(O)R b51 , OC(O)NR c51 R d51 , N.R. c51 R d51 , N.R. c51 C(O)R b51 , N.R. c51 C(O)OR a51 , N.R. c51 C(O)NR c51 R d51 , N.R. c51 S(O)R b51 , N.R. c51 S(O)2R b51 , N.R. c51 S(O)NR c51 R d51 , S(O)R b51 , S(O)NR c51 R d51 , S(O)2R b51 , S(O)NR c51 R d51 , and B.R. h51 R i51 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, C 6~10 The aryl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 52 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 52 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a52 , S.R. a52 , C(O)R b52 , C(O)NR c52 R d52 , C(O)OR a52 ,OC(O)R b52 , OC(O)NR c52 R d52 , N.R. c52 R d52 , N.R. c52 C(O)R b52 , N.R. c52 C(O)OR a52 , N.R. c52 C(O)NR c52 R d52 , N.R. c52 S(O)R b52 , N.R. c52 S(O)2R b52 , N.R. c52 S(O)NR c52 R d52 , S(O)R b52 , S(O)NR c52 R d52 , S(O)2R b52 , S(O)NR c52 R d52 , and B.R. h52 R i52 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 60 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a60 , S.R. a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 ,OC(O)R b60 , OC(O)NR c60 R d60 , N.R. c60 R d60 , N.R. c60 C(O)R b60 , N.R. c60 C(O)OR a60 , N.R. c60 C(O)NR c60 R d60 , N.R. c60 S(O)R b60 , N.R. c60 S(O)2R b60 , N.R. c60 S(O)NR c60 R d60 , S(O)R b60 , S(O)NR c60 R d60 , S(O)2R b60 , S(O)NR c60 R d60 , and B.R. h60 R i60 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C1~3 Each alkylene is optionally represented by R 61 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 61 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a61 , S.R. a61 , C(O)R b61 , C(O)NR c61 R d61 , C(O)OR a61 ,OC(O)R b61 , OC(O)NR c61 R d61 , N.R. c61 R d61 , N.R. c61 C(O)R b61 , N.R. c61 C(O)OR a61 , N.R. c61 C(O)NR c61 R d61 , N.R. c61 S(O)R b61 , N.R. c61 S(O)2R b61 , N.R. c61 S(O)NR c61 R d61 , S(O)R b61 , S(O)NR c61 R d61 , S(O)2R b61 , S(O)NR c61 R d61 , and B.R. h61 R i61 C1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 62 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 62 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a62 , S.R. a62 , C(O)R b62 , C(O)NR c62 R d62 , C(O)OR a62 ,OC(O)R b62 , OC(O)NR c62 R d62 , N.R. c62 R d62 , N.R. c62 C(O)R b62 , N.R. c62 C(O)OR a62 , N.R. c62 C(O)NR c62 R d62 , N.R. c62 S(O)R b62 , N.R. c62 S(O)2R b62 , N.R. c62 S(O)NR c62 R d62 , S(O)R b62 , S(O)NR c62 R d62 , S(O)2Rb62 , S(O)NR c62 R d62 , and B.R. h62 R i62 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 70 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a70 , S.R. a70 , C(O)R b70 , C(O)NR c70 R d70 , C(O)OR a70 ,OC(O)R b70 , OC(O)NR c70 R d70 , N.R. c70 R d70 , N.R. c70 C(O)R b70 , N.R. c70 C(O)OR a70 , N.R. c70 C(O)NR c70 R d70 , N.R. c70 S(O)R b70 , N.R. c70 S(O)2R b70 , N.R. c70S(O)NR c70 R d70 , S(O)R b70 , S(O)NR c70 R d70 , S(O)2R b70 , S(O)NR c70 R d70 , and B.R. h70 R i70 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 71 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 71 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a71 , S.R. a71 , C(O)R b71 , C(O)NR c71 R d71 , C(O)OR a71 ,OC(O)R b71, OC(O)NR c71 R d71 , N.R. c71 R d71 , N.R. c71 C(O)R b71 , N.R. c71 C(O)OR a71 , N.R. c71 C(O)NR c71 R d71 , N.R. c71 S(O)R b71 , N.R. c71 S(O)2R b71 , N.R. c71 S(O)NR c71 R d71 , S(O)R b71 , S(O)NR c71 R d71 , S(O)2R b71 , S(O)NR c71 R d71 , and B.R. h71 R i71 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 72 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 72 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a72 , S.R. a72, C(O)R b72 , C(O)NR c72 R d72 , C(O)OR a72 ,OC(O)R b72 , OC(O)NR c72 R d72 , N.R. c72 R d72 , N.R. c72 C(O)R b72 , N.R. c72 C(O)OR a72 , N.R. c72 C(O)NR c72 R d72 , N.R. c72 S(O)R b72 , N.R. c72 S(O)2R b72 , N.R. c72 S(O)NR c72 R d72 , S(O)R b72 , S(O)NR c72 R d72 , S(O)2R b72 , S(O)NR c72 R d72 , and B.R. h72 R i72 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R a1 , R b1 , R c1 , and R d1 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c1 and R d1 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h1 and R i1 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h1 and R i1 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a2 , R b2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 22 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c2 and R d2 together with the N atom to which they are attached, R 22 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e2 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h2 and R i2 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h2 and R i2 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e3 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R f3 and R j3 are respectively, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h3 and R i3 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h3 and R i3 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a4 , R b4 , R c4 , and R d4 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c4 and R d4 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h4 and R i4 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h4 and R i4 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a5 , R b5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e5 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h5 and R i5 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h5 and R i5 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a6 , R b6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 60 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e6 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h6 and R i6 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h6 and R i6 together with the B atoms to which they are bonded, 1~6 Alkyl and C1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a7 , R b7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 70 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c7 and R d7 together with the N atom to which they are attached, R 70 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e7 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C1~6 alkyl)aminosulfonyl; R h7 and R i7 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h7 and R i7 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 11 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c10 and R d10 together with the N atom to which they are attached, R 11 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e10 are H, CN, and C 1~6 Alkyl, C 2~6Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h10 and R i10 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h10 and R i10 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a11 , R b11 , R c11 , and R d11 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 12 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c11 and R d11 together with the N atom to which they are attached, R 12 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h11 and R i11 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h11 and R i11 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a12 , R b12 , R c12 , and R d12 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h12 and R i12 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h12 and R i12 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 21 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c20 and R d20 together with the N atom to which they are attached, R 21 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e20 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6alkyl)aminosulfonyl; R h20 and R i20 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h20 and R i20 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a21 , R b21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c21 and R d21 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h21 and R i21 are OH and C, respectively. 1~6 Alkoxy, and C 1~6haloalkoxy, or any R bonded to the same B atom h21 and R i21 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a22 , R b22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 23 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c22 and R d22 together with the N atom to which they are attached, R 23 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h22 and R i22 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h22 and R i22 together with the B atoms to which they are bonded, 1~6Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a23 , R b23 , R c23 , and R d23 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 24 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c23 and R d23 together with the N atom to which they are attached, R 24 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h23 and R i23 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h23 and R i23 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a24 , R b24 , R c24, and R d24 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h24 and R i24 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h24 and R i24 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atomc30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h30 and R i30 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h30 and R i30 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 32 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c31 and R d31 together with the N atom to which they are attached, R 32 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h31 and R i31 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h31 and R i31 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a32 , R b32 , R c32 , and R d32 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h32 and R i32 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h32 and R i32 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a50 , R b50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 51 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c50 and R d50 together with the N atom to which they are attached, R 51 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h50 and R i50 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h50 and R i50 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a51 , R b51 , R c51 , and R d51 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 52 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c51 and R d51 together with the N atom to which they are attached, R 52 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h51 and R i51 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h51 and R i51 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a52 , R b52 , R c52 , and R d52 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h52 and R i52 are OH and C, respectively. 1~6 Alkoxy, and C 1~6haloalkoxy, or any R bonded to the same B atom h52 and R i52 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 61 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c60 and R d60 together with the N atom to which they are attached, R 61 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h60 and R i60 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h60 and R i60 together with the B atoms to which they are bonded, 1~6Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a61 , R b61 , R c61 , and R d61 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 62 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c61 and R d61 together with the N atom to which they are attached, R 62 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h61 and R i61 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h61 and R i61 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a62 , R b62 , R c62, and R d62 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c62 and R d62 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h62 and R i62 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h62 and R i62 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a70 , R b70 , R c70 , and R d70 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 71 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c70 and R d70 together with the N atom to which they are attached, R 71 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h70 and R i70 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h70 and R i70 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a71 , R b71 , R c71 , and R d71 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 72 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c71 and R d71 together with the N atom to which they are attached, R 72 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h71 and R i71 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h71 and R i71 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a72 , R b72 , R c72 , and R d72 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R h72 and R i72 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h72 and R i72 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; Each R g D, OH, NO2, CN, halo, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 3~6 Cycloalkyl-C 1~2 Alkylene, C 1~6 Alkoxy, C 1~6 Haloalkoxy, C 1~3 Alkoxy-C 1~3 Alkyl, C 1~3 Alkoxy-C 1~3 Alkoxy, HO-C 1~3 Alkoxy, HO-C 1~3 Alkyl, Cyano-C 1~3 Alkyl, H2N-C 1~3 Alkyl, Amino, C 1~6 Alkylamino, di(C 1~6 Alkyl)amino, thio, C 1~6 Alkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkyl sulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl) carbamyl, carboxy, C 1~6 Alkyl carbonyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkylcarbonylamino, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonyloxy, aminocarbonyloxy, C 1~6 Alkylaminocarbonyloxy, di(C 1~6 alkyl)aminocarbonyloxy, C 1~6 Alkyl sulfonyl amino, amino sulfonyl, C 1~6 Alkylaminosulfonyl, di(C 1~6 Alkyl)aminosulfonyl, aminosulfonylamino, C 1~6 Alkylaminosulfonylamino, di(C1~6 Alkyl)aminosulfonylamino, aminocarbonylamino, C 1~6 Alkylaminocarbonylamino, and di(C 1~6 alkyl)aminocarbonylamino; however, [ka] is a double bond and Y is N, Cy 1 is other than 3,5-dimethylisoxazol-4-yl).
[0012] In one embodiment of Formula I or a pharmaceutically acceptable salt thereof, each [ka] independently represent a single bond or a double bond; X is N or CR 7 and; Y is N or C; R 1 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, CN, OR a1 , S.R. a1 , C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 ,OC(O)R b1 , OC(O)NR c1 R d1 , N.R. c1 R d1 , N.R. c1 C(O)R b1 , N.R. c1 C(O)OR a1 , N.R. c1 C(O)NR c1 R d1 , N.R.c1 S(O)R b1 , N.R. c1 S(O)2R b1 , N.R. c1 S(O)NR c1 R d1 , S(O)R b1 , S(O)NR c1 R d1 , S(O)2R b1 , S(O)NR c1 R d1 , and B.R. h1 R i1 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a2 , S.R. a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 ,OC(O)R b2 , OC(O)NR c2 R d2 , N.R. c2 R d2 , N.R.c2 C(O)R b2 , N.R. c2 C(O)OR a2 , N.R. c2 C(O)NR c2 R d2 , C(=NR e2 )R b2 , C(=NOR a2 )R b2 , C(=NR e2 )NR c2 R d2 , N.R. c2 C(=NR e2 )NR c2 R d2 , N.R. c2 C(=NR e2 )R b2 , N.R. c2 S(O)R b2 , N.R. c2 S(O)2R b2 , N.R. c2 S(O)NR c2 R d2 , S(O)R b2 , S(O)NR c2 R d2 , S(O)2R b2 , S(O)NR c2 R d2 , and B.R. h2 R i2 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 22 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 1 is C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 6-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and the 6-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 6-10 membered heteroaryl and the 4-10 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally represented by R 10 substituted with 1, 2, 3, or 4 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR f3 , S.R. a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 ,OC(O)R b3 , OC(O)NR c3 R d3 , N.R. c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , N.R. c3C(O)NR c3 R d3 , C(=NR e3 )R b3 , C(=NOR a3 )R b3 , C(=NR e3 )NR c3 R d3 , N.R. c3 C(=NR e3 )NR c3 R d3 , N.R. c3 C(=NR e3 )R b3 , N.R. c3 S(O)R b3 , N.R. c3 S(O)2R b3 , N.R. c3 S(O)NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O)2R b3 , S(O)NR c3 R d3 , and B.R. h3 R i3 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 30 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a single bond and Y is C, then YR 6 is selected from C=O and C=S; R 4 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, halo, CN, OR a4 , S.R. a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 ,OC(O)R b4 , OC(O)NR c4 R d4 , N.R. c4 R d4 , N.R. c4 C(O)R b4 , N.R. c4 C(O)OR a4 , N.R. c4 C(O)NR c4 R d4 , N.R. c4 S(O)R b4 , N.R. c4 S(O)2R b4 , N.R. c4 S(O)NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O)2R b4 , S(O)NR c4 R d4 , and B.R. h4 R i4 Selected from; R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 ,OC(O)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , N.R. c5 C(O)NR c5 R d5 , C(=NR e5 )R b5 , C(=NOR a5 )R b5 , C(=NR e5 )NR c5 R d5 , N.R. c5 C(=NR e5 )NR c5 R d5 , N.R. c5 C(=NR e5 )R b5 , N.R. c5 S(O)R b5 , N.R. c5 S(O)2R b5 , N.R. c5 S(O)NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O)2R b5 , S(O)NR c5 R d5 , and B.R. h5 R i5 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 50 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R 4 does not exist; R 6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 ,OC(O)R b6 , OC(O)NR c6 R d6 , N.R. c6 Rd6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , C(=NR e6 )R b6 , C(=NOR a6 )R b6 , C(=NR e6 )NR c6 R d6 , N.R. c6 C(=NR e6 )NR c6 R d6 , N.R. c6 C(=NR e6 )R b6 , N.R. c6 S(O)R b6 , N.R. c6 S(O)2R b6 , N.R. c6 S(O)NR c6 R d6 , S(O)R b6 , S(O)NR c6 R d6 , S(O)2R b6 , S(O)NR c6 R d6 , and B.R. h6 R i6 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 60 substituted with 1, 2, 3, or 4 substituents independently selected from R 7is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7 ,OC(O)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , C(=NR e7 )R b7 , C(=NOR a7 )R b7 , C(=NR e7 )NR c7 R d7 , N.R. c7 C(=NR e7 )NR c7 R d7 , N.R. c7 C(=NR e7 )R b7 , N.R. c7 S(O)R b7 , N.R. c7 S(O)2R b7 , N.R. c7 S(O)NR c7 R d7 , S(O)R b7, S(O)NR c7 R d7 , S(O)2R b7 , S(O)NR c7 R d7 , and B.R. h7 R i7 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 70 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 2 is C 3~10 Cycloalkyl, 4-14 membered heterocycloalkyl, C 6~10 aryl, and 5-10 membered heteroaryl, wherein the 4-14 membered heterocycloalkyl and the 5-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 5-10 membered heteroaryl and the 4-14 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10 Cycloalkyl, 4-14 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 20 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a10 , S.R. a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 ,OC(O)R b10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R. c10 C(O)R b10 , N.R. c10 C(O)OR a10 , N.R. c10 C(O)NR c10 R d10 , C(=NR e10 )R b10 , C(=NOR a10 )R b10 , C(=NR e10 )NR c10 R d10 , N.R. c10 C(=NR e10 )NR c10 R d10 , N.R. c10 S(O)R b10 , N.R. c10 S(O)2R b10 , N.R. c10 S(O)NR c10 R d10 , S(O)R b10 , S(O)NR c10 R d10 , S(O)2R b10 , S(O)NR c10 R d10 , and B.R. h10 R i10C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 11 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 11 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a11 , S.R. a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , N.R. c11 R d11 , N.R. c11 C(O)R b11 , N.R. c11 C(O)OR a11 , N.R. c11 C(O)NR c11 Rd11 , N.R. c11 S(O)R b11 , N.R. c11 S(O)2R b11 , N.R. c11 S(O)NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O)2R b11 , S(O)NR c11 R d11 , and B.R. h11 R i11 are independently selected from; Each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a20 , S.R. a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 ,OC(O)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , C(=NR e20 )R b20 , C(=NOR a20 )R b20, C(=NR e20 )NR c20 R d20 , N.R. c20 C(=NR e20 )NR c20 R d20 , N.R. c20 S(O)R b20 , N.R. c20 S(O)2R b20 , N.R. c20 S(O)NR c20 R d20 , S(O)R b20 , S(O)NR c20 R d20 , S(O)2R b20 , S(O)NR c20 R d20 , and B.R. h20 R i20 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 21 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 21 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a21 , S.R. a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , N.R. c21 R d21 , N.R. c21 C(O)R b21 , N.R. c21 C(O)OR a21 , N.R. c21 C(O)NR c21 R d21 , N.R. c21 S(O)R b21 , N.R. c21 S(O)2R b21 , N.R. c21 S(O)NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 , S(O)2R b21 , S(O)NR c21 R d21 , and B.R. h21 R i21 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from Each R 22 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a22 , S.R. a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 ,OC(O)R b22 , OC(O)NR c22 R d22 , N.R. c22 R d22 , N.R. c22 C(O)R b22 , N.R. c22 C(O)OR a22 , N.R. c22 C(O)NR c22 R d22 , N.R. c22 S(O)R b22 , N.R. c22 S(O)2R b22 , N.R. c22 S(O)NR c22 R d22 , S(O)R b22 , S(O)NR c22 R d22 , S(O)2R b22 , S(O)NR c22 R d22 , and B.R. h22 R i22 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 23 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 23 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a23 , S.R. a23 , C(O)R b23 , C(O)NR c23 R d23 , C(O)OR a23 ,OC(O)R b23 , OC(O)NR c23 R d23 , N.R. c23 R d23 , N.R. c23 C(O)R b23 , N.R. c23 C(O)OR a23 , N.R. c23 C(O)NR c23 R d23 , N.R. c23 S(O)R b23 , N.R. c23 S(O)2R b23 , N.R. c23S(O)NR c23 R d23 , S(O)R b23 , S(O)NR c23 R d23 , S(O)2R b23 , S(O)NR c23 R d23 , and B.R. h23 R i23 are independently selected from Each R 30 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a30 , S.R. a30 , C(O)R b30 , C(O)NR c30 R d30 , C(O)OR a30 ,OC(O)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , N.R. c30 C(O)NR c30 R d30 , N.R. c30 S(O)R b30 , N.R. c30 S(O)2R b30 , N.R. c30 S(O)NR c30 R d30 , S(O)R b30 , S(O)NR c30 Rd30 , S(O)2R b30 , S(O)NR c30 R d30 , and B.R. h30 R i30 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 31 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a31 , S.R. a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , N.R. c31 R d31 , N.R. c31C(O)R b31 , N.R. c31 C(O)OR a31 , N.R. c31 C(O)NR c31 R d31 , N.R. c31 S(O)R b31 , N.R. c31 S(O)2R b31 , N.R. c31 S(O)NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 , S(O)2R b31 , S(O)NR c31 R d31 , and B.R. h31 R i31 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 32 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 32 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, phenyl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a32 , S.R. a32 , C(O)R b32 , C(O)NR c32 R d32 , C(O)OR a32 ,OC(O)Rb32 , OC(O)NR c32 R d32 , N.R. c32 R d32 , N.R. c32 C(O)R b32 , N.R. c32 C(O)OR a32 , N.R. c32 C(O)NR c32 R d32 , N.R. c32 S(O)R b32 , N.R. c32 S(O)2R b32 , N.R. c32 S(O)NR c32 R d32 , S(O)R b32 , S(O)NR c32 R d32 , S(O)2R b32 , S(O)NR c32 R d32 , and B.R. h32 R i32 are independently selected from; Each R 50 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a50 , S.R. a50 , C(O)R b50 , C(O)NR c50 R d50 , C(O)OR a50 ,OC(O)R b50 , OC(O)NR c50 R d50 , N.R. c50 R d50 , N.R.c50 C(O)R b50 , N.R. c50 C(O)OR a50 , N.R. c50 C(O)NR c50 R d50 , N.R. c50 S(O)R b50 , N.R. c50 S(O)2R b50 , N.R. c50 S(O)NR c50 R d50 , S(O)R b50 , S(O)NR c50 R d50 , S(O)2R b50 , S(O)NR c50 R d50 , and B.R. h50 R i50 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 51 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 51 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 6~10 Aryl, 5-6 membered heteroaryl, 4-7 membered heterocycloalkyl, halo, D, CN, OR a51 , S.R. a51 , C(O)R b51 , C(O)NR c51 R d51, C(O)OR a51 ,OC(O)R b51 , OC(O)NR c51 R d51 , N.R. c51 R d51 , N.R. c51 C(O)R b51 , N.R. c51 C(O)OR a51 , N.R. c51 C(O)NR c51 R d51 , N.R. c51 S(O)R b51 , N.R. c51 S(O)2R b51 , N.R. c51 S(O)NR c51 R d51 , S(O)R b51 , S(O)NR c51 R d51 , S(O)2R b51 , S(O)NR c51 R d51 , and B.R. h51 R i51 