KRAS inhibitors

Abstract

Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.

Description

[0001] 770610: ICT-568PC / INCY0568-WO1

[0002] KRAS INHIBITORS RELATED APPLICATIONS

[0003] This application claims priority to U. S. Provisional Application No. 63 / 719,839, filed November 13, 2024, U. S. Provisional Application No. 63 / 757,695, filed February 12, 2025, and U. S. Provisional Application No. 63 / 830,831, filed June 26, 2025, the content of each of which is incorporated in its entirety.

[0004] FIELD OF THE INVENTION

[0005] This disclosure provides compounds as well as their compositions and methods of use. The compounds modulate KRAS activity and are useful in the treatment of various diseases including cancer.

[0006] BACKGROUND OF THE INVENTION

[0007] Ras proteins are part of the family of small GTPases that are activated by growth factors and various extracellular stimuli. The Ras family regulates intracellular signaling pathways responsible for growth, migration, survival and differentiation of cells. Activation of Ras proteins at the cell membrane results in the binding of key effectors and initiation of a cascade of intracellular signaling pathways within the cell, including the RAF and PI3K kinase pathways. Somatic mutations in RAS may result in uncontrolled cell growth and malignant transformation while the activation of RAS proteins is tightly regulated in normal cells (D. Simanshu, eta / ., Cell, 2017, 170(1), 17-33).

[0008] The Ras family is comprised of three members: KRAS, NRAS and HRAS. RAS mutant cancers account for about 25% of human cancers. KRAS is the most frequently mutated isoform accounting for 85% of all RAS mutations whereas NRAS and HRAS are found mutated in 12% and 3% of all Ras mutant cancers respectively (D. Simanshu, et al., Cell, 2017, 170(1), 17-33). KRAS mutations are prevalent amongst the top three most deadly cancer types: pancreatic (97%), colorectal (44%), and lung (30%) (A. D. Cox, etal., Nat. Rev. Drug. Discov., 2014, 13(11), 828-51). The majority of RAS mutations occur at amino acid residue 12, 13, and 61. The frequency of specific mutations varies between RAS gene isoforms and while G12 and Q61 mutations are predominant in KRAS and NRAS respectively, G12, G13 and Q61 mutations are most frequent in HRAS. Furthermore, the spectrum of mutations in a RAS isoform differs between cancer types. For example, KRAS G12D mutations predominate in pancreatic cancers (51%), followed by colorectal adenocarcinomas (45%) and lung cancers (17%) while KRAS G12V mutations are associated with pancreatic cancers (30%), followed by colorectal adenocarcinomas (27%), and lung adenocarcinomas (23%) (A. D. Cox, et al., Nat. Rev. Drug. Discov., 2014, 13(11), 828-51). In contrast, KRAS G12C mutations predominate in non-small cell lung cancer (NSCLC) comprising 11-16% of lung adenocarcinomas, and 2-5% of pancreatic and 770610: ICT-568PC / INCY0568-WO1

[0009] colorectal adenocarcinomas (A. D. Cox, etal., Nat. Rev. Drug. Discov., 2014, 13(11), 828-51). Genomic studies across hundreds of cancer cell lines have demonstrated that cancer cells harboring KRAS mutations are highly dependent on KRAS function for cell growth and survival (R. McDonald, et al., Cell, 2017, 170(3), 577-92). The role of mutant KRAS as an oncogenic driver is further supported by extensive in vivo experimental evidence showing mutant KRAS is required for early tumor onset and maintenance in animal models (A. D. Cox, etal., Nat. Rev. Drug. Discov., 2014, 13(11), 828-51).

[0010] Taken together, these findings indicate that KRAS mutations play a critical role in human cancers. Development of inhibitors targeting KRAS, including mutant KRAS, will therefore be useful in the clinical treatment of diseases that are characterized by involvement of KRAS, including diseases characterized by the involvement or presence of a KRAS mutation.

[0011] SUMMARY

[0012] The present disclosure provides, inter alia, a compound of Formula (I):

[0013]

[0014] (I)

[0015] or a pharmaceutically acceptable salt thereof, wherein constituent variables are defined herein.

[0016] The present disclosure further provides a pharmaceutical composition comprising a compound of the disclosure, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier or excipient.

[0017] The present disclosure further provides methods of inhibiting KRAS activity, which comprises administering to an individual a compound of the disclosure, or a pharmaceutically acceptable salt thereof. The present disclosure also provides uses of the compounds described herein in the manufacture of a medicament for use in therapy. The present disclosure also provides the compounds described herein for use in therapy.

[0018] The present disclosure further provides methods of treating a disease or disorder in a patient comprising administering to the patient a therapeutically effective amount of a compound of the disclosure, or a pharmaceutically acceptable salt thereof.

[0019] The details of one or more embodiments are set forth in the description below. Other features, objects, and advantages will be apparent from the description and from the claims. 770610: ICT-568PC / INCY0568-WO1

[0020] DETAILED DESCRIPTION

[0021] For the terms “e.g.” and “such as,” and grammatical equivalents thereof, the phrase “and without limitation” is understood to follow unless explicitly stated otherwise.

[0022] The singular forms “a,” “an,” and “the” include plural referents unless the context clearly dictates otherwise.

[0023] The term “about” means “approximately” e.g., plus or minus approximately 10% of the indicated value).

[0024] I. Compounds

[0025] In an aspect, provided herein is a compound having Formula (I):

[0026]

[0027] (I)

[0028] or a pharmaceutically acceptable salt thereof, wherein:

[0029] R1is selected from C1-3 alkyl, C1-3 haloalkyl, C3-6 cycloalkyl, and halo;

[0030] Cy1is Ce-waryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, 3, or 4 substituents independently selected from RCy1;

[0031] each RCy1is independently selected from D, C1-3 alkyl, C1-3 haloalkyl, C2-3 alkenyl, C2-3 alkynyl, halo, CN, ORaCy1, and NRcCy1RdCy1;

[0032] each RaCy1, RcCy1, and RdCy1is independently selected from H, C1-3 alkyl, and C1-3 haloalkyl;

[0033] R2is selected from C1-3 alkyl and halo;

[0034] R3is selected from H, C1-3 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, halo, D, CN, ORa3, NRb3C(O)Ra3, C(O)NRb3Rc3, N=S(O)Rb3Rc3, and NRb3Rc3; wherein the C3-w cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;

[0035] each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl; wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, 3, or 4 substituents 770610: ICT-568PC / INCY0568-WO1

[0036] independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3B; or Rb3and Rc3together with the nitrogen atom to which they are attached form a 4-10 membered heterocycloalkyl, optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A;

[0037] each Rd3is independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, and 4-10 membered heterocycloalkyl; wherein the C1-6 alkyl forming Rd3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from D, halo, CN, S(C>2)Ci-6 alkyl;

[0038] each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, 3, or 4 subtituents each independently selected from R3B;

[0039] each R3Bis independently selected from halo, D, CN, ORd3, C3-10 cycloalkyl, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the C1-3 alkoxy, and 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C;

[0040] each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 haloalkyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are each optionally substituted by 1, 2, or 3 halo;

[0041] R4is selected from H, D, C1-3 alkyl, halo, and CN;

[0042] R5is selected from Cy5and CR5AR5BCy5;

[0043] each Cy5is independently selected from C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aor (C3-6 alkylene)Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;

[0044] each Cy5Ais independently selected from C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl forming Cy5Ais optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;

[0045] R5Ais selected from H, D, C1-3 alkyl, C1-3 haloalkyl, and C3-6 cycloalkyl;

[0046] R5Bis selected from H, D, C1-3 alkyl, and C1-3 haloalkyl;

[0047] each R5Cis independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;

[0048] each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, ORa5, SRa5, S(O)Ra5, S(O)2Ra5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)ORa5, NRc5C(O)NRc5Rd5, C(=NRe5)Rb5, C(=NORa5)Rb5, 770610: ICT-568PC / INCY0568-WO1

[0049] C(=NRe5)NRc5Rd5, NRc5C(=NRe5)NRc5Rd5, NRc5S(O)Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, and S(O)2NRc5Rd5;

[0050] each Ra5, Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl, wherein each C1-6 alkyl forming each Ra5, Rb5, Rc5, and Rd5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from D and halo;

[0051] or any Rc1and Rd1attached to the same N atom, together with the N atom to which they are attached, form a 4-, 5-, 6- or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from Rg1;

[0052] each Re5is independently selected from H, C1-6 alkyl, OH and C1-6 alkoxy,, wherein each C1-6 alkyl and C1-6 alkoxy forming Re5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from D and halo;

[0053] R6is selected from H, D, C1-3 alkyl and C1-3 haloalkyl;

[0054] R6Ais selected from H, D, C1-3 alkyl and C1-3 haloalkyl;

[0055] R7is selected from H, D, C1-3 alkyl, C1-3 haloalkyl, and halo; and

[0056] R7Ais selected from H, D, C1-3 alkyl, C1-3 haloalkyl, and halo; or

[0057] R7and R7Atogether with the carbon atom to which they are attached form a spiro fused C3-7 cycloalkane ring;

[0058] wherein the ring-forming atoms of each heteroaryl and heterocycloalkyl consist of at least one ring-forming carbon atom and 1, 2, 3, or 4 heteroatoms independently selected from N, O, and S; wherein a ring-forming carbon atom of each heteroaryl and heterocycloalkyl is optionally substituted by oxo to form a carbonyl group.

[0059] In an embodiment,

[0060] R3is selected from H, C1-3 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl, halo, D, CN, ORa3, NRb3C(O)Ra3, C(O)NRb3Rc3, and NRb3Rc3; wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B; and

[0061] each R3Bis independently selected from halo, D, CN, OH, C1-3 alkoxy, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the C1-3 alkoxy, and 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C.

[0062] In an embodiment,

[0063] R3is selected from C1-3 alkyl, C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce-aryl, 5-10 membered heteroaryl, halo, ORa3, C(O)NRb3Rc3, and NRb3Rc3; wherein the C3-cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, and 5-10 membered heteroaryl 770610: ICT-568PC / INCY0568-WO1

[0064] forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;

[0065] each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl; wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3B; or Rb3and Rc3together with the nitrogen atom to which they are attached form a 4-10 membered heterocycloalkyl, optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A;

[0066] each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, 3, or 4 subtituents each independently selected from R3B;

[0067] each R3Bis independently selected from halo, D, CN, OH, C1-3 alkoxy, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C; and

[0068] each R3Cis independently selected from C1-6 alkyl, halo and C1-6 haloalkyl.

[0069] In an embodiment,

[0070] R1is selected from C1-3 alkyl and halo;

[0071] R3is selected from H, C1-3 alkyl, C2-6 alkynyl, C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl, D, CN, ORa3, NRb3C(O)Ra3, and NRb3Rc3; wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3 or 4 substituents each independently selected from R3B;

[0072] each R3Bis independently selected from halo, D, CN, C1-3 alkoxy, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the C1-3 alkoxy and 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C;

[0073] each Cy5is independently selected from C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl, wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl forming Cy5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C; 770610: ICT-568PC / INCY0568-WO1

[0074] R5Ais selected from H, D, and C1-3 alkyl;

[0075] R5Bis selected from H, D, and C1-3 alkyl;

[0076] each R5Cis independently selected from C1-3 alkyl and R5D, wherein each C1-3 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;

[0077] each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, C1-3 alkoxy, amino, C1-3 alkylamino, and di(Ci-3alkyl)amino;

[0078] R7is selected from H, D, C1-3 alkyl and C1-3 haloalkyl; and

[0079] R7Ais selected from H, D, C1-3 alkyl, and C1-3 haloalkyl; or

[0080] R7and R7Atogether with the carbon atom to which they are attached form a spiro fused C3-7 cycloalkane ring.

[0081] In an embodiment,

[0082] R3is selected from C1-3 alkyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce-w aryl, 5-10 membered heteroaryl, ORa3, and NRb3Rc3; wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl forming R3is optionally substituted by 1, 2, 3 or 4 substituents each independently selected from R3B; and

[0083] each R3Bis independently selected from halo, D, CN, C1-3 alkoxy, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C.

[0084] In some preferred embodiments:

[0085] R1is selected from C1-3 alkyl and halo;

[0086] Cy1is Ce-waryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, or 3 substituents independently selected from RCy1;

[0087] each RCy1is independently selected from D, C1-3 alkyl, C1-3 haloalkyl, C2-3 alkenyl, C2-3 alkynyl, halo, CN, ORaCy1, and NRcCy1RdCy1;

[0088] each RaCy1, RcCy1, and RdCy1is independently selected from H, C1-3 alkyl, and C1-3 haloalkyl;

[0089] R2is selected from C1-3 alkyl and halo;

[0090] R3is selected from C1-6 alkyl, C3-6 cycloalkyl, 4-6 membered heterocycloalkyl, Ce-aryl, 5-10 membered heteroaryl, halo, D, and CN;

[0091] R4is selected from H, D, C1-3 alkyl, halo, and CN;

[0092] R5is selected from Cy5and CR5AR5BCy5;

[0093] each Cy5is independently selected from C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3- cycloalkyl, 4-10 770610: ICT-568PC / INCY0568-WO1

[0094] membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl forming Cy5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;

[0095] R5Ais selected from H, D, and C1-3 alkyl;

[0096] R5Bis selected from H, D, and C1-3 alkyl;

[0097] each R5Cis independently selected from C1-3 alkyl and R5D, wherein each C1-3 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;

[0098] each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, C1-3 alkoxy, amino, C1-3 alkylamino, and di(Ci-3alkyl)amino;

[0099] R6is selected from H, D, and C1-3 alkyl;

[0100] R6Ais selected from H, D, and C1-3 alkyl;

[0101] R7is selected from H, D, and C1-3 alkyl; and

[0102] R7Ais selected from H, D, and C1-3 alkyl; or

[0103] R7and R7Atogether with the carbon atom to which they are attached form a spiro fused C3-7 cycloalkane ring.

[0104] In some preferred embodiments:

[0105] R1is selected from C1-3 alkyl, C1-3 haloalkyl, C3-6 cycloalkyl, and halo;

[0106] Cy1is Ce- aryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, 3, or 4 substituents independently selected from RCy1;

[0107] each RCy1is independently selected from C1-3 alkyl, C1-3 haloalkyl, C2-3 alkynyl, halo, CN, and NRcCy1RdCy1;

[0108] each RcCy1and RdCy1is independently selected from H and C1-3 alkyl;

[0109] R2is selected from C1-3 alkyl and halo;

[0110] R3is selected from H, C1-3 alkyl, C2-6 alkynyl, C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl, halo, D, CN, ORa3, NRb3C(O)Ra3, C(O)NRb3Rc3, N=S(O)Rb3Rc3, and NRb3Rc3; wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;

[0111] each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl; wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3B; 770610: ICT-568PC / INCY0568-WO1

[0112] each Rd3is independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, and 4-10 membered heterocycloalkyl; wherein the C1-6 alkyl forming Rd3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from D, halo, CN, S(C>2)Ci-6 alkyl;

[0113] each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, 3, or 4 subtituents each independently selected from R3B;

[0114] each R3Bis independently selected from halo, D, OH, ORd3, C3-10 cycloalkyl, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C;

[0115] each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, halo and C1-6 haloalkyl wherein C2-6 alkenyl is optionally substituted by 1, 2, or 3 halo;

[0116] R4is selected from H, D, and halo;

[0117] R5is selected from Cy5and CR5AR5BCy5;

[0118] each Cy5is independently selected from C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;

[0119] each Cy5Ais independently selected from C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl forming Cy5Ais optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;

[0120] R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl;

[0121] R5Bis selected from H, D, C1-3 alkyl, and C1-3 haloalkyl;

[0122] each R5Cis independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;

[0123] each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, ORa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, NRc5Rd5, and NRc5C(O)Rb5;

[0124] each Ra5, Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl, wherein each C1-6 alkyl forming each Ra5, Rb5, Rc5, and Rd5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from D and halo;

[0125] R6is selected from H, D, and C1-3 alkyl;

[0126] R6Ais H or D;

[0127] R7is selected from H, D, C1-3 alkyl, and halo; and

[0128] R7Ais selected from H, C1-3 alkyl, C1-3 haloalkyl, and halo. 770610: ICT-568PC / INCY0568-WO1

[0129] In an embodiment,

[0130] R3is selected from H, C1-3 alkyl, C2-6 alkynyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl, halo, D, CN, ORa3, NRb3C(O)Ra3, C(O)NRb3Rc3, and NRb3Rc3; wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;

[0131] each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl and 5-10 membered heteroaryl; wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3B;

[0132] each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, 3, or 4 subtituents each independently selected from R3B;

[0133] each R3Bis independently selected from halo, D, OH, C1-3 alkoxy, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the C1-3 alkoxy and 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C; and

[0134] each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, halo and C1-6 haloalkyl wherein C2-6 alkenyl is optionally substituted by 1, 2, or 3 halo.