are independently selected from; Each R 60 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, NO2, OR a60 , S.R. a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 ,OC(O)R b60 , OC(O)NR c60 R d60 , N.R.c60 R d60 , N.R. c60 C(O)R b60 , N.R. c60 C(O)OR a60 , N.R. c60 C(O)NR c60 R d60 , N.R. c60 S(O)R b60 , N.R. c60 S(O)2R b60 , N.R. c60 S(O)NR c60 R d60 , S(O)R b60 , S(O)NR c60 R d60 , S(O)2R b60 , S(O)NR c60 R d60 , and B.R. h60 R i60 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 61 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 61 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a61 , S.R. a61 , C(O)R b61 , C(O)NR c61 R d61 , C(O)OR a61 ,OC(O)R b61 , OC(O)NR c61 R d61 , N.R. c61 R d61 , N.R. c61 C(O)R b61 , N.R. c61 C(O)OR a61 , N.R. c61 C(O)NR c61 R d61 , N.R. c61 S(O)R b61 , N.R. c61 S(O)2R b61 , N.R. c61 S(O)NR c61 R d61 , S(O)R b61 , S(O)NR c61 R d61 , S(O)2R b61 , S(O)NR c61 R d61 , and B.R. h61 R i61 are independently selected from; Each R 70 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3Alkylene, Halo, D, CN, NO2, OR a70 , S.R. a70 , C(O)R b70 , C(O)NR c70 R d70 , C(O)OR a70 ,OC(O)R b70 , OC(O)NR c70 R d70 , N.R. c70 R d70 , N.R. c70 C(O)R b70 , N.R. c70 C(O)OR a70 , N.R. c70 C(O)NR c70 R d70 , N.R. c70 S(O)R b70 , N.R. c70 S(O)2R b70 , N.R. c70 S(O)NR c70 R d70 , S(O)R b70 , S(O)NR c70 R d70 , S(O)2R b70 , S(O)NR c70 R d70 , and B.R. h70 R i70 are independently selected from; R a1 , R b1 , R c1 , and R d1 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R gor is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c1 and R d1 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h1 and R i1 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h1 and R i1 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a2 , R b2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 22 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c2 and R d2together with the N atom to which they are attached, R 22 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e2 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h2 and R i2 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h2 and R i2 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e3 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R f3 and R j3 are respectively, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h3 and R i3 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h3 and R i3 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a4 , R b4 , R c4 , and R d4 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R gor is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c4 and R d4 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h4 and R i4 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h4 and R i4 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a5 , R b5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c5 and R d5together with the N atom to which they are attached, R 50 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e5 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h5 and R i5 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h5 and R i5 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a6 , R b6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 60 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e6 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h6 and R i6 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h6 and R i6 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a7, R b7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 70 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c7 and R d7 together with the N atom to which they are attached, R 70 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e7 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h7 and R i7 are OH and C, respectively. 1~6Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h7 and R i7 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 11 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c10 and R d10 together with the N atom to which they are attached, R 11 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e10 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h10 and R i10 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h10 and R i10 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a11 , R b11 , R c11 , and R d11 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c11 and R d11 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h11 and R i11 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h11 and R i11 together with the B atoms to which they are bonded, 1~6Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 21 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c20 and R d20 together with the N atom to which they are attached, R 21 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e20 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkyl carbonyl, C 1~6 Alkylaminosulfonyl, Carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl)carbamyl, aminosulfonyl, C 1~6Alkylaminosulfonyl, and di(C 1~6 alkyl)aminosulfonyl; R h20 and R i20 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h20 and R i20 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a21 , R b21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R g or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c21 and R d21 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h21 and R i21 are OH and C, respectively. 1~6 Alkoxy, and C 1~6haloalkoxy, or any R bonded to the same B atom h21 and R i21 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a22 , R b22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 23 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c22 and R d22 together with the N atom to which they are attached, R 23 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h22 and R i22 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h22 and R i22 together with the B atoms to which they are bonded, 1~6Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a23 , R b23 , R c23 , and R d23 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c23 and R d23 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h23 and R i23 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h23 and R i23 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h30 and R i30 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h30 and R i30 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 Cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl are each optionally represented by R 32or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c31 and R d31 together with the N atom to which they are attached, R 32 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h31 and R i31 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h31 and R i31 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a32 , R b32 , R c32 , and R d32 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R h32 and R i32 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h32 and R i32 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a50 , R b50 , R c50, and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 51 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c50 and R d50 together with the N atom to which they are attached, R 51 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h50 and R i50 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h50 and R i50 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a51 , R b51 , R c51 , and R d51 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c51 and R d51 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h51 and R i51 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h51 and R i51 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 61 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c60 and R d60 together with the N atom to which they are attached, R61 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h60 and R i60 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h60 and R i60 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a61 , R b61 , R c61 , and R d61 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c61 and R d61 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h61 and R i61 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h61 and R i61 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a70 , R b70 , R c70 , and R d70 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c70 and R d70 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h70 and R i70 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h70 and R i70 together with the B atoms to which they are bonded, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; Each R g D, OH, NO2, CN, halo, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 3~6 Cycloalkyl-C 1~2 Alkylene, C 1~6 Alkoxy, C 1~6 Haloalkoxy, C 1~3 Alkoxy-C 1~3 Alkyl, C 1~3 Alkoxy-C 1~3 Alkoxy, HO-C 1~3 Alkoxy, HO-C 1~3Alkyl, Cyano-C 1~3 Alkyl, H2N-C 1~3 Alkyl, Amino, C 1~6 Alkylamino, di(C 1~6 Alkyl)amino, thio, C 1~6 Alkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkyl sulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl) carbamyl, carboxy, C 1~6 Alkyl carbonyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkylcarbonylamino, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonyloxy, aminocarbonyloxy, C 1~6 Alkylaminocarbonyloxy, di(C 1~6 alkyl)aminocarbonyloxy, C 1~6 Alkyl sulfonyl amino, amino sulfonyl, C 1~6 Alkylaminosulfonyl, di(C 1~6 Alkyl)aminosulfonyl, aminosulfonylamino, C 1~6 Alkylaminosulfonylamino, di(C 1~6 Alkyl)aminosulfonylamino, aminocarbonylamino, C 1~6 Alkylaminocarbonylamino, and di(C 1~6 alkyl)aminocarbonylamino.
[0013] In another embodiment, the compound of formula I is a compound of formula Ia: [ka] or a pharmaceutically acceptable salt thereof; During the ceremony, Y is N or C; R 1 H, D, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, and CN; R2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a2 , S.R. a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 ,OC(O)R b2 , OC(O)NR c2 R d2 , N.R. c2 R d2 , N.R. c2 C(O)R b2 , N.R. c2 C(O)OR a2 , N.R. c2 C(O)NR c2 R d2 , N.R. c2 S(O)2R b2 , N.R. c2 S(O)NR c2 R d2 , S(O)2R b2 , and S(O)NR c2 R d2 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 22 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 1 is C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 6-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and the 6-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 6-10 membered heteroaryl and the 4-10 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally represented by R 10 substituted with 1, 2, 3, or 4 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR f3 , S.R. a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3,OC(O)R b3 , OC(O)NR c3 R d3 , N.R. c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , N.R. c3 C(O)NR c3 R d3 , N.R. c3 S(O)2R b3 , N.R. c3 S(O)NR c3 R d3 , S(O)2R b3 , and S(O)NR c3 R d3 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 30 substituted with 1, 2, 3, or 4 substituents independently selected from R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 ,OC(O)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , N.R. c5 C(O)NR c5 R d5 , N.R. c5 S(O)2R b5 , N.R. c5 S(O)NR c5 R d5 , S(O)2R b5 , and S(O)NR c5 R d5 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 50 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R 4 does not exist; R 6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 ,OC(O)R b6 , OC(O)NR c6 R d6 , N.R. c6 R d6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , N.R. c6 S(O)2R b6 , N.R. c6 S(O)NR c6 R d6 , S(O)2R b6 , and S(O)NR c6 R d6 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 60 substituted with 1, 2, 3, or 4 substituents independently selected from R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7 ,OC(O)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , N.R. c7 S(O)2R b7 , N.R. c7 S(O)NR c7 R d7 , S(O)2R b7 , and S(O)NRc7 R d7 is selected from Cy 2 is C 3~10 Cycloalkyl, 4-14 membered heterocycloalkyl, C 6~10 aryl, and 5-10 membered heteroaryl, wherein the 4-14 membered heterocycloalkyl and the 5-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 5-10 membered heteroaryl and the 4-14 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10 Cycloalkyl, 4-14 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 20 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a10 , S.R. a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 ,OC(O)R b10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R.c10 C(O)R b10 , N.R. c10 C(O)OR a10 , N.R. c10 C(O)NR c10 R d10 , N.R. c10 S(O)2R b10 , N.R. c10 S(O)NR c10 R d10 , S(O)2R b10 , and S(O)NR c10 R d10 are independently selected from; Each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a20 , S.R. a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 ,OC(O)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , N.R. c20 S(O)2R b20 , N.R. c20 S(O)NR c20 R d20, S(O)2R b20 , and S(O)NR c20 R d20 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 21 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 21 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a21 , S.R. a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , N.R. c21 R d21 , N.R. c21 C(O)R b21 , N.R. c21 C(O)ORa21 , N.R. c21 C(O)NR c21 R d21 , N.R. c21 S(O)2R b21 , N.R. c21 S(O)NR c21 R d21 , S(O)2R b21 , and S(O)NR c21 R d21 are independently selected from; Each R 22 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a22 , S.R. a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 ,OC(O)R b22 , OC(O)NR c22 R d22 , N.R. c22 R d22 , N.R. c22 C(O)R b22 , N.R. c22 C(O)OR a22 , N.R. c22 C(O)NR c22 R d22 , N.R. c22 S(O)2R b22 , N.R. c22 S(O)NR c22 R d22 , S(O)2R b22 , and S(O)NR c22 Rd22 are independently selected from; Each R 30 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a30 , S.R. a30 , C(O)R b30 , C(O)NR c30 R d30 , C(O)OR a30 ,OC(O)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , N.R. c30 C(O)NR c30 R d30 , N.R. c30 S(O)2R b30 , N.R. c30 S(O)NR c30 R d30 , S(O)2R b30 , and S(O)NR c30 R d30 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 31 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a31 , S.R. a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , N.R. c31 R d31 , N.R. c31 C(O)R b31 , N.R. c31 C(O)OR a31 , N.R. c31 C(O)NR c31 R d31 , N.R. c31 S(O)2R b31 , N.R. c31 S(O)NR c31 R d31 , S(O)2R b31 , and S(O)NR c31 R d31 are independently selected from; Each R50 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a50 , S.R. a50 , C(O)R b50 , C(O)NR c50 R d50 , C(O)OR a50 ,OC(O)R b50 , OC(O)NR c50 R d50 , N.R. c50 R d50 , N.R. c50 C(O)R b50 , N.R. c50 C(O)OR a50 , N.R. c50 C(O)NR c50 R d50 , N.R. c50 S(O)2R b50 , N.R. c50 S(O)NR c50 R d50 , S(O)2R b50 , and S(O)NR c50 R d50 are independently selected from; Each R 60 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a60 , S.R. a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 ,OC(O)R b60 , OC(O)NR c60 R d60 , N.R. c60 R d60 , N.R. c60 C(O)R b60 , N.R. c60 C(O)OR a60 , N.R. c60 C(O)NR c60 R d60 , N.R. c60 S(O)2R b60 , N.R. c60 S(O)NR c60 R d60 , S(O)2R b60 , and S(O)NR c60 R d60 are independently selected from; R a2 , R b2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 22or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c2 and R d2 together with the N atom to which they are attached, R 22 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R f3 and R j3 are respectively, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a5 , R b5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a6 , R b6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 60 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a7 , R b7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c7 and R d7 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a10 , Rb10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c10 and R d10 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 21 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c20 and R d20 together with the N atom to which they are attached, R 21 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a21 , R b21 , R c21, and R d21 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c21 and R d21 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a22 , R b22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c22 and R d22 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c31 and R d31 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a50 , R b50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c50 and R d50 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c60 and R d60 taken together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group.
[0014] In one embodiment of Formula Ia or a pharmaceutically acceptable salt thereof, Y is N or C; R 1 H, D, and C 1~6 alkyl; R 2 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a2 , and NR c2 R d2 C above is selected from 1~6 The alkyl is optionally R 22 substituted with 1 or 2 substituents independently selected from: Cy 1 is C 6~10 selected from aryl and 6-10 membered heteroaryl, wherein the 6-10 membered heteroaryl has at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and wherein the ring-forming carbon atoms of the 6-10 membered heteroaryl are optionally substituted by oxo to form a carbonyl group; C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from R 10substituted with 1, 2, or 3 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR f3 , and NR c3 R j3 C above is selected from 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 substituted with 1, 2, or 3 substituents independently selected from R 5 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a5 , C(O)NR c5 R d5 , and NR c5 R d5 C above is selected from 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 substituted with 1, 2, or 3 substituents independently selected from [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R 4does not exist; R 6 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a6 , and NR c6 R d6 C above is selected from 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 60 substituted with 1, 2, or 3 substituents independently selected from R 7 is H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; Cy 2 is selected from 4-10 membered heterocycloalkyl having at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, a ring-forming carbon atom of the 4-10 membered heterocycloalkyl optionally being substituted by oxo to form a carbonyl group, and the 4-10 membered heterocycloalkyl optionally being substituted by R 20 substituted with 1, 2, or 3 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , and NR c10 R d10 are independently selected from; Each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a20 , C(O)R b20 , C(O)NRc20 R d20 , and NR c20 R d20 C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 21 substituted with 1, 2, or 3 substituents independently selected from Each R 21 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , and NR c21 R d21 are independently selected from; Each R 22 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a22 , and NR c22 R d22 are independently selected from; Each R 30 is C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a30 , C(O)NR c30 R d30 , and NR c30 R d30 C 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 substituted with 1, 2, or 3 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a31 , and NR c31 R d31 are independently selected from; Each R50 is C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a50 , and NR c50 R d50 are independently selected from; Each R 60 is C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a60 , C(O)NR c60 R d60 , C(O)OR a60 , and NR c60 R d60 are independently selected from; R a2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, and C 1~6 haloalkyl, 1~6 The alkyl is optionally R 22 substituted with 1 or 2 substituents independently selected from: Each R c3 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 substituted with 1, 2, or 3 substituents independently selected from R f3 and R j3 are respectively, C1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, or 3 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 or is substituted with 1, 2, or 3 substituents independently selected from: Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a6 , R c6 , and R d6are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 60 or is substituted with 1, 2, or 3 substituents independently selected from: Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 21 substituted with 1, 2, or 3 substituents independently selected from R a21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; Ra22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 or is substituted with 1, 2, or 3 substituents independently selected from: Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atomc50 and R d50 together with the N atom to which they are attached form a 4-, 5-, or 6-membered heterocycloalkyl group; R a60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c60 and R d60 taken together with the N atom to which they are attached form a 4-, 5-, or 6-membered heterocycloalkyl group.
[0015] In another embodiment of Formula Ia or a pharmaceutically acceptable salt thereof, Y is N or C; R 1 is H; R 2 is H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; Cy 1 is C 6~10 aryl and 6- to 10-membered heteroaryl, wherein the 6- to 10-membered heteroaryl has at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O; 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from R 10 substituted with 1, 2, or 3 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, halo, D, CN, OR f3 , and NR c3 R j3 C above is selected from1~6 Alkyl, C 3~10 The cycloalkyl and 4- to 10-membered heterocycloalkyl are each optionally represented by R 30 substituted with 1, 2, or 3 substituents independently selected from R 5 is H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; [ka] is a double bond and Y is N, then R 6 does not exist; R 6 is H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; R 7 is H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; Cy 2 is selected from 4- to 6-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 6-membered heterocycloalkyl optionally has R 20 substituted with 1, 2, or 3 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , and NR c10 R d10 are independently selected from; Each R 20 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a20 , C(O)R b20 , C(O)NR c20 R d20 , and NR c20 R d20 C1~6 The alkyl is optionally R 21 substituted with 1 or 2 substituents independently selected from: Each R 21 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , and NR c21 R d21 are independently selected from; Each R 30 is C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a30 , C(O)NR c30 R d30 , and NR c30 R d30 C 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 substituted with 1, 2, or 3 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a31 , and NR c31 R d31 are independently selected from; Each R c3 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R30 substituted with 1, 2, or 3 substituents independently selected from R f3 and R j3 are respectively, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, or 3 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 21 substituted with 1, 2, or 3 substituents independently selected from R a21 , R c21 , and R d21are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 or is substituted with 1, 2, or 3 substituents independently selected from: Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, and C 1~6 haloalkyl.