[0135] In some preferred embodiments:

[0136] R1is selected from C1-3 alkyl and halo;

[0137] Cy1is Ce-waryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, or 3 substituents independently selected from RCy1;

[0138] each RCy1is independently selected from D, C1-3 alkyl, C1-3 haloalkyl, C2-3 alkenyl, C2-3 alkynyl, halo, CN, ORaCy1, and NRcCy1RdCy1;

[0139] each RaCy1, RcCy1, and RdCy1is independently selected from H, C1-3 alkyl, and C1-3 haloalkyl;

[0140] R2is selected from C1-3 alkyl and halo;

[0141] R3is selected from H, C1-6 alkyl, C2-6 alkynyl, C3-6 cycloalkyl, 4-6 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl, halo, D, CN, NRb3C(O)Ra3, N=S(O)Rb3Rc3, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and 770610: ICT-568PC / INCY0568-WO1

[0142] wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;

[0143] each Ra3, Rb3and Rc3is independently selected from H and C1-6 alkyl;

[0144] each Rd3is independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, and 4-10 membered heterocycloalkyl; wherein the C1-6 alkyl forming Rd3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from D, halo, CN, S(C>2)Ci-6 alkyl;

[0145] each R3Ais independently selected from C1-6 alkyl and R3B;

[0146] each R3Bis independently di(Ci-3 alkyl)amino, S(O)(=NH)CI-6 alkyl, ORd3, or C3-10 cycloalkyl;

[0147] R4is selected from H, D, C1-3 alkyl, halo, and CN;

[0148] R5is selected from Cy5and CR5AR5BCy5;

[0149] each Cy5is independently selected from C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;

[0150] each Cy5Ais independently selected from C3-10 cycloalkyl and Ce- aryl;

[0151] R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl;

[0152] R5Bis selected from H, D, and C1-3 alkyl;

[0153] each R5Cis independently selected from C1-3 alkyl and R5D, wherein each C1-3 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;

[0154] each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, C1-3 alkoxy, C(O)Rb5, and NRc5Rd5;

[0155] each Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl;

[0156] R6is selected from H, D, and C1-3 alkyl;

[0157] R6Ais selected from H, D, and C1-3 alkyl;

[0158] R7is selected from H, D, halo, and C1-3 alkyl; and

[0159] R7Ais selected from H, D, halo, and C1-3 alkyl; or

[0160] R7and R7Atogether with the carbon atom to which they are attached form a spiro fused C3-7 cycloalkane ring.

[0161] In an embodiment,

[0162] R3is selected from H, C1-6 alkyl, C2-6 alkynyl, C3-6 cycloalkyl, 4-6 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl, halo, D, CN, NRb3C(O)Ra3, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the 770610: ICT-568PC / INCY0568-WO1

[0163] Ci-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;

[0164] each R3Bis independently di(Ci-3 alkyl)amino, S(O)(=NH)CI-6 alkyl, or C1-3 alkoxy optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C; and each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, halo, and C1-6 haloalkyl, wherein C2-6 alkenyl is optionally substituted by 1, 2, or 3 halo.

[0165] In an embodiment,

[0166] R3is selected from C1-6 alkyl, C3-6 cycloalkyl, 4-6 membered heterocycloalkyl, Ce-w aryl, 5-10 membered heteroaryl, halo, D, CN, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and

[0167] each Rb3and Rc3is independently selected from H and C1-6 alkyl;

[0168] each R3Ais independently selected from C1-6 alkyl and R3B;

[0169] each R3Bis independently di(Ci-3 alkyl)amino.

[0170] In some preferred embodiments:

[0171] R1is halo;

[0172] Cy1is Ce-waryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, or 3 substituents independently selected from RCy1;

[0173] each RCy1is independently selected from C1-3 alkyl, C1-3 haloalkyl, C2-3 alkynyl, halo, CN, and NH2,

[0174] R2is halo;

[0175] R3is C1-6 alkyl;

[0176] R4is selected from H, D, C1-3 alkyl, and halo;

[0177] R5is CR5AR5BCy5;

[0178] each Cy5is independently selected from Ce- aryl and 5-10 membered heteroaryl, wherein the Ce- aryl and 5-10 membered heteroaryl forming Cy5is optionally substituted by 1, 2, or 3 substituents each independently selected from R5C;

[0179] R5Ais selected from H, D, and C1-3 alkyl;

[0180] R5Bis selected from H, D, and C1-3 alkyl;

[0181] each R5Cis independently selected from C1-3 alkyl, halo, D, CN, OH, C1-3 alkoxy, amino, C1-3 alkylamino, and di(Ci-3alkyl)amino;

[0182] R6is H;

[0183] R6Ais H;

[0184] R7is H; and

[0185] R7Ais H.

[0186] In some preferred embodiments,

[0187] R1is halo; 770610: ICT-568PC / INCY0568-WO1

[0188] Cy1is 6-10 membered heteroaryl optionally substituted with 1, 2, 3, or 4 substituents independently selected from RCy1;

[0189] each RCy1is independently selected from C1-3 alkyl, halo, CN, and NRcCy1RdCy1; each RcCy1and RdCy1is H;

[0190] R2is halo;

[0191] R3is selected from C1-3 alkyl, 4-10 membered heterocycloalkyl, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A;

[0192] each Rb3and Rc3is independently selected from H and C1-6 alkyl;

[0193] each R3Ais independently selected from C1-6 alkyl and R3B;

[0194] each R3Bis independently di(Ci-3 alkyl)amino;

[0195] R4is H;

[0196] R5is selected from Cy5and CR5AR5BCy5;

[0197] each Cy5is independently selected from 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;

[0198] each Cy5Ais independently selected from C3-10 cycloalkyl and Ce- aryl;

[0199] R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl;

[0200] R5Bis selected from H, D, and C1-3 alkyl;

[0201] each R5Cis independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;

[0202] each R5Dis independently selected from halo, D, C(O)Rb5, and NRc5Rd5;

[0203] each Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl;

[0204] R6is H;

[0205] R6Ais H;

[0206] R7is selected from H and halo; and

[0207] R7Ais selected from H and halo.

[0208] In some preferred embodiments:

[0209] R1is halo;

[0210] Cy1is 6-10 membered heteroaryl optionally substituted with 1, 2, 3, or 4 substituents independently selected from RCy1;

[0211] each RCy1is independently selected from halo, CN, and NRcCy1RdCy1;

[0212] RcCy1and RdCy1is H;

[0213] R2is halo; 770610: ICT-568PC / INCY0568-WO1

[0214] R3is selected from C1-3 alkyl, 4-10 membered heterocycloalkyl, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A;

[0215] each Ra3, Rb3, and Rc3is independently selected from H and C1-6 alkyl;

[0216] each R3Ais independently selected from C1-6 alkyl and R3B;

[0217] each R3Bis independently di(Ci-3 alkyl)amino;

[0218] R4is H;

[0219] R5is selected from Cy5and CR5AR5BCy5;

[0220] each Cy5is independently selected from 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;

[0221] each Cy5Ais independently selected from C3-10 cycloalkyl and Ce- aryl;

[0222] R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl;

[0223] R5Bis selected from H, D, and C1-3 alkyl;

[0224] each R5Cis independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;

[0225] each R5Dis independently selected from halo, D, C(O)Rb5, and NRc5Rd5,;

[0226] each Ra5, Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl;

[0227] R6is H;

[0228] R6Ais H;

[0229] R7is selected from H and halo; and

[0230] R7Ais selected from H and halo.

[0231] In some preferred embodiments, the compound of Formula I is a compound of any one of Formulae l-A to l-H:

[0232]

[0233] (l-A) (l-B) 770610: ICT-568PC / INCY0568-WO1

[0234]

[0235] or a pharmaceutically acceptable salt thereof.

[0236] In some preferred embodiment, the compound of Formula I is a compound of Formula l-G, wherein:

[0237] R3is C1-3 alkyl optionally substituted by 1 or 2 substituents each independently selected from R3B;

[0238] Gy5is pyridinyl optionally substituted with amino; and

[0239] R5Ais C1-3 alkyl.

[0240] In some embodiments: the compound of Formula I is a compound of Formula (l-l) or (l-J):

[0241]

[0242] (i-i) (i-J); 770610: ICT-568PC / INCY0568-WO1

[0243] or a pharmaceutically acceptable salt thereof.

[0244] In some embodiments, the compound of Formula I is a compound of Formula (l-J) or Formula (l-K):

[0245]

[0246] (l-J) (l-K);

[0247] or a pharmaceutically acceptable salt thereof;

[0248] wherein n is 0, 1, or 2.

[0249] In some embodiments, R1is halo (e.g., F or Cl).

[0250] In some embodiments, R1is Cl.

[0251] In some embodiments, Cy1is phenyl, napthyl, or 6-10 membered heteroaryl, each optionally substituted with 1, 2, 3, or 4 substituents (or 1, 2, or 3 substituents, or 1 or 2 substituents, or 1 substituent) independently selected from RCy1.

[0252] In some embodiments, Cy1is Ce-waryl, benzothiophenyl, benzothiazolyl, or indazolyl, each optionally substituted with 1, 2, 3 or 4 substituents (or 1, 2, or 3 substituents, or 1 or 2 substituents, or 1 substituent) independently selected from RCy1.

[0253] In some embodiments, Cy1is Ce- aryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, 3, or 4 substituents (or 1, 2, or 3 substituents, or 1 or 2 substituents, or 1 substituent) independently selected from C1-3 alkyl, C2-ealkynyl, halo, OH, and NH2.

[0254] In some embodiments, Cy1is selected from phenyl, naphthyl (such as 1-naphthyl and 2-naphthyl), benzothiazolyl (such as benzothiazol-2-yl, -4-yl, -5-yl, -6-yl, or -7-yl), benzothiophenyl (such as benzothiophen-2-yl, -4-yl, -5-yl, -6-yl, or -7-yl), and indazolyl (such as indazo-2-yl, -3-yl, -4-yl, -5-yl, or -6-yl) each optionally substituted with 1, 2, or 3 substituents independently selected from RCy1.

[0255] In some embodiments, each RCy1is independently selected from C1-3 alkyl, C2-3 alkynyl, C1-3 haloalkyl, halo, CN, and NRcCy1RdCy1.

[0256] In some embodiments, each RCy1is independently selected from C1-3 alkyl, halo, CN, and NRcCy1RdCy1.

[0257] In some embodiments, each RCy1is independently selected from C1-3 alkyl, C2-3 alkynyl, halo, CN, and NH2. 770610: ICT-568PC / INCY0568-WO1

[0258] In some embodiments, Cy1is selected from 2-amino-7-fluorobenzo[d]thiazol-4-yl, 2-amino-3-cyano-7-fluorobenzo[d]thiophen-4-yl, 1-cyanonaphth-8-yl, and 5,6-dimethyl-1 / 7-indazol-4-yl

[0259] In some embodiments, R2is halo (e.g., F or Cl).

[0260] In some embodiments, R2is F.

[0261] In some embodiments,

[0262] R3is selected from H, C1-3 alkyl, C2-6 alkynyl, 4-10 membered heterocycloalkyl, halo, CN, ORa3, NRb3C(O)Ra3, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;

[0263] each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, 4-10 membered heterocycloalkyl, and 5-10 membered heteroaryl; wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, or 3 substituents independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, or 3 substituents independently selected from R3B;

[0264] each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, or 3, subtituents each independently selected from R3B;

[0265] each R3Bis independently selected from halo, OH, C1-3 alkoxy, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the C1-3 alkoxy and 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C; and

[0266] each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, and halo, wherein C2-6 alkenyl is optionally substituted by 1, 2, or 3 halo.

[0267] In some embodiments,

[0268] R3is selected from C1-6 alkyl, C3-6 cycloalkyl, 4-10 membered heterocycloalkyl, Ce-aryl, 5-10 membered heteroaryl, halo, D, CN, N=S(O)Rb3Rc3; wherein the C3-6 cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, or 3 substituents independently selected from R3A; and wherein the C1-6 alkyl forming R3is optionally substituted by 1, 2, or 3 substituents each independently selected from R3B;

[0269] each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl and 5-10 membered heteroaryl; wherein the C3-cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, 3, or 4 substituents 770610: ICT-568PC / INCY0568-WO1

[0270] independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, or 3 substituents independently selected from R3B;

[0271] each Rd3is independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, and 4-10 membered heterocycloalkyl; wherein the C1-6 alkyl forming Rd3is optionally substituted with 1, 2, or 3 substituents independently selected from D, halo, CN, S(C>2)Ci-6 alkyl;

[0272] each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, or 3 subtituents each independently selected from R3B;

[0273] each R3Bis independently selected from halo, D, CN, ORd3, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, S(O)(=NH)CI-6 alkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, or 3 substituents independently selected from R3C; and

[0274] each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo and C1-6 haloalkyl, wherein C2-6 alkenyl, and C2-6 alkynyl are each optionally substituted by 1, 2, or 3 halo.

[0275] In some embodiments, R3is selected from C1-3 alkyl, 4-10 membered heterocycloalkyl, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A.

[0276] In some embodiments, R3is 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A. In some embodiments, R3is 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A.

[0277] In some embodiments, R3is H or C1-3 alkyl. In some embodiments, R3is selected from H, C2-6 alkynyl, D, CN, and NRb3C(O)Ra3, wherein the C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 (e.g., 1, 2, or 3, 1 or 2, or 1) substituents each independently selected from R3B.

[0278] In some embodiments, each Rb3and Rc3is independently selected from H and C1-6 alkyl.

[0279] In some embodiments, R3is C1-3 alkyl or halo.

[0280] In some embodiments, R3is C1-3 alkyl (e.g., methyl or ethyl).

[0281] In some embodiments, R3is methyl.

[0282] In some embodiments, R3is ORa3.

[0283] In some embodiments, Ra3is C1-6 alkyl (e.g., methyl) optionally substituted by 1, 2, 3, or 4 substituents independently selected from R3B.

[0284] In some embodiments, Ra3is C1-6 alkyl (e.g., methyl) optionally substituted by 1 substituent selected from R3B. 770610: ICT-568PC / INCY0568-WO1

[0285] In some embodiments, Ra3is methyl optionally substituted by 1 substituent selected from R3B.

[0286] In some embodiments, at least one R3Bis 4-10 membered heterocycloalkyl optionally substituted by 1, 2, 3 or 4 (e.g., 1, 2, or 3, 1 or 2, or 1) R3C.

[0287] In some embodiments, at least one R3Bis 5-6 membered heterocycloalkyl, wherein the at least one 5-6 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 (e.g., 1, 2, or 3, 1 or 2, or 1) R3C.

[0288] In some embodiments, each R3Bis independently di(Ci-3 alkyl)amino.

[0289] In some embodiments, at least one R3Cis C1-6 alkyl (e.g., methyl). In some such embodiments, each R3Cis C1-6 alkyl (e.g., methyl).

[0290] In some embodiments, at least one R3Cis halo (e.g., fluoro). In some such embodiments, each R3Cis halo (e.g., fluoro).

[0291] In some embodiments, at least one R3Cis C1-6 haloalkyl (e.g., C1-6 fluoroalkyl or mono-, di-, or tri-halomethyl, such as fluoromethyl, difluoromethyl or trifluormethyl). In some such embodiments, each R3Cis C1-6 haloalkyl (e.g., C1-6 fluoroalkyl or mono-, di-, or tri-halomethyl, such as fluoromethyl, difluoromethyl or trifluormethyl).

[0292] In some embodiments, R3is 4-10 membered heterocycloalkyl optionally substituted with 1, 2, 3, or 4 (e.g., 1, 2, or 3, 1 or 2, or 1) substituents independently selected from R3A.

[0293] In some embodiments, R3is 8-10 membered heterocycloalkyl optionally substituted with 1, 2, 3, or 4 (e.g., 1, 2, or 3, 1 or 2, or 1) substituents independently selected from R3A.

[0294] In some embodiments, R3is 8-10 membered fused bicyclic heterocycloalkyl optionally substituted with 1, 2, 3, or 4 (e.g., 1, 2, or 3, 1 or 2, or 1) substituents independently selected from R3A.

[0295] In some embodiments, each R3Ais C1-6 alkyl (e.g., methyl).

[0296] In some embodiments, each R3Ais independently selected from C1-6 alkyl and R3B. In some embodiments, R4is H or D.

[0297] In some embodiments, R4is H.

[0298] In some embodiments, R5is Cy5.

[0299] In some embodiments, R5is CR5AR5BCy5.

[0300] In some embodiments, R5Ais C1-3 alkyl (e.g., methyl or ethyl).

[0301] In some embodiments, R5Ais C1-3 haloalkyl (e.g., difluoromethyl or trifluoromethyl). In some embodiments, R5Bis H.

[0302] In some embodiments, each Cy5is independently selected from 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C. 770610: ICT-568PC / INCY0568-WO1

[0303] In some embodiments, Cy5is 5-10 membered heteroaryl optionally substituted by 1, 2, or 3 substituents (or 1 or 2 substituents, or 1 substituent) each independently selected from R5C.

[0304] In some embodiments, Cy5is pyridinyl (such as pyridin-2-yl, -3-yl, -4-yl, -5-yl, or -6-yl) optionally substituted with 1 or 2 substituents independently selected from R5C.

[0305] In some embodiments, each Cy5Ais independently selected from C3-10 cycloalkyl and Ce-io aryl.

[0306] In some embodiments, R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl. In some embodiments, R5Bis selected from H, D, and C1-3 alkyl.

[0307] In some embodiments, each R5Cis independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D.

[0308] In some embodiments, each R5Cis independently selected from amino, C1-3 alkylamino, and di(Ci-3alkyl)amino.

[0309] In some embodiments, each R5Cis amino.

[0310] In some embodiments, each R5Dis independently selected from halo, D, C(O)Rb5, and NRc5Rd5.

[0311] In some embodiments, each Rb5, Rc5, and Rd5is independently selected from H and Ci-6 alkyl.

[0312] In some embodiments, Cy5is 2-aminopyridin-3-yl.

[0313] In some embodiments, R6is H.

[0314] In some embodiments, R6ais H.

[0315] In some embodiments, R7is H.

[0316] In some embodiments, R7ais H.

[0317] In some embodiments, R7is halo.

[0318] In some embodiments, R7ais halo.

[0319] In other embodiments, the compound of Formula (I) is selected from the compounds in Table 1, and pharmaceutically acceptable salts thereof.

[0320] Table 1

[0321] Entry Compound Name

[0322] 1 2-amino-4-(4-(1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 2 4-(4-(1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[c(]thiazol-2-amine

[0323] 3 8-(4-(1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-1-naphthonitrile

[0324]

[0325] 770610: ICT-568PC / INCY0568-WO1

[0326] Entry Compound Name

[0327] 4 3-(1-(7-chloro-8-(5,6-dimethyl-1 / 7-indazol-4-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-4-yl)ethyl)pyridin-2-amine.

[0328] 5 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(pyridin-3-yl)ethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0329] 6 2-amino-4-(4-(1-(3-aminopyrazin-2-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 7 2-amino-4-(4-(1-(3-aminopyridazin-4-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0330] 8 2-amino-4-(4-(1-(5-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 9 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(1 -methyl- 1 / 7-pyrazol-5-yl)ethyl)-5, 6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0331] 10 2-amino-4-(4-(1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorothieno[3,2-c]pyridine-3-carbonitrile 11 2-amino-4-(4-(1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6-dimethyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0332] 12 2-amino-4-(4-(1-(2-aminopyridin-3-yl)ethyl-1-d)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0333] 13 2-amino-4-(4-(1-(2-amino-5-fluoropyridin-3-yl)ethyl-1-d)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0334] 14 2-amino-4-(4-((2-aminopyridin-3-yl)(cyclopropyl)methyl-c / )-7-chloro-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0335] 15 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-methyl-2-oxopyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0336] 16 2-amino-4-(7-chloro-4-(1-cyclopropyl-2-oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0337]

[0338] 770610: ICT-568PC / INCY0568-WO1

[0339] Entry Compound Name

[0340] 17 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(2-oxo-1-(2,2,2-trifluoroethyl) pyrrolidin-3- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0341] 18 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(2-oxo-1-phenylpyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0342] 19 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-methyl-2-oxopiperidin-4-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 20 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(3-oxooctahydroindolizin-2-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 21 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-methyl-2-oxopiperidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 22 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(1 -methyl- 1 / 7- 1,2, 4-triazol-5-yl)ethyl)- 5,6-dihydro-4 / 7-benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0343] 23 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxopyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[cte][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0344] 24 4-(4-(1-acetylpyrrolidin-3-yl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile 25 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4 / 7-benzo[cfe][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0345] 26 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(2-methyl-3-oxo-2-azabicyclo[3.1.0]hexan- 4-yl)-5,6-dihydro-4 / 7-benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0346] 27 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[cfe][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0347] 28 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4-(1- methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[cfe][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0348] 29 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-4-(1-(2-aminopyridin-3- yl)ethyl)-7-chloro-9-fluoro- / V-methyl-5,6-dihydro-4 / 7-benzo[cte][1,6]naphthyridine-2- carboxamide

[0349]

[0350] 770610: ICT-568PC / INCY0568-WO1

[0351] Entry Compound Name

[0352] 30 2-amino-4-(4-(1-(2-aminopyridin-3-yl)ethyl)-7-chloro-6,6,9-trifluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0353] 31 3-(8-(2-amino-7-fluorobenzo[d]thiazol-4-yl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-4-yl)-1-methylpyrrolidin-2-one

[0354] 32 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -methyl-4- (1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2- carboxamide

[0355] 33 2-amino-4-(7-chloro-9-fluoro-2-(1-hydroxyethyl)-4-(1-methyl-2-oxopyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0356] 34 2-amino-4-(7-chloro-9-fluoro-2-methoxy-4-(1-methyl-2-oxopyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo [b]thiophene-3- carbonitrile

[0357] 35 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-(1-methyl-2- oxopyrrolidin-3-yl)- / V-(1-methylazetidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0358] 36 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -(2-hydroxy- 2-methylpropyl)-4-(1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0359] 37 / V-(8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-(1- methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-2- yl)acetamide

[0360] 38 2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-(1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0361] 39 2-amino-4-(7-chloro-9-fluoro-4-(4-hydroxy-1-(methyl-d3)-2-oxopyrrolidin-3-yl)-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0362] 40 2-amino-4-(7-chloro-4-(4-(difluoromethoxy)-1-(methyl-d3)-2-oxopyrrolidin-3-yl)-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0363] 41 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0364]

[0365] 770610: ICT-568PC / INCY0568-WO1

[0366] Entry Compound Name

[0367] 42 2-amino-4-(7-chloro-4-(5-(difluoromethyl)-1-(methyl-d3)-2-oxopyrrolidin-3-yl)-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0368] 43 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(4-(methyl-d3)-5-oxo-4- azaspiro[2.4]heptan-6-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0369] 44 2-amino-4-(7-chloro-9-fluoro-4-(5-((methoxy-d3)methyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0370] 45 4-(8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4H-benzo[de][1,6]naphthyridin-4-yl)- / V, / V-dimethyl-1-(methyl-d3)-5- oxopyrrolidine-2-carboxamide

[0371] 46 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(2-methyl-3-oxoisoxazolidin-4-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0372] 47 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0373] 48 2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-(1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0374] 49 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0375] 50 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0376] 51 2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0377] 52 2-amino-4-(7-chloro-9-fluoro-2-((2-fluorotetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0378]

[0379] 770610: ICT-568PC / INCY0568-WO1

[0380] Entry Compound Name

[0381] 53 2-amino-4-(7-chloro-9-fluoro-4-((1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- y I) -2- ( 1 -(1 -methylpyrrolidin-2-yl)ethoxy)-5,6-dihydro-4 / 7-benzo[de][1, 6] n aphthy ri d i n- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0382] 54 2-amino-4-(7-chloro-2-((2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0383] 55 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-2-((1-methylpyrrolidin-2-yl)methoxy)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0384] 56 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- y I) -2- ( 1 -(1 -methylpyrrolidin-2-yl)ethoxy)-5,6-dihydro-4 / 7-benzo[de][1, 6] n aphthy ri d i n- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0385] 57 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0386] 58 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-(1 -(methyl- d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7-pyran-4-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[0387] 59 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-(1 -(methyl- d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[0388] 60 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[0389] 61 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[0390] 62 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[0391] 63 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[0392]

[0393] 770610: ICT-568PC / INCY0568-WO1

[0394] Entry Compound Name

[0395] 64 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[0396] 65 2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[0397] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[0398] 66 2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0399] 67 2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0400] 68 2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[0401] 69 2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0402] 70 2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0403] 71 2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-(1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0404] 72 2-amino-4-(7-chloro-9-fluoro-4-(5-fluoro-1-methyl-2-oxopiperidin-3-yl)-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0405] 73 2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-(1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0406] 74 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-(1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0407] 75 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(5-oxooctahydroindolizin-6-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0408]

[0409] 770610: ICT-568PC / INCY0568-WO1

[0410] Entry Compound Name

[0411] 76 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0412] 77 2-amino-4-(7-chloro-2-(3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9-fluoro-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0413] 78 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-2-(5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0414] 79 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5-phenylpyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0415] 80 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[0416] 81 2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0417] 82 2-amino-4-(7-chloro-2-(3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-(1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0418] 83 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9-fluoro-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0419] 84 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-2-(1-methylhexahydropyrrolo[3,4-b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0420] 85 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4-(1-(methyl- d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0421] 86 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0422]

[0423] 770610: ICT-568PC / INCY0568-WO1

[0424] Entry Compound Name

[0425] 87 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- (1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0426] 88 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[0427] 89 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[0428] 90 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[0429] 91 2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0430] 92 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0431] 93 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0432] 94 2-amino-4-(7-chloro-2-(3-(dimethylamino)-4-methoxypyrrolidin-1-yl)-9-fluoro-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0433] 95 2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4-(1-(methyl- d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0434] 96 2-amino-4-(7-chloro-9-fluoro-4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0435] 97 2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0436]

[0437] 770610: ICT-568PC / INCY0568-WO1

[0438] Entry Compound Name

[0439] 98 2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0440] 99 2-amino-4-(7-chloro-2-((2-cyanoethoxy)methyl)-9-fluoro-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0441] 100 2-amino-4-(7-chloro-9-fluoro-2-(hydroxymethyl)-4-(1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0442] 101 2-amino-4-(7-chloro-2-(3-(dimethylamino)cyclobutyl)-9-fluoro-4-(1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0443] 102 2-amino-4-(7-chloro-2-(3-(dimethylamino)-4-methoxypyrrolidin-1-yl)-9-fluoro-4-(1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0444] 103 2-amino-4-(7-chloro-2-(4-(dimethylamino)-2-azabicyclo[2.1.1]hexan-2-yl)-9-fluoro- 4-(1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0445] 104 2-amino-4-(7-chloro-4-(1-ethyl-2-oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 105 2-amino-4-(7-chloro-9-fluoro-4-(1-(isothiazol-4-yl)ethyl)-2-methyl-5,6-dihydro-4H- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0446] 106 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(5-methyl-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0447] 107 2-amino-4-(7-chloro-4-(1,4-dimethyl-2-oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0448] 108 2-amino-4-(7-chloro-4-(1,5-dimethyl-2-oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0449] 109 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(2-oxo-1-(trifluoromethyl)pyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0450]

[0451] 770610: ICT-568PC / INCY0568-WO1

[0452] In other embodiments, the compound of Formula (I) is selected from the compounds in Table 2, and pharmaceutically acceptable salts thereof.

[0453] Table 2

[0454] Entry Compound Name

[0455] 1 2-amino-4-(4-((F?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0456] 2 2-amino-4-(4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0457] 3 2-amino-4-((F?a)-4-((F?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0458] 4 2-amino-4-((Sa)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0459] 5 2-amino-4-((Sa)-4-((F?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0460] 6 2-amino-4-((F?a)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0461] 7 4-(4-((F?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[c(]thiazol-2-amine

[0462] 8 4-(4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[c(]thiazol-2-amine

[0463] 9 4-((F?a)-4-((F?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[c(]thiazol-2-amine

[0464] 10 4-((Sa)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[c(]thiazol-2-amine

[0465] 11 4-((F?a)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[c(]thiazol-2-amine

[0466] 12 4-((Sa)-4-((F?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[c(]thiazol-2-amine

[0467] 13 8-(4-((F?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-1-naphthonitrile

[0468]

[0469] 770610: ICT-568PC / INCY0568-WO1

[0470] Entry Compound Name

[0471] 14 8-(4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-1-naphthonitrile

[0472] 15 8-((Ra)-4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-1 -naphthonitrile

[0473] 16 8-((Sa)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-1 -naphthonitrile

[0474] 17 8-((Ra)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-1 -naphthonitrile

[0475] 18 8-((Sa)-4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-1 -naphthonitrile

[0476] 19 3-(1-((R)-7-chloro-8-(5,6-dimethyl-1 / 7-indazol-4-yl)-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-4-yl)ethyl)pyridin-2-amine

[0477] 20 3-(1-((S)-7-chloro-8-(5,6-dimethyl-1 / 7-indazol-4-yl)-9-fluoro-2-methyl-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-4-yl)ethyl)pyridin-2-amine

[0478] 21 3-((Ka)-1-(( / ?)-7-chloro-8-(5,6-dimethyl-1 / 7-indazol-4-yl)-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)ethyl)pyridin-2-amine

[0479] 22 3-((Sa)-1-((S)-7-chloro-8-(5,6-dimethyl-1 / 7-indazol-4-yl)-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)ethyl)pyridin-2-amine

[0480] 23 3-(( / ?a)-1-((S)-7-chloro-8-(5,6-dimethyl-1 / 7-indazol-4-yl)-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)ethyl)pyridin-2-amine

[0481] 24 3-((Sa)-1-(( / ?)-7-chloro-8-(5,6-dimethyl-1 / 7-indazol-4-yl)-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)ethyl)pyridin-2-amine.

[0482] 25 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((R)-1-(pyridin-3-yl)ethyl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0483] 26 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((R)-1-(pyridin-3-yl)ethyl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0484] 27 2-amino-(Ra)-4-(7-chloro-9-fluoro-2-methyl-4-(( / ?)-1-(pyridin-3-yl)ethyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 28 2-amino-(Sa)-4-(7-chloro-9-fluoro-2-methyl-4-((R)-1-(pyridin-3-yl)ethyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 29 2-amino-(Ra)-4-(7-chloro-9-fluoro-2-methyl-4-((S)-1-(pyridin-3-yl)ethyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 30 2-amino-(Sa)-4-(7-chloro-9-fluoro-2-methyl-4-((S)-1-(pyridin-3-yl)ethyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0485]

[0486] 770610: ICT-568PC / INCY0568-WO1

[0487] Entry Compound Name

[0488] 31 2-amino-4-(4-((R)-1-(3-aminopyrazin-2-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0489] 32 2-amino-4-(4-((R)-1-(3-aminopyrazin-2-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0490] 33 2-amino-(Ra)-4-(4-((R)-1-(3-aminopyrazin-2-yl)ethyl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0491] 34 2-amino-(Sa)-4-(4-((R)-1-(3-aminopyrazin-2-yl)ethyl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0492] 35 2-amino-(Ra)-4-(4-((S)-1-(3-aminopyrazin-2-yl)ethyl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0493] 36 2-amino-(Sa)-4-(4-((S)-1-(3-aminopyrazin-2-yl)ethyl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0494] 37 2-amino-4-(4-((R)-1-(3-aminopyridazin-4-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0495] 38 2-amino-4-(4-((R)-1-(3-aminopyridazin-4-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0496] 39 2-amino-4-((Ra)-4-((R)-1-(3-aminopyridazin-4-yl)ethyl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0497] 40 2-amino-4-((Sa)-4-((S)-1-(3-aminopyridazin-4-yl)ethyl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0498] 41 2-amino-4-((Sa)-4-((R)-1-(3-aminopyridazin-4-yl)ethyl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0499]

[0500] 770610: ICT-568PC / INCY0568-WO1

[0501] Entry Compound Name

[0502] 42 2-amino-4-(( / ?a)-4-((S)-1-(3-aminopyridazin-4-yl)ethyl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0503] 43 2-amino-4-(4-((R)-1-(5-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0504] 44 2-amino-4-(4-((S)-1-(5-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0505] 45 2-amino-4-((Ra)-4-((R)-1-(5-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0506] 46 2-amino-4-((Sa)-4-((S)-1-(5-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0507] 47 2-amino-4-((Sa)-4-((R)-1-(5-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0508] 48 2-amino-4-((Ra)-4-((S)-1-(5-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0509] 49 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((R)-1-(1-methyl-1 / 7-pyrazol-5-yl)ethyl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0510] 50 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((S)-1-(1-methyl-1 / 7-pyrazol-5-yl)ethyl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0511] 51 2-amino-4-(( / ?a)-7-chloro-9-fluoro-2-methyl-4-((R)-1-(1-methyl-1 / 7-pyrazol-5- yl)ethyl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0512] 52 2-amino-4-((Sa)-7-chloro-9-fluoro-2-methyl-4-((S)-1-(1-methyl-1 / 7-pyrazol-5- yl)ethyl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0513]

[0514] 770610: ICT-568PC / INCY0568-WO1

[0515] Entry Compound Name

[0516] 53 2-amino-4-((Sa)-7-chloro-9-fluoro-2-methyl-4-((R)-1-(1-methyl-1 / 7-pyrazol-5- yl)ethyl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0517] 54 2-amino-4-(( / ?a)-7-chloro-9-fluoro-2-methyl-4-((S)-1-(1-methyl-1 / 7-pyrazol-5- yl)ethyl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0518] 55 2-amino-4-(4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorothieno[3,2-c]pyridine-3- carbonitrile

[0519] 56 2-amino-4-(4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorothieno[3,2-c]pyridine-3- carbonitrile

[0520] 57 2-amino-4-((Ra)-4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorothieno[3,2-c]pyridine-3- carbonitrile

[0521] 58 2-amino-4-((Sa)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorothieno[3,2-c]pyridine-3- carbonitrile

[0522] 59 2-amino-4-((Sa)-4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorothieno[3,2-c]pyridine-3- carbonitrile

[0523] 60 2-amino-4-((Ra)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorothieno[3,2-c]pyridine-3- carbonitrile

[0524] 61 2-amino-4-((S)-4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6-dimethyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0525] 62 2-amino-4-((R)-4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6-dimethyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0526] 63 2-amino-(Ra)-4-((S)-4-(( / ?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6- dimethyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0527]

[0528] 770610: ICT-568PC / INCY0568-WO1

[0529] Entry Compound Name

[0530] 64 2-amino-(Sa)-4-((S)-4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6- dimethyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0531] 65 2-amino-( / ?a)-4-((R)-4-(( / ?)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6- dimethyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0532] 66 2-amino-(Sa)-4-((R)-4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6- dimethyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0533] 67 2-amino-4-((S)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6-dimethyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0534] 68 2-amino-4-((R)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6-dimethyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0535] 69 2-amino-(Ra)-4-((S)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6- dimethyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0536] 70 2-amino-(Sa)-4-((S)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6- dimethyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0537] 71 2-amino-(Ra)-4-(( / ?)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6- dimethyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0538] 72 2-amino-(Sa)-4-((R)-4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-9-fluoro-2,6- dimethyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0539] 73 2-amino-4-((Ra)-4-((R)-1-(2-aminopyridin-3-yl)ethyl-1-cf)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0540] 74 2-amino-4-((Sa)-4-((S)-1-(2-aminopyridin-3-yl)ethyl-1-d)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0541]