[0016] In one embodiment, [ka] represents a single or double bond; X is N or CR 7 and; Y is N or C; R 1 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C2~6 Alkynyl, C 1~6 Haloalkyl, Halo, CN, OR a1 , S.R. a1 , C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 ,OC(O)R b1 , OC(O)NR c1 R d1 , N.R. c1 R d1 , N.R. c1 C(O)R b1 , N.R. c1 C(O)OR a1 , N.R. c1 C(O)NR c1 R d1 , N.R. c1 S(O)2R b1 , S(O)2R b1 , and S(O)NR c1 R d1 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a2 , S.R. a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 ,OC(O)R b2 , OC(O)NR c2 R d2 , N.R. c2 R d2 , N.R. c2 C(O)R b2 , N.R. c2 C(O)OR a2 , N.R. c2 C(O)NR c2 R d2 , N.R.c2 S(O)2R b2 , S(O)2R b2 , and S(O)NR c2 R d2 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 22 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 1 is C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 6-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and the 6-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 6-10 membered heteroaryl and the 4-10 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally represented by R 10 substituted with 1, 2, 3, or 4 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene, 5-10 membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR f3 , S.R.a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 ,OC(O)R b3 , OC(O)NR c3 R d3 , N.R. c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , N.R. c3 C(O)NR c3 R d3 , N.R. c3 S(O)2R b3 , S(O)2R b3 , and S(O)NR c3 R d3 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, 4-10 membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 Alkylene and 5-10 membered heteroaryl-C 1~3 Each alkylene is optionally represented by R 30 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a single bond and Y is C, then YR 6 is selected from C=O and C=S; R 4 H, D, C 1~6 Alkyl, and C 1~6 haloalkyl, 1~6 The alkyl is optionally R g substituted with 1 or 2 substituents independently selected from: R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 ,OC(O)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , N.R. c5 C(O)NR c5 R d5 , N.R. c5 S(O)2R b5 , S(O)2R b5 , and S(O)NR c5 R d5 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R4 does not exist; R 6 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, halo, CN, OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 ,OC(O)R b6 , OC(O)NR c6 R d6 , N.R. c6 R d6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , N.R. c6 S(O)2R b6 , S(O)2R b6 , and S(O)NR c6 R d6 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 60 substituted with 1, 2, 3, or 4 substituents independently selected from R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl and 4-6 membered heterocycloalkyl, halo, D, CN, OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7,OC(O)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , N.R. c7 S(O)2R b7 , S(O)2R b7 , and S(O)NR c7 R d7 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 70 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 2 is a 4- to 14-membered heterocycloalkyl having at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, wherein N and S are optionally oxidized; a ring-forming carbon atom of the 4- to 14-membered heterocycloalkyl is optionally substituted by oxo to form a carbonyl group; and the 4- to 14-membered heterocycloalkyl optionally has R 20 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, halo, D, CN, OR a10 , S.R. a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 ,OC(O)Rb10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R. c10 C(O)R b10 , N.R. c10 C(O)OR a10 , N.R. c10 C(O)NR c10 R d10 , N.R. c10 S(O)2R b10 , S(O)2R b10 , and S(O)NR c10 R d10 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 11 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 11 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a11 , S.R. a11 , CC(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 ,OC(O)R b11 , OC(O)NR c11 R d11 , N.R. c11 R d11 , N.R. c11 C(O)R b11 , N.R. c11 C(O)OR a11 , N.R. c11 C(O)NR c11 R d11 , N.R. c11 S(O)2R b11 , S(O)2R b11 , and S(O)NR c11 R d11 are independently selected from; Each R 20 is C 1~6 Alkyl, C2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, halo, D, CN, OR a20 , S.R. a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 ,OC(O)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , N.R. c20 S(O)2R b20 , S(O)2R b20 , and S(O)NR c20 R d20 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 21 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 21 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , S.R. a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 ,OC(O)R b21 , OC(O)NR c21 R d21 , N.R. c21 R d21 , N.R. c21 C(O)Rb21 , N.R. c21 C(O)OR a21 , N.R. c21 C(O)NR c21 R d21 , N.R. c21 S(O)2R b21 , S(O)2R b21 , and S(O)NR c21 R d21 are independently selected from; Each R 22 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a22 , S.R. a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 ,OC(O)R b22 , OC(O)NR c22 R d22 , N.R. c22 R d22 , N.R. c22 C(O)R b22 , N.R. c22 C(O)OR a22 , N.R. c22 C(O)NR c22 R d22 , N.R. c22 S(O)2R b22 , S(O)2R b22 , and S(O)NR c22 R d22 are independently selected from; Each R 30 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a30 , S.R. a30 , C(O)R b30 , C(O)NR c30 R d30, C(O)OR a30 ,OC(O)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , N.R. c30 C(O)NR c30 R d30 , N.R. c30 S(O)2R b30 , S(O)2R b30 , and S(O)NR c30 R d30 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, halo, D, CN, OR a31 , S.R. a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 ,OC(O)R b31 , OC(O)NR c31 R d31 , N.R. c31 R d31 , N.R. c31 C(O)R b31 , N.R. c31 C(O)OR a31 , N.R. c31 C(O)NR c31 R d31 , N.R. c31S(O)2R b31 , S(O)2R b31 , and S(O)NR c31 R d31 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 32 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 32 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a32 , S.R. a32 , C(O)R b32 , C(O)NR c32 R d32 , C(O)OR a32 ,OC(O)R b32 , OC(O)NR c32 R d32 , N.R. c32 R d32 , N.R. c32 C(O)R b32 , N.R. c32 C(O)OR a32 , N.R. c32 C(O)NR c32 R d32 , N.R. c32 S(O)2R b32 , S(O)2R b32 , and S(O)NR c32 R d32 are independently selected from; Each R 50 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a50 , S.R. a50 , C(O)R b50 , C(O)NR c50 R d50 , C(O)OR a50,OC(O)R b50 , OC(O)NR c50 R d50 , N.R. c50 R d50 , N.R. c50 C(O)R b50 , N.R. c50 C(O)OR a50 , N.R. c50 C(O)NR c50 R d50 , N.R. c50 S(O)2R b50 , S(O)2R b50 , and S(O)NR c50 R d50 are independently selected from; Each R 60 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a60 , S.R. a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 ,OC(O)R b60 , OC(O)NR c60 R d60 , N.R. c60 R d60 , N.R. c60 C(O)R b60 , N.R. c60 C(O)OR a60 , N.R. c60 C(O)NR c60 R d60 , N.R. c60 S(O)2R b60 , S(O)2R b60 , and S(O)NR c60 R d60 are independently selected from; Each R 70 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a70 , S.R. a70 , C(O)R b70, C(O)NR c70 R d70 , C(O)OR a70 ,OC(O)R b70 , OC(O)NR c70 R d70 , N.R. c70 R d70 , N.R. c70 C(O)R b70 , N.R. c70 C(O)OR a70 , N.R. c70 C(O)NR c70 R d70 , N.R. c70 S(O)2R b70 , S(O)2R b70 , and S(O)NR c70 R d70 are independently selected from; R a1 , R b1 , R c1 , and R d1 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R g substituted with 1, 2, 3, or 4 substituents independently selected from R a2 , R b2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 22 substituted with 1, 2, 3, or 4 substituents independently selected from R a3 , R b3 , Rc3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R f3 and R j3 are respectively, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a5 , R b5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a6 , R b6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, and 4- to 6-membered heterocycloalkyl; 1~6 Alkyl, C2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 60 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a7 , R b7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, and 4- to 6-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 70 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c7 and R d7 together with the N atom to which they are attached, R 70 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C3~6 cycloalkyl, and 4- to 6-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 11 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c10 and R d10 together with the N atom to which they are attached, R 11 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a11 , R b11 , R c11 , and R d11 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, and 4- to 6-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 21 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c20 and R d20together with the N atom to which they are attached, R 21 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a21 , R b21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a22 , R b22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, and 4- to 6-membered heterocycloalkyl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 32 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c31 and R d31 together with the N atom to which they are attached, R 32 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a32 , R b32 , R c32 , and R d32 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a50 , R b50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a60 , R b60 , Rc60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a70 , R b70 , R c70 , and R d70 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; Each R g D, OH, CN, halo, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 1~6 Alkoxy, C 1~6 Haloalkoxy, C 1~3 Alkoxy-C 1~3 Alkyl, C 1~3 HO-C 1~3 Alkyl, Cyano-C 1~3 Alkyl, H2N-C 1~3 Alkyl, Amino, C 1~6 Alkylamino, di(C 1~6 Alkyl)amino, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbamyl, di(C 1~6 Alkyl) carbamyl, carboxy, C 1~6 Alkyl carbonyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkylcarbonylamino, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonyloxy, C 1~6 Alkylaminocarbonyloxy, di(C 1~6 alkyl)aminocarbonyloxy, C 1~6 Alkylaminocarbonylamino, and di(C 1~6alkyl)aminocarbonylamino.
[0017] In one embodiment of Formula I or a pharmaceutically acceptable salt thereof, [ka] represents a single or double bond; X is N or CR 7 and; Y is N or C; R 1 H, D, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, and CN; R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a2 , and NR c2 R d2 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 22 substituted with 1, 2, 3, or 4 substituents independently selected from Cy 1 is C 6~10 selected from aryl and 6-10 membered heteroaryl, each of which has at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and the ring-forming carbon atoms of the 6-10 membered heteroaryl are optionally substituted by oxo to form a carbonyl group; C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from R 10 substituted with 1, 2, 3, or 4 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, 4-10 membered heterocycloalkyl, C6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR f3 , and NR c3 R j3 C above is selected from 1~6 Alkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 substituted with 1, 2, 3, or 4 substituents independently selected from R 5 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 6~10 aryl, 5- to 10-membered heteroaryl, and D; 1~6 Alkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 substituted with 1, 2, 3, or 4 substituents independently selected from [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R 4 does not exist; R 6 H, D, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, and 4- to 6-membered heterocycloalkyl; 1~6 Alkyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 60 substituted with 1, 2, 3, or 4 substituents independently selected from R 7 is H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; Cy 2 is a 4- to 14-membered heterocycloalkyl having at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S; and the 4- to 14-membered heterocycloalkyl optionally has R 20 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , and NR c10 R d10 are independently selected from; Each R 20 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 , and NR c20 R d20 C 1~6 The alkyl is optionally R 21 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 21 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , and NR c21 R d21 are independently selected from; Each R 22 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a22 , and NR c22 R d22 are independently selected from; Each R 30 is C 1~6 Alkyl, C 1~6 Haloalkyl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, halo, D, CN, ORa30 , and NR c30 R d30 C 1~6 The alkyl, 4- to 10-membered heterocycloalkyl, and 5- to 10-membered heteroaryl are each optionally represented by R 31 substituted with 1, 2, 3, or 4 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a31 , and NR c31 R d31 are independently selected from; Each R 50 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a50 , and NR c50 R d50 are independently selected from; Each R 60 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 , and NR c60 R d60 are independently selected from; R a2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; Each R c3 is H, C 1~6 Alkyl, C 1~6 independently selected from haloalkyl, 4- to 10-membered heterocycloalkyl, and 5- to 10-membered heteroaryl; 1~6 The alkyl, 4- to 10-membered heterocycloalkyl, and 5- to 10-membered heteroaryl are each optionally represented by R 30 substituted with 1, 2, 3, or 4 substituents independently selected from R f3 and R j3 are respectively, C 1~6 Alkyl, C 1~6 independently selected from haloalkyl, 4- to 10-membered heterocycloalkyl, and 5- to 10-membered heteroaryl; 1~6 The alkyl, 4- to 10-membered heterocycloalkyl, and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1, 2, 3, or 4 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 21 substituted with 1, 2, 3, or 4 substituents independently selected from R a21 , R b21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a30, R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a50 , R b50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, and C 1~6 haloalkyl.
[0018] In another embodiment of Formula I or a pharmaceutically acceptable salt thereof, [ka] represents a single or double bond; X is CR 7 and; Y is N or C; R 1 is H; R 2 is H, C 1~6 Alkyl, C 1~6 haloalkyl, halo, D, and CN; 1~6 The alkyl is optionally R 22 substituted with 1 or 2 substituents independently selected from: Cy 1 is C 6~10aryl and 6- to 10-membered heteroaryl, each of which has at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O; C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from R 10 substituted with 1, 2, or 3 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, 4-6 membered heterocycloalkyl, OR f3 , and NR c3 R j3 C above is selected from 1~6 The alkyl and 4- to 6-membered heterocycloalkyl are each optionally selected from R 30 substituted with 1 or 2 substituents independently selected from: R 5 is H, C 1~6 Alkyl, C 1~6 haloalkyl, phenyl, 5- to 6-membered heteroaryl, and D; 1~6 Alkyl, phenyl, and 5- to 6-membered heteroaryl are each optionally represented by R 50 substituted with 1 or 2 substituents independently selected from: [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R 4 does not exist; R 6 H, D, C 1~6 Alkyl, and C 1~6 haloalkyl, 1~6 The alkyl is optionally R 60 substituted with 1 or 2 substituents independently selected from: R 7 is selected from the halo; Cy 2 is a 4- to 8-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 8-membered heterocycloalkyl optionally has R 20 substituted with 1 or 2 substituents independently selected from: Each R 10 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , and NR c10 R d10 are independently selected from; Each R 20 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, and C(O)R b20 C 1~6 The alkyl is optionally R 21 substituted with 1 or 2 substituents independently selected from: Each R 21 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , and NR c21 R d21 are independently selected from; Each R 22 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a22 , and NR c22 R d22 are independently selected from; Each R 30 is C 1~6 Alkyl, C 1~6 Haloalkyl, 4-6 membered heterocycloalkyl, 5-6 membered heteroaryl, halo, D, CN, OR a30 , and NR c30 R d30 C 1~6The alkyl, 4- to 6-membered heterocycloalkyl, and 5- to 6-membered heteroaryl are each optionally represented by R 31 substituted with 1 or 2 substituents independently selected from: Each R 31 is C 1~6 Alkyl, C 1~6 independently selected from haloalkyl, halo, D, and CN; Each R 50 is C 1~6 Alkyl, C 1~6 independently selected from haloalkyl, halo, D, and CN; Each R 60 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 , and NR c60 R d60 are independently selected from; Each R c3 is H, C 1~6 Alkyl, and C 1~6 haloalkyl, 1~6 The alkyl is optionally R 30 substituted with 1 or 2 substituents independently selected from: R f3 and R j3 are respectively, C 1~6 Alkyl and C 1~6 haloalkyl, 1~6 The alkyl is optionally R 30 substituted with 1 or 2 substituents independently selected from: R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a20 , R b20 , R c20 , and Rd20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl, 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 21 substituted with 1 or 2 substituents independently selected from: R a21 , R b21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, and C 1~6 haloalkyl.
[0019] In another embodiment, the compound of formula I is a compound of formula II: [ka] or a pharmaceutically acceptable salt thereof.
[0020] In yet another embodiment, R 1 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, CN, OR a1 , and NR c1 R d1Selected from; R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a2 , and NR c2 R d2 Selected from; Cy 1 is C 6~10 selected from aryl and 6-10 membered heteroaryl, each 6-10 membered heteroaryl having at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, wherein N and S are optionally oxidized, and a ring-forming carbon atom of the 6-10 membered heteroaryl is optionally substituted by oxo to form a carbonyl group; C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from R 10 substituted with 1 or 2 substituents independently selected from: R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR f3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 ,OC(O)R b3 , OC(O)NR c3 R d3 , N.R. c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , and S(O)2R b3 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 substituted with 1 or 2 substituents independently selected from: R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 ,OC(O)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , and S(O)2R b5 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 substituted with 1 or 2 substituents independently selected from: R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a7 , and NR c7 R d7 Selected from; Cy 2is a 4-10 membered heterocycloalkyl having at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, wherein N and S are optionally oxidized; a ring-forming carbon atom of the 4-10 membered heterocycloalkyl is optionally substituted by oxo to form a carbonyl group; and the 4-10 membered heterocycloalkyl optionally has R 20 substituted with 1 or 2 substituents independently selected from: Each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 ,OC(O)R b10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R. c10 C(O)R b10 , N.R. c10 C(O)OR a10 , and S(O)2R b10 are independently selected from; Each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 ,OC(O)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , and S(O)2Rb20 are independently selected from; Each R 30 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a30 , C(O)R b30 , C(O)NR c30 R d30 , C(O)OR a30 ,OC(O)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , and S(O)2R b30 C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 substituted with 1 or 2 substituents independently selected from: Each R 31 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a31 , and NR c31 R d31 are independently selected from; Each R 50 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a50 , and NR c50R d50 are independently selected from; R a1 , R c1 , and R d1 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 or is substituted with 1 or 2 substituents independently selected from: Alternatively, any R bonded to the same N atom c3 and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1 or 2 substituents independently selected from: R a5 , R b5 , R c5 , and Rd5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 or is substituted with 1 or 2 substituents independently selected from: Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1 or 2 substituents independently selected from: R a7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6Alkynyl, and C 1~6 independently selected from haloalkyl; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 31 or is substituted with 1 or 2 substituents independently selected from: Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1 or 2 substituents independently selected from: R a31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R a50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl.
[0021] In yet another embodiment, R 1 H, D, and C 1~3 alkyl; R 2 is H, C 1~3 Alkyl, C 1~3 selected from haloalkyl, halo, D, and CN; Cy 1 is C 6~10 aryl, C 6~10 The aryl is optionally R 10 substituted with 1 or 2 substituents independently selected from: R 3 is H, C 1~3 alkyl, 4- to 6-membered heterocycloalkyl, and D; 1~3 The alkyl and 4- to 6-membered heterocycloalkyl are each optionally selected from R 30 substituted with 1 or 2 substituents independently selected from: R 5 is H, C 1~3 alkyl, and D; R 7 is H, C 1~3 Alkyl, C 1~3 selected from haloalkyl, halo, D, and CN; Cy 2 is a 4- to 6-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 6-membered heterocycloalkyl optionally has R 20 substituted with 1 or 2 substituents independently selected from: Each R 10 is C 1~3 Alkyl, C 1~3 Haloalkyl, halo, D, CN, and OR a10 are independently selected from; Each R 20 is C 1~3 Alkyl, D, and C(O)R b20 are independently selected from; Each R 30 is C1~3 Alkyl, C 1~3 Haloalkyl, Halo, D, CN, OR a30 , and NR c30 R d30 are independently selected from; Each R a10 is H and C 1~3 independently selected from alkyl; Each R b20 is H, C 1~3 Alkyl, and C 2~3 alkenyl; R a30 , R c30 , and R d30 are H and C, respectively. 1~3 Alkyl, and C 1~3 haloalkyl.
[0022] In one embodiment, X is CR 7 and; R 1 is selected from H; R 2 is H, C 1~3 selected from haloalkyl, and halo; Cy 1 is C 10 aryl, C 10 The aryl is optionally R 10 substituted with 1 or 2 substituents independently selected from: R 3 is selected from H and 4- to 6-membered heterocycloalkyl, wherein the 4- to 6-membered heterocycloalkyl is optionally selected from R 30 substituted with 1 or 2 substituents independently selected from: R 5 is H; [ka] is a double bond, Y is N, and R 4 and R 6 does not exist; R 7 is selected from H or halo; Cy2 is a 4- to 6-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 6-membered heterocycloalkyl optionally has R 20 substituted with 1 or 2 substituents independently selected from: Each R 10 is OR a10 are independently selected from; Each R 20 is C(O)R b20 are independently selected from; Each R 30 is NR c30 R d30 are independently selected from; Each R a10 is H and C 1~3 independently selected from alkyl; Each R b20 is C 1~3 Alkyl or C 2~4 is alkenyl; R c30 and R d30 are respectively, C 1~3 alkyl.
[0023] In another embodiment of Formula I or a pharmaceutically acceptable salt thereof, [ka] represents a single or double bond; X is CH or C-halo; Y is N or C; R 1 is H; R 2 is H, C 1~6 Alkyl, C 1~6 haloalkyl, halo, and CN; 1~6 Alkyl is optionally selected from D, CN, OH, O(C 1~6 alkyl), NH2, NH(C 1~6 alkyl), and N(C 1~6substituted with 1 or 2 substituents independently selected from alkyl); Cy 1 is C 6~10 aryl and 6- to 10-membered heteroaryl, each of which has at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O; C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from OH, halo, C 1~6 Alkyl, and C 1~6 substituted with 1, 2, or 3 substituents independently selected from haloalkyl; R 3 is H, C 1~6 Alkyl, and 4- to 6-membered heterocycloalkyl, and O(C 1~6 alkyl), and 1~6 The alkyl and 4- to 6-membered heterocycloalkyl are each optionally selected from R 30 substituted with 1 or 2 substituents independently selected from: R 5 is selected from H, phenyl, and 5- to 6-membered heteroaryl, each of which is optionally selected from C 1~6 substituted with 1 or 2 substituents independently selected from alkyl; [ka] is a double bond and Y is N, then R 4 and R 6 does not exist; [ka] is a double bond and Y is C, then R 4 does not exist; R 6 is H, C 1~6 alkyl, and 5- to 10-membered heteroaryl; 1~6 The alkyl and 5- to 10-membered heteroaryl are each optionally selected from C 1~6 Alkyl, C(O)N(C1~6 alkyl)2, and C(O)OC 1~6 substituted with 1 or 2 substituents independently selected from alkyl; Cy 2 is a 4- to 8-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 8-membered heterocycloalkyl optionally has C 1~6 Alkyl-CN and C(O)R b20 substituted with 1 or 2 substituents independently selected from: Each R 30 is C 1~6 Alkyl, 4-6 membered heterocycloalkyl, halo, and N(C 1~6 alkyl)2, wherein the 4- to 6-membered heterocycloalkyl is optionally selected from C 1~6 substituted with 1 or 2 substituents independently selected from alkyl; Each R b20 is C 2~6 Alkenyl and C 2~6 alkynyl, independently selected from C 2~6 Alkenyl and C 2~6 Each alkynyl is optionally selected from C 1~6 Alkyl, C 1~6 AlkylO(C 1~6 alkyl), C 1~6 Haloalkyl, halo, and C 1~6 Alkyl-N(C 1~6 and substituted with 1 or 2 substituents independently selected from alkyl).
[0024] In another embodiment, the compound of formula I is a compound of formula III: [ka] or a pharmaceutically acceptable salt thereof.
[0025] In yet another embodiment, the compound of formula I is a compound of formula IV: [ka] or a pharmaceutically acceptable salt thereof.
[0026] In yet another embodiment, the compound of formula I is a compound of formula V: [ka] or a pharmaceutically acceptable salt thereof.
[0027] In one embodiment, the compound of formula I is a compound of formula VI: [ka] or a pharmaceutically acceptable salt thereof.
[0028] In another embodiment, the compound of formula I is a compound of formula VII: [ka] or a pharmaceutically acceptable salt thereof.
[0029] In yet another embodiment, X is CR 7 In yet another embodiment, X is N.
[0030] In one embodiment, [ka] is a double bond, Y is N, and R 4 and R 6 is not present. [ka] is a single bond, and YR 6 is C=O. In one embodiment, [ka] is a double bond, Y is C, and R 4 does not exist.
[0031] In yet another embodiment, R 1 H, D, C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, OR a1 , and NR c1 R d1 In yet another embodiment, R 1 H, D, C 1~6 Alkyl, C 1~6 In yet another embodiment, R is selected from haloalkyl, halo, and CN. 1 H, D, and C 1~3 In yet another embodiment, R 1 is H.
[0032] In one embodiment, R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a2 , and NR c2 R d2 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 22 In another embodiment, R 2 is H, C 1~6 Alkyl, C 1~6 haloalkyl, halo, D, and CN; 1~6 The alkyl is optionally R 22 In another embodiment, R 2 is C 1~6 alkyl and halo, 1~6 The alkyl is optionally R 22 is substituted with 1 or 2 substituents independently selected from
[0033] In one embodiment, R2 H, D, C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, OR a1 , and NR c1 R d1 In another embodiment, R 2 H, D, C 1~6 In yet another embodiment, R 2 H, D, C 1~6 Alkyl, C 1~6 In one embodiment, R is selected from haloalkyl, halo, and CN. 2 H, D, C 1~2 Alkyl, C 1~2 In yet another embodiment, R is selected from haloalkyl, halo, and CN. 2 is halo. In another embodiment, R 2 is chloro.
[0034] In one embodiment, each R 22 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a22 , and NR c22 R d22 In one embodiment, each R 22 is C 1~6 Alkyl, C 1~6 In one embodiment, R is independently selected from haloalkyl, halo, and CN. 22 is CN.
[0035] In yet another embodiment, Cy 1 is C 6~10 selected from aryl and 6-10 membered heteroaryl, each 6-10 membered heteroaryl having at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, wherein N and S are optionally oxidized, and a ring-forming carbon atom of the 6-10 membered heteroaryl is optionally substituted by oxo to form a carbonyl group; C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from R10 is substituted with 1 or 2 substituents independently selected from
[0036] In one embodiment, Cy 1 is R 10 C optionally substituted with 1 or 2 substituents independently selected from 6~10 In another embodiment, Cy is aryl. 1 is R 10 C optionally substituted with 1 or 2 substituents independently selected from 6~10 In yet another embodiment, Cy is aryl. 1 is optionally R 10 C substituted once with 6~10 In yet another embodiment, Cy is aryl. 1 is optionally R 10 In yet another embodiment, Cy is substituted once with 1 is 3-hydroxy-naphthalen-1-yl.
[0037] In one embodiment, Cy 1 is C 6~10 aryl and 6- to 10-membered heteroaryl, each of which has at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O; C 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from R 10 In yet another embodiment, Cy is substituted with 1, 2, or 3 substituents independently selected from 1 is R 10 and 1H-indazolyl optionally substituted with 1 or 2 substituents independently selected from:
[0038] In yet another embodiment, Cy 1 is a 5- to 10-membered heteroaryl, provided that Cy 1 is other than 3,5-dimethylisoxazol-4-yl. 1is other than 3,5-dimethylisoxazol-4-yl.
[0039] In yet another embodiment, each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , and NR c10 R d10 C 1~6 Alkyl, C 2~6 Alkenyl, and C 2~6 Each alkynyl is optionally represented by R 11 is substituted with 1 or 2 substituents independently selected from
[0040] In yet another embodiment, each R 10 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , and NR c10 R d10 In another embodiment, each R 10 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, and OR a10 In one embodiment, each R 10 is C 1~6 Alkyl, Halo, and OR a10 In another embodiment, each R 10 is independently selected from methyl, chloro, fluoro, trifluoromethyl, and hydroxyl. 10 is independently selected from methyl, fluoro, and hydroxyl.
[0041] In one embodiment, each R 10 is C 1~3 Alkyl, C 1~3 Haloalkyl, halo, D, CN, and OR a10 In one embodiment, each R 10Halo and OR a10 In one embodiment, each R 10 is independently selected from halo and OH. In one embodiment, R 10 is OH.
[0042] In yet another embodiment, each R 11 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a11 , and NR c11 R d11 are independently selected from
[0043] In yet another embodiment, R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, OR f3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 ,OC(O)R b3 , OC(O)NR c3 R d3 , and NR c3 R j3 C above is selected from 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 is substituted with 1 or 2 substituents independently selected from
[0044] In one embodiment, R 3 is H, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10Aryl, 5-10 membered heteroaryl, halo, and OR f3 C above is selected from 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 30 In one embodiment, R 3 is H, 4-10 membered heterocycloalkyl, C 6~10 Aryl and OR f3 The 4- to 10-membered heterocycloalkyl and C 6~10 Each aryl is optionally selected from R 30 is substituted with 1 or 2 substituents independently selected from
[0045] In another embodiment, R 3 is H or a 4- to 7-membered heterocycloalkyl, and said 4- to 7-membered heterocycloalkyl is optionally selected from R 30 In yet another embodiment, R 3 is a 4- to 7-membered heterocycloalkyl, and the 4- to 7-membered heterocycloalkyl is optionally selected from R 30 In yet another embodiment, R 3 is a 4-membered heterocycloalkyl, and R 30 is optionally substituted with 1 or 2 substituents independently selected from
[0046] In another embodiment, R 3 is H, 4-6 membered heterocycloalkyl, and OR f3 wherein the 4- to 6-membered heterocycloalkyl is optionally selected from R 30 In one embodiment, R 3 is a 4-membered heterocycloalkyl, optionally R 30 In another embodiment, R 3is selected from H and 3-(dimethylamino)azetidin-1-yl. 3 is selected from H, 3-(dimethylamino)azetidin-1-yl, and -(S)-1-methylpyrrolidin-2-yl)methoxy. 3 is 3-(dimethylamino)azetidin-1-yl. In yet another embodiment, R 3 is H.
[0047] In one embodiment, each R 30 is C 1~6 Alkyl, C 1~6 Haloalkyl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, halo, D, CN, OR a30 , and NR c30 R d30 C 1~6 The alkyl, 4- to 10-membered heterocycloalkyl, and 5- to 10-membered heteroaryl are each optionally represented by R 31 In one embodiment, each R 30 is C 1~6 Alkyl, C 1~6 Haloalkyl, 4-6 membered heterocycloalkyl, 5-6 membered heteroaryl, halo, D, CN, OR a30 , and NR c30 R d30 C 1~6 The alkyl, 4- to 6-membered heterocycloalkyl, and 5- to 6-membered heteroaryl are each optionally represented by R 31 is substituted with 1 or 2 substituents independently selected from
[0048] In another embodiment, R 30 is NR c30 R d30 In yet another embodiment, R 30 is NR c30 R d30 and R c30 and R d30 are each independently C 1~3 It is alkyl.
[0049] In another embodiment, each R 30 is a 4- to 10-membered heterocycloalkyl, a 5- to 10-membered heteroaryl, halo, OR a30 , and NR c30 R d30 wherein each of the 4- to 10-membered heterocycloalkyl and 5- to 10-membered heteroaryl is optionally selected from R 31 is substituted with 1 or 2 substituents independently selected from
[0050] In yet another embodiment, each R 31 is C 1~6 Alkyl, Halo, D, CN, OR a31 , and NR c31 R d31 In one embodiment, each R 31 is C 1~6 Alkyl, C 1~6 In one embodiment, each R 31 independently C 1~6 In another embodiment, each R 31 are independently methyl.
[0051] In another embodiment, R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, and C 1~6 haloalkyl, 1~6 The alkyl is optionally R 30 In another embodiment, R f3 and R j3 are respectively, C 1~6 Alkyl and C 1~6 haloalkyl, 1~6 The alkyl is optionally R 30 is substituted with 1 or 2 substituents independently selected from
[0052] In yet another embodiment, each R a3 independently C 1~6 alkyl, and the C 1~6 The alkyl is optionally R 30 In yet another embodiment, each R a3 are independently methyl, and the methyl is R 30 is substituted with one substituent independently selected from
[0053] In another embodiment, each R f3 independently C 1~6 alkyl, and the C 1~6 The alkyl is optionally R 30 In yet another embodiment, each R f3 are independently methyl, and the methyl is R 30 is substituted with one substituent independently selected from
[0054] In one embodiment, R 4 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, halo, CN, OR a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 ,OC(O)R b4 , OC(O)NR c4 R d4 , N.R. c4 R d4 , N.R. c4 C(O)R b4 , N.R. c4 C(O)OR a4 , N.R. c4 C(O)NR c4 R d4 , N.R. c4 S(O)2R b4 , S(O)2Rb4 , and S(O)NR c4 R d4 In another embodiment, R 4 H, D, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, 4-6 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, halo, CN, OR a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 , and OC(O)R b4 In yet another embodiment, R 4 H, D, C 1~6 Alkyl, C 1~6 In yet another embodiment, R is selected from haloalkyl, halo, and CN. 4 is H.
[0055] In one embodiment, R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 Alkylene, Halo, D, CN, OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 ,OC(O)R b5 , N.R. c5 R d5 , and NR c5 C(O)R b5 In another embodiment, R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 In yet another embodiment, R is selected from aryl, 5-10 membered heteroaryl, D, CN, and halo. 5 is H, C 1~6 Alkyl, C 1~6 In yet another embodiment, R is selected from haloalkyl, D, CN, and halo. 5 is H or C 1~3 In another embodiment, R 5 is H.
[0056] In one embodiment, R 5 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 6~10 aryl, 5- to 10-membered heteroaryl, and D; 1~6 Alkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 In another embodiment, R 5 is H, C 1~6 Alkyl, C 1~6 haloalkyl, phenyl, 5- to 6-membered heteroaryl, and D; 1~6 Alkyl, phenyl, and 5- to 6-membered heteroaryl are each optionally represented by R 50 is substituted with 1 or 2 substituents independently selected from
[0057] In one embodiment, R 5 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a5 , C(O)NR c5 R d5 , and NR c5 R d5 C above is selected from 1~6Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 In another embodiment, R 5 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, CN, OR a5 , and C(O)NR c5 R d5 C above is selected from 1~6 Alkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 50 and is substituted with 1, 2, or 3 substituents independently selected from:
[0058] In another embodiment, each R 50 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a50 , and NR c50 R d50 In one embodiment, each R 50 is C 1~6 Alkyl, C 1~6 In one embodiment, each R 50 is C 1~6 It is alkyl.
[0059] In one embodiment, each R 50 is C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a50 , and NR c50 R d50In another embodiment, each R 50 is C 1~6 Alkyl, C 1~6 Haloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, CN, OR a50 , and NR c50 R d50 are independently selected from
[0060] In one embodiment, each R 51 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a51 , and NR c51 R d51 In another embodiment, each R 51 is C 1~6 Alkyl, C 1~6 Independently selected from haloalkyl, halo, D, and CN.
[0061] In one embodiment, R 6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, NO2, OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 ,OC(O)R b6 , OC(O)NR c6 R d6 , N.R. c6 R d6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , N.R. c6 S(O)Rb6 , N.R. c6 S(O)2R b6 , N.R. c6 S(O)NR c6 R d6 , S(O)R b6 , S(O)NR c6 R d6 , S(O)2R b6 , and S(O)NR c6 R d6 In another embodiment, R 6 H, D, C 1~6 Alkyl, C 1~6 Haloalkyl, OR a6 , and NR c6 R d6 In another embodiment, R 6 H, D, C 1~6 Alkyl, and C 1~6 haloalkyl.
[0062] In one embodiment, R 6 H, D, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, and 4- to 6-membered heterocycloalkyl; 1~6 Alkyl, C 3~6 The cycloalkyl and 4- to 6-membered heterocycloalkyl are each optionally represented by R 60 In another embodiment, R 6 H, D, C 1~6 Alkyl, and C 1~6 haloalkyl, 1~6 The alkyl is optionally R 60 is substituted with 1 or 2 substituents independently selected from
[0063] In yet another embodiment, R 6 is H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a6 , and NR c6 R d6 C above is selected from 1~6 Alkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 60 and is substituted with 1, 2, or 3 substituents independently selected from:
[0064] In one embodiment, each R 60 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 , and NR c60 R d60 In another embodiment, each R 60 is C 1~6 Alkyl, C 1~6 Haloalkyl, CN, C(O)NR c60 R d60 , and C(O)OR a60 are independently selected from
[0065] In one embodiment, each R 60 is C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a60 , C(O)NR c60 R d60 , C(O)OR a60 , and NR c60 R d60 In another embodiment, each R 60 is C 1~6 Alkyl, C 1~6 Haloalkyl, C 6~10Aryl, Halo, D, CN, OR a60 , C(O)NR c60 R d60 , C(O)OR a60 , and NR c60 R d60 are independently selected from
[0066] In yet another embodiment, R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, NO2, OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7 ,OC(O)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , N.R. c7 S(O)2R b7 , N.R. c7 S(O)NR c7 R d7 , S(O)2R b7 , and S(O)NR c7 R d7 In yet another embodiment, R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10aryl, 5-10 membered heteroaryl, and halo. In one embodiment, R 7 H, D, C 1~3 Alkyl, C 1~3 In yet another embodiment, R is selected from haloalkyl, CN, and halo. 7 is halo. In yet another embodiment, R 7 is fluoro.
[0067] In one embodiment, Cy 2 is a 4- to 6-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 6-membered heterocycloalkyl optionally has R 20 is substituted with 1 or 2 substituents independently selected from
[0068] In another embodiment, Cy 2 is C 3~6 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 aryl, and 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and the 5-10 membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and N and S are optionally oxidized; and the ring-forming carbon atoms of the 5-10 membered heteroaryl and the 4-10 membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; C 3~6 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 The aryl and 5- to 10-membered heteroaryl are each optionally represented by R 20 is substituted with 1 or 2 substituents independently selected from
[0069] In another embodiment, Cy 2is a 4- to 10-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 10-membered heterocycloalkyl optionally has R 20 is substituted with 1 or 2 substituents independently selected from
[0070] In yet another embodiment, Cy 2 is a 4- to 6-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 6-membered heterocycloalkyl optionally has R 20 is replaced once by
[0071] In yet another embodiment, Cy 2 is selected from 4-(piperidin-1-yl)prop-2-en-1-one, 3-(piperidin-1-yl)prop-2-en-1-one, 3-azetidin-1-yl)prop-2-en-1-one, and 3-pyrrolidin-1-yl)prop-2-en-1-one. 2 is 4-(piperidin-1-yl)prop-2-en-1-one. In one embodiment, Cy 2 is 3-(piperidin-1-yl)prop-2-en-1-one. In another embodiment, Cy 2 is 3-(azetidin-1-yl)prop-2-en-1-one. 2 is 3-(pyrrolidin-1-yl)prop-2-en-1-one.
[0072] In one embodiment, Cy 2 is one or two R 20 In yet another embodiment, R is a 4-6 membered heterocycloalkyl optionally substituted with 20 is C(O)R b20 is.
[0073] In one embodiment, Cy2 teeth, [Table 1] is selected from.
[0074] In another embodiment, Cy 2 Cy 2 In yet another embodiment, Cy 2 Cy 2 In yet another embodiment, Cy 2 Cy 2 In one embodiment, Cy 2 Cy 2 -d.
[0075] In yet another embodiment, Cy 2 teeth, [Table 2] is selected from In the formula, n is 0, 1, or 2.
[0076] In one embodiment, Cy 2 Cy 2 In another embodiment, Cy 2 Cy 2 In yet another embodiment, Cy 2 Cy 2 In yet another embodiment, Cy 2 Cy 2 -d1. In one embodiment, Cy 2 Cy 2 -e.
[0077] In one embodiment, n is 0. In another embodiment, n is 1. In yet another embodiment, n is 2.
[0078] In one embodiment, each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C1~6 Haloalkyl, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 ,OC(O)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , N.R. c20 S(O)2R b20 , N.R. c20 S(O)NR c20 R d20 , S(O)2R b20 , and S(O)NR c20 R d20 are independently selected from
[0079] In yet another embodiment, each R 20 is C(O)R b20 , C(O)NR c20 R d20 , and C(O)OR a20 In yet another embodiment, each R 20 is C(O)R b20 is.
[0080] In one embodiment, each R 20 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 , and NR c20 R d20 C1~6 The alkyl is optionally R 21 and is substituted with 1, 2, 3, or 4 substituents independently selected from:
[0081] In one embodiment, each R 20 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, and C(O)R b20 C 1~6 The alkyl is optionally R 21 In one embodiment, each R 20 is C 1~6 Alkyl, CN, and C(O)R b20 C 1~6 The alkyl is optionally R 21 is substituted with 1 or 2 substituents independently selected from
[0082] In another embodiment, each R 21 is C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , and NR c21 R d21 In another embodiment, each R 21 is C 1~6 Alkyl, C 1~6 Haloalkyl, halo, D, CN, and OR a21 In another embodiment, R 21 is CN.
[0083] In another embodiment, each R g D, OH, CN, halo, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 1~6 Alkoxy, C 1~6 Haloalkoxy, C 1~3 Alkoxy-C 1~3 Alkyl, C1~3 Alkoxy-C 1~3 Alkoxy, HO-C 1~3 Alkoxy, HO-C 1~3 Alkyl, Cyano-C 1~3 Alkyl, H2N-C 1~3 Alkyl, Amino, C 1~6 Alkylamino, di(C 1~6 Alkyl)amino, C 1~6 Alkylthio, C 1~6 Alkyl sulfonyl, carbamyl, C 1~6 Alkylcarbamyl and di(C 1~6 alkyl)carbamyl.
[0084] In one embodiment of Formula Ia or a pharmaceutically acceptable salt thereof, Y is N or C; R 1 is H; R 2 is H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, and halo, wherein alkyl is optionally substituted one time with CN; Cy 1 is C 6~10 aryl and 6- to 10-membered heteroaryl, wherein the 6- to 10-membered heteroaryl has at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O; 6~10 The aryl and 6- to 10-membered heteroaryl are each optionally selected from OH, halo, C 1~6 Alkyl, C 1~6 substituted with 1, 2, or 3 substituents independently selected from haloalkyl, and CN; R 3 is H, C 3~10 Cycloalkyl, 4-10 membered heterocycloalkyl, halo, and OC 1~6 alkyl, and 1~6 Alkyl, C 3~10 The cycloalkyl and 4- to 10-membered heterocycloalkyl are each optionally selected from N(C 1~6 Alkyl)2, C 1~6Alkyl, and optionally C 1~6 substituted with 1, 2, or 3 substituents independently selected from 4- to 6-membered heterocycloalkyl substituted with alkyl; R 5 is H, C 1~6 Alkyl, C 6~10 Aryl, 5-6 membered heteroaryl, C 1~6 Haloalkyl, halo, C(O)NH(C 1~6 alkyl), and 4- to 6-membered heterocycloalkyl, wherein the heteroaryl, heterocycloalkyl, and alkyl are optionally selected from C 1~6 Alkyl, OH, C 6~10 Aryl, and N(C 1~6 substituted with 1 or 2 substituents selected from alkyl); If Y is N, then R 6 does not exist; R 6 is H, C 1~6 Alkyl, 5-6 membered heteroaryl, and C 1~6 haloalkyl, wherein alkyl and heteroaryl are optionally selected from C 1~6 Alkyl, C(O)OC 1~6 Alkyl, C(O)N(C 1~6 Alkyl)2, C 6~10 substituted with 1 or 2 substituents selected from aryl, and C(O)(4-6 membered heterocycloalkyl); R 7 is selected from H and halo; Cy 2 is selected from 4- to 6-membered heterocycloalkyl, wherein the 4- to 6-membered heterocycloalkyl has at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 6-membered heterocycloalkyl is optionally C(O)C 2~6 Alkenyl, C(O)C 2~6 Alkynyl, C 1~6 and alkyl, wherein the alkenyl and alkyl are optionally substituted with 1, 2, or 3 substituents independently selected from CN, N(C 1~6 Alkyl)2, OC 1~6It is substituted once or twice with a substituent selected from alkyl and halo.
[0085] In one embodiment, the compound of formula I is 1-(4-(8-chloro-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-1H-pyrazolo[4,3-c]-quinolin-1-yl)-piperidin-1-yl)prop-2-en-1-one or 1-(4-(8-chloro-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-1-yl)prop-2-en-1-one, or a pharmaceutically acceptable salt thereof.
[0086] In another embodiment, the compound of formula I is 2-((2S,4S)-1-acryloyl-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4,4-difluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4,4-difluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4,4-difluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(5-fluoroquinolin-8-yl)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-Acryloyl-4-(8-chloro-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(isoquinolin-4-yl)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-Acryloyl-4-(8-chloro-7-(2-chloro-3-methylphenyl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(2-chloro-3-methylphenyl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-Acryloyl-4-(8-chloro-7-(2,3-dichlorophenyl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(2,3-dichlorophenyl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(3-methyl-2-(trifluoromethyl)phenyl)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-6-fluoro-7-(3-methyl-2-(trifluoromethyl)phenyl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; Methyl 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-2-yl)propanoate; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-2-yl)-N,N-dimethylpropanamide; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-2-propyl-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-2-(1-methyl-1H-pyrazol-4-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-phenyl-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-(pyridin-3-yl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-3-(2-methyloxazol-5-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-(2-methylthiazol-5-yl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; and 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-3-(1-methyl-1H-pyrazol-4-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; or a pharmaceutically acceptable salt thereof.