[0542] 770610: ICT-568PC / INCY0568-WO1

[0543] Entry Compound Name

[0544] 75 2-amino-4-((Ra)-4-((S)-1-(2-aminopyridin-3-yl)ethyl-1-c / )-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0545] 76 2-amino-4-((Sa)-4-((R)-1-(2-aminopyridin-3-yl)ethyl-1-c / )-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0546] 77 2-amino-4-(( / ?a)-4-(( / ?)-1-(2-amino-5-fluoropyridin-3-yl)ethyl-1-c / )-7-chloro- 9- fluoro- 2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0547] 78 2-amino-4-((Sa)-4-((S)-1-(2-amino-5-fluoropyridin-3-yl)ethyl-1-d)-7-chloro-9-fluoro- 2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0548] 79 2-amino-4-(( / ?a)-4-((S)-1-(2-amino-5-fluoropyridin-3-yl)ethyl-1-c / )-7-chloro-9-fluoro- 2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0549] 80 2-amino-4-((Sa)-4-((R)-1-(2-amino-5-fluoropyridin-3-yl)ethyl-1-c / )-7-chloro-9-fluoro- 2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0550] 81 2-amino-4-((Ra)-4-(( / ?)-(2-aminopyridin-3-yl)(cyclopropyl)methyl-c / )-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0551] 82 2-amino-4-((Sa)-4-((S)-(2-aminopyridin-3-yl)(cyclopropyl)methyl-c / )-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0552] 83 2-amino-4-(( / ?a)-4-((S)-(2-aminopyridin-3-yl)(cyclopropyl)methyl-c / )-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0553] 84 2-amino-4-((Sa)-4-((R)-(2-aminopyridin-3-yl)(cyclopropyl)methyl-c / )-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0554] 85 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((R)-1-methyl-2-oxopyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0555]

[0556] 770610: ICT-568PC / INCY0568-WO1

[0557] Entry Compound Name

[0558] 86 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-methyl-2-oxopyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0559] 87 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-methyl-2-oxopyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0560] 88 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((R)-1-methyl-2-oxopyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0561] 89 2-amino-4-( / ?a)-(7-chloro-4-(1-cyclopropyl-2-oxopyrrolidin-3-yl)-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0562] 90 2-amino-4-(Sa)-(7-chloro-4-(1-cyclopropyl-2-oxopyrrolidin-3-yl)-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0563] 91 2-amino-4-( / ?a)-(7-chloro-4-((R)-1-cyclopropyl-2-oxopyrrolidin-3-yl)-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0564] 92 2-amino-4-(Sa)-(7-chloro-4-((S)-1-cyclopropyl-2-oxopyrrolidin-3-yl)-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0565] 93 2-amino-4-( / ?a)-(7-chloro-4-((S)-1-cyclopropyl-2-oxopyrrolidin-3-yl)-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0566] 94 2-amino-4-(Sa)-(7-chloro-4-((R)-1-cyclopropyl-2-oxopyrrolidin-3-yl)-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0567] 95 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-(2-oxo-1-(2,2,2-trifluoroethyl) pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0568] 96 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-(2-oxo-1-(2,2,2-trifluoroethyl) pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0569]

[0570] 770610: ICT-568PC / INCY0568-WO1

[0571] Entry Compound Name

[0572] 97 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-(( / ?)-2-oxo-1-(2,2,2-trifluoroethyl) pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0573] 98 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((S)-2-oxo-1-(2,2,2-trifluoroethyl) pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0574] 99 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((S)-2-oxo-1-(2,2,2-trifluoroethyl) pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0575] 100 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((R)-2-oxo-1-(2,2,2-trifluoroethyl) pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0576] 101 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-(2-oxo-1-phenylpyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0577] 102 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-(2-oxo-1-phenylpyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0578] 103 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((R)-2-oxo-1-phenylpyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0579] 104 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((S)-2-oxo-1-phenylpyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0580] 105 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((S)-2-oxo-1-phenylpyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0581] 106 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((R)-2-oxo-1-phenylpyrrolidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0582] 107 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-(1-methyl-2-oxopiperidin-4-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0583]

[0584] 770610: ICT-568PC / INCY0568-WO1

[0585] Entry Compound Name

[0586] 108 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-(1-methyl-2-oxopiperidin-4-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0587] 109 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-(( / ?)-1-methyl-2-oxopiperidin-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0588] 110 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-methyl-2-oxopiperidin-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0589] 111 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-methyl-2-oxopiperidin-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0590] 112 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((R)-1-methyl-2-oxopiperidin-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0591] 113 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((2 / ?,8a / ?)-3-oxooctahydroindolizin-2- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0592] 114 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((2S,8aS)-3-oxooctahydroindolizin-2- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0593] 115 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((2S,8a / ?)-3-oxooctahydroindolizin-2- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0594] 116 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((2R,8aS)-3-oxooctahydroindolizin-2- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0595] 117 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((2 / ?,8aS)-3-oxooctahydroindolizin-2- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0596] 118 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((2S,8a / ?)-3-oxooctahydroindolizin-2- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0597]

[0598] 770610: ICT-568PC / INCY0568-WO1

[0599] Entry Compound Name

[0600] 119 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((2S,8aS)-3-oxooctahydroindolizin-2- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0601] 120 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((2R,8a / ?)-3-oxooctahydroindolizin-2- yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0602] 121 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-(( / ?)-1-methyl-2-oxopiperidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0603] 122 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-methyl-2-oxopiperidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0604] 123 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-methyl-2-oxopiperidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0605] 124 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((R)-1-methyl-2-oxopiperidin-3-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0606] 125 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-(( / ?)-1-(1-methyl-1H-1,2,4-triazol-5- yl)ethyl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0607] 126 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-(1-methyl-1H-1,2,4-triazol-5- yl)ethyl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0608] 127 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-(1-methyl-1H-1,2,4-triazol-5- yl)ethyl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0609] 128 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((R)-1-(1-methyl-1H-1,2,4-triazol-5- yl)ethyl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0610] 129 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-(( / ?)-1-(methyl-cf3)-2-oxopyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0611]

[0612] 770610: ICT-568PC / INCY0568-WO1

[0613] Entry Compound Name

[0614] 130 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0615] 131 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((S)-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0616] 132 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((R)-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0617] 133 4-( / ?a)-(4-(( / ?)-1-acetylpyrrolidin-3-yl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile 134 4-(Sa)-(4-((S)-1-acetylpyrrolidin-3-yl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile 135 4-( / ?a)-(4-((S)-1-acetylpyrrolidin-3-yl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile 136 4-(Sa)-(4-((R)-1-acetylpyrrolidin-3-yl)-7-chloro-9-fluoro-2-methyl-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile 137 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((3R,3a / ?,6a / ?)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0618] 138 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((3S,3aS,6aS)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0619] 139 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((3S,3a / ?,6a / ?)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0620] 140 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((3R,3aS,6aS)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0621] 141 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((3R,3aS,6aS)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0622] 142 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((3S,3a / ?,6a / ?)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0623]

[0624] 770610: ICT-568PC / INCY0568-WO1

[0625] Entry Compound Name

[0626] 143 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((3S,3aS,6aS)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0627] 144 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((3R,3a / ?,6a / ?)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0628] 145 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((3R,3a / ?,6aS)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0629] 146 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((3S,3aS,6a / ?)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0630] 147 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((3S,3a / ?,6aS)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0631] 148 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((3R,3aS,6a / ?)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0632] 149 2-amino-4-( / ?a)-(7-chloro-9-fluoro-2-methyl-4-((3R,3a / ?,6aS)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0633] 150 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((3S,3aS,6a / ?)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0634] 151 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((3S,3a / ?,6aS)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0635] 152 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((3R,3aS,6a / ?)-1-methyl-2- oxooctahydrocyclopenta[b]pyrrol-3-yl)-5,6-dihydro-4H-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0636] 153 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-(2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0637]

[0638] 770610: ICT-568PC / INCY0568-WO1

[0639] Entry Compound Name

[0640] 154 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-(2-methyl-3-oxo-2- azabicyclo[3.1,0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0641] 155 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((1S,4 / ?,5R)-2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0642] 156 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((1R,4S,5S)-2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0643] 157 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((1 / ?,4R,5S)-2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0644] 158 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((1S,4S,5R)-2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0645] 159 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((1S,4S,5 / ?)-2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0646] 160 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((1R,4R,5S)-2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0647] 161 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((1 / ?,4S,5S)-2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0648] 162 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((1S,4R,5R)-2-methyl-3-oxo-2- azabicyclo[3.1.0]hexan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1, 6]naphthyridi n-8-y l)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0649] 163 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-(2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0650] 164 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-(2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0651]

[0652] 770610: ICT-568PC / INCY0568-WO1

[0653] Entry Compound Name

[0654] 165 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((1S,4R,5R)-2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0655] 166 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((1R,4S,5S)-2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0656] 167 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((1R,4R,5S)-2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0657] 168 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((1S,4R,5R)-2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0658] 169 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((1S,4S,5R)-2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0659] 170 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((1R,4R,5S)-2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0660] 171 2-amino-4-(Ra)-(7-chloro-9-fluoro-2-methyl-4-((1R,4S,5S)-2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0661] 172 2-amino-4-(Sa)-(7-chloro-9-fluoro-2-methyl-4-((1S,4S,5S)-2-methyl-3-oxo-2- azabicyclo[3.2.0]heptan-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0662] 173 2-amino-4-(Ra)-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((R)- 1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0663] 174 2-amino-4-(Sa)-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)- 7-fluorobenzo[b]thiophene-3-carbonitrile

[0664] 175 2-amino-4-(Ra)-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)- 7-fluorobenzo[b]thiophene-3-carbonitrile

[0665]

[0666] 770610: ICT-568PC / INCY0568-WO1

[0667] Entry Compound Name

[0668] 176 2-amino-4-(Sa)-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((R)- 1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0669] 177 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-4-((R)-1-(2-aminopyridin-3- yl)ethyl)-7-chloro-9-fluoro-N-methyl-5,6-dihydro-4H-(Ra)- benzo[de][1,6]naphthyridine-2-carboxamide

[0670] 178 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-4-((S)-1-(2-aminopyridin-3- yl)ethyl)-7-chloro-9-fluoro-N-methyl-5,6-dihydro-4H-(Sa)- benzo[de][1,6]naphthyridine-2-carboxamide

[0671] 179 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-4-((S)-1-(2-aminopyridin-3- yl)ethyl)-7-chloro-9-fluoro-N-methyl-5,6-dihydro-4H-(Ra)- benzo[de][1,6]naphthyridine-2-carboxamide

[0672] 180 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-4-((R)-1-(2-aminopyridin-3- yl)ethyl)-7-chloro-9-fluoro-N-methyl-5,6-dihydro-4H-(Sa)- benzo[de][1,6]naphthyridine-2-carboxamide

[0673] 181 2-amino-4-(Ra)-(4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-6,6,9-trifluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0674] 182 2-amino-4-(Sa)-(4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-6,6,9-trifluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0675] 183 2-amino-4-(Ra)-(4-((S)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-6,6,9-trifluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0676] 184 2-amino-4-(Sa)-(4-((R)-1-(2-aminopyridin-3-yl)ethyl)-7-chloro-6,6,9-trifluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[0677] 185 (3R)-3-(8-(2-amino-7-fluorobenzo[d]thiazol-4-yl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)-1-methylpyrrolidin-2-one

[0678] 186 (3S)-3-(8-(2-amino-7-fluorobenzo[c(]thiazol-4-yl)-7-chloro-9-fluoro-2-methyl-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)-1-methylpyrrolidin-2-one

[0679] 187 (3R)-3-(8-(Ra)-(2-amino-7-fluorobenzo[c(]thiazol-4-yl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)-1-methylpyrrolidin-2-one

[0680] 188 (3S)-3-(8-(Ra)-(2-amino-7-fluorobenzo[c(]thiazol-4-yl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)-1-methylpyrrolidin-2-one

[0681]

[0682] 770610: ICT-568PC / INCY0568-WO1

[0683] Entry Compound Name

[0684] 189 (3R)-3-(8-(Sa)-(2-amino-7-fluorobenzo[c(]thiazol-4-yl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)-1-methylpyrrolidin-2-one

[0685] 190 (3S)-3-(8-(Sa)-(2-amino-7-fluorobenzo[c(]thiazol-4-yl)-7-chloro-9-fluoro-2-methyl- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)-1-methylpyrrolidin-2-one

[0686] 191 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -methyl-4- ((R)- 1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2- carboxamide

[0687] 192 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -methyl-4- ((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2- carboxamide

[0688] 193 8-(Ra)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / - methyl-4-((R)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0689] 194 8-(Ra)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / - methyl-4-((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0690] 195 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / - methyl-4-((R)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0691] 196 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / - methyl-4-((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0692] 197 2-amino-4-(7-chloro-9-fluoro-2-(1-hydroxyethyl)-4-((R)-1-methyl-2-oxopyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0693] 198 2-amino-4-(7-chloro-9-fluoro-2-(1-hydroxyethyl)-4-((S)-1-methyl-2-oxopyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0694] 199 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-((R)-1-hydroxyethyl)-4-((R)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0695] 200 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-((R)-1-hydroxyethyl)-4-((R)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0696]

[0697] 770610: ICT-568PC / INCY0568-WO1

[0698] Entry Compound Name

[0699] 201 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-((S)-1-hydroxyethyl)-4-((R)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0700] 202 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-((S)-1-hydroxyethyl)-4-((R)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0701] 203 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-((S)-1-hydroxyethyl)-4-((S)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0702] 204 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-((S)-1-hydroxyethyl)-4-((S)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0703] 205 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-((R)-1-hydroxyethyl)-4-((S)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0704] 206 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-((R)-1-hydroxyethyl)-4-((S)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0705] 207 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((R)-1- methyl-2-oxopyrrolidin-3-yl)- / V-(1-methylazetidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0706] 208 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((S)-1- methyl-2-oxopyrrolidin-3-yl)- / V-(1-methylazetidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0707] 209 8-(Ra)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((R)-1- methyl-2-oxopyrrolidin-3-yl)- / V-(1-methylazetidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0708] 210 8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((S)-1- methyl-2-oxopyrrolidin-3-yl)- / V-(1-methylazetidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0709] 211 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((R)-1- methyl-2-oxopyrrolidin-3-yl)- / V-(1-methylazetidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0710]

[0711] 770610: ICT-568PC / INCY0568-WO1

[0712] Entry Compound Name

[0713] 212 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[£>]thiophen-4-yl)-7-chloro-9-fluoro-4-((S)-1- methyl-2-oxopyrrolidin-3-yl)- / V-(1-methylazetidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0714] 213 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -(2-hydroxy- 2-methylpropyl)-4-((R)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0715] 214 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -(2-hydroxy- 2-methylpropyl)-4-((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0716] 215 8-(Ra)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -(2- hydroxy-2-methylpropyl)-4-((R)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0717] 216 8-(Ra)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -(2- hydroxy-2-methylpropyl)-4-((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0718] 217 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -(2- hydroxy-2-methylpropyl)-4-((R)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0719] 218 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro- / \ / -(2- hydroxy-2-methylpropyl)-4-((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carboxamide

[0720] 219 / V-(8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((R)-1- methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-2- yl)acetamide

[0721] 220 / V-(8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((S)-1- methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-2- yl)acetamide

[0722] 221 / V-(8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((R)- 1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-2- yl)acetamide

[0723] 222 / V-(8-(Ra)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-2- yl)acetamide

[0724]

[0725] 770610: ICT-568PC / INCY0568-WO1

[0726] Entry Compound Name

[0727] 223 / V-(8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[£>]thiophen-4-yl)-7-chloro-9-fluoro-4- ((R)- 1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-2- yl)acetamide

[0728] 224 / V-(8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((S)-1-methyl-2-oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-2- yl)acetamide

[0729] 225 2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((R)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0730] 226 2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((S)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0731] 227 (Ra)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((R)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0732] 228 (Ra)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((S)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0733] 229 (Sa)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((R)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0734] 230 (Sa)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((S)-1-methyl-2- oxopyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0735] 231 2-amino-4-(7-chloro-9-fluoro-4-((3R,4S)-4-hydroxy-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0736] 232 2-amino-4-(7-chloro-9-fluoro-4-((3S,4R)-4-hydroxy-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0737] 233 2-amino-4-(7-chloro-9-fluoro-4-((3R,4R)-4-hydroxy-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0738]

[0739] 770610: ICT-568PC / INCY0568-WO1

[0740] Entry Compound Name

[0741] 234 2-amino-4-(7-chloro-9-fluoro-4-((3S,4S)-4-hydroxy-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0742] 235 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3R,4S)-4-hydroxy-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0743] 236 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,4R)-4-hydroxy-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0744] 237 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3R,4R)-4-hydroxy-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0745] 238 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,4S)-4-hydroxy-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0746] 239 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,4S)-4-hydroxy-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0747] 240 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,4R)-4-hydroxy-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0748] 241 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,4R)-4-hydroxy-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0749] 242 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,4S)-4-hydroxy-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0750] 243 2-amino-4-(7-chloro-4-((3R,4S)-4-(difluoromethoxy)-1-(methyl-d3)-2-oxopyrrolidin- 3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0751] 244 2-amino-4-(7-chloro-4-((3S,4R)-4-(difluoromethoxy)-1-(methyl-d3)-2-oxopyrrolidin- 3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0752]