[0087] In yet another embodiment, the compound of formula I is 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-2-(1-methyl-1H-pyrazol-3-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(2-benzyl-1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-(1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-(6-oxo-1,6-dihydropyridin-3-yl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-3-chloro-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 1-(2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-6-fluoro-N-(2-hydroxyethyl)-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinoline-3-carboxamide; N-benzyl-1-(2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinoline-3-carboxamide; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-3-(hydroxymethyl)-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 3-(1-((1R,4R,5S)-2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-4-ethoxy-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-1H-pyrrolo[3,2-c]quinolin-2-yl)-N,N-dimethylpropanamide; Methyl 3-(1-((1R,4R,5S)-2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-3-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-methoxy-1H-pyrrolo[3,2-c]quinolin-2-yl)propanoate; 3-(2-(3-(azetidin-1-yl)-3-oxopropyl)-1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(7-fluoronaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-fluorobut-2-enoyl)piperidin-4-yl)-6-fluoro-8-methyl-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-(2-fluoroacryloyl)piperidin-4-yl)-6-fluoro-8-methyl-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-1-(but-2-ynoyl)-2-(cyanomethyl)piperidin-4-yl)-6-fluoro-8-methyl-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-methoxybut-2-enoyl)piperidin-4-yl)-6-fluoro-8-methyl-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-fluorobut-2-enoyl)piperidin-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-(2-fluoroacryloyl)piperidin-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-methoxybut-2-enoyl)piperidin-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-fluorobut-2-enoyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-(2-fluoroacryloyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-1-(but-2-ynoyl)-2-(cyanomethyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-methoxybut-2-enoyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; and 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; or a pharmaceutically acceptable salt thereof.
[0088] In another aspect, the present disclosure provides a pharmaceutical composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
[0089] In one aspect, the description provides a method of inhibiting a KRAS protein having a G12C mutation, the method comprising contacting KRAS with a compound of the present disclosure.
[0090] In another aspect, the present disclosure provides a method of inhibiting a KRAS protein having a G12D mutation, the method comprising contacting KRAS with a compound of the present disclosure.
[0091] In yet another aspect, the present disclosure provides a method of inhibiting a KRAS protein having a G12V mutation, the method comprising contacting KRAS with a compound of the present disclosure.
[0092] In one embodiment, the compound of the formula herein is a compound of that formula or a pharmaceutically acceptable salt thereof.
[0093] It will be further recognized that certain features of the invention, which are, for clarity, described in the context of separate embodiments, may also be provided in combination in a single embodiment (with the understanding that the embodiments are also intended to be combined as if set forth in multiple sub-embodiments). Conversely, various features of the invention, which are, for brevity, described in the context of a single embodiment, may also be provided separately or in any suitable subcombination. Thus, it is contemplated that features described as embodiments of compounds of Formula I may be combined in any suitable combination.
[0094] At various places in the present specification, certain features of compounds are disclosed in groups or ranges. It is specifically intended that such disclosures include any and all individual subcombinations of the members of such groups and ranges. For example, "C 1~6 The term "alkyl" is specifically intended to individually disclose (but not be limited to) methyl, ethyl, C3 alkyl, C4 alkyl, C5 alkyl, and C6 alkyl.
[0095] The term "n-membered," where n is an integer, typically refers to the number of ring-forming atoms in a moiety having n ring-forming atoms. For example, piperidinyl is an example of a 6-membered heterocycloalkyl ring, pyrazolyl is an example of a 5-membered heteroaryl ring, pyridyl is an example of a 6-membered heteroaryl ring, and 1,2,3,4-tetrahydro-naphthalene is an example of a 10-membered cycloalkyl group.
[0096] At various points in this specification, variable letters may be found that define divalent linking groups. Each linking substituent is specifically intended to include both the forward and reverse forms of the linking substituent. For example, -NR(CR'R'') n -NR(CR'R'') n -and-(CR'R'')n It is intended that both NR- and NR- are included, and each form is individually disclosed. When a structure requires a linking group, it is understood that the Markush variable listed for that group is the linking group. For example, when a structure requires a linking group and the Markush group definition for that variable lists "alkyl" or "aryl," it is understood that "alkyl" or "aryl" represents a linking alkylene group or arylene group, respectively.
[0097] The term "substituted" means that an atom or group of atoms formally replaces hydrogen as a "substituent" attached to another group. The term "substituted," unless otherwise indicated, refers to any level of substitution, where such substitution is possible, e.g., mono-, di-, tri-, tetra-, or penta-substitution. Substituents are independently selected, and substitution may occur at any chemically accessible position. It should be understood that substitution at a given atom is limited by valence. It should be understood that substitution at a given atom results in a chemically stable molecule. The phrase "optionally substituted" means unsubstituted or substituted. The term "substituted" means that a hydrogen atom has been removed and replaced with a substituent. A single divalent substituent, e.g., oxo, can be replaced with two hydrogen atoms.
[0098] "C n~m " denotes an inclusive range, where n and m are integers and indicate the number of carbons. Examples include C 1~4 , C 1~6 etc.
[0099] The term "alkyl", used alone or in combination with other terms, refers to a saturated hydrocarbon group which may be straight-chained or branched. n~mThe term "alkyl" refers to an alkyl group having n to m carbon atoms. An alkyl group formally corresponds to an alkane with one C-H bond replaced at the point of attachment of the alkyl group to the remainder of the compound. In some embodiments, an alkyl group contains 1 to 6 carbon atoms, 1 to 4 carbon atoms, 1 to 3 carbon atoms, or 1 to 2 carbon atoms. Examples of alkyl moieties include, but are not limited to, chemical groups such as methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, isobutyl, sec-butyl; higher homologs such as 2-methyl-1-butyl, n-pentyl, 3-pentyl, n-hexyl, 1,2,2-trimethylpropyl, and the like.
[0100] The term "alkenyl," used alone or in combination with other terms, refers to a straight-chain or branched hydrocarbon group corresponding to an alkyl group having one or more double carbon-carbon bonds. An alkenyl group formally corresponds to an alkene in which one C-H bond is replaced at the point of attachment of the alkenyl group to the remainder of the compound. The term "Cn-m alkenyl" refers to an alkenyl group having n to m carbons. In some embodiments, the alkenyl moiety contains 2 to 6, 2 to 4, or 2 to 3 carbon atoms. Examples of alkenyl groups include, but are not limited to, ethenyl, n-propenyl, isopropenyl, n-butenyl, sec-butenyl, and the like.
[0101] The term "alkynyl," used alone or in combination with other terms, refers to a straight-chain or branched hydrocarbon group corresponding to an alkyl group having one or more triple carbon-carbon bonds. An alkynyl group formally corresponds to an alkyne in which one C-H bond is replaced at the point of attachment of the alkyl group to the remainder of the compound. n~mThe term "alkynyl" refers to an alkynyl group having n to m carbons. Examples of alkynyl groups include, but are not limited to, ethynyl, propyn-1-yl, propyn-2-yl, and the like. In some embodiments, the alkynyl moiety contains 2 to 6, 2 to 4, or 2 to 3 carbon atoms.
[0102] The term "alkylene," used alone or in combination with other terms, refers to a divalent alkyl linking group. An alkylene group formally corresponds to an alkane in which two C-H bonds are replaced at the alkylene group's attachment points to the remainder of the compound. The term "Cn-m alkylene" refers to an alkylene group having n to m carbon atoms. Examples of alkylene groups include, but are not limited to, ethane-1,2-diyl, ethane-1,1-diyl, propane-1,3-diyl, propane-1,2-diyl, propane-1,1-diyl, butane-1,4-diyl, butane-1,3-diyl, butane-1,2-diyl, 2-methyl-propane-1,3-diyl, and the like.
[0103] The term "alkoxy", used alone or in combination with other terms, refers to a radical of the formula -O-alkyl, where the alkyl group is as defined above. n~m The term "alkoxy" refers to an alkoxy group, the alkyl group of which has n to m carbons. Examples of alkoxy groups include methoxy, ethoxy, propoxy (e.g., n-propoxy and isopropoxy), t-butoxy, and the like. In some embodiments, the alkyl group has 1 to 6, 1 to 4, or 1 to 3 carbon atoms. "C n~m The term "dialkoxy" refers to a group of the formula -O-(C n~m Dialkyloxy refers to a linking group of -O-, where the alkyl group has n to m carbon atoms. Examples of dialkyloxy groups include -OCH2CH2O- and OCH2CH2CH2O-. In some embodiments, C n~m Two O atoms of a dialkoxy group may be attached to the same B atom to form a 5- or 6-membered heterocycloalkyl group.
[0104] The term "alkylthio", employed alone or in combination with other terms, refers to a radical of the formula --S-alkyl, where the alkyl radical is as defined above.
[0105] The term "amino," used alone or in combination with other terms, refers to a group of formula -NH, where the hydrogen atom can be optionally substituted with a substituent described herein. For example, "alkylamino" can refer to both -NH(alkyl) and -N(alkyl).
[0106] The term "carbonyl", used alone or in combination with other terms, refers to a -C(=O)- group, which can also be written as C(O).
[0107] The term "cyano" or "nitrile" refers to a group of formula -C≡N, which can also be written as -CN.
[0108] The term "carbamyl," as used herein, refers to an -NHC(O)O- or -OC(O)NH- group in which the carbon atom ...
Claims
1. 1. A medicament for treating solid tumors, comprising a compound of formula I: 【Chemistry 1】 (In the formula, each 【Chemistry 2】 independently represent a single or double bond; X is N or CR 7 and Y is N or C; R 1 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, CN, OR a1 , S.R. a1 , C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 , O.C.(O.)R b1 , OC(O)NR c1 R d1 , N.R. c1 R d1 , N.R. c1 C(O)R b1 , N.R. c1 C(O)OR a1 , N.R. c1 C(O)NR c1 R d1 , N.R. c1 S(O)R b1 , N.R. c1 S (O) 2 R b1 , N.R. c1 S (O) 2 NR c1 R d1 , S(O)R b1 , S(O)NR c1 R d1 , S(O) 2 R b1 , S(O) 2 NR c1 R d1 , and B.R. h1 R i1 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a2 , S.R. a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 , O.C.(O.)R b2 , OC(O)NR c2 R d2 , N.R. c2 R d2 , N.R. c2 C(O)R b2 , N.R. c2 C(O)OR a2 , N.R. c2 C(O)NR c2 R d2 , C(=NR e2 ) R b2 , C(=NOR a2 ) R b2 , C(=NR e2 ) NR c2 R d2 , N.R. c2 C (=NR e2 ) NR c2 R d2 , N.R. c2 C (=NR e2 ) R b2 , N.R. c2 S(O)R b2 , N.R. c2 S (O) 2 R b2 , N.R. c2 S (O) 2 NR c2 R d2 , S(O)R b2 , S(O)NR c2 R d2 , S(O) 2 R b2 , S(O) 2 NR c2 R d2 , and B.R. h2 R i2 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 22 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Cy 1 is C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl, wherein the 4- to 10-membered heterocycloalkyl and the 5- to 10-membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and the N and the S are optionally oxidized; the ring-forming carbon atoms of the 5- to 10-membered heteroaryl and the 4- to 10-membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; and the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 10 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR f3 , S.R. a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , O.C.(O.)R b3 , OC(O)NR c3 R d3 , N.R. c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , N.R. c3 C(O)NR c3 R d3 , C(=NR e3 ) R b3 , C(=NOR a3 ) R b3 , C(=NR e3 ) NR c3 R d3 , N.R. c3 C (=NR e3 ) NR c3 R d3 , N.R. c3 C (=NR e3 ) R b3 , N.R. c3 S(O)R b3 , N.R. c3 S (O) 2 R b3 , N.R. c3 S (O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , S(O) 2 NR c3 R d3 , and B.R. h3 R i3 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 30 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from 【Transformation 3】 is a single bond and Y is C, 6 is selected from C=O and C=S; R 4 H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, 4-6 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, halo, CN, OR a4 , S.R. a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 , O.C.(O.)R b4 , OC(O)NR c4 R d4 , N.R. c4 R d4 , N.R. c4 C(O)R b4 , N.R. c4 C(O)OR a4 , N.R. c4 C(O)NR c4 R d4 , N.R. c4 S(O)R b4 , N.R. c4 S (O) 2 R b4 , N.R. c4 S (O) 2 NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , S(O) 2 NR c4 R d4 , and B.R. h4 R i4 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the 4- to 6-membered heterocycloalkyl, the phenyl, and the 5- to 6-membered heteroaryl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , O.C.(O.)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , N.R. c5 C(O)NR c5 R d5 , C(=NR e5 ) R b5 , C(=NOR a5 ) R b5 , C(=NR e5 ) NR c5 R d5 , N.R. c5 C (=NR e5 ) NR c5 R d5 , N.R. c5 C (=NR e5 ) R b5 , N.R. c5 S(O)R b5 , N.R. c5 S (O) 2 R b5 , N.R. c5 S (O) 2 NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , S(O) 2 NR c5 R d5 , and B.R. h5 R i5 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 50 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from 【Chemistry 4】 is a double bond and Y is N, then R 4 and R 6 does not exist; 【Transformation 5】 is a double bond and Y is C, then R 4 does not exist; R 6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 , O.C.(O.)R b6 , OC(O)NR c6 R d6 , N.R. c6 R d6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , C(=NR e6 ) R b6 , C(=NOR a6 ) R b6 , C(=NR e6 ) NR c6 R d6 , N.R. c6 C (=NR e6 ) NR c6 R d6 , N.R. c6 C (=NR e6 ) R b6 , N.R. c6 S(O)R b6 , N.R. c6 S (O) 2 R b6 , N.R. c6 S (O) 2 NR c6 R d6 , S(O)R b6 , S(O)NR c6 R d6 , S(O) 2 R b6 , S(O) 2 NR c6 R d6 , and B.R. h6 R i6 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 60 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7 , O.C.(O.)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , C(=NR e7 ) R b7 , C(=NOR a7 ) R b7 , C(=NR e7 ) NR c7 R d7 , N.R. c7 C (=NR e7 ) NR c7 R d7 , N.R. c7 C (=NR e7 ) R b7 , N.R. c7 S(O)R b7 , N.R. c7 S (O) 2 R b7 , N.R. c7 S (O) 2 NR c7 R d7 , S(O)R b7 , S(O)NR c7 R d7 , S(O) 2 R b7 , S(O) 2 NR c7 R d7 , and B.R. h7 R i7 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 70 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Cy 2 is C 3~10 cycloalkyl, 4- to 14-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl, wherein the 4- to 14-membered heterocycloalkyl and the 5- to 10-membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and the N and the S are optionally oxidized; the ring-forming carbon atoms of the 5- to 10-membered heteroaryl and the 4- to 14-membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; and the C 3~10 cycloalkyl, the 4- to 14-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 20 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a10 , S.R. a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 , O.C.(O.)R b10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R. c10 C(O)R b10 , N.R. c10 C(O)OR a10 , N.R. c10 C(O)NR c10 R d10 , C(=NR e10 ) R b10 , C(=NOR a10 ) R b10 , C(=NR e10 ) NR c10 R d10 , N.R. c10 C (=NR e10 ) NR c10 R d10 , N.R. c10 S(O)R b10 , N.R. c10 S (O) 2 R b10 , N.R. c10 S (O) 2 NR c10 R d10 , S(O)R b10 , S(O)NR c10 R d10 , S(O) 2 R b10 , S(O) 2 NR c10 R d10 , and B.R. h10 R i10 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 11 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 11 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a11 , S.R. a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 , O.C.(O.)R b11 , OC(O)NR c11 R d11 , N.R. c11 R d11 , N.R. c11 C(O)R b11 , N.R. c11 C(O)OR a11 , N.R. c11 C(O)NR c11 R d11 , N.R. c11 S(O)R b11 , N.R. c11 S (O) 2 R b11 , N.R. c11 S (O) 2 NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , S(O) 2 NR c11 R d11 , and B.R. h11 R i11 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 12 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 12 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a12 , S.R. a12 , C(O)R b12 , C(O)NR c12 R d12 , C(O)OR a12 , O.C.(O.)R b12 , OC(O)NR c12 R d12 , N.R. c12 R d12 , N.R. c12 C(O)R b12 , N.R. c12 C(O)OR a12 , N.R. c12 C(O)NR c12 R d12 , N.R. c12 S(O)R b12 , N.R. c12 S (O) 2 R b12 , N.R. c12 S (O) 2 NR c12 R d12 , S(O)R b12 , S(O)NR c12 R d12 , S(O) 2 R b12 , S(O) 2 NR c12 R d12 , and B.R. h12 R i12 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a20 , S.R. a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 , O.C.(O.)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , C(=NR e20 ) R b20 , C(=NOR a20 ) R b20 , C(=NR e20 ) NR c20 R d20 , N.R. c20 C (=NR e20 ) NR c20 R d20 , N.R. c20 S(O)R b20 , N.R. c20 S (O) 2 R b20 , N.R. c20 S (O) 2 NR c20 R d20 , S(O)R b20 , S(O)NR c20 R d20 , S(O) 2 R b20 , S(O) 2 NR c20 R d20 , and B.R. h20 R i20 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 21 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 21 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a21 , S.R. a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 , O.C.(O.)R b21 , OC(O)NR c21 R d21 , N.R. c21 R d21 , N.R. c21 C(O)R b21 , N.R. c21 C(O)OR a21 , N.R. c21 C(O)NR c21 R d21 , N.R. c21 S(O)R b21 , N.R. c21 S (O) 2 R b21 , N.R. c21 S (O) 2 NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 , S(O) 2 R b21 , S(O) 2 NR c21 R d21 , and B.R. h21 R i21 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 22 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a22 , S.R. a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 , O.C.(O.)R b22 , OC(O)NR c22 R d22 , N.R. c22 R d22 , N.R. c22 C(O)R b22 , N.R. c22 C(O)OR a22 , N.R. c22 C(O)NR c22 R d22 , N.R. c22 S(O)R b22 , N.R. c22 S (O) 2 R b22 , N.R. c22 S (O) 2 NR c22 R d22 , S(O)R b22 , S(O)NR c22 R d22 , S(O) 2 R b22 , S(O) 2 NR c22 R d22 , and B.R. h22 R i22 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 23 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 23 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a23 , S.R. a23 , C(O)R b23 , C(O)NR c23 R d23 , C(O)OR a23 , O.C.(O.)R b23 , OC(O)NR c23 R d23 , N.R. c23 R d23 , N.R. c23 C(O)R b23 , N.R. c23 C(O)OR a23 , N.R. c23 C(O)NR c23 R d23 , N.R. c23 S(O)R b23 , N.R. c23 S (O) 2 R b23 , N.R. c23 S (O) 2 NR c23 R d23 , S(O)R b23 , S(O)NR c23 R d23 , S(O) 2 R b23 , S(O) 2 NR c23 R d23 , and B.R. h23 R i23 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 24 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 24 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a24 , S.R. a24 , C(O)R b24 , C(O)NR c24 R d24 , C(O)OR a24 , O.C.(O.)R b24 , OC(O)NR c24 R d24 , N.R. c24 R d24 , N.R. c24 C(O)R b24 , N.R. c24 C(O)OR a24 , N.R. c24 C(O)NR c24 R d24 , N.R. c24 S(O)R b24 , N.R. c24 S (O) 2 R b24 , N.R. c24 S (O) 2 NR c24 R d24 , S(O)R b24 , S(O)NR c24 R d24 , S(O) 2 R b24 , S(O) 2 NR c24 R d24 , and B.R. h24 R i24 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 30 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a30 , S.R. a30 , C(O)R b30 , C(O)NR c30 R d30 , C(O)OR a30 , O.C.(O.)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , N.R. c30 C(O)NR c30 R d30 , N.R. c30 S(O)R b30 , N.R. c30 S (O) 2 R b30 , N.R. c30 S (O) 2 NR c30 R d30 , S(O)R b30 , S(O)NR c30 R d30 , S(O) 2 R b30 , S(O) 2 NR c30 R d30 , and B.R. h30 R i30 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 31 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 31 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a31 , S.R. a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 , O.C.(O.)R b31 , OC(O)NR c31 R d31 , N.R. c31 R d31 , N.R. c31 C(O)R b31 , N.R. c31 C(O)OR a31 , N.R. c31 C(O)NR c31 R d31 , N.R. c31 S(O)R b31 , N.R. c31 S (O) 2 R b31 , N.R. c31 S (O) 2 NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 , S(O) 2 R b31 , S(O) 2 NR c31 R d31 , and B.R. h31 R i31 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 32 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 32 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a32 , S.R. a32 , C(O)R b32 , C(O)NR c32 R d32 , C(O)OR a32 , O.C.(O.)R b32 , OC(O)NR c32 R d32 , N.R. c32 R d32 , N.R. c32 C(O)R b32 , N.R. c32 C(O)OR a32 , N.R. c32 C(O)NR c32 R d32 , N.R. c32 S(O)R b32 , N.R. c32 S (O) 2 R b32 , N.R. c32 S (O) 2 NR c32 R d32 , S(O)R b32 , S(O)NR c32 R d32 , S(O) 2 R b32 , S(O) 2 NR c32 R d32 , and B.R. h32 R i32 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 50 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a50 , S.R. a50 , C(O)R b50 , C(O)NR c50 R d50 , C(O)OR a50 , O.C.(O.)R b50 , OC(O)NR c50 R d50 , N.R. c50 R d50 , N.R. c50 C(O)R b50 , N.R. c50 C(O)OR a50 , N.R. c50 C(O)NR c50 R d50 , N.R. c50 S(O)R b50 , N.R. c50 S (O) 2 R b50 , N.R. c50 S (O) 2 NR c50 R d50 , S(O)R b50 , S(O)NR c50 R d50 , S(O) 2 R b50 , S(O) 2 NR c50 R d50 , and B.R. h50 R i50 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 51 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 51 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 6~10 Aryl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a51 , S.R. a51 , C(O)R b51 , C(O)NR c51 R d51 , C(O)OR a51 , O.C.(O.)R b51 , OC(O)NR c51 R d51 , N.R. c51 R d51 , N.R. c51 C(O)R b51 , N.R. c51 C(O)OR a51 , N.R. c51 C(O)NR c51 R d51 , N.R. c51 S(O)R b51 , N.R. c51 S (O) 2 R b51 , N.R. c51 S (O) 2 NR c51 R d51 , S(O)R b51 , S(O)NR c51 R d51 , S(O) 2 R b51 , S(O) 2 NR c51 R d51 , and B.R. h51 R i51 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 cycloalkyl, the C 6~10 The aryl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R 52 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 52 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a52 , S.R. a52 , C(O)R b52 , C(O)NR c52 R d52 , C(O)OR a52 , O.C.(O.)R b52 , OC(O)NR c52 R d52 , N.R. c52 R d52 , N.R. c52 C(O)R b52 , N.R. c52 C(O)OR a52 , N.R. c52 C(O)NR c52 R d52 , N.R. c52 S(O)R b52 , N.R. c52 S (O) 2 R b52 , N.R. c52 S (O) 2 NR c52 R d52 , S(O)R b52 , S(O)NR c52 R d52 , S(O) 2 R b52 , S(O) 2 NR c52 R d52 , and B.R. h52 R i52 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 60 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a60 , S.R. a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 , O.C.(O.)R b60 , OC(O)NR c60 R d60 , N.R. c60 R d60 , N.R. c60 C(O)R b60 , N.R. c60 C(O)OR a60 , N.R. c60 C(O)NR c60 R d60 , N.R. c60 S(O)R b60 , N.R. c60 S (O) 2 R b60 , N.R. c60 S (O) 2 NR c60 R d60 , S(O)R b60 , S(O)NR c60 R d60 , S(O) 2 R b60 , S(O) 2 NR c60 R d60 , and B.R. h60 R i60 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 61 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 61 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a61 , S.R. a61 , C(O)R b61 , C(O)NR c61 R d61 , C(O)OR a61 , O.C.(O.)R b61 , OC(O)NR c61 R d61 , N.R. c61 R d61 , N.R. c61 C(O)R b61 , N.R. c61 C(O)OR a61 , N.R. c61 C(O)NR c61 R d61 , N.R. c61 S(O)R b61 , N.R. c61 S (O) 2 R b61 , N.R. c61 S (O) 2 NR c61 R d61 , S(O)R b61 , S(O)NR c61 R d61 , S(O) 2 R b61 , S(O) 2 NR c61 R d61 , and B.R. h61 R i61 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 62 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 62 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a62 , S.R. a62 , C(O)R b62 , C(O)NR c62 R d62 , C(O)OR a62 , O.C.(O.)R b62 , OC(O)NR c62 R d62 , N.R. c62 R d62 , N.R. c62 C(O)R b62 , N.R. c62 C(O)OR a62 , N.R. c62 C(O)NR c62 R d62 , N.R. c62 S(O)R b62 , N.R. c62 S (O) 2 R b62 , N.R. c62 S (O) 2 NR c62 R d62 , S(O)R b62 , S(O)NR c62 R d62 , S(O) 2 R b62 , S(O) 2 NR c62 R d62 , and B.R. h62 R i62 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 70 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a70 , S.R. a70 , C(O)R b70 , C(O)NR c70 R d70 , C(O)OR a70 , O.C.(O.)R b70 , OC(O)NR c70 R d70 , N.R. c70 R d70 , N.R. c70 C(O)R b70 , N.R. c70 C(O)OR a70 , N.R. c70 C(O)NR c70 R d70 , N.R. c70 S(O)R b70 , N.R. c70 S (O) 2 R b70 , N.R. c70 S (O) 2 NR c70 R d70 , S(O)R b70 , S(O)NR c70 R d70 , S(O) 2 R b70 , S(O) 2 NR c70 R d70 , and B.R. h70 R i70 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 71 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 71 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a71 , S.R. a71 , C(O)R b71 , C(O)NR c71 R d71 , C(O)OR a71 , O.C.(O.)R b71 , OC(O)NR c71 R d71 , N.R. c71 R d71 , N.R. c71 C(O)R b71 , N.R. c71 C(O)OR a71 , N.R. c71 C(O)NR c71 R d71 , N.R. c71 S(O)R b71 , N.R. c71 S (O) 2 R b71 , N.R. c71 S (O) 2 NR c71 R d71 , S(O)R b71 , S(O)NR c71 R d71 , S(O) 2 R b71 , S(O) 2 NR c71 R d71 , and B.R. h71 R i71 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 72 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from Each R 72 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a72 , S.R. a72 , C(O)R b72 , C(O)NR c72 R d72 , C(O)OR a72 , O.C.(O.)R b72 , OC(O)NR c72 R d72 , N.R. c72 R d72 , N.R. c72 C(O)R b72 , N.R. c72 C(O)OR a72 , N.R. c72 C(O)NR c72 R d72 , N.R. c72 S(O)R b72 , N.R. c72 S (O) 2 R b72 , N.R. c72 S (O) 2 NR c72 R d72 , S(O)R b72 , S(O)NR c72 R d72 , S(O) 2 R b72 , S(O) 2 NR c72 R d72 , and B.R. h72 R i72 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R a1 , R b1 , R c1 , and R d1 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R g optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c1 and R d1 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h1 and R i1 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h1 and R i1 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a2 , R b2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 22 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c2 and R d2 together with the N atom to which they are attached, R 22 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e2 are H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h2 and R i2 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h2 and R i2 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c3 and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e3 are H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R f3 and R j3 are respectively, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h3 and R i3 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h3 and R i3 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a4 , R b4 , R c4 , and R d4 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R g optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c4 and R d4 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h4 and R i4 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h4 and R i4 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a5 , R b5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 50 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e5 are H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h5 and R i5 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h5 and R i5 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a6 , R b6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 60 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e6 are H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h6 and R i6 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h6 and R i6 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a7 , R b7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 70 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c7 and R d7 together with the N atom to which they are attached, R 70 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e7 are H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h7 and R i7 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h7 and R i7 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 11 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c10 and R d10 together with the N atom to which they are attached, R 11 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e10 are H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h10 and R i10 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h10 and R i10 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a11 , R b11 , R c11 , and R d11 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R 12 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c11 and R d11 together with the N atom to which they are attached, R 12 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h11 and R i11 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h11 and R i11 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a12 , R b12 , R c12 , and R d12 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl; 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R h12 and R i12 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h12 and R i12 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 21 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c20 and R d20 together with the N atom to which they are attached, R 21 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e20 are H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h20 and R i20 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h20 and R i20 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a21 , R b21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R g optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c21 and R d21 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h21 and R i21 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h21 and R i21 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a22 , R b22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 23 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c22 and R d22 together with the N atom to which they are attached, R 23 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h22 and R i22 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h22 and R i22 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a23 , R b23 , R c23 , and R d23 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R 24 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c23 and R d23 together with the N atom to which they are attached, R 24 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h23 and R i23 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h23 and R i23 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a24 , R b24 , R c24 , and R d24 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl; 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R h24 and R i24 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h24 and R i24 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 31 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h30 and R i30 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h30 and R i30 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R 32 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c31 and R d31 together with the N atom to which they are attached, R 32 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h31 and R i31 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h31 and R i31 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a32 , R b32 , R c32 , and R d32 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl; 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R h32 and R i32 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h32 and R i32 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a50 , R b50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 51 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c50 and R d50 together with the N atom to which they are attached, R 51 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h50 and R i50 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h50 and R i50 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a51 , R b51 , R c51 , and R d51 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R 52 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c51 and R d51 together with the N atom to which they are attached, R 52 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h51 and R i51 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h51 and R i51 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a52 , R b52 , R c52 , and R d52 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl; 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R h52 and R i52 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy; or any R bonded to the same B atom h52 and R i52 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 61 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c60 and R d60 together with the N atom to which they are attached, R 61 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h60 and R i60 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h60 and R i60 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a61 , R b61 , R c61 , and R d61 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R 62 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c61 and R d61 together with the N atom to which they are attached, R 62 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h61 and R i61 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h61 and R i61 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a62 , R b62 , R c62 , and R d62 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl; 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R g optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c62 and R d62 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h62 and R i62 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h62 and R i62 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a70 , R b70 , R c70 , and R d70 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 71 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c70 and R d70 together with the N atom to which they are attached, R 71 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h70 and R i70 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h70 and R i70 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a71 , R b71 , R c71 , and R d71 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R 72 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c71 and R d71 together with the N atom to which they are attached, R 72 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h71 and R i71 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h71 and R i71 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a72 , R b72 , R c72 , and R d72 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl; 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R h72 and R i72 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h72 and R i72 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; Each R g D, OH, NO 2 , CN, Halo, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 3~6 Cycloalkyl-C 1~2 Alkylene, C 1~6 Alkoxy, C 1~6 Haloalkoxy, C 1~3 Alkoxy-C 1~3 Alkyl, C 1~3 Alkoxy-C 1~3 Alkoxy, HO-C 1~3 Alkoxy, HO-C 1~3 Alkyl, cyano-C 1~3 Alkyl, H 2 N-C 1~3 Alkyl, amino, C 1~6 Alkylamino, di(C 1~6 alkyl) amino, thio, C 1~6 Alkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkyl sulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, carboxy, C 1~6 Alkylcarbonyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkylcarbonylamino, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonyloxy, aminocarbonyloxy, C 1~6 Alkylaminocarbonyloxy, di(C 1~6 alkyl)aminocarbonyloxy, C 1~6 Alkyl sulfonyl amino, amino sulfonyl, C 1~6 Alkylaminosulfonyl, di(C 1~6 alkyl)aminosulfonyl, aminosulfonylamino, C 1~6 Alkylaminosulfonylamino, di(C 1~6 alkyl)aminosulfonylamino, aminocarbonylamino, C 1~6 Alkylaminocarbonylamino, and di(C 1~6 independently selected from: (alkyl)aminocarbonylamino; however, 【Transformation 6】 is a double bond and Y is N, Cy 1 is other than 3,5-dimethylisoxazol-4-yl) or a pharmaceutically acceptable salt thereof.
2. each 【Transformation 7】 independently represent a single bond or a double bond; X is N or CR 7 and Y is N or C; R 1 But H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, CN, OR a1 , S.R. a1 , C(O)R b1 , C(O)NR c1 R d1 , C(O)OR a1 , O.C.(O.)R b1 , OC(O)NR c1 R d1 , N.R. c1 R d1 , N.R. c1 C(O)R b1 , N.R. c1 C(O)OR a1 , N.R. c1 C(O)NR c1 R d1 , N.R. c1 S(O)R b1 , N.R. c1 S (O) 2 R b1 , N.R. c1 S (O) 2 NR c1 R d1 , S(O)R b1 , S(O)NR c1 R d1 , S(O) 2 R b1 , S(O) 2 NR c1 R d1 , and B.R. h1 R i1 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from R 2 But H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a2 , S.R. a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 , O.C.(O.)R b2 , OC(O)NR c2 R d2 , N.R. c2 R d2 , N.R. c2 C(O)R b2 , N.R. c2 C(O)OR a2 , N.R. c2 C(O)NR c2 R d2 , C(=NR e2 ) R b2 , C(=NOR a2 ) R b2 , C(=NR e2 ) NR c2 R d2 , N.R. c2 C (=NR e2 ) NR c2 R d2 , N.R. c2 C (=NR e2 ) R b2 , N.R. c2 S(O)R b2 , N.R. c2 S (O) 2 R b2 , N.R. c2 S (O) 2 NR c2 R d2 , S(O)R b2 , S(O)NR c2 R d2 , S(O) 2 R b2 , S(O) 2 NR c2 R d2 , and B.R. h2 R i2 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 22 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Cy 1 But C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 6- to 10-membered heteroaryl, wherein the 4- to 10-membered heterocycloalkyl and the 6- to 10-membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and the N and the S are optionally oxidized; the ring-forming carbon atoms of the 6- to 10-membered heteroaryl and the 4- to 10-membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; and the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 6- to 10-membered heteroaryl are each R 10 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R 3 But H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR f3 , S.R. a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , O.C.(O.)R b3 , OC(O)NR c3 R d3 , N.R. c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , N.R. c3 C(O)NR c3 R d3 , C(=NR e3 ) R b3 , C(=NOR a3 ) R b3 , C(=NR e3 ) NR c3 R d3 , N.R. c3 C (=NR e3 ) NR c3 R d3 , N.R. c3 C (=NR e3 ) R b3 , N.R. c3 S(O)R b3 , N.R. c3 S (O) 2 R b3 , N.R. c3 S (O) 2 NR c3 R d3 , S(O)R b3 , S(O)NR c3 R d3 , S(O) 2 R b3 , S(O) 2 NR c3 R d3 , and B.R. h3 R i3 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 30 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: 【Transformation 8】 is a single bond and Y is C, 6 is selected from C=O and C=S; R 4 But H, D, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, 4-6 membered heterocycloalkyl, phenyl, 5-6 membered heteroaryl, halo, CN, OR a4 , S.R. a4 , C(O)R b4 , C(O)NR c4 R d4 , C(O)OR a4 , O.C.(O.)R b4 , OC(O)NR c4 R d4 , N.R. c4 R d4 , N.R. c4 C(O)R b4 , N.R. c4 C(O)OR a4 , N.R. c4 C(O)NR c4 R d4 , N.R. c4 S(O)R b4 , N.R. c4 S (O) 2 R b4 , N.R. c4 S (O) 2 NR c4 R d4 , S(O)R b4 , S(O)NR c4 R d4 , S(O) 2 R b4 , S(O) 2 NR c4 R d4 , and B.R. h4 R i4 Selected from: R 5 But H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , O.C.(O.)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , N.R. c5 C(O)NR c5 R d5 , C(=NR e5 ) R b5 , C(=NOR a5 ) R b5 , C(=NR e5 ) NR c5 R d5 , N.R. c5 C (=NR e5 ) NR c5 R d5 , N.R. c5 C (=NR e5 ) R b5 , N.R. c5 S(O)R b5 , N.R. c5 S (O) 2 R b5 , N.R. c5 S (O) 2 NR c5 R d5 , S(O)R b5 , S(O)NR c5 R d5 , S(O) 2 R b5 , S(O) 2 NR c5 R d5 , and B.R. h5 R i5 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 50 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: 【Chemistry 9】 is a double bond and Y is N, then R 4 and R 6 does not exist; 【Chemistry 10】 is a double bond and Y is C, then R 4 does not exist; R 6 But H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 , O.C.(O.)R b6 , OC(O)NR c6 R d6 , N.R. c6 R d6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , C(=NR e6 ) R b6 , C(=NOR a6 ) R b6 , C(=NR e6 ) NR c6 R d6 , N.R. c6 C (=NR e6 ) NR c6 R d6 , N.R. c6 C (=NR e6 ) R b6 , N.R. c6 S(O)R b6 , N.R. c6 S (O) 2 R b6 , N.R. c6 S (O) 2 NR c6 R d6 , S(O)R b6 , S(O)NR c6 R d6 , S(O) 2 R b6 , S(O) 2 NR c6 R d6 , and B.R. h6 R i6 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 60 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R 7 But H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7 , O.C.(O.)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , C(=NR e7 ) R b7 , C(=NOR a7 ) R b7 , C(=NR e7 ) NR c7 R d7 , N.R. c7 C (=NR e7 ) NR c7 R d7 , N.R. c7 C (=NR e7 ) R b7 , N.R. c7 S(O)R b7 , N.R. c7 S (O) 2 R b7 , N.R. c7 S (O) 2 NR c7 R d7 , S(O)R b7 , S(O)NR c7 R d7 , S(O) 2 R b7 , S(O) 2 NR c7 R d7 , and B.R. h7 R i7 and C is selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 70 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Cy 2 But C 3~10 cycloalkyl, 4- to 14-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl, wherein the 4- to 14-membered heterocycloalkyl and the 5- to 10-membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and the N and the S are optionally oxidized; the ring-forming carbon atoms of the 5- to 10-membered heteroaryl and the 4- to 14-membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; and the C 3~10 cycloalkyl, the 4- to 14-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 20 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 10 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a10 , S.R. a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 , O.C.(O.)R b10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R. c10 C(O)R b10 , N.R. c10 C(O)OR a10 , N.R. c10 C(O)NR c10 R d10 , C(=NR e10 ) R b10 , C(=NOR a10 ) R b10 , C(=NR e10 ) NR c10 R d10 , N.R. c10 C (=NR e10 ) NR c10 R d10 , N.R. c10 S(O)R b10 , N.R. c10 S (O) 2 R b10 , N.R. c10 S (O) 2 NR c10 R d10 , S(O)R b10 , S(O)NR c10 R d10 , S(O) 2 R b10 , S(O) 2 NR c10 R d10 , and B.R. h10 R i10 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 11 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 11 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a11 , S.R. a11 , C(O)R b11 , C(O)NR c11 R d11 , C(O)OR a11 , O.C.(O.)R b11 , OC(O)NR c11 R d11 , N.R. c11 R d11 , N.R. c11 C(O)R b11 , N.R. c11 C(O)OR a11 , N.R. c11 C(O)NR c11 R d11 , N.R. c11 S(O)R b11 , N.R. c11 S (O) 2 R b11 , N.R. c11 S (O) 2 NR c11 R d11 , S(O)R b11 , S(O)NR c11 R d11 , S(O) 2 R b11 , S(O) 2 NR c11 R d11 , and B.R. h11 R i11 are independently selected from Each R 20 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a20 , S.R. a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 , O.C.(O.)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , C(=NR e20 ) R b20 , C(=NOR a20 ) R b20 , C(=NR e20 ) NR c20 R d20 , N.R. c20 C (=NR e20 ) NR c20 R d20 , N.R. c20 S(O)R b20 , N.R. c20 S (O) 2 R b20 , N.R. c20 S (O) 2 NR c20 R d20 , S(O)R b20 , S(O)NR c20 R d20 , S(O) 2 R b20 , S(O) 2 NR c20 R d20 , and B.R. h20 R i20 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 21 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 21 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a21 , S.R. a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 , O.C.(O.)R b21 , OC(O)NR c21 R d21 , N.R. c21 R d21 , N.R. c21 C(O)R b21 , N.R. c21 C(O)OR a21 , N.R. c21 C(O)NR c21 R d21 , N.R. c21 S(O)R b21 , N.R. c21 S (O) 2 R b21 , N.R. c21 S (O) 2 NR c21 R d21 , S(O)R b21 , S(O)NR c21 R d21 , S(O) 2 R b21 , S(O) 2 NR c21 R d21 , and B.R. h21 R i21 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R g and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 22 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a22 , S.R. a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 , O.C.(O.)R b22 , OC(O)NR c22 R d22 , N.R. c22 R d22 , N.R. c22 C(O)R b22 , N.R. c22 C(O)OR a22 , N.R. c22 C(O)NR c22 R d22 , N.R. c22 S(O)R b22 , N.R. c22 S (O) 2 R b22 , N.R. c22 S (O) 2 NR c22 R d22 , S(O)R b22 , S(O)NR c22 R d22 , S(O) 2 R b22 , S(O) 2 NR c22 R d22 , and B.R. h22 R i22 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 23 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 23 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a23 , S.R. a23 , C(O)R b23 , C(O)NR c23 R d23 , C(O)OR a23 , O.C.