[0753] 770610: ICT-568PC / INCY0568-WO1

[0754] Entry Compound Name

[0755] 245 2-amino-4-(7-chloro-4-((3R,4 / ?)-4-(difluoromethoxy)-1-(methyl-d3)-2-oxopyrrolidin- 3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0756] 246 2-amino-4-(7-chloro-4-((3S,4S)-4-(difluoromethoxy)-1-(methyl-d3)-2-oxopyrrolidin- 3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0757] 247 (Ra)-2-amino-4-(7-chloro-4-((3R,4S)-4-(difluoromethoxy)-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0758] 248 (Ra)-2-amino-4-(7-chloro-4-((3S,4R)-4-(difluoromethoxy)-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0759] 249 (Ra)-2-amino-4-(7-chloro-4-((3R,4R)-4-(difluoromethoxy)-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0760] 250 (Ra)-2-amino-4-(7-chloro-4-((3S,4S)-4-(difluoromethoxy)-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0761] 251 (Sa)-2-amino-4-(7-chloro-4-((3R,4S)-4-(difluoromethoxy)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0762] 252 (Sa)-2-amino-4-(7-chloro-4-((3S,4R)-4-(difluoromethoxy)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0763] 253 (Sa)-2-amino-4-(7-chloro-4-((3R,4R)-4-(difluoromethoxy)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0764] 254 (Sa)-2-amino-4-(7-chloro-4-((3S,4S)-4-(difluoromethoxy)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0765] 255 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0766]

[0767] 770610: ICT-568PC / INCY0568-WO1

[0768] Entry Compound Name

[0769] 256 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0770] 257 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0771] 258 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0772] 259 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0773] 260 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0774] 261 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0775] 262 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0776] 263 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0777] 264 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0778] 265 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0779] 266 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0780]

[0781] 770610: ICT-568PC / INCY0568-WO1

[0782] Entry Compound Name

[0783] 267 2-amino-4-(7-chloro-4-((3R,5S)-5-(difluoromethyl)-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0784] 268 2-amino-4-(7-chloro-4-((3S,5R)-5-(difluoromethyl)-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0785] 269 2-amino-4-(7-chloro-4-((3R,5R)-5-(difluoromethyl)-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0786] 270 2-amino-4-(7-chloro-4-((3S,5S)-5-(difluoromethyl)-1-(methyl-d3)-2-oxopyrrolidin-3- yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0787] 271 (Ra)-2-amino-4-(7-chloro-4-((3R,5S)-5-(difluoromethyl)-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0788] 272 (Ra)-2-amino-4-(7-chloro-4-((3S,5R)-5-(difluoromethyl)-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0789] 273 (Ra)-2-amino-4-(7-chloro-4-((3R,5R)-5-(difluoromethyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0790] 274 (Ra)-2-amino-4-(7-chloro-4-((3S,5S)-5-(difluoromethyl)-1-(methyl-cf3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0791] 275 (Sa)-2-amino-4-(7-chloro-4-((3R,5S)-5-(difluoromethyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0792] 276 (Sa)-2-amino-4-(7-chloro-4-((3S,5R)-5-(difluoromethyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0793] 277 (Sa)-2-amino-4-(7-chloro-4-((3R,5R)-5-(difluoromethyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0794]

[0795] 770610: ICT-568PC / INCY0568-WO1

[0796] Entry Compound Name

[0797] 278 (Sa)-2-amino-4-(7-chloro-4-((3S,5S)-5-(difluoromethyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-9-fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0798] 279 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((R)-4-(methyl-d3)-5-oxo-4- azaspiro[2.4]heptan-6-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0799] 280 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((S)-4-(methyl-d3)-5-oxo-4- azaspiro[2.4]heptan-6-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0800] 281 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(( / ?)-4-(methyl-d3)-5-oxo-4- azaspiro[2.4]heptan-6-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0801] 282 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((S)-4-(methyl-cf3)-5-oxo-4- azaspiro[2.4]heptan-6-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0802] 283 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((R)-4-(methyl-d3)-5-oxo-4- azaspiro[2.4]heptan-6-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0803] 284 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((S)-4-(methyl-d3)-5-oxo-4- azaspiro[2.4]heptan-6-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0804] 285 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-5-((methoxy-d3)methyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0805] 286 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-5-((methoxy-d3)methyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0806] 287 2-amino-4-(7-chloro-9-fluoro-4-((3R,5R)-5-((methoxy-d3)methyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0807] 288 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-5-((methoxy-d3)methyl)-1-(methyl-d3)-2- oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0808]

[0809] 770610: ICT-568PC / INCY0568-WO1

[0810] Entry Compound Name

[0811] 289 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-5-((methoxy-d3)methyl)-1-(methyl-cf3)- 2-oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0812] 290 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-5-((methoxy-d3)methyl)-1-(methyl-cf3)- 2-oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0813] 291 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5R)-5-((methoxy-d3)methyl)-1-(methyl-cf3)- 2-oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0814] 292 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-5-((methoxy-d3)methyl)-1-(methyl-cf3)- 2-oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0815] 293 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-5-((methoxy-d3)methyl)-1-(methyl-d3)- 2-oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0816] 294 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-5-((methoxy-d3)methyl)-1-(methyl-d3)- 2-oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0817] 295 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5R)-5-((methoxy-d3)methyl)-1-(methyl-d3)- 2-oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0818] 296 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-5-((methoxy-d3)methyl)-1-(methyl-d3)- 2-oxopyrrolidin-3-yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0819] 297 (2S,4R)-4-(8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1-(methyl- d3)-5-oxopyrrolidine-2-carboxamide

[0820] 298 (2R,4S)-4-(8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1-(methyl- d3)-5-oxopyrrolidine-2-carboxamide

[0821] 299 (2R,4R)-4-(8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1-(methyl- d3)-5-oxopyrrolidine-2-carboxamide

[0822]

[0823] 770610: ICT-568PC / INCY0568-WO1

[0824] Entry Compound Name

[0825] 300 (2S,4S)-4-(8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1-(methyl- d3)-5-oxopyrrolidine-2-carboxamide

[0826] 301 (2S,4R)-4-(8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1- (methyl-d3)-5-oxopyrrolidine-2-carboxamide

[0827] 302 (2R,4S)-4-(8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1- (methyl-d3)-5-oxopyrrolidine-2-carboxamide

[0828] 303 (2R,4R)-4-(8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1- (methyl-d3)-5-oxopyrrolidine-2-carboxamide

[0829] 304 (2S,4S)-4-(8-(Ra)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1- (methyl-d3)-5-oxopyrrolidine-2-carboxamide

[0830] 305 (2S,4R)-4-(8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1- (methyl-d3)-5-oxopyrrolidine-2-carboxamide

[0831] 306 (2R,4S)-4-(8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1- (methyl-d3)-5-oxopyrrolidine-2-carboxamide

[0832] 307 (2R,4R)-4-(8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1- (methyl-d3)-5-oxopyrrolidine-2-carboxamide

[0833] 308 (2S,4S)-4-(8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9- fluoro-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-4-yl)- / \ / , / \ / -dimethyl-1- (methyl-d3)-5-oxopyrrolidine-2-carboxamide

[0834] 309 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((R)-2-methyl-3-oxoisoxazolidin-4-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0835] 310 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((S)-2-methyl-3-oxoisoxazolidin-4-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0836]

[0837] 770610: ICT-568PC / INCY0568-WO1

[0838] Entry Compound Name

[0839] 311 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-(( / ?)-2-methyl-3-oxoisoxazolidin-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0840] 312 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((S)-2-methyl-3-oxoisoxazolidin-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0841] 313 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((R)-2-methyl-3-oxoisoxazolidin-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0842] 314 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((S)-2-methyl-3-oxoisoxazolidin-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0843] 315 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0844] 316 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0845] 317 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0846] 318 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0847] 319 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0848] 320 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0849] 321 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0850]

[0851] 770610: ICT-568PC / INCY0568-WO1

[0852] Entry Compound Name

[0853] 322 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0854] 323 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0855] 324 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0856] 325 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0857] 326 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0858] 327 2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 328 2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 329 2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 330 2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 331 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3 / ?,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 332 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3S,5 / ?)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0859]

[0860] 770610: ICT-568PC / INCY0568-WO1

[0861] Entry Compound Name

[0862] 333 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3R,5 / ?)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 334 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 335 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 336 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 337 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 338 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 339 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 340 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 341 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 342 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 343 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0863]

[0864] 770610: ICT-568PC / INCY0568-WO1

[0865] Entry Compound Name

[0866] 344 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 345 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 346 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 347 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 348 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 349 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 350 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 351 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0867] 352 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0868] 353 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0869] 354 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6-

[0870]

[0871] 770610: ICT-568PC / INCY0568-WO1

[0872] Entry Compound Name

[0873] dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0874] 355 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0875] 356 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0876] 357 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl)azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0877] 358 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl)azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0878] 359 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0879] 360 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0880] 361 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0881] 362 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(3-(S-methylsulfonimidoyl) azetidin-1-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0882]

[0883] 770610: ICT-568PC / INCY0568-WO1

[0884] Entry Compound Name

[0885] 363 2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 364 2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 365 2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 366 2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 367 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 368 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 369 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 370 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 371 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 372 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 373 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[0886]

[0887] 770610: ICT-568PC / INCY0568-WO1

[0888] Entry Compound Name

[0889] 374 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(3-methyl-3-(pyrrolidin-1-yl)azetidin-1-yl)-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 375 2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0890] 376 2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0891] 377 2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0892] 378 2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0893] 379 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0894] 380 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0895] 381 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0896] 382 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0897]

[0898] 770610: ICT-568PC / INCY0568-WO1

[0899] Entry Compound Name

[0900] 383 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0901] 384 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0902] 385 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0903] 386 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0904] 387 f / ?a)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,7a / ?)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0905] 388 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,7a / ?)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0906] 389 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,7a / ?)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0907] 390 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,7a / ?)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0908] 391 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,7a / ?)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-

[0909]

[0910] 770610: ICT-568PC / INCY0568-WO1

[0911] Entry Compound Name

[0912] yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0913] 392 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,7a / ?)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0914] 393 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,7a / ?)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0915] 394 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,7a / ?)-2-fluorotetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0916] 395 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0917] 396 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0918] 397 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0919] 398 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0920] 399 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0921]

[0922] 770610: ICT-568PC / INCY0568-WO1

[0923] Entry Compound Name

[0924] 400 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0925] 401 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0926] 402 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0927] 403 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0928] 404 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0929] 405 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0930] 406 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0931] 407 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((R)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0932] 408 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((R)-1-methylpyrrolidin-2-yl)ethoxy)-5,6-

[0933]

[0934] 770610: ICT-568PC / INCY0568-WO1

[0935] Entry Compound Name

[0936] dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0937] 409 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((R)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0938] 410 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((R)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0939] 411 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((R)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0940] 412 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((R)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0941] 413 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((R)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0942] 414 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((R)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0943] 415 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0944] 416 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0945]

[0946] 770610: ICT-568PC / INCY0568-WO1

[0947] Entry Compound Name

[0948] 417 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0949] 418 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0950] 419 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0951] 420 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0952] 421 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((S)-1-((S)-1-methylpyrrolidin-2-yl)ethoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0953] 422 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)- 1 -(( / ?)- 1-methylpyrrolidin-2-yl)ethoxy)-5, 6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0954] 423 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)- 1 -(( / ?)- 1-methylpyrrolidin-2-yl)ethoxy)-5, 6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0955] 424 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)- 1 -(( / ?)- 1-methylpyrrolidin-2-yl)ethoxy)-5, 6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0956] 425 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)-1 -(( / ?)- 1-methylpyrrolidin-2-yl)ethoxy)-5, 6-

[0957]

[0958] 770610: ICT-568PC / INCY0568-WO1

[0959] Entry Compound Name

[0960] dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0961] 426 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)- 1 -(( / ?)- 1-methylpyrrolidin-2-yl)ethoxy)-5, 6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0962] 427 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)- 1 -(( / ?)- 1-methylpyrrolidin-2-yl)ethoxy)-5, 6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0963] 428 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)- 1 -(( / ?)- 1-methylpyrrolidin-2-yl)ethoxy)-5, 6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0964] 429 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((R)- 1 -(( / ?)- 1-methylpyrrolidin-2-yl)ethoxy)-5, 6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0965] 430 2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0966] 431 2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0967] 432 2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-9-fluoro-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0968] 433 2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin-7a(5 / 7)- yl)methoxy)-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0969]

[0970] 770610: ICT-568PC / INCY0568-WO1

[0971] Entry Compound Name

[0972] 434 (Ra)-2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0973] 435 (Ra)-2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0974] 436 (Ra)-2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0975] 437 (Ra)-2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0976] 438 (Ra)-2-amino-4-(7-chloro-2-(((R)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0977] 439 (Sa)-2-amino-4-(7-chloro-2-(((R)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0978] 440 (Ra)-2-amino-4-(7-chloro-2-(((R)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0979] 441 (Sa)-2-amino-4-(7-chloro-2-(((R)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0980] 442 (Ra)-2-amino-4-(7-chloro-2-(((R)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-

[0981]

[0982] 770610: ICT-568PC / INCY0568-WO1

[0983] Entry Compound Name

[0984] (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0985] 443 (Sa)-2-amino-4-(7-chloro-2-(((R)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0986] 444 (Ra)-2-amino-4-(7-chloro-2-(((R)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0987] 445 (Sa)-2-amino-4-(7-chloro-2-(((R)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0988] 446 (Sa)-2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)- 4057-fluorobenzo[b]thiophene-3-carbonitrile

[0989] 447 (Sa)-2amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0990] 448 (Sa)-2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0991] 449 (Sa)-2-amino-4-(7-chloro-2-(((S)-2-(difluoromethylene)tetrahydro-1 / 7-pyrrolizin- 7a(5 / - / )-yl)methoxy)-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[0992] 450 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0993]

[0994] 770610: ICT-568PC / INCY0568-WO1

[0995] Entry Compound Name

[0996] 451 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0997] 452 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0998] 453 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[0999] 454 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1000] 455 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1001] 4564 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1002] 457 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1003] 458 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1004] 459 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6-

[1005]

[1006] 770610: ICT-568PC / INCY0568-WO1

[1007] Entry Compound Name

[1008] dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1009] 460 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1010] 461 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1011] 462 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((R)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1012] 463 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((R)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1013] 464 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((R)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1014] 465 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((R)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1015] 466 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((R)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1016] 467 Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((R)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1017]

[1018] 770610: ICT-568PC / INCY0568-WO1

[1019] Entry Compound Name

[1020] 468 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((R)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1021] 469 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(((R)-1-methylpyrrolidin-2-yl)methoxy)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1022] 470 2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2-yl)methoxy)- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1023] 471 2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2-yl)methoxy)- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1024] 472 2-amino-4-(7-chloro-9-fluoro-2-(((2R,4R)-4-fluoro-1-methylpyrrolidin-2-yl)methoxy)- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1025] 473 2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2-yl)methoxy)- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1026] 474 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1027] 475 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1028] 476 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4 / ?)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1029] 477 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-

[1030]

[1031] 770610: ICT-568PC / INCY0568-WO1

[1032] Entry Compound Name

[1033] dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1034] 478 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1035] 479 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1036] 480 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1037] 481 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1038] 482 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1039] 483 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1040] 484 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1041] 485 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4 / ?)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1042]

[1043] 770610: ICT-568PC / INCY0568-WO1

[1044] Entry Compound Name

[1045] 486 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1046] 487 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4 / ?)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1047] 488 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1048] 489 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4 / ?)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1049] 490 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1050] 491 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1051] 492 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1052] 493 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1053] 494 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-

[1054]

[1055] 770610: ICT-568PC / INCY0568-WO1

[1056] Entry Compound Name

[1057] dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1058] 495 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1059] 496 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1060] 497 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1061] 498 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1062] 499 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1063] 500 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1064] 501 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1065] 502 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1066]

[1067] 770610: ICT-568PC / INCY0568-WO1

[1068] Entry Compound Name

[1069] 503 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1070] 504 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2R,4R)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1071] 505 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(((2S,4S)-4-fluoro-1-methylpyrrolidin-2- yl)methoxy)-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1072] 506 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 507 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 508 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 509 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 510 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 511 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 512 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1073]

[1074] 770610: ICT-568PC / INCY0568-WO1

[1075] Entry Compound Name

[1076] 513 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1077] 514 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1078] 515 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1079] 516 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1080] 517 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1 / 7-1,2,4-triazol-1-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1081] 518 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7-pyran-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1082] 519 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7-pyran-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1083] 520 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7-pyran-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1084] 521 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7-pyran-4-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1085] 522 8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7- pyran-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1086] 523 8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7- pyran-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1087]

[1088] 770610: ICT-568PC / INCY0568-WO1

[1089] Entry Compound Name

[1090] 524 8-(Ka)-(2-amino-3-cyano-7-fluorobenzo[£>]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7- pyran-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1091] 525 8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7- pyran-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1092] 526 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7- pyran-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1093] 527 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7- pyran-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1094] 528 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7- pyran-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1095] 529 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)- / \ / -(tetrahydro-2 / 7- pyran-4-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridine-2-carboxamide

[1096] 530 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1097] 531 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1098] 532 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1099] 533 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1100] 534 8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1101]

[1102] 770610: ICT-568PC / INCY0568-WO1

[1103] Entry Compound Name

[1104] 535 8-(Ka)-(2-amino-3-cyano-7-fluorobenzo[£>]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-2-carbonitrile

[1105] 536 8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1106] 537 8-( / ?a)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1107] 538 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1108] 539 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1109] 540 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1110] 541 8-(Sa)-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-2-carbonitrile

[1111] 542 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1112] 543 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1113] 544 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1114] 545 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1115]

[1116] 770610: ICT-568PC / INCY0568-WO1

[1117] Entry Compound Name

[1118] 546 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1119] 547 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1120] 548 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1121] 549 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1122] 550 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1123] 551 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1124] 552 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1125] 553 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1126] 554 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1127] 555 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1128] 556 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1129]

[1130] 770610: ICT-568PC / INCY0568-WO1

[1131] Entry Compound Name

[1132] 557 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1133] 558 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1134] 559 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1135] 560 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1136] 561 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1137] 562 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1138] 563 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1139] 564 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1140] 565 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5- fluorobenzo[b]thiophene-3-carbonitrile

[1141] 566 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1142] 567 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1143]

[1144] 770610: ICT-568PC / INCY0568-WO1

[1145] Entry Compound Name

[1146] 568 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1147] 569 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1148] 570 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1149] 571 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1150] 572 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1151] 573 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1152] 574 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1153] 575 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1154] 576 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1155] 577 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-6,7- difluorobenzo[b]thiophene-3-carbonitrile

[1156] 578 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1157]

[1158] 770610: ICT-568PC / INCY0568-WO1

[1159] Entry Compound Name

[1160] 579 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1161] 580 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1162] 581 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1163] 582 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1164] 583 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1165] 584 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1166] 585 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1167] 586 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1168] 587 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1169] 588 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1170] 589 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-5,7- difluorobenzo[b]thiophene-3-carbonitrile

[1171]

[1172] 770610: ICT-568PC / INCY0568-WO1

[1173] Entry Compound Name

[1174] 590 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1175] 591 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1176] 592 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1177] 593 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1178] 594 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1179] 595 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1180] 596 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1181] 597 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1182] 598 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1183] 599 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1184] 600 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1185]

[1186] 770610: ICT-568PC / INCY0568-WO1

[1187] Entry Compound Name

[1188] 601 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorothieno[3,2-c]pyridine-3-carbonitrile

[1189] 602 2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1190] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1191] 603 2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1192] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1193] 604 2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1194] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1195] 605 2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1196] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1197] 606 (Ra)-2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1198] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1199] 607 (Ra)-2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1200] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1201] 608 (Ra)-2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1202] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1203] 609 (Ra)-2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1204] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1205] 610 (Sa)-2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1206] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1207] 611 (Sa)-2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1208] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1209]

[1210] 770610: ICT-568PC / INCY0568-WO1

[1211] Entry Compound Name

[1212] 612 (Sa)-2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1213] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1214] 613 (Sa)-2-amino-7-fluoro-4-(9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-7-(trifluoromethyl)-5,6-dihydro-4 / 7-benzo[de]

[1215] [1,6]naphthyridin-8-yl)benzo[b]thiophene-3-carbonitrile

[1216] 614 2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1217] 615 2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1218] 616 2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1219] 617 2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1220] 618 (Ra)-2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1221] 619 (Ra)-2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-cf3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1222] 620 (Ra)-2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3R,5R)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1223] 621 (Ra)-2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1224] 622 (Sa)-2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1225]

[1226] 770610: ICT-568PC / INCY0568-WO1

[1227] Entry Compound Name

[1228] 623 (Sa)-2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1229] 624 (Sa)-2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3R,5R)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1230] 625 (Sa)-2-amino-4-(7-(difluoromethyl)-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1231] 626 2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1232] 627 2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1233] 628 2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1234] 629 2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1235] 630 (Ra)-2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1236] 631 (Ra)-2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1237] 632 (Ra)-2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1238] 633 (Ra)-2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1239]

[1240] 770610: ICT-568PC / INCY0568-WO1

[1241] Entry Compound Name

[1242] 634 (Sa)-2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1243] 635 (Sa)-2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1244] 636 (Sa)-2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1245] 637 (Sa)-2-amino-4-(7-chloro-3,9-difluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1246] 638 2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1247] 639 2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1248] 640 2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1249] 641 2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1250] 642 (Ra)-2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1251] 643 (Ra)-2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1252] 644 (Ra)-2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1253]

[1254] 770610: ICT-568PC / INCY0568-WO1

[1255] Entry Compound Name

[1256] 645 (Ra)-2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1257] 646 (Sa)-2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1258] 647 (Sa)-2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1259] 648 (Sa)-2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1260] 649 (Sa)-2-amino-7-fluoro-4-(9-fluoro-2,7-dimethyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)benzo[b]thiophene-3-carbonitrile

[1261] 650 2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1262] 651 2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1263] 652 2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1264] 653 2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1265] 654 (Ra)-2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1266] 655 (Ra)-2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3S,5R)-1-(methyl-cf3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1267]

[1268] 770610: ICT-568PC / INCY0568-WO1

[1269] Entry Compound Name

[1270] 656 (Ra)-2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3R,5R)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1271] 657 (Ra)-2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3S,5S)-1-(methyl-cf3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1272] 658 (Sa)-2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3R,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1273] 659 (Sa)-2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3S,5R)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1274] 660 (Sa)-2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3R,5R)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1275] 661 (Sa)-2-amino-4-(2-(difluoromethyl)-9-fluoro-7-methyl-4-((3S,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1276] 662 2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1277] 663 2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1278] 664 2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1279] 665 2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1280] 666 (Ra)-2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1281]

[1282] 770610: ICT-568PC / INCY0568-WO1

[1283] Entry Compound Name

[1284] 667 (Ra)-2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 668 (Ra)-2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 669 (Ra)-2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 670 (Sa)-2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 671 (Sa)-2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 672 (Sa)-2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 673 (Sa)-2-amino-4-(2-(3-(dimethylamino)-3-methylazetidin-1-yl)-9-fluoro-7-methyl-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 674 2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1285] 675 2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1286] 676 2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1287] 677 2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1288]

[1289] 770610: ICT-568PC / INCY0568-WO1

[1290] Entry Compound Name

[1291] 678 (Ra)-2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3 / ?,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de]

[1292] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1293] 679 (Ra)-2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3S,5 / ?)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de]

[1294] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1295] 680 (Ra)-2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3R,5 / ?)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de]

[1296] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1297] 681 (Ra)-2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de]

[1298] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1299] 682 (Sa)-2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de]

[1300] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1301] 683 (Sa)-2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de]

[1302] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1303] 684 (Sa)-2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de]

[1304] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1305] 685 (Sa)-2-amino-4-(2-(3-(dimethylamino)azetidin-1-yl)-9-fluoro-7-methyl-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de]

[1306] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1307] 686 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-5-fluoro-1-methyl-2-oxopiperidin-3-yl)-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[1308] 687 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-5-fluoro-1-methyl-2-oxopiperidin-3-yl)-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[1309] 688 2-amino-4-(7-chloro-9-fluoro-4-((3R,5R)-5-fluoro-1-methyl-2-oxopiperidin-3-yl)-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[1310]

[1311] 770610: ICT-568PC / INCY0568-WO1

[1312] Entry Compound Name

[1313] 689 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-5-fluoro-1-methyl-2-oxopiperidin-3-yl)-2- methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene- 3-carbonitrile

[1314] 690 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-5-fluoro-1-methyl-2-oxopiperidin-3- yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1315] 691 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-5-fluoro-1-methyl-2-oxopiperidin-3- yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1316] 692 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-5-fluoro-1-methyl-2-oxopiperidin-3- yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1317] 693 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-5-fluoro-1-methyl-2-oxopiperidin-3-yl)- 2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1318] 694 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-5-fluoro-1-methyl-2-oxopiperidin-3-yl)- 2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1319] 695 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-5-fluoro-1-methyl-2-oxopiperidin-3-yl)- 2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1320] 696 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5R)-5-fluoro-1-methyl-2-oxopiperidin-3- yl)-2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1321] 697 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-5-fluoro-1-methyl-2-oxopiperidin-3-yl)- 2-methyl-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1322] 698 2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1323] 699 2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1324]

[1325] 770610: ICT-568PC / INCY0568-WO1

[1326] Entry Compound Name

[1327] 700 2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 701 2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 702 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3R,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 703 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3S,5R)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 704 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3R,5 / ?)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 705 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3S,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 706 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3R,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 707 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3S,5R)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 708 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3R,5R)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 709 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-(3-hydroxy-3-methylbut-1-yn-1-yl)-4-((3S,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 710 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1328]

[1329] 770610: ICT-568PC / INCY0568-WO1

[1330] Entry Compound Name

[1331] 711 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1332] 712 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1333] 713 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1334] 714 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3 / ?,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1335] 715 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5 / ?)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1336] 716 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3R,5 / ?)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1337] 717 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1338] 718 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3R,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1339] 719 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5R)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1340] 720 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3R,5R)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1341] 721 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1342]

[1343] 770610: ICT-568PC / INCY0568-WO1

[1344] Entry Compound Name

[1345] 722 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1346] 723 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1347] 724 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1348] 725 2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1349] 726 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3 / ?,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1350] 727 (Ra)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5 / ?)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1351] 728 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3R,5S)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1352] 729 (Sa)-2-amino-4-(7-chloro-2-(3-(dimethylamino)prop-1-yn-1-yl)-9-fluoro-4-((3S,5R)- 1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de] [1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1353] 730 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6S,8a / ?)-5-oxooctahydroindolizin-6-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1354] 731 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6S,8aS)-5-oxooctahydroindolizin-6-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1355] 732 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6R,8a / ?)-5-oxooctahydroindolizin-6-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1356]

[1357] 770610: ICT-568PC / INCY0568-WO1

[1358] Entry Compound Name

[1359] 733 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6R,8aS)-5-oxooctahydroindolizin-6-yl)- 5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1360] 734 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6S,8a / ?)-5-oxooctahydroindolizin-6- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1361] 735 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6S,8a / ?)-5-oxooctahydroindolizin-6- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1362] 736 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6S,8aS)-5-oxooctahydroindolizin-6- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1363] 737 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6S,8aS)-5-oxooctahydroindolizin-6- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1364] 738 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6R,8a / ?)-5-oxooctahydroindolizin-6- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1365] 739 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6R,8a / ?)-5-oxooctahydroindolizin-6- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1366] 740 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6 / ?,8aS)-5-oxooctahydroindolizin-6- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1367] 741 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((6R,8aS)-5-oxooctahydroindolizin-6- yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1368] 742 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1369] 743 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1370]

[1371] 770610: ICT-568PC / INCY0568-WO1

[1372] Entry Compound Name

[1373] 744 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1374] 745 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1375] 746 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1376] 747 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1377] 748 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1378] 749 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1379] 750 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1380] 751 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1381] 752 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6-

[1382]

[1383] 770610: ICT-568PC / INCY0568-WO1

[1384] Entry Compound Name

[1385] dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1386] 753 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(1-methyl-1,6-diazaspiro[3.3]heptan-6-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1387] 754 2-amino-4-(7-chloro-2-(3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1388] 755 2-amino-4-(7-chloro-2-(3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1389] 756 2-amino-4-(7-chloro-2-(3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1390] 757 2-amino-4-(7-chloro-2-(3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1391] 758 (Ra)-2-amino-4-(7-chloro-2-((3 / ?,4S)-3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 759 (Sa)-2-amino-4-(7-chloro-2-((3R,4S)-3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 760 (Ra)-2-amino-4-(7-chloro-2-((3S,4 / ?)-3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 761 (Sa)-2-amino-4-(7-chloro-2-((3S,4R)-3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 762 (Ra)-2-amino-4-(7-chloro-2-((3 / ?,4S)-3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1392]

[1393] 770610: ICT-568PC / INCY0568-WO1

[1394] Entry Compound Name

[1395] 763 (Sa)-2-amino-4-(7-chloro-2-((3R,4S)-3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 764 (Ra)-2-amino-4-(7-chloro-2-((3S,4 / ?)-3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 765 (Sa)-2-amino-4-(7-chloro-2-((3S,4R)-3-(dimethylamino)-4-fluoropyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 766 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1396] 767 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1397] 768 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1398] 769 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1399] 770 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan- 2-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1400] 771 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan- 2-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1401] 772 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-

[1402]

[1403] 770610: ICT-568PC / INCY0568-WO1

[1404] Entry Compound Name

[1405] 2-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1406] 773 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan- 2-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1407] 774 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan- 2-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1408] 775 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan- 2-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1409] 776 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan- 2-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1410] 777 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]heptan- 2-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1411] 778 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1412] 779 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1413] 780 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1414] 781 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1415]

[1416] 770610: ICT-568PC / INCY0568-WO1

[1417] Entry Compound Name

[1418] 782 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1419] 783 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1420] 784 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1421] 785 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1422] 786 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1423] 787 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1424] 788 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1425] 789 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- phenylpyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1426] 790 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1427] 791 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1428] 792 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1429]

[1430] 770610: ICT-568PC / INCY0568-WO1

[1431] Entry Compound Name

[1432] 793 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1433] 794 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1434] 795 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1435] 796 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1436] 797 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1437] 798 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1438] 799 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1439] 800 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1440] 801 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-b]pyridine-3-carbonitrile

[1441] 802 2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 803 2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1442]

[1443] 770610: ICT-568PC / INCY0568-WO1

[1444] Entry Compound Name

[1445] 804 2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1446] 805 2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1447] 806 (Ra)-2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile; and 807 (Sa)-2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1448] 808 (Ra)-2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1449] 809 (Sa)-2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1450] 810 (Ra)-2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile; and 811 (Sa)-2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1451] 812 (Ra)-2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile; and 813 (Sa)-2-amino-4-(7-chloro-2-((dimethyl(oxo)-A6-sulfaneylidene)amino)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1452] 814 2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1453]

[1454] 770610: ICT-568PC / INCY0568-WO1

[1455] Entry Compound Name

[1456] 815 2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1457] 816 2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1458] 817 2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-((3R,5 / ?)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1459] 818 2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1460] 819 2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1461] 820 2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1462] 821 2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1463] 822 (Ra)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1464] 823 (Sa)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1465] 824 (Ra)-2-amino-4-(7-chloro-2-(( / ?)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1466] 825 (Sa)-2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1467]

[1468] 770610: ICT-568PC / INCY0568-WO1

[1469] Entry Compound Name

[1470] 826 (Ra)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1471] 827 (Sa)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1472] 828 (Ra)-2-amino-4-(7-chloro-2-(( / ?)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1473] 829 (Sa)-2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1474] 830 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1475] 831 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1476] 832 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1477] 833 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1478] 834 (Ra)-2-amino-4-(7-chloro-2-(( / ?)-3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 835 (Sa)-2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9- fluoro- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1479] 836 (Ra)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9- fluoro- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1480]

[1481] 770610: ICT-568PC / INCY0568-WO1

[1482] Entry Compound Name

[1483] 837 (Sa)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9-fluoro- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1484] 838 (Ra)-2-amino-4-(7-chloro-2-(( / ?)-3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 839 (Sa)-2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9- fluoro- 4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1485] 840 (Ra)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9- fluoro- 4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1486] 841 (Sa)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)-3-methylpyrrolidin-1-yl)-9-fluoro- 4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1487] 842 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3aS,6aS)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1488] 843 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3aS,6aS)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1489] 844 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3a / ?,6a / ?)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1490] 845 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3a / ?,6a / ?)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1491] 846 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3aS,6aS)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1492]

[1493] 770610: ICT-568PC / INCY0568-WO1

[1494] Entry Compound Name

[1495] 847 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3aS,6aS)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1496] 848 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3a / ?,6a / ?)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1497] 849 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3a / ?,6a / ?)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1498] 850 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3aS,6aS)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1499] 851 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3aS,6aS)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1500] 852 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3a / ?,6a / ?)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1501] 853 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((3a / ?,6a / ?)-1-methylhexahydropyrrolo[3,4- b]pyrrol-5(1 / - / )-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1502] 854 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1503] 855 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1504]

[1505] 770610: ICT-568PC / INCY0568-WO1

[1506] Entry Compound Name

[1507] 856 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1508] 857 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1509] 858 (Ra)-2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1510] 859 (Sa)-2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1511] 860 (Ra)-2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1512] 861 (Sa)-2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1513] 862 (Ra)-2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1514] 863 (Sa)-2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1515] 864 (Ra)-2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1516] 865 (Sa)-2-amino-4-(7-chloro-2-(3-cyclopropyl-3-hydroxyazetidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1517] 867 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1518]

[1519] 770610: ICT-568PC / INCY0568-WO1

[1520] Entry Compound Name

[1521] 868 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1522] 869 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1523] 870 2-amino-4-(7-chloro-2-(3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1524] 871 (Ra)-2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9- fluoro- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1525] 872 (Sa)-2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1526] 873 (Ra)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1527] 874 (Sa)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1528] 875 (Ra)-2-amino-4-(7-chloro-2-(( / ?)-3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9- fluoro- 4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1529] 876 (Sa)-2-amino-4-(7-chloro-2-((R)-3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro- 4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1530] 878 (Ra)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro- 4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1531] 879 (Sa)-2-amino-4-(7-chloro-2-((S)-3-(dimethylamino)-3-ethylpyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1532]

[1533] 770610: ICT-568PC / INCY0568-WO1

[1534] Entry Compound Name

[1535] 880 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1536] 881 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1537] 882 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1538] 883 2-amino-4-(7-chloro-2-(3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1539] 884 (Ra)-2-amino-4-(7-chloro-2-((S)-3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 885 (Sa)-2-amino-4-(7-chloro-2-((S)-3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 886 (Ra)-2-amino-4-(7-chloro-2-(( / ?)-3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 887 (Sa)-2-amino-4-(7-chloro-2-((R)-3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 888 (Ra)-2-amino-4-(7-chloro-2-((S)-3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 889 (Sa)-2-amino-4-(7-chloro-2-((S)-3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 890 (Ra)-2-amino-4-(7-chloro-2-(( / ?)-3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1540]

[1541] 770610: ICT-568PC / INCY0568-WO1

[1542] Entry Compound Name

[1543] 891 (Sa)-2-amino-4-(7-chloro-2-((R)-3-cyclopropyl-3-(dimethylamino)pyrrolidin-1-yl)-9- fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 892 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1544] 893 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1545] 894 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1546] 895 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1547] 896 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1548] 897 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1549] 898 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1550] 899 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1551] 900 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1552] 901 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1553]

[1554] 770610: ICT-568PC / INCY0568-WO1

[1555] Entry Compound Name

[1556] 902 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1557] 903 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)thieno[2,3-c]pyridine-3-carbonitrile

[1558] 904 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1559] 905 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1560] 906 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1561] 907 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1562] 908 (Ra)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1563] 909 (Sa)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1564] 910 (Ra)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1565] 911 (Sa)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1566] 912 (Ra)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1567]

[1568] 770610: ICT-568PC / INCY0568-WO1

[1569] Entry Compound Name

[1570] 913 (Sa)-8-(2-amino-3-cyano-7-fluorobenzo[£>]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-3-carbonitrile

[1571] 914 (Ra)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1572] 915 (Sa)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-7-chloro-9-fluoro-2-methyl- 4-((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1573] 916 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1574] 917 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1575] 918 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1576] 919 8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1577] 920 (Ra)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1578] 921 (Sa)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1579] 922 (Ra)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1580] 923 (Sa)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1581]

[1582] 770610: ICT-568PC / INCY0568-WO1

[1583] Entry Compound Name

[1584] 924 (Ra)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridine-3-carbonitrile

[1585] 925 (Sa)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1586] 926 (Ra)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1587] 927 (Sa)-8-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-9-fluoro-2,7-dimethyl-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridine-3-carbonitrile

[1588] 928 2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1589] 929 2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1590] 930 2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1591] 931 2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1592] 932 (Ra)-2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1593] 933 (Sa)-2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1594] 934 (Ra)-2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1595]

[1596] 770610: ICT-568PC / INCY0568-WO1

[1597] Entry Compound Name

[1598] 935 (Sa)-2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1599] 936 (Ra)-2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1600] 937 (Sa)-2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1601] 938 (Ra)-2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1602] 939 (Sa)-2-amino-4-(2-(azetidin-1-ylmethyl)-7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1603] 940 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1604] 941 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1605] 942 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1606] 943 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1607] 944 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1608] 945 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1609]

[1610] 770610: ICT-568PC / INCY0568-WO1

[1611] Entry Compound Name

[1612] 946 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 947 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 948 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 949 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 950 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 951 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-(trifluoromethyl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 952 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5R)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1613] 953 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1614] 954 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1615] 955 2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1616] 956 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5 / ?)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1617]

[1618] 770610: ICT-568PC / INCY0568-WO1

[1619] Entry Compound Name

[1620] 957 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5R)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1621] 958 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5 / ?)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1622] 959 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5R)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1623] 960 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3 / ?,5S)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1624] 961 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3R,5S)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1625] 962 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1626] 963 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-methyl-4-((3S,5S)-1-methyl-2-oxo-5- (trifluoromethyl)piperidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7- fluorobenzo[b]thiophene-3-carbonitrile

[1627] 964 2-amino-4-(7-chloro-2-((3S,4R)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 965 2-amino-4-(7-chloro-2-((3R,4R)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 966 2-amino-4-(7-chloro-2-((3S,4S)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 967 2-amino-4-(7-chloro-2-((3R,4R)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)-9- fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 968 (Ra)-2-amino-4-(7-chloro-2-((3S,4 / ?)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)- 9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-

[1628]

[1629] 770610: ICT-568PC / INCY0568-WO1

[1630] Entry Compound Name

[1631] dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1632] 969 (Sa)-2-amino-4-(7-chloro-2-((3S,4R)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)- 9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1633] 970 (Ra)-2-amino-4-(7-chloro-2-((3 / ?,4S)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)- 9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1634] 971 (Sa)-2-amino-4-(7-chloro-2-((3R,4S)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)- 9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1635] 972 (Ra)-2-amino-4-(7-chloro-2-((3S,4 / ?)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)- 9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1636] 973 (Sa)-2-amino-4-(7-chloro-2-((3S,4R)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)- 9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1637] 974 (Ra)-2-amino-4-(7-chloro-2-((3 / ?,4S)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)- 9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1638] 975 (Sa)-2-amino-4-(7-chloro-2-((3R,4S)-3-(dimethylamino)-4-methoxypyrrolidin-1-yl)- 9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6- dihydro-4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3- carbonitrile

[1639] 976 2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1640]

[1641] 770610: ICT-568PC / INCY0568-WO1

[1642] Entry Compound Name

[1643] 977 2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1644] 978 2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1645] 979 2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1646] 980 (Ra)-2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1647] 981 (Sa)-2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4- ((3R,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1648] 982 (Ra)-2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1649] 983 (Sa)-2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4- ((3S,5R)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1650] 984 (Ra)-2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1651] 985 (Sa)-2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4- ((3R,5 / ?)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1652] 986 (Ra)-2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1653] 987 (Sa)-2-amino-4-(7-chloro-2-(((1,1-dioxidothietan-3-yl)oxy)methyl)-9-fluoro-4- ((3S,5S)-1-(methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1654]

[1655] 770610: ICT-568PC / INCY0568-WO1

[1656] Entry Compound Name

[1657] 988 2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 989 2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 990 2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 991 2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 992 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 993 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 994 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 995 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5R)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 996 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3 / ?,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 997 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 998 (Ra)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-cf3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1658]

[1659] 770610: ICT-568PC / INCY0568-WO1

[1660] Entry Compound Name

[1661] 999 (Sa)-2-amino-4-(7-chloro-9-fluoro-4-((3S,5S)-1-(methyl-d3)-2-oxo-5- (trifluoromethyl)pyrrolidin-3-yl)-2-((2-(methylsulfonyl)ethoxy)methyl)-5,6-dihydro- 4 / 7-benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 1000 2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-((3R,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1662] 1001 2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-((3R,5 / ?)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1663] 1002 2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-((3S,5S)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1664] 1003 2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-((3S,5R)-1-(methyl-d3)-2- oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin-8- yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1665] 1004 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-((methoxy-c / 3)methyl)-4-((3 / ?,5S)-1-(methyl- d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1666] 1005 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-((3 / ?,5S)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1667] 1006 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-((methoxy-c / 3)methyl)-4-((3S,5 / ?)-1-(methyl- d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1668] 1007 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-((3S,5 / ?)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1669] 1008 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-((methoxy-c / 3)methyl)-4-((3 / ?,5 / ?)-1-(methyl- d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1670] 1009 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-((3R,5 / ?)-1-(methyl- d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1671]

[1672] 770610: ICT-568PC / INCY0568-WO1

[1673] Entry Compound Name

[1674] 1010 (Ra)-2-amino-4-(7-chloro-9-fluoro-2-((methoxy-c / 3)methyl)-4-((3S,5S)-1-(methyl-cf3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1675] 1011 (Sa)-2-amino-4-(7-chloro-9-fluoro-2-((methoxy-d3)methyl)-4-((3S,5S)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1676] 1012 2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3R,5S)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1677] 1013 2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3R,5 / ?)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1678] 1014 2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3S,5S)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1679] 1015 2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3S,5R)-1-(methyl-d3)- 2-oxo- 5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7-benzo[de][1,6]naphthyridin- 8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1680] 1016 (Ra)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3 / ?,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1681] 1017 (Sa)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3R,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1682] 1018 (Ra)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3S,5 / ?)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1683] 1019 (Sa)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3S,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1684] 1020 (Ra)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3R,5 / ?)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[de][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile

[1685]

[1686] 770610: ICT-568PC / INCY0568-WO1

[1687] Entry Compound Name

[1688] 1021 (Sa)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3R,5R)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[cfe][1,6]naphthyridin-8-yl)-7-fluorobenzo[b]thiophene-3-carbonitrile 1022 (Ra)-2-amino-4-(7-chloro-2-((difluoromethoxy)methyl)-9-fluoro-4-((3S,5S)-1- (methyl-d3)-2-oxo-5-(trifluoromethyl)pyrrolidin-3-yl)-5,6-dihydro-4 / 7- benzo[...

Claims

770610: ICT-568PC / INCY0568-WO1CLAIMSWhat is claimed is:

1. A compound of Formula I:(I)or a pharmaceutically acceptable salt thereof;whereinR1is selected from C1-3 alkyl, C1-3 haloalkyl, C3-6 cycloalkyl, and halo;Cy1is Ce-waryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, 3, or 4 substituents independently selected from RCy1;each RCy1is independently selected from D, C1-3 alkyl, C1-3 haloalkyl, C2-3 alkenyl, C2-3 alkynyl, halo, CN, ORaCy1, and NRcCy1RdCy1;each RaCy1, RcCy1, and RdCy1is independently selected from H, C1-3 alkyl, and C1-3 haloalkyl;R2is selected from C1-3 alkyl and halo;R3is selected from H, C1-3 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, halo, D, CN, ORa3, NRb3C(O)Ra3, C(O)NRb3Rc3, N=S(O)Rb3Rc3, and NRb3Rc3; wherein the C3-w cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl; wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3B; or Rb3and Rc3together with the nitrogen atom to which they are attached form a 4-10 membered heterocycloalkyl, optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A;770610: ICT-568PC / INCY0568-WO1each Rd3is independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, and 4-10 membered heterocycloalkyl; wherein the C1-6 alkyl forming Rd3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from D, halo, CN, S(C>2)Ci-6 alkyl;each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, 3, or 4 subtituents each independently selected from R3B;each R3Bis independently selected from halo, D, CN, ORd3, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, S(O)(=NH)CI-6 alkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C;each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo and C1-6 haloalkyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are each optionally substituted by 1, 2, or 3 halo;R4is selected from H, D, C1-3 alkyl, halo, and CN;R5is selected from Cy5and CR5AR5BCy5;each Cy5is independently selected from C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aor (C3-6 alkylene)Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;each Cy5Ais independently selected from C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl forming Cy5Ais optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;R5Ais selected from H, D, C1-3 alkyl, C1-3 haloalkyl, and C3-6 cycloalkyl;R5Bis selected from H, D, C1-3 alkyl, and C1-3 haloalkyl;each R5Cis independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, ORa5, SRa5, S(O)Ra5, S(O)2Ra5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)ORa5, NRc5C(O)NRc5Rd5, C(=NRe5)Rb5, C(=NORa5)Rb5, C(=NRe5)NRc5Rd5, NRc5C(=NRe5)NRc5Rd5, NRc5S(O)Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, and S(O)2NRc5Rd5;each Ra5, Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl, wherein each C1-6 alkyl forming each Ra5, Rb5, Rc5, and Rd5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from D and halo;770610: ICT-568PC / INCY0568-WO1or any Rc1and Rd1attached to the same N atom, together with the N atom to which they are attached, form a 4-, 5-, 6- or 7-membered heterocycloalkyl group optionally substituted with 1, 2, 3, or 4 substituents independently selected from Rg1;each Re5is independently selected from H, C1-6 alkyl, OH and C1-6 alkoxy,, wherein each C1-6 alkyl and C1-6 alkoxy forming Re5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from D and halo;R6is selected from H, D, C1-3 alkyl, and C1-3 haloalkyl;R6Ais selected from H, D, C1-3 alkyl, and C1-3 haloalkyl;R7is selected from H, D, C1-3 alkyl, C1-3 haloalkyl, and halo; andR7Ais selected from H, D, C1-3 alkyl, C1-3 haloalkyl, and halo; orR7and R7Atogether with the carbon atom to which they are attached form a spiro fused C3-7 cycloalkane ring;wherein the ring-forming atoms of each heteroaryl and heterocycloalkyl consist of at least one ring-forming carbon atom and 1, 2, 3, or 4 heteroatoms independently selected from N, O, and S; wherein a ring-forming carbon atom of each heteroaryl and heterocycloalkyl is optionally substituted by oxo to form a carbonyl group.

2. The compound or pharmaceutically acceptable salt thereof of claim 1, wherein R1is selected from C1-3 alkyl and halo;Cy1is Ce-waryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, 3, or 4 substituents independently selected from RCy1;each RCy1is independently selected from D, C1-3 alkyl, C1-3 haloalkyl, C2-3 alkenyl, C2-3 alkynyl, halo, CN, ORaCy1, and NRcCy1RdCy1;each RaCy1, RcCy1, and RdCy1is independently selected from H, C1-3 alkyl, and C1-3 haloalkyl;R2is selected from C1-3 alkyl and halo;R3is selected from H, C1-3 alkyl, C2-6 alkynyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, D, CN, ORa3, NRb3C(O)Ra3, N=S(O)Rb3Rc3, and NRb3Rc3; wherein the C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3 or 4 substituents each independently selected from R3B;each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl; wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, 3, or 4 substituents770610: ICT-568PC / INCY0568-WO1independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3B;each Rd3is independently selected from H, C1-6 alkyl, C3-10 cycloalkyl, and 4-10 membered heterocycloalkyl; wherein the C1-6 alkyl forming Rd3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from D, halo, CN, S(C>2)Ci-6 alkyl;each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, 3, or 4 subtituents each independently selected from R3B;each R3Bis independently selected from halo, D, CN, ORd3, C3-10 cycloalkyl, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C;each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl halo, and C1-6 haloalkyl, wherein C2-6 alkenyl is optionally substituted by 1, 2, or 3 halo;R4is selected from H, D, C1-3 alkyl, halo, and CN;R5is selected from Cy5and CR5AR5BCy5;each Cy5is independently selected from C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl forming Cy5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;R5Ais selected from H, D, and C1-3 alkyl;R5Bis selected from H, D, and C1-3 alkyl;each R5Cis independently selected from C1-3 alkyl and R5D, wherein each C1-3 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, C1-3 alkoxy, amino, C1-3 alkylamino, and di(Ci-3alkyl)amino;R6is selected from H, D, C1-3 alkyl and C1-3 haloalkyl;R6Ais selected from H, D, C1-3 alkyl and C1-3 haloalkyl;R7is selected from H, D, C1-3 alkyl and C1-3 haloalkyl; andR7Ais selected from H, D, C1-3 alkyl, and C1-3 haloalkyl; orR7and R7Atogether with the carbon atom to which they are attached form a spiro fused C3-7 cycloalkane ring;wherein the ring-forming atoms of each heteroaryl and heterocycloalkyl consist of at least one ring-forming carbon atom and 1, 2, 3, or 4 heteroatoms independently selected from N, O, and S; wherein a ring-forming carbon atom of each heteroaryl and heterocycloalkyl is optionally substituted by oxo to form a carbonyl group.770610: ICT-568PC / INCY0568-WO13. The compound or pharmaceutically acceptable salt thereof of claim 1, wherein R1is selected from C1-3 alkyl and halo;Cy1is Ce-waryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, or 3 substituents independently selected from RCy1;each RCy1is independently selected from D, C1-3 alkyl, C1-3 haloalky I, C2-3 alkenyl, C2-3 alkynyl, halo, CN, ORaCy1, and NRcCy1RdCy1;each RaCy1, RcCy1, and RdCy1is independently selected from H, C1-3 alkyl, and C1-3 haloalkyl;R2is selected from C1-3 alkyl and halo;R3is selected from H, C1-6 alkyl, C2-6 alkynyl, C3-6 cycloalkyl, 4-6 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, halo, D, CN, NRb3C(O)Ra3, N=S(O)Rb3Rc3, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;each Ra3, Rb3and Rc3is independently selected from H and C1-6 alkyl;each Rd3is independently selected from H, C1-6 alkyl, C3- cycloalkyl, and 4-10 membered heterocycloalkyl; wherein the C1-6 alkyl forming Rd3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from D, halo, CN, S(C>2)Ci-6 alkyl;each R3Ais independently selected from C1-6 alkyl and R3B;each R3Bis independently di(Ci-3 alkyl)amino, S(O)(=NH)CI-6 alkyl, ORd3, or C3-cycloalkyl;R4is selected from H, D, C1-3 alkyl, halo, and CN;R5is selected from Cy5and CR5AR5BCy5;each Cy5is independently selected from C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;each Cy5Ais independently selected from C3-W cycloalkyl and Ce-waryl;R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl;R5Bis selected from H, D, and C1-3 alkyl;each R5Cis independently selected from C1-3 alkyl and R5D, wherein each C1-3 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, C1-3 alkoxy, C(O)Rb5, and NRc5Rd5;770610: ICT-568PC / INCY0568-WO1each Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl;R6is selected from H, D, and C1-3 alkyl;R6Ais selected from H, D, and C1-3 alkyl;R7is selected from H, D, halo, and C1-3 alkyl; andR7Ais selected from H, D, halo, and C1-3 alkyl; orR7and R7Atogether with the carbon atom to which they are attached form a spiro fused C3-7 cycloalkane ring.

4. The compound of pharmaceutically acceptable salt of claim 1, whereinR1is selected from C1-3 alkyl, C1-3 haloalkyl, C3-6 cycloalkyl, and halo;Cy1is Ce-waryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, 3, or 4 substituents independently selected from RCy1;each RCy1is independently selected from C1-3 alkyl, C1-3 haloalkyl, C2-3 alkynyl, halo, CN, and NRcCy1RdCy1;each RcCy1and RdCy1is independently selected from H and C1-3 alkyl;R2is selected from C1-3 alkyl and halo;R3is selected from H, C1-3 alkyl, C2-6 alkynyl, C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, halo, CN, ORa3, NRb3C(O)Ra3, C(O)NRb3Rc3, and NRb3Rc3; wherein the C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, and 5-10 membered heteroaryl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl; wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3B;each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, 3, or 4 subtituents each independently selected from R3B;each R3Bis independently selected from halo, D, OH, C1-3 alkoxy, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the C1-3 alkoxy and 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C;770610: ICT-568PC / INCY0568-WO1each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, halo and C1-6 haloalkyl wherein C2-6 alkenyl is optionally substituted by 1, 2, or 3 halo;R4is selected from H, D, and halo;R5is selected from Cy5and CR5AR5BCy5;each Cy5is independently selected from C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-10 cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;each Cy5Ais independently selected from C3- cycloalkyl, 4-10 membered heterocycloalkyl, Ce- aryl, 5-10 membered heteroaryl, wherein the C3-W cycloalkyl, 4-10 membered heterocycloalkyl, Ce-waryl, 5-10 membered heteroaryl forming Cy5Ais optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl;R5Bis selected from H, D, C1-3 alkyl, and C1-3 haloalkyl;each R5Cis independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;each R5Dis independently selected from C2-6 alkenyl, C2-6 alkynyl, halo, D, CN, OH, ORa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, NRc5Rd5, and NRc5C(O)Rb5;each Ra5, Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl, wherein each C1-6 alkyl forming each Ra5, Rb5, Rc5, and Rd5is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from D and halo;R6is selected from H, D, and C1-3 alkyl;R6Ais H or D;R7is selected from H, D, C1-3 alkyl, and halo; andR7Ais selected from H, C1-3 alkyl, C1-3 haloalkyl, and halo.

5. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 4, whereinR1is halo;Cy1is 6-10 membered heteroaryl optionally substituted with 1, 2, 3, or 4 substituents independently selected from RCy1;each RCy1is independently selected from C1-3 alkyl, halo, CN, and NRcCy1RdCy1; each RcCy1and RdCy1is H;R2is halo;770610: ICT-568PC / INCY0568-WO1R3is selected from H, C1-3 alkyl, C2-6 alkynyl, 4-10 membered heterocycloalkyl, CN, NRb3C(O)Ra3, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;each R3Bis independently selected from halo, D, CN, OH, C1-3 alkoxy, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the C1-3 alkoxy, and 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C;each R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, halo, and C1-6 haloalkyl, wherein C2-6 alkenyl is optionally substituted by 1, 2, or 3 halo;each Ra3, Rb3and Rc3is independently selected from H and C1-6 alkyl;each R3Ais independently selected from C1-6 alkyl and R3B;each R3Bis independently di(Ci-3 alkyl)amino;R4is H;R5is selected from Cy5and CR5AR5BCy5;each Cy5is independently selected from 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C;each Cy5Ais independently selected from C3-10 cycloalkyl and Ce- aryl;R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl;R5Bis selected from H, D, and C1-3 alkyl;each R5Cis independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D;each R5Dis independently selected from halo, D, C(O)Rb5, and NRc5Rd5;each Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl;R6is H;R6Ais H;R7is selected from H and halo; andR7Ais selected from H and halo.

6. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 5, wherein the compound of Formula I is a compound of any one of Formulae l-A to l-H:770610: ICT-568PC / INCY0568-WO1or a pharmaceutically acceptable salt thereof.

7. The compound or pharmaceutically acceptable salt thereof of claim 6, wherein the compound of Formula I is a compound of Formula l-G, wherein:R3is C1-3 alkyl optionally substituted by 1 or 2 substituents each independently selected from R3B;Gy5is pyridinyl optionally substituted with amino; andR5Ais C1-3 alkyl.770610: ICT-568PC / INCY0568-WO18. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 5, wherein the compound of Formula I is a compound of Formula (l-l) or (l-J):(l-l) (l-J).

9. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 5 and 8, wherein the compound of Formula I is a compound of Formula (l-J) or Formula (I-K):(l-J) (l-K);or a pharmaceutically acceptable salt thereof;wherein n is 0, 1, or 2.

10. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 4 and 6 to 9, wherein R1is halo (e.g., F or Cl).

11. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 10, wherein R1is Cl.

12. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 11, wherein Cy1is Ce- aryl or 6-10 membered heteroaryl, each optionally substituted with 1, 2, 3, or 4 substituents (or 1, 2, or 3 substituents, or 1 or 2 substituents, or 1 substituent) independently selected from C1-3 alkyl, C2-ealkynyl, halo, OH, and NH2.

13. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 12, wherein Cy1is selected from phenyl, naphthyl (such as 1-naphthyl and 2-naphthyl), benzothiazolyl (such as benzothiazol-2-yl, -4-yl, -5-yl, -6-yl, or -7-yl), benzothiophenyl (such as benzothiophen-2-yl, -4-yl, -5-yl, -6-yl, or -7-yl), and indazolyl (such as indazo-2-yl, -3-yl, -4-yl, -5-yl, or -6-yl) each optionally substituted with 1, 2, or 3 substituents independently selected from RCy1.770610: ICT-568PC / INCY0568-WO114. The compound or pharmaceutically acceptable salt thereof of any one of claims 1, 2, 4, and 6 to 13, wherein each RCy1is independently selected from C1-3 alkyl, C2-3 alkynyl, C1-3 haloalkyl, halo, CN, and NRcCy1RdCy1.

15. The compound or pharmaceutically acceptable salt thereof of any one of claims 1, 2, 4, and 6 to 14, wherein each RCy1is independently selected from C1-3 alkyl, C2-3 alkynyl, halo, CN, and NH2.

16. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 17. wherein Cy1is selected from 2-amino-7-fluorobenzo[d]thiazol-4-yl, 2-amino-3-cyano-7-fluorobenzo[d]thiophen-4-yl, 1-cyanonaphth-8-yl, and 5,6-dimethyl-1 / 7-indazol-4-yl.

17. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 4 and 6 to 16, wherein R2is halo (e.g., F or Cl).

18. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 17, wherein R2is F.

19. The compound or pharmaceutically acceptable salt thereof of any one of claims 1, 4, and 6 to 18, whereinR3is selected from H, C1-3 alkyl, C2-6 alkynyl, 4-10 membered heterocycloalkyl, halo, CN, ORa3, NRb3C(O)Ra3, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3are each optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A; and wherein the C1-6 alkyl and C2-6 alkynyl forming R3is optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R3B;each Ra3, Rb3, and Rc3is independently selected from H, C1-6 alkyl, 4-10 membered heterocycloalkyl, and 5-10 membered heteroaryl; wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Ra3, Rb3, and Rc3are each optionally substituted with 1, 2, or 3 substituents independently selected from R3Aand wherein the C1-6 alkyl forming Ra3, Rb3and Rc3is optionally substituted with 1, 2, or 3 substituents independently selected from R3B;each R3Ais independently selected from C1-6 alkyl and R3B, wherein the C1-6 alkyl forming R3Ais optionally substituted by 1, 2, or 3, subtituents each independently selected from R3B;each R3Bis independently selected from halo, OH, C1-3 alkoxy, S(O)(=NH)CI-6 alkyl, 4-10 membered heterocycloalkyl, amino, C1-3 alkylamino and di(Ci-3 alkyl)amino, wherein the C1-3 alkoxy and 4-10 membered heterocycloalkyl forming R3Bis optionally substituted by 1, 2, 3 or 4 substituents independently selected from R3C; andeach R3Cis independently selected from C1-6 alkyl, C2-6 alkenyl, and halo, wherein C2-6 alkenyl is optionally substituted by 1, 2, or 3 halo.770610: ICT-568PC / INCY0568-WO120. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 4 and 6 to 19, wherein R3is C1-3 alkyl or halo.

21. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 19, wherein R3is C1-3 alkyl (e.g., methyl or ethyl).

22. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 18, wherein R3is selected from C1-3 alkyl, 4-10 membered heterocycloalkyl, and C(O)NRb3Rc3; wherein the 4-10 membered heterocycloalkyl forming R3is optionally substituted with 1, 2, 3, or 4 substituents independently selected from R3A.

23. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 22, wherein each Rb3and Rc3is independently selected from H and C1-6 alkyl.

24. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 23, wherein each R3Bis independently di(Ci-3 alkyl)amino.

25. The compound or pharmaceutically acceptable salt thereof of any one of claims 1, 2, and 4 to 18, wherein R3is 4-10 membered heterocycloalkyl optionally substituted with 1, 2, 3, or 4 (e.g., 1, 2, or 3, 1 or 2, or 1) substituents independently selected from R3A.

26. The compound or pharmaceutically acceptable salt thereof of claim 25, wherein R3is 4-6 membered heterocycloalkyl optionally substituted with 1, 2, 3, or 4 (e.g., 1, 2, or 3, 1 or 2, or 1) substituents independently selected from R3A.

27. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 26, wherein each R3Ais independently selected from C1-6 alkyl and R3B.

28. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 27, wherein each R3Ais C1-6 alkyl (e.g., methyl).

29. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 28, wherein each R3Ais R3B.

30. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 4 and 6 to 29, wherein R4is H or D.

31. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 4 and 6 to 30, wherein R4is H.

32. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 31, wherein R5is Cy5.

33. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 31, wherein R5is CR5AR5BCy5.770610: ICT-568PC / INCY0568-WO134. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 33, wherein R5Ais selected from H, D, C1-3 alkyl, and C3-6 cycloalkyl.

35. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 34, wherein R5Ais C1-3 alkyl (e.g., methyl or ethyl).

36. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 33, wherein R5Ais C1-3 haloalkyl (e.g., difluoromethyl or trifluoromethyl).

37. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 34, wherein R5Ais H.

38. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 34, wherein R5Ais D.

39. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 34, wherein R5Ais C3-6 cycloalkyl (e.g., cyclopropyl).

40. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 39, wherein R5Bis selected from H, D, and C1-3 alkyl.

41. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 40, wherein R5Bis H.

42. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 40, wherein R5Bis D.

43. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 40, wherein R5Bis C1-3 alkyl.

44. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 43, wherein Cy5is 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl, wherein the 4-10 membered heterocycloalkyl and 5-10 membered heteroaryl forming Cy5is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C.

45. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 44, wherein Cy5is 5-10 membered heteroaryl optionally substituted by 1, 2, or 3 substituents (or 1 or 2 substituents, or 1 substituent) each independently selected from R5C.

46. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 45, wherein Cy5is pyridinyl (such as pyridin-2-yl, -3-yl, -4-yl, -5-yl, or -6-yl) optionally substituted with 1 or 2 substituents independently selected from R5C.770610: ICT-568PC / INCY0568-WO147. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 45, wherein Cy5is 5-10 membered heteroaryl is optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C.

48. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 44, wherein Cy5is 4-10 membered heterocycloalkyl optionally substituted by Cy5Aand also optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5C.

49. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 48, wherein each R5Cis is independently selected from C1-6 alkyl and R5D, wherein each C1-6 alkyl forming R5Cis optionally substituted by 1, 2, 3, or 4 substituents each independently selected from R5D.

50. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 49, wherein each R5Cis independently selected from amino, C1-3 alkylamino, and di(Ci-3 alkyl)amino.

51. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 50, wherein R5Cis amino.

52. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 48, wherein each Cy5Ais independently C3-10 cycloalkyl.

53. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 48, wherein each Cy5Ais independently Ce- aryl.

54. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 49, wherein each R5Dis independently halo.

55. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 49, wherein each R5Dis independently D.

56. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 49, wherein each R5Dis independently C(O)Rb5.

57. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 49, wherein each R5Dis independently NRc5Rd5.

58. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 57, wherein each Rb5, Rc5, and Rd5is independently selected from H and C1-6 alkyl.

59. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 4 and 6 to 58, wherein R6is H.770610: ICT-568PC / INCY0568-WO160. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 4 and 6 to 59, wherein R6ais H.

61. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 60, wherein R7is H.

62. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to to 61, wherein R7ais H.

63. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 60, wherein R7is halo.

64. The compound or pharmaceutically acceptable salt thereof of any one of claims 1 to 61, wherein R7ais halo.

65. The compound of any one of claims 1 to 64, wherein the compound of Formula (I) is selected from the compounds in Tables 1 and 2, and pharmaceutically acceptable salts thereof.

66. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, and at least one pharmaceutically acceptable carrier or excipient.

67. A method of inhibiting KRAS activity, the method comprising contacting the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66, with KRAS.

68. The method of claim 67, wherein the contacting comprises administering the compound to a patient.

69. The method of claim 67 or 68, wherein KRAS is characterized as having a somatic mutation of G12C.

70. The method of claim 67 or 68, wherein KRAS is characterized as having a somatic mutation of G12D.

71. The method of claim 67 or 68, wherein KRAS is characterized as having a somatic mutation of G 12V.

72. A method of treating a disease or disorder associated with activity of KRAS, the method comprising administering to a patient in need thereof a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

73. A method of treating a disease or disorder associated with activity of a KRAS protein harboring a G12C mutation, the method comprising administering to a patient in need770610: ICT-568PC / INCY0568-WO1thereof a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

74. A method of treating a disease or disorder associated with activity of a KRAS protein harboring a G12D mutation, the method comprising administering to a patient in need thereof a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

75. A method of treating a disease or disorder associated with activity of a KRAS protein harboring a G12V mutation, the method comprising administering to a patient in need thereof a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

76. A method for treating a cancer in a patient, the method comprising administering to the patient a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

77. The method of claim 76, wherein the cancer is selected from a carcinoma, a hematological cancer, a sarcoma, and glioblastoma.

78. The method of claim 76, wherein the cancer is a hematological cancer selected from myeloproliferative neoplasms, myelodysplastic syndrome, chronic and juvenile myelomonocytic leukemia, acute myeloid leukemia, acute lymphocytic leukemia, and multiple myeloma.

79. The method of claim 76, wherein the cancer is a carcinoma selected from pancreatic, colorectal, lung, bladder, gastric, esophageal, breast, head and neck, cervical, skin, and thyroid carcinomas.

80. The method of any one of claims 76 to 79, wherein abnormally proliferating cells of the cancer comprise KRAS having a G12C mutation.

81. The method of any one of claims 76 to 79, wherein abnormally proliferating cells of the cancer comprise KRAS having a G12D mutation.

82. The method of any one of claims 76 to 79, wherein abnormally proliferating cells of the cancer comprise KRAS having a G12V mutation.770610: ICT-568PC / INCY0568-WO183. The method of any one of claims 76 and 79 to 82, wherein the cancer is colorectal cancer.

84. The method of any one of claims 76 and 79 to 82, wherein the cancer is pancreatic cancer.

85. The method of any one of claims 76 and 79 to 82, wherein the cancer is pancreatic ductal cancer.

86. The method of any one of claims 76 and 79 to 82, wherein the cancer is lung cancer.

87. The method of any one of claims 76 and 79 to 82, wherein the cancer is non-small cell lung cancer (NCSLC).

88. The method of any one of claims 76 to 87, wherein the cancer is metastatic.

89. A method of treating an immunological or inflammatory disorder comprising administering to a patient in need thereof a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

90. The method of claim 89, wherein the immunological or inflammatory disorder is associated with activity of KRAS.

91. The method of claim 89, wherein the immunological or inflammatory disorder is associated with activity of KRAS having a G12C mutation.

92. The method of claim 89, wherein the immunological or inflammatory disorder is associated with activity of KRAS having a G12D mutation.

93. The method of claim 89, wherein the immunological or inflammatory disorder is associated with activity of KRAS having a G12V mutation.

94. The method of any one of claims 89 to 93, wherein the immunological or inflammatory disorder is Ras-associated lymphoproliferative disorder or juvenile myelomonocytic leukemia caused by a somatic mutation of KRAS.

95. A method of treating a cancer in a patient comprising:identifying that the patient is in need of treatment of a cancer and that abnormally proliferating cells of the cancer comprise KRAS having a G12C mutation;administering to the patient a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

96. A method of treating a cancer in a patient comprising:770610: ICT-568PC / INCY0568-WO1identifying that the patient is in need of treatment of a cancer and that abnormally proliferating cells of the cancer comprise KRAS having a G12D mutation;administering to the patient a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

97. A method of treating a cancer in a patient comprising:identifying that the patient is in need of treatment of a cancer and that abnormally proliferating cells of the cancer comprise KRAS having a G12V mutation;administering to the patient a therapeutically effective amount of the compound or pharmaceutically acceptable salt thereof according to any one of claims 1 to 65, or the pharmaceutical composition of claim 66.

Images