(O.)R b23 , OC(O)NR c23 R d23 , N.R. c23 R d23 , N.R. c23 C(O)R b23 , N.R. c23 C(O)OR a23 , N.R. c23 C(O)NR c23 R d23 , N.R. c23 S(O)R b23 , N.R. c23 S (O) 2 R b23 , N.R. c23 S (O) 2 NR c23 R d23 , S(O)R b23 , S(O)NR c23 R d23 , S(O) 2 R b23 , S(O) 2 NR c23 R d23 , and B.R. h23 R i23 are independently selected from Each R 30 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a30 , S.R. a30 , C(O)R b30 , C(O)NR c30 R d30 , C(O)OR a30 , O.C.(O.)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , N.R. c30 C(O)NR c30 R d30 , N.R. c30 S(O)R b30 , N.R. c30 S (O) 2 R b30 , N.R. c30 S (O) 2 NR c30 R d30 , S(O)R b30 , S(O)NR c30 R d30 , S(O) 2 R b30 , S(O) 2 NR c30 R d30 , and B.R. h30 R i30 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 31 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 31 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a31 , S.R. a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 , O.C.(O.)R b31 , OC(O)NR c31 R d31 , N.R. c31 R d31 , N.R. c31 C(O)R b31 , N.R. c31 C(O)OR a31 , N.R. c31 C(O)NR c31 R d31 , N.R. c31 S(O)R b31 , N.R. c31 S (O) 2 R b31 , N.R. c31 S (O) 2 NR c31 R d31 , S(O)R b31 , S(O)NR c31 R d31 , S(O) 2 R b31 , S(O) 2 NR c31 R d31 , and B.R. h31 R i31 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 32 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 32 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a32 , S.R. a32 , C(O)R b32 , C(O)NR c32 R d32 , C(O)OR a32 , O.C.(O.)R b32 , OC(O)NR c32 R d32 , N.R. c32 R d32 , N.R. c32 C(O)R b32 , N.R. c32 C(O)OR a32 , N.R. c32 C(O)NR c32 R d32 , N.R. c32 S(O)R b32 , N.R. c32 S (O) 2 R b32 , N.R. c32 S (O) 2 NR c32 R d32 , S(O)R b32 , S(O)NR c32 R d32 , S(O) 2 R b32 , S(O) 2 NR c32 R d32 , and B.R. h32 R i32 are independently selected from Each R 50 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a50 , S.R. a50 , C(O)R b50 , C(O)NR c50 R d50 , C(O)OR a50 , O.C.(O.)R b50 , OC(O)NR c50 R d50 , N.R. c50 R d50 , N.R. c50 C(O)R b50 , N.R. c50 C(O)OR a50 , N.R. c50 C(O)NR c50 R d50 , N.R. c50 S(O)R b50 , N.R. c50 S (O) 2 R b50 , N.R. c50 S (O) 2 NR c50 R d50 , S(O)R b50 , S(O)NR c50 R d50 , S(O) 2 R b50 , S(O) 2 NR c50 R d50 , and B.R. h50 R i50 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 51 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 51 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 6~10 Aryl, 5- to 6-membered heteroaryl, 4- to 7-membered heterocycloalkyl, halo, D, CN, OR a51 , S.R. a51 , C(O)R b51 , C(O)NR c51 R d51 , C(O)OR a51 , O.C.(O.)R b51 , OC(O)NR c51 R d51 , N.R. c51 R d51 , N.R. c51 C(O)R b51 , N.R. c51 C(O)OR a51 , N.R. c51 C(O)NR c51 R d51 , N.R. c51 S(O)R b51 , N.R. c51 S (O) 2 R b51 , N.R. c51 S (O) 2 NR c51 R d51 , S(O)R b51 , S(O)NR c51 R d51 , S(O) 2 R b51 , S(O) 2 NR c51 R d51 , and B.R. h51 R i51 are independently selected from Each R 60 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a60 , S.R. a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 , O.C.(O.)R b60 , OC(O)NR c60 R d60 , N.R. c60 R d60 , N.R. c60 C(O)R b60 , N.R. c60 C(O)OR a60 , N.R. c60 C(O)NR c60 R d60 , N.R. c60 S(O)R b60 , N.R. c60 S (O) 2 R b60 , N.R. c60 S (O) 2 NR c60 R d60 , S(O)R b60 , S(O)NR c60 R d60 , S(O) 2 R b60 , S(O) 2 NR c60 R d60 , and B.R. h60 R i60 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 61 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 61 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a61 , S.R. a61 , C(O)R b61 , C(O)NR c61 R d61 , C(O)OR a61 , O.C.(O.)R b61 , OC(O)NR c61 R d61 , N.R. c61 R d61 , N.R. c61 C(O)R b61 , N.R. c61 C(O)OR a61 , N.R. c61 C(O)NR c61 R d61 , N.R. c61 S(O)R b61 , N.R. c61 S (O) 2 R b61 , N.R. c61 S (O) 2 NR c61 R d61 , S(O)R b61 , S(O)NR c61 R d61 , S(O) 2 R b61 , S(O) 2 NR c61 R d61 , and B.R. h61 R i61 are independently selected from Each R 70 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, halo, D, CN, NO 2 , OR a70 , S.R. a70 , C(O)R b70 , C(O)NR c70 R d70 , C(O)OR a70 , O.C.(O.)R b70 , OC(O)NR c70 R d70 , N.R. c70 R d70 , N.R. c70 C(O)R b70 , N.R. c70 C(O)OR a70 , N.R. c70 C(O)NR c70 R d70 , N.R. c70 S(O)R b70 , N.R. c70 S (O) 2 R b70 , N.R. c70 S (O) 2 NR c70 R d70 , S(O)R b70 , S(O)NR c70 R d70 , S(O) 2 R b70 , S(O) 2 NR c70 R d70 , and B.R. h70 R i70 are independently selected from R a1 , R b1 , R c1 , and R d1 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R g optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c1 and R d1 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h1 and R i1 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h1 and R i1 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a2 , R b2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 22 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c2 and R d2 together with the N atom to which they are attached, R 22 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e2 But H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h2 and R i2 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h2 and R i2 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c3 and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e3 are H, CN, and C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R f3 and R j3 are respectively, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h3 and R i3 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h3 and R i3 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a4 , R b4 , R c4 , and R d4 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R g optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c4 and R d4 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h4 and R i4 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h4 and R i4 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a5 , R b5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 50 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e5 But H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h5 and R i5 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h5 and R i5 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a6 , R b6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 60 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e6 But H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h6 and R i6 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h6 and R i6 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a7 , R b7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 70 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c7 and R d7 together with the N atom to which they are attached, R 70 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e7 But H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h7 and R i7 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h7 and R i7 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 11 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c10 and R d10 together with the N atom to which they are attached, R 11 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e10 But H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h10 and R i10 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h10 and R i10 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a11 , R b11 , R c11 , and R d11 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c11 and R d11 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h11 and R i11 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h11 and R i11 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 21 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c20 and R d20 together with the N atom to which they are attached, R 21 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R e20 But H, CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 1~6 Alkylthio, C 1~6 Alkylsulfonyl, C 1~6 Alkylcarbonyl, C 1~6 Alkylaminosulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, aminosulfonyl, C 1~6 Alkylaminosulfonyl, and di(C 1~6 independently selected from: (alkyl)aminosulfonyl; R h20 and R i20 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h20 and R i20 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a21 , R b21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R g optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c21 and R d21 together with the N atom to which they are attached, R g forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h21 and R i21 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h21 and R i21 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a22 , R b22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 23 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c22 and R d22 together with the N atom to which they are attached, R 23 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h22 and R i22 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h22 and R i22 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a23 , R b23 , R c23 , and R d23 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c23 and R d23 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h23 and R i23 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h23 and R i23 together with the B atom to which they are attached, form C 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 31 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h30 and R i30 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h30 and R i30 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~6 The cycloalkyl, the phenyl, the 5- to 6-membered heteroaryl, and the 4- to 7-membered heterocycloalkyl are each R 32 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c31 and R d31 together with the N atom to which they are attached, R 32 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h31 and R i31 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h31 and R i31 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a32 , R b32 , R c32 , and R d32 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 independently selected from haloalkyl; R h32 and R i32 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h32 and R i32 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a50 , R b50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 51 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c50 and R d50 together with the N atom to which they are attached, R 51 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R h50 and R i50 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h50 and R i50 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a51 , R b51 , R c51 , and R d51 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c51 and R d51 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h51 and R i51 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h51 and R i51 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 61 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c60 and R d60 together with the N atom to which they are attached, R 61 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R h60 and R i60 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h60 and R i60 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a61 , R b61 , R c61 , and R d61 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c61 and R d61 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h61 and R i61 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h61 and R i61 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; R a70 , R b70 , R c70 , and R d70 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c70 and R d70 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R h70 and R i70 are OH and C, respectively. 1~6 Alkoxy, and C 1~6 haloalkoxy, or any R bonded to the same B atom h70 and R i70 together with the B atom to which they are attached, 1~6 Alkyl and C 1~6 forming a 5- or 6-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from haloalkyl; Each R g But D, OH, NO 2 , CN, Halo, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 Cycloalkyl, C 3~6 Cycloalkyl-C 1~2 Alkylene, C 1~6 Alkoxy, C 1~6 Haloalkoxy, C 1~3 Alkoxy-C 1~3 Alkyl, C 1~3 Alkoxy-C 1~3 Alkoxy, HO-C 1~3 Alkoxy, HO-C 1~3 Alkyl, cyano-C 1~3 Alkyl, H 2 N-C 1~3 Alkyl, amino, C 1~6 Alkylamino, di(C 1~6 alkyl) amino, thio, C 1~6 Alkylthio, C 1~6 Alkylsulfinyl, C 1~6 Alkyl sulfonyl, carbamyl, C 1~6 Alkylcarbamyl, di(C 1~6 alkyl) carbamyl, carboxy, C 1~6 Alkylcarbonyl, C 1~6 Alkoxycarbonyl, C 1~6 Alkylcarbonylamino, C 1~6 Alkoxycarbonylamino, C 1~6 Alkylcarbonyloxy, aminocarbonyloxy, C 1~6 Alkylaminocarbonyloxy, di(C 1~6 alkyl)aminocarbonyloxy, C 1~6 Alkyl sulfonyl amino, amino sulfonyl, C 1~6 Alkylaminosulfonyl, di(C 1~6 alkyl)aminosulfonyl, aminosulfonylamino, C 1~6 Alkylaminosulfonylamino, di(C 1~6 alkyl)aminosulfonylamino, aminocarbonylamino, C 1~6 Alkylaminocarbonylamino, and di(C 1~6 alkyl)aminocarbonylamino; The pharmaceutical composition according to claim 1.
3. The compound of formula I or a pharmaceutically acceptable salt thereof may be represented by formula Ia: 【Chemistry 11】 (In the formula, Y is N or C; R 1 H, D, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, and CN; R 2 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a2 , S.R. a2 , C(O)R b2 , C(O)NR c2 R d2 , C(O)OR a2 , O.C.(O.)R b2 , OC(O)NR c2 R d2 , N.R. c2 R d2 , N.R. c2 C(O)R b2 , N.R. c2 C(O)OR a2 , N.R. c2 C(O)NR c2 R d2 , N.R. c2 S (O) 2 R b2 , N.R. c2 S (O) 2 NR c2 R d2 , S(O) 2 R b2 , and S(O) 2 NR c2 R d2 and C is selected from 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 22 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Cy 1 is C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 6- to 10-membered heteroaryl, wherein the 4- to 10-membered heterocycloalkyl and the 6- to 10-membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and the N and the S are optionally oxidized; the ring-forming carbon atoms of the 6- to 10-membered heteroaryl and the 4- to 10-membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; and the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, C 6~10 The aryl and the 6- to 10-membered heteroaryl are each R 10 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R 3 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR f3 , S.R. a3 , C(O)R b3 , C(O)NR c3 R d3 , C(O)OR a3 , O.C.(O.)R b3 , OC(O)NR c3 R d3 , N.R. c3 R j3 , N.R. c3 C(O)R b3 , N.R. c3 C(O)OR a3 , N.R. c3 C(O)NR c3 R d3 , N.R. c3 S (O) 2 R b3 , N.R. c3 S (O) 2 NR c3 R d3 , S(O) 2 R b3 , and S(O) 2 NR c3 R d3 and C is selected from 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 30 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R 5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a5 , S.R. a5 , C(O)R b5 , C(O)NR c5 R d5 , C(O)OR a5 , O.C.(O.)R b5 , OC(O)NR c5 R d5 , N.R. c5 R d5 , N.R. c5 C(O)R b5 , N.R. c5 C(O)OR a5 , N.R. c5 C(O)NR c5 R d5 , N.R. c5 S (O) 2 R b5 , N.R. c5 S (O) 2 NR c5 R d5 , S(O) 2 R b5 , and S(O) 2 NR c5 R d5 and C is selected from 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 50 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: 【Chemistry 12】 is a double bond and Y is N, then R 4 and R 6 does not exist; 【Chemistry 13】 is a double bond and Y is C, then R 4 does not exist; R 6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a6 , S.R. a6 , C(O)R b6 , C(O)NR c6 R d6 , C(O)OR a6 , O.C.(O.)R b6 , OC(O)NR c6 R d6 , N.R. c6 R d6 , N.R. c6 C(O)R b6 , N.R. c6 C(O)OR a6 , N.R. c6 C(O)NR c6 R d6 , N.R. c6 S (O) 2 R b6 , N.R. c6 S (O) 2 NR c6 R d6 , S(O) 2 R b6 , and S(O) 2 NR c6 R d6 and C is selected from 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 60 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R 7 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a7 , S.R. a7 , C(O)R b7 , C(O)NR c7 R d7 , C(O)OR a7 , O.C.(O.)R b7 , OC(O)NR c7 R d7 , N.R. c7 R d7 , N.R. c7 C(O)R b7 , N.R. c7 C(O)OR a7 , N.R. c7 C(O)NR c7 R d7 , N.R. c7 S (O) 2 R b7 , N.R. c7 S (O) 2 NR c7 R d7 , S(O) 2 R b7 , and S(O) 2 NR c7 R d7 Selected from: Cy 2 is C 3~10 cycloalkyl, 4- to 14-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl, wherein the 4- to 14-membered heterocycloalkyl and the 5- to 10-membered heteroaryl each have at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and the N and the S are optionally oxidized; the ring-forming carbon atoms of the 5- to 10-membered heteroaryl and the 4- to 14-membered heterocycloalkyl are optionally substituted by oxo to form a carbonyl group; and the C 3~10 cycloalkyl, the 4- to 14-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 20 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a10 , S.R. a10 , C(O)R b10 , C(O)NR c10 R d10 , C(O)OR a10 , O.C.(O.)R b10 , OC(O)NR c10 R d10 , N.R. c10 R d10 , N.R. c10 C(O)R b10 , N.R. c10 C(O)OR a10 , N.R. c10 C(O)NR c10 R d10 , N.R. c10 S (O) 2 R b10 , N.R. c10 S (O) 2 NR c10 R d10 , S(O) 2 R b10 , and S(O) 2 NR c10 R d10 are independently selected from Each R 20 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a20 , S.R. a20 , C(O)R b20 , C(O)NR c20 R d20 , C(O)OR a20 , O.C.(O.)R b20 , OC(O)NR c20 R d20 , N.R. c20 R d20 , N.R. c20 C(O)R b20 , N.R. c20 C(O)OR a20 , N.R. c20 C(O)NR c20 R d20 , N.R. c20 S (O) 2 R b20 , N.R. c20 S (O) 2 NR c20 R d20 , S(O) 2 R b20 , and S(O) 2 NR c20 R d20 and wherein C is independently selected from 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 21 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 21 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a21 , S.R. a21 , C(O)R b21 , C(O)NR c21 R d21 , C(O)OR a21 , O.C.(O.)R b21 , OC(O)NR c21 R d21 , N.R. c21 R d21 , N.R. c21 C(O)R b21 , N.R. c21 C(O)OR a21 , N.R. c21 C(O)NR c21 R d21 , N.R. c21 S (O) 2 R b21 , N.R. c21 S (O) 2 NR c21 R d21 , S(O) 2 R b21 , and S(O) 2 NR c21 R d21 are independently selected from Each R 22 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a22 , S.R. a22 , C(O)R b22 , C(O)NR c22 R d22 , C(O)OR a22 , O.C.(O.)R b22 , OC(O)NR c22 R d22 , N.R. c22 R d22 , N.R. c22 C(O)R b22 , N.R. c22 C(O)OR a22 , N.R. c22 C(O)NR c22 R d22 , N.R. c22 S (O) 2 R b22 , N.R. c22 S (O) 2 NR c22 R d22 , S(O) 2 R b22 , and S(O) 2 NR c22 R d22 are independently selected from Each R 30 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a30 , S.R. a30 , C(O)R b30 , C(O)NR c30 R d30 , C(O)OR a30 , O.C.(O.)R b30 , OC(O)NR c30 R d30 , N.R. c30 R d30 , N.R. c30 C(O)R b30 , N.R. c30 C(O)OR a30 , N.R. c30 C(O)NR c30 R d30 , N.R. c30 S (O) 2 R b30 , N.R. c30 S (O) 2 NR c30 R d30 , S(O) 2 R b30 , and S(O) 2 NR c30 R d30 and wherein C is independently selected from 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 aryl, the 5- to 10-membered heteroaryl, the C 3~10 Cycloalkyl-C 1~3 alkylene, the 4- to 10-membered heterocycloalkyl-C 1~3 alkylene, 6~10 Aryl-C 1~3 alkylene, and the 5- to 10-membered heteroaryl-C 1~3 Each alkylene is represented by R 31 and optionally substituted with 1, 2, 3, or 4 substituents independently selected from: Each R 31 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a31 , S.R. a31 , C(O)R b31 , C(O)NR c31 R d31 , C(O)OR a31 , O.C.(O.)R b31 , OC(O)NR c31 R d31 , N.R. c31 R d31 , N.R. c31 C(O)R b31 , N.R. c31 C(O)OR a31 , N.R. c31 C(O)NR c31 R d31 , N.R. c31 S (O) 2 R b31 , N.R. c31 S (O) 2 NR c31 R d31 , S(O) 2 R b31 , and S(O) 2 NR c31 R d31 are independently selected from Each R 50 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a50 , S.R. a50 , C(O)R b50 , C(O)NR c50 R d50 , C(O)OR a50 , O.C.(O.)R b50 , OC(O)NR c50 R d50 , N.R. c50 R d50 , N.R. c50 C(O)R b50 , N.R. c50 C(O)OR a50 , N.R. c50 C(O)NR c50 R d50 , N.R. c50 S (O) 2 R b50 , N.R. c50 S (O) 2 NR c50 R d50 , S(O) 2 R b50 , and S(O) 2 NR c50 R d50 are independently selected from Each R 60 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5- to 10-membered heteroaryl, C 3~10 Cycloalkyl-C 1~3 alkylene, 4- to 10-membered heterocycloalkyl-C 1~3 Alkylene, C 6~10 Aryl-C 1~3 alkylene, 5- to 10-membered heteroaryl-C 1~3 Alkylene, Halo, D, CN, OR a60 , S.R. a60 , C(O)R b60 , C(O)NR c60 R d60 , C(O)OR a60 , O.C.(O.)R b60 , OC(O)NR c60 R d60 , N.R. c60 R d60 , N.R. c60 C(O)R b60 , N.R. c60 C(O)OR a60 , N.R. c60 C(O)NR c60 R d60 , N.R. c60 S (O) 2 R b60 , N.R. c60 S (O) 2 NR c60 R d60 , S(O) 2 R b60 , and S(O) 2 NR c60 R d60 are independently selected from R a2 , R b2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 22 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c2 and R d2 together with the N atom to which they are attached, R 22 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a3 , R b3 , R c3 , and R d3 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c3 and R d3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R f3 and R j3 are respectively, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a5 , R b5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 50 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a6 , R b6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 60 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a7 , R b7 , R c7 , and R d7 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c7 and R d7 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a10 , R b10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c10 and R d10 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 21 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c20 and R d20 together with the N atom to which they are attached, R 21 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a21 , R b21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c21 and R d21 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a22 , R b22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c22 and R d22 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a30 , R b30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 31 optionally substituted with 1, 2, 3, or 4 substituents independently selected from Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, 6-, or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from: R a31 , R b31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~6 independently selected from cycloalkyl, phenyl, 5- to 6-membered heteroaryl, and 4- to 7-membered heterocycloalkyl; Alternatively, any R bonded to the same N atom c31 and R d31 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a50 , R b50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c50 and R d50 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group; R a60 , R b60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c60 and R d60 together with the N atom to which they are attached form a 4-, 5-, 6-, or 7-membered heterocycloalkyl group.
3. The pharmaceutical agent according to claim 1, which is a compound represented by the following formula (I): or a pharmaceutically acceptable salt thereof.
4. Y is N or C; R 1 However, H, D, and C 1~6 alkyl; R 2 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a2 , and N.R. c2 R d2 and C is selected from 1~6 The alkyl is R 22 and optionally substituted with 1 or 2 substituents independently selected from: Cy 1 But C 6~10 and a 6- to 10-membered heteroaryl having at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, wherein a ring-forming carbon atom of the 6- to 10-membered heteroaryl is optionally substituted by oxo to form a carbonyl group; and wherein the C 6~10 The aryl and the 6- to 10-membered heteroaryl are each R 10 and optionally substituted with 1, 2, or 3 substituents independently selected from R 3 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR f3 , and N.R. c3 R j3 and C is selected from 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 and optionally substituted with 1, 2, or 3 substituents independently selected from R 5 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a5 , C(O)NR c5 R d5 , and N.R. c5 R d5 and C is selected from 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 50 and optionally substituted with 1, 2, or 3 substituents independently selected from 【Chemistry 14】 is a double bond and Y is N, then R 4 and R 6 does not exist; 【Chemistry 15】 is a double bond and Y is C, then R 4 does not exist; R 6 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a6 , and N.R. c6 R d6 and C is selected from 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 60 and optionally substituted with 1, 2, or 3 substituents independently selected from R 7 But H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; Cy 2 is selected from 4- to 10-membered heterocycloalkyl having at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, a ring-forming carbon atom of the 4- to 10-membered heterocycloalkyl optionally being substituted by oxo to form a carbonyl group, and the 4- to 10-membered heterocycloalkyl is selected from R 20 and optionally substituted with 1, 2, or 3 substituents independently selected from Each R 10 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , and N.R. c10 R d10 are independently selected from Each R 20 But C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, Halo, D, CN, OR a20 , C(O)R b20 , C(O)NR c20 R d20 , and N.R. c20 R d20 and wherein C is independently selected from 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R 21 and optionally substituted with 1, 2, or 3 substituents independently selected from Each R 21 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , and N.R. c21 R d21 are independently selected from Each R 22 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a22 , and N.R. c22 R d22 are independently selected from Each R 30 But C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a30 , C(O)NR c30 R d30 , and N.R. c30 R d30 and wherein C is independently selected from 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 31 and optionally substituted with 1, 2, or 3 substituents independently selected from Each R 31 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a31 , and N.R. c31 R d31 are independently selected from Each R 50 But C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a50 , and N.R. c50 R d50 are independently selected from Each R 60 But C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a60 , C(O)NR c60 R d60 , C(O)OR a60 , and N.R. c60 R d60 are independently selected from R a2 , R c2 , and R d2 are H and C, respectively. 1~6 Alkyl, and C 1~6 haloalkyl; 1~6 Alkyl is R 22 and optionally substituted with 1 or 2 substituents independently selected from: Each R c3 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 and optionally substituted with 1, 2, or 3 substituents independently selected from R f3 and R j3 are respectively, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 optionally substituted with 1, 2, or 3 substituents independently selected from Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a5 , R c5 , and R d5 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 50 optionally substituted with 1, 2, or 3 substituents independently selected from Alternatively, any R bonded to the same N atom c5 and R d5 together with the N atom to which they are attached, R 50 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a6 , R c6 , and R d6 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 60 optionally substituted with 1, 2, or 3 substituents independently selected from Alternatively, any R bonded to the same N atom c6 and R d6 together with the N atom to which they are attached, R 60 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl; 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R 21 and optionally substituted with 1, 2, or 3 substituents independently selected from R a21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a22 , R c22 , and R d22 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 Alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 31 optionally substituted with 1, 2, or 3 substituents independently selected from Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a50 , R c50 , and R d50 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c50 and R d50 together with the N atom to which they are attached form a 4-, 5-, or 6-membered heterocycloalkyl group; R a60 , R c60 , and R d60 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 independently selected from aryl, and 5-10 membered heteroaryl; Alternatively, any R bonded to the same N atom c60 and R d60 together with the N atom to which they are attached form a 4-, 5-, or 6-membered heterocycloalkyl group; The pharmaceutical composition according to claim 3.
5. Y is N or C; R 1 is H; R 2 But H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; Cy 1 But C 6~10 aryl and 6- to 10-membered heteroaryl, wherein the 6- to 10-membered heteroaryl has at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the C 6~10 The aryl and the 6- to 10-membered heteroaryl are each R 10 and optionally substituted with 1, 2, or 3 substituents independently selected from R 3 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4-10 membered heterocycloalkyl, halo, D, CN, OR f3 , and N.R. c3 R j3 and C is selected from 1~6 alkyl, the C 3~10 The cycloalkyl and the 4- to 10-membered heterocycloalkyl are each R 30 and optionally substituted with 1, 2, or 3 substituents independently selected from R 5 But H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; 【Chemistry 16】 is a double bond and Y is N, then R 6 does not exist; R 6 But H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; R 7 But H, C 1~6 Alkyl, C 1~6 selected from haloalkyl, halo, D, and CN; Cy 2 is selected from 4- to 6-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and said 4- to 6-membered heterocycloalkyl is selected from R 20 and optionally substituted with 1, 2, or 3 substituents independently selected from Each R 10 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a10 , and N.R. c10 R d10 are independently selected from Each R 20 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a20 , C(O)R b20 , C(O)NR c20 R d20 , and N.R. c20 R d20 and wherein C is independently selected from 1~6 Alkyl is R 21 and optionally substituted with 1 or 2 substituents independently selected from: Each R 21 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , and N.R. c21 R d21 are independently selected from Each R 30 But C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a30 , C(O)NR c30 R d30 , and N.R. c30 R d30 and wherein C is independently selected from 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 31 and optionally substituted with 1, 2, or 3 substituents independently selected from Each R 31 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a31 , and N.R. c31 R d31 are independently selected from Each R c3 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 and optionally substituted with 1, 2, or 3 substituents independently selected from R f3 and R j3 are respectively, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 30 optionally substituted with 1, 2, or 3 substituents independently selected from Alternatively, any R bonded to the same N atom c3 and R j3 together with the N atom to which they are attached, R 30 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a10 , R c10 , and R d10 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a20 , R b20 , R c20 , and R d20 are H and C, respectively. 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, and C 1~6 haloalkyl; 1~6 alkyl, the C 2~6 alkenyl, and the C 2~6 Each alkynyl is R 21 and optionally substituted with 1, 2, or 3 substituents independently selected from R a21 , R c21 , and R d21 are H and C, respectively. 1~6 Alkyl, and C 1~6 independently selected from haloalkyl; R a30 , R c30 , and R d30 are H and C, respectively. 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 aryl, and 5- to 10-membered heteroaryl; 1~6 alkyl, the C 2~6 alkenyl, the C 2~6 Alkynyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 31 optionally substituted with 1, 2, or 3 substituents independently selected from Alternatively, any R bonded to the same N atom c30 and R d30 together with the N atom to which they are attached, R 31 forming a 4-, 5-, or 6-membered heterocycloalkyl group optionally substituted with 1, 2, or 3 substituents independently selected from: R a31 , R c31 , and R d31 are H and C, respectively. 1~6 Alkyl, and C 1~6 haloalkyl; The pharmaceutical composition according to any one of claims 1 to 4.
6. The compound of formula I or a pharmaceutically acceptable salt thereof may be represented by formula II: 【Chemistry 17】 2. The pharmaceutical composition according to claim 1, which is a compound represented by the formula: or a pharmaceutically acceptable salt thereof.
7. X is CR 7 and R 1 is selected from H; R 2 But H, C 1~3 selected from haloalkyl, and halo; Cy 1 But C 10 aryl, and 10 Aryl is R 10 and optionally substituted with 1 or 2 substituents independently selected from: R 3 is selected from H and 4- to 6-membered heterocycloalkyl, said 4- to 6-membered heterocycloalkyl being R 30 and optionally substituted with 1 or 2 substituents independently selected from: R 5 is H; [Chemistry 18] is a double bond, Y is N, and R 4 and R 6 does not exist; R 7 is selected from H or halo; Cy 2 is a 4- to 6-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 6-membered heterocycloalkyl is 20 and optionally substituted with 1 or 2 substituents independently selected from: Each R 10 But OR a10 are independently selected from Each R 20 But C(O)R b20 are independently selected from Each R 30 But NR c30 R d30 are independently selected from Each R a10 However, H and C 1~3 independently selected from alkyl; Each R b20 But C 1~3 Alkyl or C 2~4 alkenyl; R c30 and R d30 are respectively, C 1~3 independently selected from alkyl, The pharmaceutical composition according to any one of claims 1 to 3.
8. The compound of formula I or a pharmaceutically acceptable salt thereof may be represented by formula III: 【Chemistry 19】 2. The pharmaceutical composition according to claim 1, which is a compound represented by the formula: or a pharmaceutically acceptable salt thereof.
9. The compound of formula I or a pharmaceutically acceptable salt thereof may be represented by formula IV: 【Chemistry 20】 2. The pharmaceutical composition according to claim 1, which is a compound represented by the formula: or a pharmaceutically acceptable salt thereof.
10. The compound of formula I or a pharmaceutically acceptable salt thereof may be represented by formula V: 【Chemistry 21】 2. The pharmaceutical composition according to claim 1, which is a compound represented by the formula: or a pharmaceutically acceptable salt thereof.
11. The compound of formula I or a pharmaceutically acceptable salt thereof may be represented by formula VI: 【Chemistry 22】 The pharmaceutical agent according to any one of claims 1 to 4, which is a compound represented by the following formula (I): or a pharmaceutically acceptable salt thereof.
12. The compound of formula I or a pharmaceutically acceptable salt thereof may be represented by formula VII: 【Chemistry 23】 3. The pharmaceutical agent according to claim 1, which is a compound represented by the following formula (I): or a pharmaceutically acceptable salt thereof.
13. X is CR 7 The pharmaceutical composition according to claim 1, wherein
14. The pharmaceutical composition of claim 1, wherein X is N. 【Request Item 15】 【Chemistry 24】 is a double bond, Y is N, and R 4 and R 6 The pharmaceutical composition of any one of claims 1, 13, and 14, wherein 【Request Item 16】 【Chemistry 25】 is a double bond, Y is C, and R 4 The pharmaceutical composition of any one of claims 1, 13, and 14, wherein
17. R 1 But H, D, C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, OR a1 , and N.R. c1 R d1 The pharmaceutical composition according to any one of claims 1, 2, and 6 to 16, which is selected from the group consisting of
18. R 1 The pharmaceutical agent according to any one of claims 1 to 17, wherein is H.
19. R 2 But H, C 1~6 Alkyl, C 1~6 haloalkyl, halo, D, and CN; 1~6 Alkyl is R 22 The pharmaceutical agent according to any one of claims 1, 2, and 6 to 18, which is optionally substituted with 1 or 2 substituents independently selected from:
20. Each R 22 But C 1~6 Alkyl, C 1~6 The medicament of any one of claims 1, 2, and 6 to 19, wherein the aryl group is independently selected from haloalkyl, halo, and CN.
21. R 2 The pharmaceutical agent according to any one of claims 1 to 20, wherein is halo.
22. Cy 1 But C 6~10 and aryl and 6- to 10-membered heteroaryl, each of which has at least one ring-forming carbon atom and 1, 2, 3, or 4 ring-forming heteroatoms independently selected from N, O, and S, and wherein N and S are optionally oxidized; and wherein a ring-forming carbon atom of a 6- to 10-membered heteroaryl is optionally substituted by oxo to form a carbonyl group; and wherein C 6~10 The aryl and the 6- to 10-membered heteroaryl are each R 10 The pharmaceutical agent according to any one of claims 1 to 21, which is optionally substituted with 1 or 2 substituents independently selected from:
23. Cy 1 But, R 10 C optionally substituted with 1 or 2 substituents independently selected from 6~10 The pharmaceutical agent according to any one of claims 1 to 22, which is aryl.
24. Cy 1 But, R 10 The pharmaceutical agent according to any one of claims 1 to 22, wherein the heteroaryl is a 6- to 10-membered heteroaryl optionally substituted with 1 or 2 substituents independently selected from:
25. R 10 But C 1~3 Alkyl, C 1~3 Haloalkyl, halo, D, CN, and OR a10 The pharmaceutical agent according to any one of claims 1 to 22, which is selected from the group consisting of
26. R 3 is H, 4-10 membered heterocycloalkyl, C 6~10 Aryl and OR f3 wherein said 4 to 10 membered heterocycloalkyl and said C 6~10 Each aryl is R 30 The pharmaceutical agent according to any one of claims 1 to 4 and 6 to 25, which is optionally substituted with 1 or 2 substituents independently selected from:
27. R 3 is H, 4-6 membered heterocycloalkyl, and OR f3 wherein said 4-6 membered heterocycloalkyl is selected from R 30 The pharmaceutical agent according to any one of claims 1 to 26, which is optionally substituted with 1 or 2 substituents independently selected from:
28. Each R 30 But C 1~6 Alkyl, C 1~6 haloalkyl, 4-6 membered heterocycloalkyl, 5-6 membered heteroaryl, halo, D, CN, OR a30 , and N.R. c30 R d30 and wherein C is independently selected from 1~6 The alkyl, the 4- to 6-membered heterocycloalkyl, and the 5- to 6-membered heteroaryl are each R 31 The pharmaceutical agent according to any one of claims 1 to 27, which is optionally substituted with 1 or 2 substituents independently selected from:
29. Each R 31 But C 1~6 Alkyl, C 1~6 The medicament of any one of claims 1 to 28, wherein the aryl group is independently selected from haloalkyl, halo, D, and CN.
30. R 5 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a5 , C(O)NR c5 R d5 , and N.R. c5 R d5 and C is selected from 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 50 The pharmaceutical agent according to any one of claims 1 to 29, which is optionally substituted with 1, 2, or 3 substituents independently selected from:
31. R 5 The pharmaceutical agent according to any one of claims 1 to 30, wherein is H.
32. Each R 50 But C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a50 , and N.R. c50 R d50 The pharmaceutical agent according to any one of claims 1 to 31, independently selected from:
33. R 6 But H, C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a6 , and N.R. c6 R d6 and C is selected from 1~6 alkyl, the C 3~10 cycloalkyl, the 4- to 10-membered heterocycloalkyl, the C 6~10 The aryl and the 5- to 10-membered heteroaryl are each R 60 The pharmaceutical agent according to any one of claims 1 to 32, which is optionally substituted with 1, 2, or 3 substituents independently selected from:
34. Each R 60 But C 1~6 Alkyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 4- to 10-membered heterocycloalkyl, C 6~10 Aryl, 5-10 membered heteroaryl, halo, D, CN, OR a60 , C(O)NR c60 R d60 , C(O)OR a60 , and N.R. c60 R d60 The pharmaceutical agent according to any one of claims 1 to 33, independently selected from:
35. R 7 But H, C 1~3 Alkyl, C 1~3 The medicament according to any one of claims 1 to 34, wherein the aryl group is selected from haloalkyl and halo.
36. R 7 The pharmaceutical agent according to any one of claims 1 to 35, wherein is halo.
37. Cy 2 is a 4- to 6-membered heterocycloalkyl having at least one ring-forming carbon atom and 1 or 2 ring-forming heteroatoms independently selected from N and O, and the 4- to 6-membered heterocycloalkyl is 20 The pharmaceutical agent according to any one of claims 1 to 36, which is optionally substituted with 1 or 2 substituents independently selected from:
38. Cy 2 but, Table 1 (wherein n is 0, 1, or 2) The pharmaceutical agent according to any one of claims 1 to 37, selected from the group consisting of:
39. Cy 2 But Cy 2 The pharmaceutical composition according to claim 38, wherein the compound is -a1.
40. Cy 2 But Cy 2 The pharmaceutical composition of claim 38, wherein the compound is -e.
41. Each R 20 But C 1~6 Alkyl, C 1~6 Haloalkyl, halo, D, CN, and C(O)R b20 and wherein C is independently selected from 1~6 Alkyl is R 21 The pharmaceutical agent according to any one of claims 1 to 40, which is optionally substituted with 1 or 2 substituents independently selected from:
42. Each R 21 But C 1~6 Alkyl, C 1~6 Haloalkyl, Halo, D, CN, OR a21 , and N.R. c21 R d21 The pharmaceutical agent according to any one of claims 1 to 41, independently selected from:
43. The compound of formula I or a pharmaceutically acceptable salt thereof is 1-(4-(8-chloro-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-1H-pyrazolo[4,3-c]-quinolin-1-yl)-piperidin-1-yl)prop-2-en-1-one, 1-(4-(8-chloro-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-1-yl)prop-2-en-1-one, 2-((2S,4S)-1-acryloyl-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4,4-difluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4,4-difluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-7-(6-chloro-5-methyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(5-fluoroquinolin-8-yl)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(isoquinolin-4-yl)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-7-(2-chloro-3-methylphenyl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(2-chloro-3-methylphenyl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-7-(2,3-dichlorophenyl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(2,3-dichlorophenyl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(3-methyl-2-(trifluoromethyl)phenyl)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-acryloyl-4-(8-chloro-6-fluoro-7-(3-methyl-2-(trifluoromethyl)phenyl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; methyl 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-2-yl)propanoate; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-2-yl)-N,N-dimethylpropanamide; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-2-propyl-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-2-(1-methyl-1H-pyrazol-4-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-phenyl-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-(pyridin-3-yl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-3-(2-methyloxazol-5-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-(2-methylthiazol-5-yl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-3-(1-methyl-1H-pyrazol-4-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-2-(1-methyl-1H-pyrazol-3-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(2-benzyl-1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-(1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-3-(6-oxo-1,6-dihydropyridin-3-yl)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-3-chloro-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 1-(2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-6-fluoro-N-(2-hydroxyethyl)-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinoline-3-carboxamide; N-benzyl-1-(2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinoline-3-carboxamide; 3-(1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-3-(hydroxymethyl)-7-(3-hydroxynaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 3-(1-((1R,4R,5S)-2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-4-ethoxy-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-1H-pyrrolo[3,2-c]quinolin-2-yl)-N,N-dimethylpropanamide; methyl 3-(1-((1R,4R,5S)-2-azabicyclo[2.1.1]hexan-5-yl)-8-(2-cyanoethyl)-3-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-7-(3-hydroxynaphthalen-1-yl)-4-methoxy-1H-pyrrolo[3,2-c]quinolin-2-yl)propanoate; 3-(2-(3-(azetidin-1-yl)-3-oxopropyl)-1-(2-azabicyclo[2.1.1]hexan-5-yl)-6-fluoro-7-(7-fluoronaphthalen-1-yl)-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-8-yl)propanenitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-fluorobut-2-enoyl)piperidin-4-yl)-6-fluoro-8-methyl-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-(2-fluoroacryloyl)piperidin-4-yl)-6-fluoro-8-methyl-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-1-(but-2-ynoyl)-2-(cyanomethyl)piperidin-4-yl)-6-fluoro-8-methyl-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-methoxybut-2-enoyl)piperidin-4-yl)-6-fluoro-8-methyl-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-fluorobut-2-enoyl)piperidin-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-(2-fluoroacryloyl)piperidin-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-methoxybut-2-enoyl)piperidin-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-fluorobut-2-enoyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-(2-fluoroacryloyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-1-(but-2-ynoyl)-2-(cyanomethyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-methoxybut-2-enoyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 8-(1-((2S,4S)-2-(cyanomethyl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-7-yl)-1-naphthonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-8-methyl-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-8-methyl-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)azetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-(2-fluoroacryloyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile; 2-((2S,4S)-4-(8-chloro-7-(8-chloronaphthalen-1-yl)-6-fluoro-4-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-1H-pyrazolo[4,3-c]quinolin-1-yl)-1-((E)-4-(dimethylamino)but-2-enoyl)piperidin-2-yl)acetonitrile; and 2-((2S,4S)-1-(but-2-ynoyl)-4-(8-chloro-7-(5,6-dimethyl-1H-indazol-4-yl)-6-fluoro-4-(((S)-1-methylpyrrolidin-2-yl)methoxy)-1H-pyrrolo[3,2-c]quinolin-1-yl)piperidin-2-yl)acetonitrile; The pharmaceutical agent according to any one of claims 1 to 7, which is a compound selected from the following: