Acetamido-phenylbenzamide derivatives and methods of use thereof
Acetamido-phenylbenzamide derivatives modulate P-glycoprotein and cytochrome P450 enzymes to address multidrug resistance and improve the delivery and efficacy of anticancer drugs, particularly in tumors and the brain, with reduced side effects.
Patent Information
- Application Number
- JP2023521297
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Priority Date
- 2020-10-07
- Filing Date
- 2021-10-07
- Publication Date
- 2026-03-03
- Estimated Expiration
- 2041-10-07
AI Technical Summary
Existing anticancer drugs face challenges due to multidrug resistance caused by overexpression of P-glycoprotein and cytochrome P450 enzymes, leading to reduced efficacy and bioavailability, particularly in tumors and the brain, with conventional modulators causing significant adverse effects.
Development of acetamido-phenylbenzamide derivatives that modulate P-glycoprotein and cytochrome P450 enzymes to enhance the bioavailability and delivery of therapeutic agents to tumors and the brain while minimizing side effects.
The compounds improve the efficacy of anticancer drugs by overcoming multidrug resistance and enhancing their delivery to tumor cells and the brain, reducing adverse effects.
Smart Images

Figure 0007823035000001 
Figure 0007823035000002 
Figure 0007823035000003
Abstract
Description
[Technical Field]
[0001] Related Applications This application claims priority to and benefit of U.S. Provisional Application No. 63 / 088,778, filed October 7, 2020, the entire contents of which are incorporated herein by reference.
[0002] Field of Disclosure The present disclosure relates to acetamido-phenylbenzamide derivatives that have P-glycoprotein-modulating activity and / or modulating activity against the drug-metabolizing enzyme cytochrome P450 (e.g., CYP3A4 and / or CYP3A5 isoforms) and are useful for treating the human or animal body. The present disclosure also relates to methods for preparing these compounds, pharmaceutical compositions containing them, and their use in treating disorders in which the expression of P-glycoprotein and / or cytochrome P450 isoforms (e.g., CYP3A4 or CYP3A5) is modulated (e.g., multidrug-resistant cancers). The present disclosure also relates to the use of compounds of the present disclosure to improve the oral bioavailability of therapeutic agents that are substrates of P-glycoprotein and / or cytochrome P450. The present disclosure also relates to the use of compounds of the present disclosure to increase the brain distribution of therapeutic agents that are substrates of P-glycoprotein and / or cytochrome P450. [Background technology]
[0003] background Many anticancer drugs (e.g., vinca alkaloids, anthracyclines, epipodophyllotoxins, paclitaxel, and docetaxel) are ineffective when administered to patients with multidrug resistance (MDR) caused by overexpression of P-glycoprotein. P-glycoprotein regulates the intracellular accumulation of administered anticancer drugs by extruding them from tumor cells. Expression of the drug-metabolizing CYP3A4 protein in breast, colorectal, and esophageal tumors, and Ewing's sarcoma, can suppress the intracellular concentration of anticancer drugs by forming metabolites with reduced antitumor activity. This action of CYP3A4 limits the efficacy of anticancer drugs or contributes to the development of resistance to these drugs. Modulation of P-glycoprotein and / or cytochrome P450 enzymes (e.g., CYP3A4) in tumor cells can increase the sensitivity of these cells to anticancer drugs.
[0004] P-glycoprotein is also expressed in normal healthy tissues, such as the small intestine. Intestinal P-glycoprotein does not allow its substrates to pass through the epithelial cells that line the intestinal wall, thus reducing the oral bioavailability of these substrates. In addition, anticancer drugs may also undergo first-pass metabolism by cytochrome P450 enzymes (e.g., CYP3A4 and / or CYP3A5 isoforms) present in the small intestine and liver, further reducing oral bioavailability. Therefore, it is necessary to improve the bioavailability of anticancer drugs by dual targeting and regulating P-glycoprotein and cytochrome P450 enzymes (e.g., CYP3A4 and / or CYP3A5 isoforms).
[0005] Furthermore, the localization of P-glycoprotein in the endothelial cells of the blood-brain barrier significantly restricts the transport of P-glycoprotein substrates from the blood to the brain. Modulating P-glycoprotein at the blood-brain barrier may be beneficial in the treatment of several central nervous system (CNS) disorders, such as brain tumors such as glioblastoma. Conventional P-glycoprotein modulators, such as verapamil and cyclosporine A, cause significant adverse effects (e.g., hypotension and immunosuppression). Therefore, several novel P-glycoprotein modulators, such as piperidine-2-carboxylate, acridine, piperazine-2,5-dione, anthranilic acid, and methanodibenzosuberane derivatives, have been developed. However, these newly introduced P-glycoprotein modulators have been reported to exhibit toxicity and other adverse effects. The present disclosure arises from a need to provide additional compounds for the modulation of P-glycoprotein and cytochrome P450 (e.g., CYP3A4 and CYP3A5 isoforms) enzymes that a) significantly improve the bioavailability of substrates of these enzymes, including anticancer drugs, b) overcome multidrug resistance in tumors, and c) improve delivery of P-glycoprotein substrates to the brain while reducing significant side effects. Summary of the Invention
[0006] overview In one aspect, the disclosure provides compounds of formula (I), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000001.tif53128In formula, A is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, or -NH2; R1 and R4 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, where neither R2 nor R3 is H; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R5 and R6 together with the atoms to which they are attached form a heterocyclyl or heteroaryl, A may be phenyl or It's not TIFF0007823035000002.tif18128 either.
[0007] In one aspect, the disclosure provides a compound of formula (I'), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000003.tif53128In formula, A is TIFF0007823035000004.tif22128; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6alkoxy, halogen, -CN, -OH, or -NH2; R1 and R4 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, where neither R2 nor R3 is H; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R5 and R6 together with the atoms to which they are attached form a heterocyclyl, A is The file is TIFF0007823035000005.tif23128.
[0008] In one aspect, the disclosure provides a compound of formula (II), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000006.tif60128In formula, R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, or -NH2; R1 and R4 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, where neither R2 nor R3 is H; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3.
[0009] In one aspect, the disclosure provides compounds obtainable or obtainable by a method for preparing a compound described herein (e.g., a method comprising one or more steps described in Schemes 1-10).
[0010] In one aspect, the present disclosure provides a pharmaceutical composition comprising a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, and a pharmaceutically acceptable diluent or carrier.
[0011] In one aspect, the disclosure provides intermediates described herein that are suitable for use in the methods for preparing the compounds described herein (e.g., the intermediates are selected from the intermediates described in Examples 1-284).
[0012] In one aspect, the present disclosure provides a method of modulating P-glycoprotein activity (e.g., in vitro or in vivo) and / or cytochrome P450 activity (e.g., in vitro or in vivo), comprising contacting a cell with an effective amount of a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof.
[0013] In one aspect, the present disclosure provides a method of treating or preventing a disease or disorder disclosed herein in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, or a pharmaceutical composition of the present disclosure.
[0014] In one aspect, the present disclosure provides compounds of the present disclosure, or pharmaceutically acceptable prodrugs, solvates, enantiomers, stereoisomers, tautomers, or salts thereof, for use in modulating P-glycoprotein activity (e.g., in vitro or in vivo) and / or cytochrome P450 activity (e.g., in vitro or in vivo).
[0015] In one aspect, the present disclosure provides a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, for use in treating or preventing a disease or disorder disclosed herein.
[0016] In one aspect, the present disclosure provides the use of a compound of the present disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, in the manufacture of a medicament for modulating P-glycoprotein activity (e.g., in vitro or in vivo) and / or cytochrome P450 activity (e.g., in vitro or in vivo).
[0017] In one aspect, the disclosure provides the use of a compound of the disclosure, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, in the manufacture of a medicament for treating or preventing a disease or disorder disclosed herein.
[0018] In one aspect, the disclosure provides methods of preparing the compounds of the disclosure.
[0019] In one aspect, the disclosure provides a method of preparing a compound, comprising one or more steps described herein.
[0020] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this disclosure belongs. As used herein, the singular also includes the plural unless the context clearly dictates otherwise. Although methods and materials similar or equivalent to those described herein can be used in the practice or testing of this disclosure, suitable methods and materials are described below. All publications, patent applications, patents, and other references mentioned herein are incorporated by reference. References cited herein are not admitted to be prior art to the claimed invention. In case of conflict, the present specification, including definitions, will control. Furthermore, the materials, methods, and examples are illustrative only and are not intended to be limiting. In the event of a conflict between a chemical structure and the name of a compound disclosed herein, the chemical structure will control.
[0021] [The present invention 1001] A compound of formula (I) or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000007.tif53128 During the ceremony, A is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, halogen, -CN, -OH, or -NH 2 and; R 1 and R 4 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R 2 and R 3 are independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , -C(O)NR 11 -S(O) 2 R 11 , -C(O)NR 11 -S(O) 2 -OR 11 , or -C(O)NR 11 -S(O) 2 -N(R 11 ) 2 where R 2 MoR 3 Also not H; R 5 and R 6 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 or R 5 and R 6 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 may be substituted with; Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 ) 2 、C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -O-(CH 2 ) t -R 8 , -NH-(CH 2 ) t -R 8 、C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 9 may be substituted with; Each R 9 are independently -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 aryl), wherein the heteroaryl or aryl is selected from one or more halogen, —CN, —OH, or —NH 2 may be substituted with; Each R 10 are independently halogen, -OH, -NH 2 , -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, oxo, halogen, -CN, -OH, or -NH 2 or 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 may be substituted with; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R 5 and R 6 together with the atom to which they are attached form a heterocyclyl or heteroaryl, and A is either phenyl or TIFF0007823035000008.tif18128 But not. [The present invention 1002] A compound of formula (I) or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000009.tif53128 During the ceremony, A is TIFF0007823035000010.tif22128 and; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, halogen, -CN, -OH, or -NH 2 and; R 1 and R 4 are independently H, C 1~6 Alkyl, C2~6 Alkenyl, or C 2~6 is alkynyl; R 2 and R 3 are independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , -C(O)NR 11 -S(O) 2 R 11 , -C(O)NR 11 -S(O) 2 -OR 11 , or -C(O)NR 11 -S(O) 2 -N(R 11 ) 2 where R 2 MoR 3 Also not H; R 5 and R 6 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 or R 5 and R 6 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 may be substituted with; Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 ) 2 、C1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -O-(CH 2 ) t -R 8 , -NH-(CH 2 ) t -R 8 、C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 9 may be substituted with; Each R 9 are independently -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 aryl), wherein the heteroaryl or aryl is selected from one or more halogen, —CN, —OH, or —NH 2 may be substituted with; Each R 10 are independently halogen, -OH, -NH 2 , -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, oxo, halogen, -CN, -OH, or -NH 2 or 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 may be substituted with; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R 5 and R 6 together with the atoms to which they are attached form a heterocyclyl, and A is TIFF0007823035000011.tif20128 is. [The present invention 1003] A compound of formula (II) or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000012.tif60128 During the ceremony, R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, halogen, -CN, -OH, or -NH 2 and; R 1 and R 4 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R 2 and R 3 are independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , -C(O)NR 11 -S(O) 2 R 11 , -C(O)NR 11 -S(O) 2 -OR 11 , or -C(O)NR 11 -S(O) 2 -N(R 11 ) 2 where R 2 MoR 3 Also not H; R 5 and R 6 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 or R 5 and R 6 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 may be substituted with; Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 ) 2 、C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -O-(CH 2 ) t -R 8 , -NH-(CH 2 ) t -R 8 、C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R 8 -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -NH(C 1~6 alkyl), -N(C 1~6 alkyl) 2 , -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 9 may be substituted with; Each R 9 are independently -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 aryl), wherein the heteroaryl or aryl is selected from one or more halogen, —CN, —OH, or —NH 2 may be substituted with; Each R 10 are independently halogen, -OH, -NH 2 , -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, oxo, halogen, -CN, -OH, or -NH 2 or 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 may be substituted with; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3. [The present invention 1004] R x and R y are independently H, C 1~6 Any of the compounds of the present invention described above, wherein the aryl group is alkyl, or -OH. [The present invention 1005] R 1 and R 4 are each independently H or C 1~6 Any of the compounds of the present invention above, wherein the compound is alkyl. [The present invention 1006] R 2 and R 3 are each independently, -OC 1~6 Alkyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 ) 2 , or -C(O)NR 11 -S(O) 2 R 11The compound of the present invention 1001 or 1002, [The present invention 1007] R 5 and R 6 are independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or -C(O)R 7 wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 Any of the compounds of the present invention described above, optionally substituted with [The present invention 1008] R 5 and R 6 are independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 Any of the compounds of the present invention described above, optionally substituted with [The present invention 1009] R 5 and R 6 are independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 7 Any of the compounds of the present invention substituted with: [The present invention 1010] R 5 and R 6 together with the atoms to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more R 7 Any of the compounds of the present invention substituted with: [The present invention 1011] Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10 、C 1~3 Alkyl, C 2~6 Alkynyl, -O-(CH 2 ) t -R 8 、C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkynyl, aryl, or heteroaryl is selected from one or more R 10 Any of the compounds of the present invention described above, optionally substituted with [The present invention 1012] Each R 7 are independently oxo, halogen, -OH, -NH 2 , -CN, -C(O)R 10、C 1~3 Alkyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -O-(CH 2 ) t -R 8 、C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkynyl, aryl, or heteroaryl is selected from one or more R 10 Any of the compounds of the present invention substituted with: [The present invention 1013] R 8 But -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -N(C 1~6 alkyl) 2 , -S(C 1~6 alkyl), 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, heterocyclyl, or heteroaryl is selected from one or more R 9 Any of the compounds of the present invention described above, optionally substituted with [The present invention 1014] R 8 But -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH 2 , -N(C 1~6 alkyl) 2 , -S(C 1~6 alkyl), 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, heterocyclyl, or heteroaryl is selected from one or more R 9 Any of the compounds of the present invention substituted with: [The present invention 1015] Each R 9 are independent, -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 Any of the preceding compounds of the present invention wherein said heteroaryl or aryl is optionally substituted with one or more halogens or -OH. [The present invention 1016] Each R 9 are independent, -(CH 2 ) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH 2 ) u -(C 6~10 Any of the preceding compounds of the present invention is a heteroaryl or aryl), wherein said heteroaryl or aryl is substituted with one or more halogen or -OH. [The present invention 1017] Each R 10 independently, C 1~6 Alkyl, C 1~6 Any of the compounds of the present invention which is haloalkyl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. [The present invention 1018] Each R 11 became independent, H; One or more 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 Aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S optionally substituted with C 1~6 Alkyl wherein the heterocyclyl, aryl, or heteroaryl is a 5-10 membered heteroaryl containing one or more heteroatoms selected from N, O, and S; C 1~6 Any of the compounds of the present invention described above may be substituted with alkyl or oxo. [The present invention 1019] Each R 11 became independent, H; One or more 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 Aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S optionally substituted with C 1~6 Alkyl wherein the heterocyclyl, aryl, or heteroaryl is a 5-10 membered heteroaryl containing one or more heteroatoms selected from N, O, and S; C 1~6 Any of the compounds of the present invention substituted with alkyl, or oxo. [The present invention 1020] Each R 11 became independent, H; One or more 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 Aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S Replaced by C 1~6 Alkyl wherein the heterocyclyl, aryl, or heteroaryl is a 5-10 membered heteroaryl containing one or more heteroatoms selected from N, O, and S; C 1~6 Any of the compounds of the present invention described above may be substituted with alkyl or oxo. [The present invention 1021] 2 R's11 together with the atoms to which they are bonded, One or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 4- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with Any of the compounds of the present invention which form: [The present invention 1022] 2 R's 11 together with the atoms to which they are bonded, One or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, halogen, -CN, -OH, or -NH 2 4- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with Any of the compounds of the present invention which form: [The present invention 1023] Any of the compounds of the present invention wherein each n is 0. [The present invention 1024] Any of the compounds of the present invention wherein each n is 1. [The present invention 1025] Any of the preceding compounds of the present invention wherein each m is 0. [The present invention 1026] Any of the preceding compounds of the present invention wherein each m is 1. [The present invention 1027] Any of the compounds of the present invention wherein each p is 0. [The present invention 1028] Any of the compounds of the present invention wherein each p is 1. [The present invention 1029] R 2 MoR 3 or H. [The present invention 1030] R 5 and R 6 together with the atom to which they are attached form a heterocyclyl or heteroaryl, A TIFF0007823035000013.tif18128 Any of the compounds of the present invention which are not [The present invention 1031] Compounds of formula (Ia) or (Ib): TIFF0007823035000014.tif110128 or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [The present invention 1032] A compound of formula (Ic), (Id), or (Ie): TIFF0007823035000015.tif169128 or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [The present invention 1033] Compounds of formula (I-a') or (I-b'): TIFF0007823035000016.tif110128 or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [The present invention 1034] Compound of formula (II-a): TIFF0007823035000017.tif57128 or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [This invention 1035] Compound of formula (II-a'): TIFF0007823035000018.tif57128 or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof. [The present invention 1036] Any of compounds 1001 to 1003 of the present invention selected from Table 1. [This invention 1037] A pharmaceutical composition comprising any one of the compounds of the present invention 1001 to 1036, or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof, and a pharmaceutically acceptable diluent or carrier. [The present invention 1038] A method for regulating P-glycoprotein activity and / or cytochrome P450 activity, comprising contacting a cell with an effective amount of any of the compounds of the present inventions 1001 to 1036 or the pharmaceutical composition of the present invention 1037. [This invention 1039] A method for treating or preventing a disease or disorder disclosed herein in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of any of the compounds of inventions 1001 to 1036 or the pharmaceutical composition of invention 1037. [The present invention 1040] A method for treating or preventing cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of any of the compounds of the present inventions 1001 to 1036 or the pharmaceutical composition of the present invention 1037. [This invention 1041] A compound of any of claims 1001 to 1036 or a pharmaceutical composition of claim 1037 for use in modulating P-glycoprotein activity and / or cytochrome P450 activity. [The present invention 1042] A compound of any of claims 1001 to 1036 or a pharmaceutical composition of claim 1037 for use in treating or preventing a disease or disorder disclosed herein. [This invention 1043] A compound of any one of claims 1001 to 1036 or a pharmaceutical composition of claim 1037 for use in treating or preventing cancer. [This invention 1044] Use of any of the compounds of Inventions 1001 to 1036 or the pharmaceutical composition of Invention 1037 in the manufacture of a medicament for modulating P-glycoprotein activity and / or cytochrome P450 activity. [This invention 1045] Use of any of the compounds of inventions 1001 to 1036 or the pharmaceutical composition of invention 1037 in the manufacture of a medicament for treating or preventing a disease or disorder disclosed herein. [The present invention 1046] Use of any of the compounds of the present inventions 1001 to 1036 or the pharmaceutical composition of the present invention 1037 in the manufacture of a medicament for treating or preventing cancer. Other features and advantages of the present disclosure will be apparent from the following detailed description and claims. DETAILED DESCRIPTION OF THE INVENTION
[0022] Detailed Description The present disclosure arises from a need to provide additional compounds for modulating P-glycoprotein and / or cytochrome P450 (e.g., CYP3A4 and / or CYP3A5 isoform) enzymes that significantly improve the bioavailability of drugs that are substrates of P-glycoprotein and / or cytochrome P450 (e.g., CYP3A4 and / or CYP3A5 isoform) enzymes, including anticancer drugs, antihypertensive drugs, antiarrhythmic drugs, HIV protease inhibitors, antibiotics, antifungals, immunosuppressants, antidepressants, neuroleptics, antiepileptic drugs, antacids, opioids, and antiemetic drugs, while reducing significant adverse effects. The compounds of the present disclosure may also be useful in overcoming P-glycoprotein and / or cytochrome P450 (e.g., CYP3A4)-driven multidrug resistance in cancer cells. Compounds of the present disclosure may also be useful for modulating P-glycoprotein at the blood-brain barrier, thereby allowing drugs to penetrate the brain and improving the efficacy of these drugs in brain diseases (e.g., brain tumors). Compounds of the present disclosure may also be useful for modulating P-glycoprotein in the bile canaliculi, thereby modulating the enterohepatic recirculation of P-glycoprotein substrate drugs (e.g., irinotecan) that are affected by this phenomenon. Compounds of the present disclosure may also be useful for modulating P-glycoprotein expressed in renal proximal tubule cells, thereby affecting the renal excretion of substrate drugs.
[0023] Compounds of the Disclosure In one aspect, the disclosure provides compounds of formula (I), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000019.tif48128In formula, A is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said cycloalkyl or heterocyclyl is optionally substituted with oxo; R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, or -NH2; R1 and R4 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, where neither R2 nor R3 is H; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R5 and R6 together with the atoms to which they are attached form a heterocyclyl or heteroaryl, and A is either phenyl or Neither is TIFF0007823035000020.tif18128.
[0024] In one aspect, the disclosure provides a compound of formula (I'), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000021.tif53128In formula, A is TIFF0007823035000022.tif22128; R x and R y are independently H, C 1~6 Alkyl, C 2~6Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, or -NH2; R1 and R4 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, where neither R2 nor R3 is H; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3, where R5 and R6 together with the atoms to which they are attached form a heterocyclyl, and A is The file is TIFF0007823035000023.tif20128.
[0025] In one aspect, the disclosure provides a compound of formula (II), or a pharmaceutically acceptable prodrug, solvate, enantiomer, stereoisomer, tautomer, or salt thereof: TIFF0007823035000024.tif60128In formula, R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 alkoxy, halogen, -CN, -OH, or -NH2; R1 and R4 are each independently H, C 1~6 Alkyl, C 2~6Alkenyl, or C 2~6 is alkynyl; R2 and R3 are each independently H, C 2~6 Alkenyl, C 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, where neither R2 nor R3 is H; R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7; Each R7 is independently oxo, halogen, -OH, -NH2, -CN, or -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with; R8 is -OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein said alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9; Each R9 independently represents -(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH; Each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; Each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, halogen, -CN, -OH, or -NH; n, m, and p are each independently 0 or 1; t is 1, 2, or 3; u is 0, 1, 2, or 3.
[0026] For compounds of formula (I), (I'), or (II), A, R x、 R y , R1, R2, R3, R4, R5, R6, R7, R8, R9, R 10 , R 11 , n, m, p, t, and u can be appropriately selected from the groups described herein; A, R x、 R y , R1, R2, R3, R4, R5, R6, R7, R8, R9, R 10 , R 11 , n, m, p, t, and u may be any group described herein in A, R x、 R y , R1, R2, R3, R4, R5, R6, R7, R8, R9, R 10 , R 11 , n, m, p, t, and u may be combined with any of the groups described herein, as appropriate.
[0027] In some embodiments, the N atom of the compound is an N-oxide.
[0028] In some embodiments, the N-oxide has the formula TIFF0007823035000025.tif16128, wherein TIFF0007823035000026.tif9128 shows the bond to a compound of formula (I), (I'), or (II).
[0029] In some embodiments, the N-oxide has the formula TIFF0007823035000027.tif14128, wherein TIFF0007823035000028.tif9128 shows the bond to a compound of formula (I), (I'), or (II).
[0030] In some embodiments, the N-oxide has the formula TIFF0007823035000029.tif15128, wherein TIFF0007823035000030.tif9128 shows the bond to a compound of formula (I), (I'), or (II).
[0031] In some embodiments, A is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl may be substituted with oxo.
[0032] In some embodiments, A is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0033] In some embodiments, A is C 3~10 cycloalkyl or 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O and S, wherein the cycloalkyl or heterocyclyl may be substituted with oxo.
[0034] In some embodiments, A is C 3~10 cycloalkyl, or a 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0035] In some embodiments, A is C optionally substituted with oxo. 3~10 It is cycloalkyl.
[0036] In some embodiments, A is C3 cycloalkyl. In some embodiments, A is C4 cycloalkyl. In some embodiments, A is C5 cycloalkyl. In some embodiments, A is C6 cycloalkyl. In some embodiments, A is C7 cycloalkyl. In some embodiments, A is C8 cycloalkyl. In some embodiments, A is C9 cycloalkyl. In some embodiments, A is C 10 It is cycloalkyl.
[0037] In some embodiments, A is a C3 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C4 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C5 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C6 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C7 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C8 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C9 cycloalkyl optionally substituted with oxo. In some embodiments, A is a C6 cycloalkyl optionally substituted with oxo. 10 It is cycloalkyl.
[0038] In some embodiments, A is a C3-C7 monocyclic cycloalkyl. In some embodiments, A is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, A is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, A is a C9-C 10 In some embodiments, A is a C-C 10 In some embodiments, A is a C-C bicyclic saturated cycloalkyl. 10 In some embodiments, A is a C-C bicyclic partially saturated cycloalkyl. 10 It is a polycyclic cycloalkyl.
[0039] In some embodiments, A is a C3-C7 monocyclic cycloalkyl optionally substituted with oxo. In some embodiments, A is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with oxo. In some embodiments, A is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with oxo. In some embodiments, A is a C9-C monocyclic partially saturated cycloalkyl optionally substituted with oxo. 10 In some embodiments, A is a C9-C cycloalkyl optionally substituted with oxo. 10 In some embodiments, A is a C9-C10 alkyl group optionally substituted with oxo. 10 In some embodiments, A is a C8-C10 alkyl group optionally substituted with oxo. 10 It is a polycyclic cycloalkyl.
[0040] In some embodiments, A is a 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0041] In some embodiments, A is a 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0042] In some embodiments, A is a 3-membered heterocyclyl containing one heteroatom selected from N, O, and S. In some embodiments, A is a 4-membered heterocyclyl containing one to two heteroatoms selected from N, O, and S. In some embodiments, A is a 5-membered heterocyclyl containing one to three heteroatoms selected from N, O, and S. In some embodiments, A is a 6-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is a 7-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is an 8-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is a 9-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S. In some embodiments, A is a 10-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S.
[0043] In some embodiments, A is a 3-membered heterocyclyl containing one heteroatom selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 4-membered heterocyclyl containing one to two heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 5-membered heterocyclyl containing one to three heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 6-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 7-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is an 8-membered heterocyclyl containing one to four heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0044] In some embodiments, A is a 7-10 membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0045] In some embodiments, A is a 7-10 membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0046] In some embodiments, A is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0047] In some embodiments, A is a 7-membered bicyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is an 8-membered bicyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 9-membered bicyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo. In some embodiments, A is a 10-membered bicyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0048] In some embodiments, A is an 8-10 membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0049] In some embodiments, A is an 8-10 membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with oxo.
[0050] In some embodiments, A is C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0051] In some embodiments, A is C 6~10In some embodiments, A is aryl. In some embodiments, A is C5-C6 aryl. In some embodiments, A is phenyl.
[0052] In some embodiments, A is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0053] In some embodiments, A is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0054] In some embodiments, A is a 9-10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0055] In some embodiments, A is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, A is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0056] In some embodiments, A is a 9-10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0057] In some embodiments, A is The file is TIFF0007823035000031.tif22128.
[0058] In some embodiments, A is The file is TIFF0007823035000032.tif21128.
[0059] In some embodiments, A is The file is TIFF0007823035000033.tif15128.
[0060] In some embodiments, A is The file is TIFF0007823035000034.tif15128.
[0061] In some embodiments, R x and R y are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0062] In some embodiments, R x and R y are H respectively.
[0063] In some embodiments, R x and R y are each independently, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0064] In some embodiments, R x and R y are independently H, C 1~6 alkyl, or -OH.
[0065] In some embodiments, R x is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6It is alkoxy, halogen, -CN, -OH, or -NH2.
[0066] In some embodiments, R x is H.
[0067] In some embodiments, R x is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0068] In some embodiments, R x is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, or C 1~6 It is an alkoxy.
[0069] In some embodiments, R x is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0070] In some embodiments, R x is C 1~6 In some embodiments, R x is methyl. In some embodiments, R x is ethyl. In some embodiments, R x is propyl. In some embodiments, R x is butyl. In some embodiments, R x is pentyl. In some embodiments, R x is hexyl. In some embodiments, R x is isopropyl. In some embodiments, R x is isobutyl. In some embodiments, R x is isopentyl. In some embodiments, R x is isohexyl. In some embodiments, R xis sec butyl. In some embodiments, R x is sec pentyl. In some embodiments, R x is sec hexyl. In some embodiments, R x is tert butyl.
[0071] In some embodiments, R x is C 2~6 In some embodiments, R is alkenyl. x is C alkenyl. In some embodiments, R x is C alkenyl. In some embodiments, R x is C4 alkenyl. In some embodiments, R x is C5 alkenyl. In some embodiments, R x is a C6 alkenyl.
[0072] In some embodiments, R x is C 2~6 In some embodiments, R is alkynyl. x is C alkynyl. In some embodiments, R x is C alkynyl. In some embodiments, R x is C4 alkynyl. In some embodiments, R x is C5 alkynyl. In some embodiments, R x is a C6 alkynyl.
[0073] In some embodiments, R x is C 1~6 In some embodiments, R is alkoxy. x is methoxy. In some embodiments, R x is ethoxy. In some embodiments, R x is propoxy. In some embodiments, R x is butoxy. In some embodiments, R x is pentoxy. In some embodiments, R x is hexoxy.
[0074] In some embodiments, Rx is a halogen, -CN, -OH, or -NH2.
[0075] In some embodiments, R x is a halogen. In some embodiments, R x is F, Cl, Br, or I. In some embodiments, R x is F, Cl, or Br. In some embodiments, R x is F. In some embodiments, R x is Cl. In some embodiments, R x is Br. In some embodiments, R x is I.
[0076] In some embodiments, R x is -CN. In some embodiments, R x is —OH. In some embodiments, R x is -NH2.
[0077] In some embodiments, each R x is H, C 1~6 alkyl, or -OH.
[0078] In some embodiments, R y is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0079] In some embodiments, R y is H.
[0080] In some embodiments, R y is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 It is alkoxy, halogen, -CN, -OH, or -NH2.
[0081] In some embodiments, Ry is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, or C 1~6 It is an alkoxy.
[0082] In some embodiments, R y is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0083] In some embodiments, R y is C 1~6 In some embodiments, R y is methyl. In some embodiments, R y is ethyl. In some embodiments, R y is propyl. In some embodiments, R y is butyl. In some embodiments, R y is pentyl. In some embodiments, R y is hexyl. In some embodiments, R y is isopropyl. In some embodiments, R y is isobutyl. In some embodiments, R y is isopentyl. In some embodiments, R y is isohexyl. In some embodiments, R y is sec butyl. In some embodiments, R y is sec pentyl. In some embodiments, R y is sec hexyl. In some embodiments, R y is tert butyl.
[0084] In some embodiments, R y is C 2~6 In some embodiments, R is alkenyl. y is C alkenyl. In some embodiments, R y is C alkenyl. In some embodiments, R y is C4 alkenyl. In some embodiments, Ry is C5 alkenyl. In some embodiments, R y is a C6 alkenyl.
[0085] In some embodiments, R y is C 2~6 In some embodiments, R is alkynyl. y is C alkynyl. In some embodiments, R y is C alkynyl. In some embodiments, R y is C4 alkynyl. In some embodiments, R y is C5 alkynyl. In some embodiments, R y is a C6 alkynyl.
[0086] In some embodiments, R y is C 1~6 In some embodiments, R is alkoxy. y is methoxy. In some embodiments, R y is ethoxy. In some embodiments, R y is propoxy. In some embodiments, R y is butoxy. In some embodiments, R y is pentoxy. In some embodiments, R y is hexoxy.
[0087] In some embodiments, R y is a halogen, -CN, -OH, or -NH2.
[0088] In some embodiments, R y is a halogen. In some embodiments, R y is F, Cl, Br, or I. In some embodiments, R y is F, Cl, or Br. In some embodiments, R y is F. In some embodiments, R y is Cl. In some embodiments, R y is Br. In some embodiments, R y is I.
[0089] In some embodiments, R y is -CN. In some embodiments, R y is —OH. In some embodiments, R y is -NH2.
[0090] In some embodiments, each R y is H, C 1~6 alkyl, or -OH.
[0091] In some embodiments, R and R are each independently selected from H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0092] In some embodiments, R1 and R4 are each independently H.
[0093] In some embodiments, R and R are each independently C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0094] In some embodiments, R and R are each independently H or C 1~6 It is alkyl.
[0095] In some embodiments, R is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0096] In some embodiments, R1 is H.
[0097] In some embodiments, R is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0098] In some embodiments, R is C 1~6In some embodiments, R1 is alkyl. In some embodiments, R1 is methyl. In some embodiments, R1 is ethyl. In some embodiments, R1 is propyl. In some embodiments, R1 is butyl. In some embodiments, R1 is pentyl. In some embodiments, R1 is hexyl. In some embodiments, R1 is isopropyl. In some embodiments, R1 is isobutyl. In some embodiments, R1 is isopentyl. In some embodiments, R1 is isohexyl. In some embodiments, R1 is secbutyl. In some embodiments, R1 is secpentyl. In some embodiments, R1 is sechexyl. In some embodiments, R1 is tertbutyl.
[0099] In some embodiments, R is C 2~6 In some embodiments, R1 is C2 alkenyl. In some embodiments, R1 is C3 alkenyl. In some embodiments, R1 is C4 alkenyl. In some embodiments, R1 is C5 alkenyl. In some embodiments, R1 is C6 alkenyl.
[0100] In some embodiments, R is C 2~6 In some embodiments, R1 is C2 alkynyl. In some embodiments, R1 is C3 alkynyl. In some embodiments, R1 is C4 alkynyl. In some embodiments, R1 is C5 alkynyl. In some embodiments, R1 is C6 alkynyl.
[0101] In some embodiments, each R is H or C 1~6 It is alkyl.
[0102] In some embodiments, R4 is H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0103] In some embodiments, R4 is H.
[0104] In some embodiments, R4 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0105] In some embodiments, R4 is C 1~6 In some embodiments, R4 is alkyl. In some embodiments, R4 is methyl. In some embodiments, R4 is ethyl. In some embodiments, R4 is propyl. In some embodiments, R4 is butyl. In some embodiments, R4 is pentyl. In some embodiments, R4 is hexyl. In some embodiments, R4 is isopropyl. In some embodiments, R4 is isobutyl. In some embodiments, R4 is isopentyl. In some embodiments, R4 is isohexyl. In some embodiments, R4 is secbutyl. In some embodiments, R4 is secpentyl. In some embodiments, R4 is sechexyl. In some embodiments, R4 is tertbutyl.
[0106] In some embodiments, R4 is C 2~6 In some embodiments, R4 is C2 alkenyl. In some embodiments, R4 is C3 alkenyl. In some embodiments, R4 is C4 alkenyl. In some embodiments, R4 is C5 alkenyl. In some embodiments, R4 is C6 alkenyl.
[0107] In some embodiments, R4 is C 2~6 In some embodiments, R4 is C2 alkynyl. In some embodiments, R4 is C3 alkynyl. In some embodiments, R4 is C4 alkynyl. In some embodiments, R4 is C5 alkynyl. In some embodiments, R4 is C6 alkynyl.
[0108] In some embodiments, each R4 is H or C 1~6 It is alkyl.
[0109] In some embodiments, R2 and R3 are each independently selected from H, C2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2, where neither R2 nor R3 is H.
[0110] In some embodiments, R2 and R3 are each independently C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0111] In some embodiments, R2 and R3 are each independently -OC 1~6 Alkyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, or -C(O)NR 11 -S(O)2R 11 is.
[0112] In some embodiments, either R2 or R3 is not H.
[0113] In some embodiments, R2 is not H.
[0114] In some embodiments, R3 is not H.
[0115] In some embodiments, R2 is H, C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0116] In some embodiments, R2 is H.
[0117] In some embodiments, R2 is C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0118] In some embodiments, R2 is C 2~6 Alkenyl or C 2~6 It is alkynyl.
[0119] In some embodiments, R2 is C 2~6 In some embodiments, R2 is C2 alkenyl. In some embodiments, R2 is C3 alkenyl. In some embodiments, R2 is C4 alkenyl. In some embodiments, R2 is C5 alkenyl. In some embodiments, R2 is C6 alkenyl.
[0120] In some embodiments, R2 is C 2~6 In some embodiments, R2 is C2 alkynyl. In some embodiments, R2 is C3 alkynyl. In some embodiments, R2 is C4 alkynyl. In some embodiments, R2 is C5 alkynyl. In some embodiments, R2 is C6 alkynyl.
[0121] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0122] In some embodiments, R2 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 It is alkynyl.
[0123] In some embodiments, R2 is -OC 1~6In some embodiments, R2 is -O-methyl. In some embodiments, R2 is -O-ethyl. In some embodiments, R2 is -O-propyl. In some embodiments, R2 is -O-butyl. In some embodiments, R2 is -O-pentyl. In some embodiments, R2 is -O-hexyl. In some embodiments, R2 is -O-isopropyl. In some embodiments, R2 is -O-isobutyl. In some embodiments, R2 is -O-isopentyl. In some embodiments, R2 is -O-isohexyl. In some embodiments, R2 is -O-secbutyl. In some embodiments, R2 is -O-secpentyl. In some embodiments, R2 is -O-sechexyl. In some embodiments, R2 is -O-tertbutyl.
[0124] In some embodiments, R2 is -OC 2~6 In some embodiments, R2 is -O-C2 alkenyl. In some embodiments, R2 is -O-C3 alkenyl. In some embodiments, R2 is -O-C4 alkenyl. In some embodiments, R2 is -O-C5 alkenyl. In some embodiments, R2 is -O-C6 alkenyl.
[0125] In some embodiments, R2 is -OC 2~6 In some embodiments, R2 is -O-C2 alkynyl. In some embodiments, R2 is -O-C3 alkynyl. In some embodiments, R2 is -O-C4 alkynyl. In some embodiments, R2 is -O-C5 alkynyl. In some embodiments, R2 is -O-C6 alkynyl.
[0126] In some embodiments, R2 is -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR11 -S(O)2-N(R 11 )2.
[0127] In some embodiments, R2 is -C(O)R 11 , -C(O)OR 11 , or -C(O)N(R 11 )2.
[0128] In some embodiments, R2 is -C(O)R 11 In some embodiments, R2 is -C(O)OR 11 In some embodiments, R2 is —C(O)N(R 11 )2.
[0129] In some embodiments, R2 is -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0130] In some embodiments, R2 is -C(O)NR 11 -S(O)2R 11 In some embodiments, R2 is -C(O)NR 11 -S(O)2-OR 11 In some embodiments, R2 is -C(O)NR 11 -S(O)2-N(R 11 )2.
[0131] In some embodiments, R2 is -OC 1~6 Alkyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, or -C(O)NR 11 -S(O)2R 11 is.
[0132] In some embodiments, R3 is H, C 2~6 Alkenyl, C 2~6Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0133] In some embodiments, R3 is H.
[0134] In some embodiments, R3 is C 2~6 Alkenyl, C 2~6 Alkynyl, -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0135] In some embodiments, R3 is C 2~6 Alkenyl or C 2~6 It is alkynyl.
[0136] In some embodiments, R3 is C 2~6 In some embodiments, R3 is C2 alkenyl. In some embodiments, R3 is C3 alkenyl. In some embodiments, R3 is C4 alkenyl. In some embodiments, R3 is C5 alkenyl. In some embodiments, R3 is C6 alkenyl.
[0137] In some embodiments, R3 is C 2~6 In some embodiments, R3 is C2 alkynyl. In some embodiments, R3 is C3 alkynyl. In some embodiments, R3 is C4 alkynyl. In some embodiments, R3 is C5 alkynyl. In some embodiments, R3 is C6 alkynyl.
[0138] In some embodiments, R3 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, -OC 2~6 Alkynyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0139] In some embodiments, R3 is -OC 1~6 Alkyl, -OC 2~6 Alkenyl, or -OC 2~6 It is alkynyl.
[0140] In some embodiments, R3 is -OC 1~6In some embodiments, R3 is -O-methyl. In some embodiments, R3 is -O-ethyl. In some embodiments, R3 is -O-propyl. In some embodiments, R3 is -O-butyl. In some embodiments, R3 is -O-pentyl. In some embodiments, R3 is -O-hexyl. In some embodiments, R3 is -O-isopropyl. In some embodiments, R3 is -O-isobutyl. In some embodiments, R3 is -O-isopentyl. In some embodiments, R3 is -O-isohexyl. In some embodiments, R3 is -O-secbutyl. In some embodiments, R3 is -O-secpentyl. In some embodiments, R3 is -O-sechexyl. In some embodiments, R3 is -O-tertbutyl.
[0141] In some embodiments, R3 is -OC 2~6 In some embodiments, R3 is -O-C2 alkenyl. In some embodiments, R3 is -O-C3 alkenyl. In some embodiments, R3 is -O-C4 alkenyl. In some embodiments, R3 is -O-C5 alkenyl. In some embodiments, R3 is -O-C6 alkenyl.
[0142] In some embodiments, R3 is -OC 2~6 In some embodiments, R3 is -O-C2 alkynyl. In some embodiments, R3 is -O-C3 alkynyl. In some embodiments, R3 is -O-C4 alkynyl. In some embodiments, R3 is -O-C5 alkynyl. In some embodiments, R3 is -O-C6 alkynyl.
[0143] In some embodiments, R3 is -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR11 -S(O)2-N(R 11 )2.
[0144] In some embodiments, R3 is -C(O)R 11 , -C(O)OR 11 , or -C(O)N(R 11 )2.
[0145] In some embodiments, R3 is -C(O)R 11 In some embodiments, R3 is -C(O)OR 11 In some embodiments, R3 is —C(O)N(R 11 )2.
[0146] In some embodiments, R3 is -C(O)NR 11 -S(O)2R 11 , -C(O)NR 11 -S(O)2-OR 11 , or -C(O)NR 11 -S(O)2-N(R 11 )2.
[0147] In some embodiments, R3 is -C(O)NR 11 -S(O)2R 11 In some embodiments, R3 is -C(O)NR 11 -S(O)2-OR 11 In some embodiments, R3 is -C(O)NR 11 -S(O)2-N(R 11 )2.
[0148] In some embodiments, R3 is -OC 1~6 Alkyl, -C(O)R 11 , -C(O)OR 11 , -C(O)N(R 11 )2, or -C(O)NR 11 -S(O)2R 11 is.
[0149] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7.
[0150] In some embodiments, R5 and R6 are each independently C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7; or R5 and R6, together with the atoms to which they are attached, form a 4- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7.
[0151] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0152] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0153] In some embodiments, R5 and R6 are each independently H.
[0154] In some embodiments, R5 and R6 are each independently C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0155] In some embodiments, R5 and R6 are each independently C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0156] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0157] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0158] In some embodiments, R5 and R6 are each independently H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is substituted with one or more R7.
[0159] In some embodiments, R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is substituted with one or more R7.
[0160] In some embodiments, R5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0161] In some embodiments, R5 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0162] In some embodiments, R5 is H.
[0163] In some embodiments, R5 is C1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0164] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0165] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is optionally substituted with one or more R7.
[0166] In some embodiments, R5 is a C optionally substituted with one or more R7 1~6In some embodiments, R5 is alkyl. In some embodiments, R5 is methyl, optionally substituted with one or more R7. In some embodiments, R5 is ethyl, optionally substituted with one or more R7. In some embodiments, R5 is propyl, optionally substituted with one or more R7. In some embodiments, R5 is butyl, optionally substituted with one or more R7. In some embodiments, R5 is pentyl, optionally substituted with one or more R7. In some embodiments, R5 is hexyl, optionally substituted with one or more R7. In some embodiments, R5 is isopropyl, optionally substituted with one or more R7. In some embodiments, R5 is isobutyl, optionally substituted with one or more R7. In some embodiments, R5 is isopentyl, optionally substituted with one or more R7. In some embodiments, R5 is isohexyl, optionally substituted with one or more R7. In some embodiments, R5 is secbutyl, optionally substituted with one or more R7. In some embodiments, R5 is sec-pentyl, optionally substituted with one or more R7. In some embodiments, R5 is sec-hexyl, optionally substituted with one or more R7. In some embodiments, R5 is tert-butyl, optionally substituted with one or more R7.
[0167] In some embodiments, R5 is a C optionally substituted with one or more R7 2~6 In some embodiments, R5 is C2 alkenyl optionally substituted with one or more R7. In some embodiments, R5 is C3 alkenyl optionally substituted with one or more R7. In some embodiments, R5 is C4 alkenyl optionally substituted with one or more R7. In some embodiments, R5 is C5 alkenyl optionally substituted with one or more R7. In some embodiments, R5 is C6 alkenyl optionally substituted with one or more R7.
[0168] In some embodiments, R5 is a C optionally substituted with one or more R7 2~6 In some embodiments, R5 is C2 alkynyl optionally substituted with one or more R7. In some embodiments, R5 is C3 alkynyl optionally substituted with one or more R7. In some embodiments, R5 is C4 alkynyl optionally substituted with one or more R7. In some embodiments, R5 is C5 alkynyl optionally substituted with one or more R7. In some embodiments, R5 is C6 alkynyl optionally substituted with one or more R7.
[0169] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is substituted with one or more R7.
[0170] In some embodiments, R5 is a C substituted with one or more R7 1~6In some embodiments, R5 is alkyl. In some embodiments, R5 is methyl substituted with one or more R7. In some embodiments, R5 is ethyl substituted with one or more R7. In some embodiments, R5 is propyl substituted with one or more R7. In some embodiments, R5 is butyl substituted with one or more R7. In some embodiments, R5 is pentyl substituted with one or more R7. In some embodiments, R5 is hexyl substituted with one or more R7. In some embodiments, R5 is isopropyl substituted with one or more R7. In some embodiments, R5 is isobutyl substituted with one or more R7. In some embodiments, R5 is isopentyl substituted with one or more R7. In some embodiments, R5 is isohexyl substituted with one or more R7. In some embodiments, R5 is secbutyl substituted with one or more R7. In some embodiments, R5 is sec-pentyl substituted with one or more R7. In some embodiments, R5 is sec-hexyl substituted with one or more R7. In some embodiments, R5 is tert-butyl substituted with one or more R7.
[0171] In some embodiments, R5 is a C substituted with one or more R7 2~6 In some embodiments, R5 is C2 alkenyl substituted with one or more R7. In some embodiments, R5 is C3 alkenyl substituted with one or more R7. In some embodiments, R5 is C4 alkenyl substituted with one or more R7. In some embodiments, R5 is C5 alkenyl substituted with one or more R7. In some embodiments, R5 is C6 alkenyl substituted with one or more R7.
[0172] In some embodiments, R5 is a C substituted with one or more R7 2~6In some embodiments, R5 is a C2 alkynyl substituted with one or more R7. In some embodiments, R5 is a C3 alkynyl substituted with one or more R7. In some embodiments, R5 is a C4 alkynyl substituted with one or more R7. In some embodiments, R5 is a C5 alkynyl substituted with one or more R7. In some embodiments, R5 is a C6 alkynyl substituted with one or more R7.
[0173] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is substituted with one R7.
[0174] In some embodiments, R5 is C substituted with 1 R7 1~6 In some embodiments, R5 is alkyl. In some embodiments, R5 is methyl substituted with one R7. In some embodiments, R5 is ethyl substituted with one R7. In some embodiments, R5 is propyl substituted with one R7. In some embodiments, R5 is butyl substituted with one R7. In some embodiments, R5 is pentyl substituted with one R7. In some embodiments, R5 is hexyl substituted with one R7. In some embodiments, R5 is isopropyl substituted with one R7. In some embodiments, R5 is isobutyl substituted with one R7. In some embodiments, R5 is isopentyl substituted with one R7. In some embodiments, R5 is isohexyl substituted with one R7. In some embodiments, R5 is secbutyl substituted with one R7. In some embodiments, R5 is secpentyl substituted with one R7. In some embodiments, R5 is sechexyl substituted with 1 R7. In some embodiments, R5 is tertbutyl substituted with 1 R7.
[0175] In some embodiments, R5 is C substituted with 1 R72~6 In some embodiments, R5 is C2 alkenyl substituted with 1 R7. In some embodiments, R5 is C3 alkenyl substituted with 1 R7. In some embodiments, R5 is C4 alkenyl substituted with 1 R7. In some embodiments, R5 is C5 alkenyl substituted with 1 R7. In some embodiments, R5 is C6 alkenyl substituted with 1 R7.
[0176] In some embodiments, R5 is C substituted with 1 R7 2~6 In some embodiments, R5 is C2 alkynyl substituted with 1 R7. In some embodiments, R5 is C3 alkynyl substituted with 1 R7. In some embodiments, R5 is C4 alkynyl substituted with 1 R7. In some embodiments, R5 is C5 alkynyl substituted with 1 R7. In some embodiments, R5 is C6 alkynyl substituted with 1 R7.
[0177] In some embodiments, R5 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0178] In some embodiments, R5 is C 1~6 In some embodiments, R5 is alkyl. In some embodiments, R5 is methyl. In some embodiments, R5 is ethyl. In some embodiments, R5 is propyl. In some embodiments, R5 is butyl. In some embodiments, R5 is pentyl. In some embodiments, R5 is hexyl. In some embodiments, R5 is isopropyl. In some embodiments, R5 is isobutyl. In some embodiments, R5 is isopentyl. In some embodiments, R5 is isohexyl. In some embodiments, R5 is secbutyl. In some embodiments, R5 is secpentyl. In some embodiments, R5 is sechexyl. In some embodiments, R5 is tertbutyl.
[0179] In some embodiments, R5 is C 2~6 In some embodiments, R5 is C2 alkenyl. In some embodiments, R5 is C3 alkenyl. In some embodiments, R5 is C4 alkenyl. In some embodiments, R5 is C5 alkenyl. In some embodiments, R5 is C6 alkenyl.
[0180] In some embodiments, R5 is C 2~6 In some embodiments, R5 is C2 alkynyl. In some embodiments, R5 is C3 alkynyl. In some embodiments, R5 is C4 alkynyl. In some embodiments, R5 is C5 alkynyl. In some embodiments, R5 is C6 alkynyl.
[0181] In some embodiments, R5 is C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0182] In some embodiments, R5 is C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0183] In some embodiments, R5 is C 3~10 cycloalkyl or 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R7.
[0184] In some embodiments, R5 is C 3~10 cycloalkyl or a 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0185] In some embodiments, R5 is a C optionally substituted with one or more R7 3~10 It is cycloalkyl.
[0186] In some embodiments, R5 is a C3 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C4 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C5 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C6 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C7 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C8 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C9 cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C6 cycloalkyl optionally substituted with one or more R7. 10 It is cycloalkyl.
[0187] In some embodiments, R5 is a C3-C7 monocyclic cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R7. In some embodiments, R5 is a C9-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R7. 10 In some embodiments, R5 is a C9-C cycloalkyl optionally substituted with one or more R7. 10 In some embodiments, R5 is a C9-C cycloalkyl group optionally substituted with one or more R7.10 In some embodiments, R5 is a C8-C6 bicyclic partially saturated cycloalkyl optionally substituted with one or more R7. 10 It is a polycyclic cycloalkyl.
[0188] In some embodiments, R5 is a C substituted with one or more R7 3~10 It is cycloalkyl.
[0189] In some embodiments, R5 is a C3 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C4 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C5 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C6 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C7 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C8 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C9 cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C6 cycloalkyl substituted with one or more R7. 10 It is cycloalkyl.
[0190] In some embodiments, R5 is a C3-C7 monocyclic cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C3-C7 monocyclic saturated cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one or more R7. In some embodiments, R5 is a C9-C7 monocyclic partially saturated cycloalkyl substituted with one or more R7. 10 In some embodiments, R5 is a C9-C substituted with one or more R7. 10 In some embodiments, R5 is a C9-C substituted bicyclic saturated cycloalkyl. 10 In some embodiments, R5 is a C8-C substituted with one or more R7.10 It is a polycyclic cycloalkyl.
[0191] In some embodiments, R5 is C substituted with 1 R7 3~10 It is cycloalkyl.
[0192] In some embodiments, R5 is C3 cycloalkyl substituted with one R7. In some embodiments, R5 is C4 cycloalkyl substituted with one R7. In some embodiments, R5 is C5 cycloalkyl substituted with one R7. In some embodiments, R5 is C6 cycloalkyl substituted with one R7. In some embodiments, R5 is C7 cycloalkyl substituted with one R7. In some embodiments, R5 is C8 cycloalkyl substituted with one R7. In some embodiments, R5 is C9 cycloalkyl substituted with one R7. In some embodiments, R5 is C6 cycloalkyl substituted with one R7. In some embodiments, R5 is C7 cycloalkyl substituted with one R7. 10 It is cycloalkyl.
[0193] In some embodiments, R5 is a C3-C7 monocyclic cycloalkyl substituted with one R7. In some embodiments, R5 is a C3-C7 monocyclic saturated cycloalkyl substituted with one R7. In some embodiments, R5 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one R7. In some embodiments, R5 is a C9-C1 monocyclic partially saturated cycloalkyl substituted with one R7. 10 In some embodiments, R5 is a C9-C cycloalkyl substituted with one R7. 10 In some embodiments, R5 is a C9-C substituted with one R7. 10 In some embodiments, R5 is a C8-C substituted with one R7. 10 It is a polycyclic cycloalkyl.
[0194] In some embodiments, R5 is C 3~10 It is cycloalkyl.
[0195] In some embodiments, R5 is C3 cycloalkyl. In some embodiments, R5 is C4 cycloalkyl. In some embodiments, R5 is C5 cycloalkyl. In some embodiments, R5 is C6 cycloalkyl. In some embodiments, R5 is C7 cycloalkyl. In some embodiments, R5 is C8 cycloalkyl. In some embodiments, R5 is C9 cycloalkyl. In some embodiments, R5 is C 10 It is cycloalkyl.
[0196] In some embodiments, R5 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R5 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R5 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R5 is a C9-C 10 In some embodiments, R5 is a C9-C 10 In some embodiments, R5 is a C9-C 10 In some embodiments, R5 is a C8-C 10 It is a polycyclic cycloalkyl.
[0197] In some embodiments, R5 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0198] In some embodiments, R5 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0199] In some embodiments, R5 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0200] In some embodiments, R5 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0201] In some embodiments, R5 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0202] In some embodiments, R5 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0203] In some embodiments, R5 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0204] In some embodiments, R5 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0205] In some embodiments, R5 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered polycyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0206] In some embodiments, R5 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0207] In some embodiments, R5 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0208] In some embodiments, R5 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0209] In some embodiments, R5 is C 6~10 aryl, or a 5- to 13-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl is optionally substituted with one or more R7.
[0210] In some embodiments, R5 is C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0211] In some embodiments, R5 is a C optionally substituted with one or more R7 6~10 It is aryl.
[0212] In some embodiments, R5 is a C optionally substituted with one or more R7 6~8 In some embodiments, R5 is phenyl optionally substituted with one or more R7.
[0213] In some embodiments, R5 is a C substituted with one or more R7 6~8 In some embodiments, R5 is phenyl substituted with one or more R7.
[0214] In some embodiments, R5 is C substituted with 1 R7 6~8 In some embodiments, R5 is phenyl substituted with 1 R7.
[0215] In some embodiments, R5 is C 6~10 It is aryl.
[0216] In some embodiments, R5 is C 6~8 In some embodiments, R5 is phenyl.
[0217] In some embodiments, R5 is a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0218] In some embodiments, R5 is a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0219] In some embodiments, R5 is a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0220] In some embodiments, R5 is a 5- to 13-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0221] In some embodiments, R5 is a 9- to 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0222] In some embodiments, R5 is a 9-13 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0223] In some embodiments, R5 is a 9-13 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0224] In some embodiments, R5 is a 9- to 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0225] In some embodiments, R5 is a 9- to 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 9-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 10-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is an 11-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 12-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 is a 13-membered polycyclic heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0226] In some embodiments, R5 is a 9-13 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 9 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is an 11 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 12 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0227] In some embodiments, R5 is a 9-13 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 9 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is an 11 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 12 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0228] In some embodiments, R5 is a 9- to 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 9-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 10-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is an 11-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 12-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0229] In some embodiments, R5 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl, a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0230] In some embodiments, R5 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0231] In some embodiments, R5 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is substituted with one or more R7.
[0232] In some embodiments, R5 is cyclopropyl, piperidine, tetrahydropyran, morpholine, phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0233] In some embodiments, R5 is cyclopropyl, piperidine, tetrahydropyran, or morpholine.
[0234] In some embodiments, R5 is phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0235] In some embodiments, R5 is pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0236] In some embodiments, R5 is pyridine or pyrimidine.
[0237] In some embodiments, R5 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0238] In some embodiments, R5 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, or imidazole.
[0239] In some embodiments, R5 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0240] In some embodiments, R5 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, or benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole.
[0241] In some embodiments, R5 is 9H-carbazole.
[0242] In some embodiments, R6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0243] In some embodiments, R6 is H, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0244] In some embodiments, R6 is H.
[0245] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0246] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0247] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is optionally substituted with one or more R7.
[0248] In some embodiments, R6 is a C optionally substituted with one or more R7 1~6In some embodiments, R6 is alkyl. In some embodiments, R6 is methyl, optionally substituted with one or more R7. In some embodiments, R6 is ethyl, optionally substituted with one or more R7. In some embodiments, R6 is propyl, optionally substituted with one or more R7. In some embodiments, R6 is butyl, optionally substituted with one or more R7. In some embodiments, R6 is pentyl, optionally substituted with one or more R7. In some embodiments, R6 is hexyl, optionally substituted with one or more R7. In some embodiments, R6 is isopropyl, optionally substituted with one or more R7. In some embodiments, R6 is isobutyl, optionally substituted with one or more R7. In some embodiments, R6 is isopentyl, optionally substituted with one or more R7. In some embodiments, R6 is isohexyl, optionally substituted with one or more R7. In some embodiments, R6 is secbutyl, optionally substituted with one or more R7. In some embodiments, R6 is sec-pentyl, optionally substituted with one or more R7. In some embodiments, R6 is sec-hexyl, optionally substituted with one or more R7. In some embodiments, R6 is tert-butyl, optionally substituted with one or more R7.
[0249] In some embodiments, R6 is a C optionally substituted with one or more R7 2~6 In some embodiments, R6 is C2 alkenyl optionally substituted with one or more R7. In some embodiments, R6 is C3 alkenyl optionally substituted with one or more R7. In some embodiments, R6 is C4 alkenyl optionally substituted with one or more R7. In some embodiments, R6 is C5 alkenyl optionally substituted with one or more R7. In some embodiments, R6 is C6 alkenyl optionally substituted with one or more R7.
[0250] In some embodiments, R6 is a C optionally substituted with one or more R7 2~6 In some embodiments, R6 is C2 alkynyl optionally substituted with one or more R7. In some embodiments, R6 is C3 alkynyl optionally substituted with one or more R7. In some embodiments, R6 is C4 alkynyl optionally substituted with one or more R7. In some embodiments, R6 is C5 alkynyl optionally substituted with one or more R7. In some embodiments, R6 is C6 alkynyl optionally substituted with one or more R7.
[0251] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is substituted with one or more R7.
[0252] In some embodiments, R6 is a C substituted with one or more R7 1~6In some embodiments, R6 is alkyl. In some embodiments, R6 is methyl substituted with one or more R7. In some embodiments, R6 is ethyl substituted with one or more R7. In some embodiments, R6 is propyl substituted with one or more R7. In some embodiments, R6 is butyl substituted with one or more R7. In some embodiments, R6 is pentyl substituted with one or more R7. In some embodiments, R6 is hexyl substituted with one or more R7. In some embodiments, R6 is isopropyl substituted with one or more R7. In some embodiments, R6 is isobutyl substituted with one or more R7. In some embodiments, R6 is isopentyl substituted with one or more R7. In some embodiments, R6 is isohexyl substituted with one or more R7. In some embodiments, R6 is secbutyl substituted with one or more R7. In some embodiments, R6 is sec-pentyl substituted with one or more R7. In some embodiments, R6 is sec-hexyl substituted with one or more R7. In some embodiments, R6 is tert-butyl substituted with one or more R7.
[0253] In some embodiments, R6 is a C substituted with one or more R7 2~6 In some embodiments, R6 is C2 alkenyl substituted with one or more R7. In some embodiments, R6 is C3 alkenyl substituted with one or more R7. In some embodiments, R6 is C4 alkenyl substituted with one or more R7. In some embodiments, R6 is C5 alkenyl substituted with one or more R7. In some embodiments, R6 is C6 alkenyl substituted with one or more R7.
[0254] In some embodiments, R6 is a C substituted with one or more R7 2~6In some embodiments, R6 is a C2 alkynyl substituted with one or more R7. In some embodiments, R6 is a C3 alkynyl substituted with one or more R7. In some embodiments, R6 is a C4 alkynyl substituted with one or more R7. In some embodiments, R6 is a C5 alkynyl substituted with one or more R7. In some embodiments, R6 is a C6 alkynyl substituted with one or more R7.
[0255] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 Alkynyl, wherein said alkyl, alkenyl, or alkynyl is substituted with one R7.
[0256] In some embodiments, R6 is C substituted with 1 R7 1~6 In some embodiments, R6 is alkyl. In some embodiments, R6 is methyl substituted with one R7. In some embodiments, R6 is ethyl substituted with one R7. In some embodiments, R6 is propyl substituted with one R7. In some embodiments, R6 is butyl substituted with one R7. In some embodiments, R6 is pentyl substituted with one R7. In some embodiments, R6 is hexyl substituted with one R7. In some embodiments, R6 is isopropyl substituted with one R7. In some embodiments, R6 is isobutyl substituted with one R7. In some embodiments, R6 is isopentyl substituted with one R7. In some embodiments, R6 is isohexyl substituted with one R7. In some embodiments, R6 is secbutyl substituted with one R7. In some embodiments, R6 is secpentyl substituted with one R7. In some embodiments, R6 is sechexyl substituted with 1 R7. In some embodiments, R6 is tertbutyl substituted with 1 R7.
[0257] In some embodiments, R6 is C substituted with 1 R72~6 In some embodiments, R6 is C2 alkenyl substituted with 1 R7. In some embodiments, R6 is C3 alkenyl substituted with 1 R7. In some embodiments, R6 is C4 alkenyl substituted with 1 R7. In some embodiments, R6 is C5 alkenyl substituted with 1 R7. In some embodiments, R6 is C6 alkenyl substituted with 1 R7.
[0258] In some embodiments, R6 is C substituted with 1 R7 2~6 In some embodiments, R6 is a C2 alkynyl substituted with 1 R7. In some embodiments, R6 is a C3 alkynyl substituted with 1 R7. In some embodiments, R6 is a C4 alkynyl substituted with 1 R7. In some embodiments, R6 is a C5 alkynyl substituted with 1 R7. In some embodiments, R6 is a C6 alkynyl substituted with 1 R7.
[0259] In some embodiments, R6 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0260] In some embodiments, R6 is C 1~6 In some embodiments, R6 is alkyl. In some embodiments, R6 is methyl. In some embodiments, R6 is ethyl. In some embodiments, R6 is propyl. In some embodiments, R6 is butyl. In some embodiments, R6 is pentyl. In some embodiments, R6 is hexyl. In some embodiments, R6 is isopropyl. In some embodiments, R6 is isobutyl. In some embodiments, R6 is isopentyl. In some embodiments, R6 is isohexyl. In some embodiments, R6 is secbutyl. In some embodiments, R6 is secpentyl. In some embodiments, R6 is sechexyl. In some embodiments, R6 is tertbutyl.
[0261] In some embodiments, R6 is C 2~6 In some embodiments, R6 is C2 alkenyl. In some embodiments, R6 is C3 alkenyl. In some embodiments, R6 is C4 alkenyl. In some embodiments, R6 is C5 alkenyl. In some embodiments, R6 is C6 alkenyl.
[0262] In some embodiments, R6 is C 2~6 In some embodiments, R6 is C2 alkynyl. In some embodiments, R6 is C3 alkynyl. In some embodiments, R6 is C4 alkynyl. In some embodiments, R6 is C5 alkynyl. In some embodiments, R6 is C6 alkynyl.
[0263] In some embodiments, R6 is C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0264] In some embodiments, R6 is C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0265] In some embodiments, R6 is C 3~10 cycloalkyl or 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R7.
[0266] In some embodiments, R6 is C 3~10 cycloalkyl or a 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0267] In some embodiments, R6 is a C optionally substituted with one or more R7 3~10 It is cycloalkyl.
[0268] In some embodiments, R6 is a C3 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C4 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C5 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C6 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C7 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C8 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C9 cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C6 cycloalkyl optionally substituted with one or more R7. 10 It is cycloalkyl.
[0269] In some embodiments, R6 is a C3-C7 monocyclic cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R7. In some embodiments, R6 is a C9-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R7. 10 In some embodiments, R6 is a C9-C cycloalkyl optionally substituted with one or more R7. 10 In some embodiments, R6 is a C9-C cycloalkyl group optionally substituted with one or more R7.10 In some embodiments, R6 is a C8-C6 bicyclic partially saturated cycloalkyl optionally substituted with one or more R7. 10 It is a polycyclic cycloalkyl.
[0270] In some embodiments, R6 is a C substituted with one or more R7 3~10 It is cycloalkyl.
[0271] In some embodiments, R6 is a C3 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C4 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C5 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C6 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C7 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C8 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C9 cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C6 cycloalkyl substituted with one or more R7. 10 It is cycloalkyl.
[0272] In some embodiments, R6 is a C3-C7 monocyclic cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C3-C7 monocyclic saturated cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one or more R7. In some embodiments, R6 is a C9-C7 monocyclic partially saturated cycloalkyl substituted with one or more R7. 10 In some embodiments, R6 is a C9-C substituted with one or more R7. 10 In some embodiments, R6 is a C9-C substituted bicyclic saturated cycloalkyl. 10 In some embodiments, R6 is a C8-C substituted bicyclic partially saturated cycloalkyl.10 It is a polycyclic cycloalkyl.
[0273] In some embodiments, R6 is C substituted with 1 R7 3~10 It is cycloalkyl.
[0274] In some embodiments, R6 is a C3 cycloalkyl substituted with one R7. In some embodiments, R6 is a C4 cycloalkyl substituted with one R7. In some embodiments, R6 is a C5 cycloalkyl substituted with one R7. In some embodiments, R6 is a C6 cycloalkyl substituted with one R7. In some embodiments, R6 is a C7 cycloalkyl substituted with one R7. In some embodiments, R6 is a C8 cycloalkyl substituted with one R7. In some embodiments, R6 is a C9 cycloalkyl substituted with one R7. In some embodiments, R6 is a C6 cycloalkyl substituted with one R7. 10 It is cycloalkyl.
[0275] In some embodiments, R6 is a C3-C7 monocyclic cycloalkyl substituted with one R7. In some embodiments, R6 is a C3-C7 monocyclic saturated cycloalkyl substituted with one R7. In some embodiments, R6 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one R7. In some embodiments, R6 is a C9-C monocyclic partially saturated cycloalkyl substituted with one R7. 10 In some embodiments, R6 is a C9-C cycloalkyl substituted with one R7. 10 In some embodiments, R6 is a C9-C substituted with one R7. 10 In some embodiments, R6 is a C8-C substituted with one R7. 10 It is a polycyclic cycloalkyl.
[0276] In some embodiments, R6 is C 3~10 It is cycloalkyl.
[0277] In some embodiments, R6 is C3 cycloalkyl. In some embodiments, R6 is C4 cycloalkyl. In some embodiments, R6 is C5 cycloalkyl. In some embodiments, R6 is C6 cycloalkyl. In some embodiments, R6 is C7 cycloalkyl. In some embodiments, R6 is C8 cycloalkyl. In some embodiments, R6 is C9 cycloalkyl. In some embodiments, R6 is C 10 It is cycloalkyl.
[0278] In some embodiments, R6 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R6 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R6 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R6 is a C9-C 10 In some embodiments, R6 is a C9-C 10 In some embodiments, R6 is a C9-C 10 In some embodiments, R6 is a C8-C 10 It is a polycyclic cycloalkyl.
[0279] In some embodiments, R6 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0280] In some embodiments, R6 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0281] In some embodiments, R6 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0282] In some embodiments, R6 is a 3- to 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0283] In some embodiments, R6 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0284] In some embodiments, R6 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0285] In some embodiments, R6 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0286] In some embodiments, R6 is a 7- to 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 7-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 8-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered bicyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0287] In some embodiments, R6 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered polycyclic heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0288] In some embodiments, R6 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0289] In some embodiments, R6 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0290] In some embodiments, R6 is a 9- to 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered polycyclic heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0291] In some embodiments, R6 is C 6~10 aryl, or a 5- to 13-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl is optionally substituted with one or more R7.
[0292] In some embodiments, R6 is C 6~10 aryl or 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0293] In some embodiments, R6 is a C optionally substituted with one or more R7 6~10 It is aryl.
[0294] In some embodiments, R6 is a C optionally substituted with one or more R7 6~8 In some embodiments, R6 is phenyl optionally substituted with one or more R7.
[0295] In some embodiments, R6 is a C substituted with one or more R7 6~8 In some embodiments, R6 is phenyl substituted with one or more R7.
[0296] In some embodiments, R6 is C substituted with 1 R7 6~8 In some embodiments, R6 is phenyl substituted with 1 R7.
[0297] In some embodiments, R6 is C 6~10 It is aryl.
[0298] In some embodiments, R6 is C 6~8 In some embodiments, R6 is phenyl.
[0299] In some embodiments, R6 is a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0300] In some embodiments, R6 is a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0301] In some embodiments, R6 is a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0302] In some embodiments, R6 is a 5- to 13-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0303] In some embodiments, R6 is a 9- to 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered bicyclic heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0304] In some embodiments, R6 is a 9-13 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0305] In some embodiments, R6 is a 9-13 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12 membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0306] In some embodiments, R6 is a 9- to 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0307] In some embodiments, R6 is a 9- to 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 9-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 10-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is an 11-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 12-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R6 is a 13-membered polycyclic heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0308] In some embodiments, R6 is a 9-13 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 9 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is an 11 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 12 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R6 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0309] In some embodiments, R6 is a 9-13 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 9 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 10 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is an 11 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 12 membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R6 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0310] In some embodiments, R6 is a 9- to 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 9-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 10-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is an 11-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 12-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R6 is a 13-membered polycyclic heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0311] In some embodiments, R6 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10aryl, a 5- to 13-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, or —C(O)R7, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0312] In some embodiments, R6 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R7.
[0313] In some embodiments, R6 is H, C 1~6 Alkyl, C 3~10 cycloalkyl, 3- to 13-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-13 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is substituted with one or more R7.
[0314] In some embodiments, R6 is cyclopropyl, piperidine, tetrahydropyran, morpholine, phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0315] In some embodiments, R6 is cyclopropyl, piperidine, tetrahydropyran, or morpholine.
[0316] In some embodiments, R6 is phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0317] In some embodiments, R6 is pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0318] In some embodiments, R6 is pyridine or pyrimidine.
[0319] In some embodiments, R6 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0320] In some embodiments, R6 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, or imidazole.
[0321] In some embodiments, R6 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0322] In some embodiments, R6 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, or benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole.
[0323] In some embodiments, R6 is 9H-carbazole.
[0324] In some embodiments, R5 and R6, together with the atoms to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is optionally substituted with one or more R7.
[0325] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0326] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0327] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0328] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0329] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0330] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0331] In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0332] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0333] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0334] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0335] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0336] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0337] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0338] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0339] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0340] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0341] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R7.
[0342] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0343] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with one or more R7.
[0344] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atoms to which they are attached, form a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7. In some embodiments, R5 and R6, together with the atoms to which they are attached, form a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R7.
[0345] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0346] In some embodiments, R5 and R6, together with the atom to which they are attached, form a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R5 and R6, together with the atom to which they are attached, form a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0347] In some embodiments, R5 and R6 together with the atoms to which they are attached form a piperidine optionally substituted with one or more R7.
[0348] In some embodiments, R5 and R6 together with the atoms to which they are attached form a piperidine substituted with one or more R7.
[0349] In some embodiments, R5 and R6 together with the atom to which they are attached form a piperidine substituted with one R7.
[0350] In some embodiments, R5 and R6 together with the atom to which they are attached form a piperidine.
[0351] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroquinoline optionally substituted with one or more R7.
[0352] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroquinoline substituted with one or more R7.
[0353] In some embodiments, R5 and R6 together with the atom to which they are attached form a tetrahydroquinoline substituted with one R7.
[0354] In some embodiments, R5 and R6 together with the atoms to which they are attached form a tetrahydroquinoline.
[0355] In some embodiments, each R7 is independently oxo, halogen, -OH, -NH2, -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with.
[0356] In some embodiments, each R7 is independently oxo, halogen, -OH, -NH2, -CN, -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Alkoxy, -NH(C 1~6 alkyl), -N(C 1~6 alkyl)2, -O-(CH2) t -R8, -NH-(CH2) t -R8, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0357] In some embodiments, R7 is oxo, halogen, —OH, —NH2, —CN, —C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, -O-(CH2) t -R8, or -NH-(CH2) t -R8.
[0358] In some embodiments, R7 is oxo, halogen, -OH, -NH2, or -CN.
[0359] In some embodiments, R7 is oxo.
[0360] In some embodiments, R7 is halogen. In some embodiments, R7 is F, Cl, Br, or I. In some embodiments, R7 is F, Cl, or Br. In some embodiments, R7 is F. In some embodiments, R7 is Cl. In some embodiments, R7 is Br. In some embodiments, R7 is I.
[0361] In some embodiments, R7 is -OH. In some embodiments, R7 is -NH2. In some embodiments, R7 is -CN.
[0362] In some embodiments, R7 is -C(O)R 10 , -C(O)OR 10 , -C(O)N(R 10 )2, -O-(CH2) t -R8, or -NH-(CH2) t -R8.
[0363] In some embodiments, R7 is -C(O)R 10 In some embodiments, R7 is -C(O)OR 10 In some embodiments, R7 is —C(O)N(R 10 )2. In some embodiments, R7 is -O-(CH2) t In some embodiments, R7 is -NH-(CH2) t -R8.
[0364] In some embodiments, R7 is C 1~6 Alkoxy, -NH(C 1~6 alkyl), or -N(C 1~6 alkyl)2.
[0365] In some embodiments, R7 is C 1~6 In some embodiments, R7 is alkoxy. In some embodiments, R7 is methoxy. In some embodiments, R7 is ethoxy. In some embodiments, R7 is propoxy. In some embodiments, R7 is butoxy. In some embodiments, R7 is pentoxy. In some embodiments, R7 is hexoxy. In some embodiments, R7 is isopropoxy. In some embodiments, R7 is isobutoxy. In some embodiments, R7 is isopentoxy. In some embodiments, R7 is isohexoxy. In some embodiments, R7 is secbutoxy. In some embodiments, R7 is secpentoxy. In some embodiments, R7 is sechexoxy. In some embodiments, R7 is tertbutoxy.
[0366] In some embodiments, R7 is —NH(C 1~6 alkyl) or -N(C 1~6 In some embodiments, R7 is -NH(C 1~6 In some embodiments, R7 is -N(C alkyl). 1~6 alkyl)2.
[0367] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with.
[0368] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0369] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more R 10 may be substituted with.
[0370] In some embodiments, R7 is one or more R 10C optionally substituted with 1~3 In some embodiments, R7 is one or more R 10 In some embodiments, R7 is methyl optionally substituted with one or more R 10 In some embodiments, R7 is ethyl optionally substituted with one or more R 10 In some embodiments, R7 is propyl optionally substituted with one or more R 10 isopropyl which may be substituted with
[0371] In some embodiments, R7 is one or more R 10 C optionally substituted with 2~6 In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a C2 alkenyl optionally substituted with one or more R 10 In some embodiments, R7 is a C3 alkenyl optionally substituted with one or more R 10 In some embodiments, R7 is a C4 alkenyl optionally substituted with one or more R 10 In some embodiments, R7 is a C5 alkenyl optionally substituted with one or more R 10 and C6 alkenyl optionally substituted with.
[0372] In some embodiments, R7 is one or more R 10 C optionally substituted with 2~6 In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a C2 alkynyl optionally substituted with one or more R 10 In some embodiments, R7 is a C3 alkynyl optionally substituted with one or more R 10 In some embodiments, R7 is a C4 alkynyl optionally substituted with one or more R 10In some embodiments, R7 is a C5 alkynyl optionally substituted with one or more R 10 and C6 alkynyl optionally substituted with.
[0373] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more R 10 is replaced by .
[0374] In some embodiments, R7 is one or more R 10 C replaced with 1~3 In some embodiments, R7 is one or more R 10 In some embodiments, R7 is methyl substituted with one or more R 10 In some embodiments, R7 is ethyl substituted with one or more R 10 In some embodiments, R7 is propyl substituted with one or more R 10 isopropyl substituted with
[0375] In some embodiments, R7 is one or more R 10 C replaced with 2~6 In some embodiments, R7 is one or more R 10 In some embodiments, R is a C alkenyl substituted with one or more R 10 In some embodiments, R is a C alkenyl substituted with one or more R 10 In some embodiments, R7 is a C4 alkenyl substituted with one or more R 10 In some embodiments, R7 is a C5 alkenyl substituted with one or more R 10 and C6 alkenyl substituted with
[0376] In some embodiments, R7 is one or more R 10C replaced with 2~6 In some embodiments, R7 is one or more R 10 In some embodiments, R is a C alkynyl substituted with one or more R 10 In some embodiments, R is a C alkynyl substituted with one or more R 10 In some embodiments, R7 is a C4 alkynyl substituted with one or more R 10 In some embodiments, R7 is a C5 alkynyl substituted with one or more R 10 is a C6 alkynyl substituted with
[0377] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one R 10 is replaced by .
[0378] In some embodiments, R7 is one R 10 C replaced with 1~3 In some embodiments, R7 is an alkyl group. 10 In some embodiments, R7 is methyl substituted with one R 10 In some embodiments, R7 is ethyl substituted with one R 10 In some embodiments, R7 is propyl substituted with one R 10 isopropyl substituted with
[0379] In some embodiments, R7 is one R 10 C replaced with 2~6 In some embodiments, R7 is an alkenyl. 10 In some embodiments, R is a C alkenyl substituted with one R 10 In some embodiments, R is a C alkenyl substituted with one R 10 In some embodiments, R7 is a C4 alkenyl substituted with one R10 In some embodiments, R7 is a C5 alkenyl substituted with one R 10 and C6 alkenyl substituted with
[0380] In some embodiments, R7 is one R 10 C replaced with 2~6 In some embodiments, R7 is alkynyl. 10 In some embodiments, R7 is a C2 alkynyl substituted with one R 10 In some embodiments, R is a C alkynyl substituted with one R 10 In some embodiments, R is a C alkynyl substituted with one R 10 In some embodiments, R7 is a C5 alkynyl substituted with one R 10 is a C6 alkynyl substituted with
[0381] In some embodiments, R7 is C 1~3 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0382] In some embodiments, R7 is C 1~3 In some embodiments, R7 is alkyl. In some embodiments, R7 is methyl. In some embodiments, R7 is ethyl. In some embodiments, R7 is propyl. In some embodiments, R7 is isopropyl.
[0383] In some embodiments, R7 is C 2~6 In some embodiments, R7 is C2 alkenyl. In some embodiments, R7 is C3 alkenyl. In some embodiments, R7 is C4 alkenyl. In some embodiments, R7 is C5 alkenyl. In some embodiments, R7 is C6 alkenyl.
[0384] In some embodiments, R7 is C 2~6In some embodiments, R7 is C2 alkynyl. In some embodiments, R7 is C3 alkynyl. In some embodiments, R7 is C4 alkynyl. In some embodiments, R7 is C5 alkynyl. In some embodiments, R7 is C6 alkynyl.
[0385] In some embodiments, R7 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with.
[0386] In some embodiments, R7 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0387] In some embodiments, R7 is C 3~10 cycloalkyl or 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is selected from one or more R 10 may be substituted with.
[0388] In some embodiments, R7 is C 3~10 cycloalkyl, or a 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0389] In some embodiments, R7 is one or more R 10 C optionally substituted with 3~10 It is cycloalkyl.
[0390] In some embodiments, R7 is one or more R 10 In some embodiments, R is a C cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C4 cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C5 cycloalkyl optionally substituted with one or more R 10 In some embodiments, R is a C cycloalkyl optionally substituted with one or more R 10 In some embodiments, R is a C cycloalkyl optionally substituted with one or more R 10 In some embodiments, R is a C cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C9 cycloalkyl optionally substituted with one or more R 10 C optionally substituted with 10 It is cycloalkyl.
[0391] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R 10 C9 to C optionally substituted 10 In some embodiments, R7 is a bicyclic cycloalkyl. In some embodiments, R7 is one or more R 10 C9 to C optionally substituted 10 In some embodiments, R7 is a bicyclic saturated cycloalkyl. 10 C9 to C optionally substituted 10In some embodiments, R7 is a bicyclic partially saturated cycloalkyl. 10 C8 to C optionally substituted 10 It is a polycyclic cycloalkyl.
[0392] In some embodiments, R7 is one or more R 10 C replaced with 3~10 It is cycloalkyl.
[0393] In some embodiments, R7 is one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 In some embodiments, R is a C cycloalkyl substituted with one or more R 10 C replaced with 10 It is cycloalkyl.
[0394] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic cycloalkyl substituted with one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic saturated cycloalkyl substituted with one or more R 10 In some embodiments, R7 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one or more R 10 C9~C substituted with 10In some embodiments, R7 is a bicyclic cycloalkyl. In some embodiments, R7 is one or more R 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic saturated cycloalkyl. 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic partially saturated cycloalkyl. 10 C8~C substituted with 10 It is a polycyclic cycloalkyl.
[0395] In some embodiments, R7 is one R 10 C replaced with 3~10 It is cycloalkyl.
[0396] In some embodiments, R7 is one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 In some embodiments, R is a C cycloalkyl substituted with one R 10 C replaced with 10 It is cycloalkyl.
[0397] In some embodiments, R7 is one R 10 In some embodiments, R7 is a C3-C7 monocyclic cycloalkyl substituted with one R 10 In some embodiments, R7 is a C3-C7 monocyclic saturated cycloalkyl substituted with one R 10In some embodiments, R7 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one R 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic cycloalkyl. 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic saturated cycloalkyl. 10 C9~C substituted with 10 In some embodiments, R7 is a bicyclic partially saturated cycloalkyl. 10 C8~C substituted with 10 It is a polycyclic cycloalkyl.
[0398] In some embodiments, R7 is C 3~10 It is cycloalkyl.
[0399] In some embodiments, R7 is C3 cycloalkyl. In some embodiments, R7 is C4 cycloalkyl. In some embodiments, R7 is C5 cycloalkyl. In some embodiments, R7 is C6 cycloalkyl. In some embodiments, R7 is C7 cycloalkyl. In some embodiments, R7 is C8 cycloalkyl. In some embodiments, R7 is C9 cycloalkyl. In some embodiments, R7 is C 10 It is cycloalkyl.
[0400] In some embodiments, R7 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R7 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R7 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R7 is a C9-C 10 In some embodiments, R7 is a C9-C 10 In some embodiments, R7 is a C9-C 10 In some embodiments, R7 is a C8-C 10 It is a polycyclic cycloalkyl.
[0401] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 3-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 4-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 5-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 6-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 and 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with
[0402] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10In some embodiments, R7 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 and a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with
[0403] In some embodiments, R7 is one R 10 In some embodiments, R7 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 4-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with one R 10In some embodiments, R7 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 and a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with
[0404] In some embodiments, R7 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0405] In some embodiments, R7 is C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl is selected from one or more R 10 may be substituted with.
[0406] In some embodiments, R7 is C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0407] In some embodiments, R7 is one or more R 10 C optionally substituted with 6~10 It is aryl.
[0408] In some embodiments, R7 is one or more R 10 C optionally substituted with 6~8 In some embodiments, R7 is one or more R 10 and phenyl optionally substituted with .
[0409] In some embodiments, R7 is one or more R 10 C replaced with 6~8 In some embodiments, R7 is one or more R 10 is a phenyl substituted with
[0410] In some embodiments, R7 is one R 10 C replaced with 6~8 In some embodiments, R7 is aryl. 10 is a phenyl substituted with
[0411] In some embodiments, R7 is C 6~10 It is aryl.
[0412] In some embodiments, R7 is C 6~8In some embodiments, R7 is phenyl.
[0413] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 In some embodiments, R7 is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with one or more R 10 and 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, optionally substituted with
[0414] In some embodiments, R7 is one or more R 10 In some embodiments, R7 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10In some embodiments, R7 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 In some embodiments, R7 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R 10 and 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with
[0415] In some embodiments, R7 is one R 10 In some embodiments, R7 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 In some embodiments, R7 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R 10 and 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S, substituted with
[0416] In some embodiments, R7 is a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R7 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0417] In some embodiments, R7 is cyclopropyl, piperidine, tetrahydropyran, morpholine, phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0418] In some embodiments, R7 is cyclopropyl, piperidine, tetrahydropyran, or morpholine.
[0419] In some embodiments, R7 is phenyl, pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0420] In some embodiments, R7 is pyridine, pyrimidine, tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0421] In some embodiments, R7 is pyridine or pyrimidine.
[0422] In some embodiments, R7 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0423] In some embodiments, R7 is tetrazole, triazole, pyrazole, thiazole, oxazole, furan, pyrrole, isoxazole, or imidazole.
[0424] In some embodiments, R7 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole, or 9H-carbazole.
[0425] In some embodiments, R7 is 1,3-dihydro-2H-benzo[d]imidazol-2-one, indoline, indole, 2,3-dihydrobenzofuran, 1H-benzo[d][1,2,3]triazole, 1H-indazole, imidazo[1,2-a]pyrazine, naphthalene, quinoline, 2,3-dihydrobenzo[b][1,4]dioxine, or benzo[d]oxazol-2(3H)-one, benzo[d]isoxazole.
[0426] In some embodiments, R7 is 9H-carbazole.
[0427] In some embodiments, R7 is oxo, halogen, —OH, —NH2, —CN, —C(O)R 10 , C 1~6 Alkyl, C 2~6 Alkynyl, -O-(CH2) t -R8, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkynyl, aryl, or heteroaryl is selected from one or more R 10 may be substituted with.
[0428] In some embodiments, R7 is oxo, halogen, —OH, —NH2, —CN, —C(O)R 10 , C 1~6 Alkyl, C 2~6 Alkynyl, -O-(CH2) t -R8, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkyl, alkynyl, aryl, or heteroaryl is selected from one or more R 10 is replaced by .
[0429] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9.
[0430] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl), C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0431] In some embodiments, R8 is —OH, C1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, or -S(C 1~6 alkyl), wherein the alkoxy or alkyl is optionally substituted with one or more R9.
[0432] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, or -S(C 1~6 alkyl), wherein the alkoxy or alkyl is substituted with one or more R9.
[0433] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, or -S(C 1~6 alkyl), wherein the alkoxy or alkyl is substituted with one R9.
[0434] In some embodiments, R8 is a C optionally substituted with one or more R9 1~6 It is an alkoxy.
[0435] In some embodiments, R8 is C 1~6 Alkoxy-OH, wherein the alkoxy is optionally substituted with one or more R9.
[0436] In some embodiments, R8 is C substituted with one or more R9 1~6 It is an alkoxy.
[0437] In some embodiments, R8 is C 1~6Alkoxy-OH, wherein the alkoxy is substituted with one or more R9.
[0438] In some embodiments, R8 is C substituted with 1 R9 1~6 It is an alkoxy.
[0439] In some embodiments, R8 is C 1~6 Alkoxy-OH, wherein the alkoxy is substituted with one R9.
[0440] In some embodiments, R8 is —NH(C 1~6 alkyl), wherein the alkyl is optionally substituted with one or more R9.
[0441] In some embodiments, R8 is —N(C 1~6 alkyl)2, wherein the alkyl is optionally substituted with one or more R9.
[0442] In some embodiments, R8 is —NH(C 1~6 alkyl), wherein the alkyl is substituted with one or more R9.
[0443] In some embodiments, R8 is —N(C 1~6 alkyl)2, wherein the alkyl is substituted with one or more R9.
[0444] In some embodiments, R8 is —NH(C 1~6 alkyl), wherein the alkyl is substituted with one R9.
[0445] In some embodiments, R8 is —N(C 1~6 alkyl)2, wherein the alkyl is substituted with one R9.
[0446] In some embodiments, R8 is -S(C 1~6 alkyl), wherein the alkyl is optionally substituted with one or more R9.
[0447] In some embodiments, R8 is -S(C 1~6 alkyl), wherein the alkyl is substituted with one or more R9.
[0448] In some embodiments, R8 is -S(C 1~6 alkyl), wherein the alkyl is substituted with one R9.
[0449] In some embodiments, R8 is —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -NH(C 1~6 alkyl), -N(C 1~6 alkyl), -SH, -S(C 1~6 alkyl).
[0450] In some embodiments, R8 is —OH, C 1~6 Alkoxy, or C 1~6 It is alkoxy-OH.
[0451] In some embodiments, R8 is -OH.
[0452] In some embodiments, R8 is C 1~6 In some embodiments, R is alkoxy. In some embodiments, R is methoxy. In some embodiments, R is ethoxy. In some embodiments, R is propoxy. In some embodiments, R is butoxy. In some embodiments, R is pentoxy. In some embodiments, R is hexoxy. In some embodiments, R is isopropoxy. In some embodiments, R is isobutoxy. In some embodiments, R is isopentoxy. In some embodiments, R is isohexoxy. In some embodiments, R is secbutoxy. In some embodiments, R is secpentoxy. In some embodiments, R is sechexoxy. In some embodiments, R is tertbutoxy.
[0453] In some embodiments, R8 is C1~6 In some embodiments, R is alkoxy-OH. In some embodiments, R is methoxy-OH. In some embodiments, R is ethoxy-OH. In some embodiments, R is propoxy-OH. In some embodiments, R is butoxy-OH. In some embodiments, R is pentoxy-OH. In some embodiments, R is hexoxy-OH. In some embodiments, R is isopropoxy-OH. In some embodiments, R is isobutoxy-OH. In some embodiments, R is isopentoxy-OH. In some embodiments, R is isohexoxy-OH. In some embodiments, R is sec-butoxy-OH. In some embodiments, R is sec-pentoxy-OH. In some embodiments, R is sec-hexoxy-OH. In some embodiments, R is tert-butoxy-OH.
[0454] In some embodiments, R is —NH, —NH(C 1~6 alkyl), or -N(C 1~6 alkyl)2.
[0455] In some embodiments, R8 is -NH2.
[0456] In some embodiments, R8 is —NH(C 1~6In some embodiments, R is -NH(methyl). In some embodiments, R is -NH(ethyl). In some embodiments, R is -NH(propyl). In some embodiments, R is -NH(butyl). In some embodiments, R is -NH(pentyl). In some embodiments, R is -NH(hexyl). In some embodiments, R is -NH(isopropyl). In some embodiments, R is -NH(isobutyl). In some embodiments, R is -NH(isopentyl). In some embodiments, R is -NH(isohexyl). In some embodiments, R is -NH(secbutyl). In some embodiments, R is -NH(secpentyl). In some embodiments, R is -NH(sechexyl). In some embodiments, R is -NH(tertbutyl).
[0457] In some embodiments, R8 is —N(C 1~6 In some embodiments, R is -N(methyl) . In some embodiments, R is -N(ethyl) . In some embodiments, R is -N(propyl) . In some embodiments, R is -N(butyl) . In some embodiments, R is -N(pentyl) . In some embodiments, R is -N(hexyl) . In some embodiments, R is -N(isopropyl) . In some embodiments, R is -N(isobutyl) . In some embodiments, R is -N(isopentyl) . In some embodiments, R is -N(isohexyl) . In some embodiments, R is -N(secbutyl) . In some embodiments, R is -N(secpentyl) . In some embodiments, R is -N(sechexyl) . In some embodiments, R is -N(tertbutyl) .
[0458] In some embodiments, R8 is -SH or -S(C 1~6 alkyl).
[0459] In some embodiments, R8 is -SH.
[0460] In some embodiments, R8 is -S(C 1~6 alkyl).
[0461] In some embodiments, R8 is -S(methyl). In some embodiments, R8 is -S(ethyl). In some embodiments, R8 is -S(propyl). In some embodiments, R8 is -S(butyl). In some embodiments, R8 is -S(pentyl). In some embodiments, R8 is -S(hexyl). In some embodiments, R8 is -S(isopropyl). In some embodiments, R8 is -S(isobutyl). In some embodiments, R8 is -S(isopentyl). In some embodiments, R8 is -S(isohexyl). In some embodiments, R8 is -S(secbutyl). In some embodiments, R8 is -S(secpentyl). In some embodiments, R8 is -S(sechexyl). In some embodiments, R8 is -S(tertbutyl).
[0462] In some embodiments, R8 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more R9.
[0463] In some embodiments, R8 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0464] In some embodiments, R8 is C 3~10cycloalkyl or 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R9.
[0465] In some embodiments, R8 is C 3~10 cycloalkyl, or a 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0466] In some embodiments, R8 is a C optionally substituted with one or more R9 3~10 It is cycloalkyl.
[0467] In some embodiments, R8 is a C3 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C4 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C5 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C6 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C7 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C8 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C9 cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C6 cycloalkyl optionally substituted with one or more R9. 10 It is cycloalkyl.
[0468] In some embodiments, R8 is a C3-C7 monocyclic cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C3-C7 monocyclic saturated cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C3-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R9. In some embodiments, R8 is a C9-C7 monocyclic partially saturated cycloalkyl optionally substituted with one or more R9.10 In some embodiments, R is a C-C alkyl group optionally substituted with one or more R. 10 In some embodiments, R8 is a C9-C10 alkyl group optionally substituted with one or more R9. 10 In some embodiments, R is a C-C bicyclic partially saturated cycloalkyl optionally substituted with one or more R. 10 It is a polycyclic cycloalkyl.
[0469] In some embodiments, R8 is C substituted with one or more R9 3~10 It is cycloalkyl.
[0470] In some embodiments, R8 is a C3 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C4 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C5 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C6 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C7 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C8 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C9 cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C6 cycloalkyl substituted with one or more R9. 10 It is cycloalkyl.
[0471] In some embodiments, R8 is a C3-C7 monocyclic cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C3-C7 monocyclic saturated cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one or more R9. In some embodiments, R8 is a C9-C7 monocyclic partially saturated cycloalkyl substituted with one or more R9. 10In some embodiments, R is a C-C alkyl group substituted with one or more R. 10 In some embodiments, R is a C-C alkyl group substituted with one or more R. 10 In some embodiments, R is a C-C bicyclic partially saturated cycloalkyl substituted with one or more R. 10 It is a polycyclic cycloalkyl.
[0472] In some embodiments, R8 is C substituted with 1 R9 3~10 It is cycloalkyl.
[0473] In some embodiments, R8 is a C3 cycloalkyl substituted with one R9. In some embodiments, R8 is a C4 cycloalkyl substituted with one R9. In some embodiments, R8 is a C5 cycloalkyl substituted with one R9. In some embodiments, R8 is a C6 cycloalkyl substituted with one R9. In some embodiments, R8 is a C7 cycloalkyl substituted with one R9. In some embodiments, R8 is a C8 cycloalkyl substituted with one R9. In some embodiments, R8 is a C9 cycloalkyl substituted with one R9. In some embodiments, R8 is a C6 cycloalkyl substituted with one R9. In some embodiments, R8 is a C7 cycloalkyl substituted with one R9. In some embodiments, R8 is a C8 cycloalkyl substituted with one R9. In some embodiments, R8 is a C9 cycloalkyl substituted with one R9. In some embodiments, R8 is a C8 cycloalkyl substituted with one R9. 10 It is cycloalkyl.
[0474] In some embodiments, R8 is a C3-C7 monocyclic cycloalkyl substituted with one R9. In some embodiments, R8 is a C3-C7 monocyclic saturated cycloalkyl substituted with one R9. In some embodiments, R8 is a C3-C7 monocyclic partially saturated cycloalkyl substituted with one R9. In some embodiments, R8 is a C9-C7 monocyclic partially saturated cycloalkyl substituted with one R9. 10 In some embodiments, R is a C-C substituted with one R. 10 In some embodiments, R8 is a C9-C substituted with one R9. 10In some embodiments, R is a C-C bicyclic partially saturated cycloalkyl substituted with one R. 10 It is a polycyclic cycloalkyl.
[0475] In some embodiments, R8 is C 3~10 It is cycloalkyl.
[0476] In some embodiments, R8 is C3 cycloalkyl. In some embodiments, R8 is C4 cycloalkyl. In some embodiments, R8 is C5 cycloalkyl. In some embodiments, R8 is C6 cycloalkyl. In some embodiments, R8 is C7 cycloalkyl. In some embodiments, R8 is C8 cycloalkyl. In some embodiments, R8 is C9 cycloalkyl. In some embodiments, R8 is C 10 It is cycloalkyl.
[0477] In some embodiments, R8 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R8 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R8 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R8 is a C9-C 10 In some embodiments, R is a C-C 10 In some embodiments, R is a C-C bicyclic saturated cycloalkyl. 10 In some embodiments, R is a C-C bicyclic partially saturated cycloalkyl. 10 It is a polycyclic cycloalkyl.
[0478] In some embodiments, R8 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9.
[0479] In some embodiments, R8 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9.
[0480] In some embodiments, R8 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with 1 R9. In some embodiments, R8 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with 1 R9. In some embodiments, R8 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, substituted with 1 R9.
[0481] In some embodiments, R8 is a 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 3-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 4-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 5-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 6-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 7-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is an 8-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 9-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S.
[0482] In some embodiments, R8 is C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl is optionally substituted with one or more R9.
[0483] In some embodiments, R8 is C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0484] In some embodiments, R8 is a C optionally substituted with one or more R9 6~10 It is aryl.
[0485] In some embodiments, R8 is a C optionally substituted with one or more R9 6~8In some embodiments, R8 is phenyl optionally substituted with one or more R9.
[0486] In some embodiments, R8 is C substituted with one or more R9 6~8 In some embodiments, R8 is phenyl substituted with one or more R9.
[0487] In some embodiments, R8 is C substituted with 1 R9 6~8 In some embodiments, R8 is phenyl substituted with 1 R9.
[0488] In some embodiments, R8 is C 6~10 It is aryl.
[0489] In some embodiments, R8 is C 6~8 In some embodiments, R8 is phenyl.
[0490] In some embodiments, R8 is a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9. In some embodiments, R8 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, optionally substituted with one or more R9.
[0491] In some embodiments, R8 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9. In some embodiments, R8 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one or more R9.
[0492] In some embodiments, R8 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with one R9. In some embodiments, R8 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, substituted with 1 R9.
[0493] In some embodiments, R8 is a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is an 8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R8 is a 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0494] In some embodiments, R8 is H, —OH, C 1~6 Alkoxy, C 1~6Alkoxy-OH, -NH2, -N(C 1~6 alkyl)2, -S(C 1~6 alkyl), 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, heterocyclyl, or heteroaryl is optionally substituted with one or more R9.
[0495] In some embodiments, R8 is H, —OH, C 1~6 Alkoxy, C 1~6 Alkoxy-OH, -NH2, -N(C 1~6 alkyl)2, -S(C 1~6 alkyl), 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the alkoxy, alkyl, heterocyclyl, or heteroaryl is substituted with one or more R9.
[0496] In some embodiments, each R9 is independently —(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein the heteroaryl or aryl may be optionally substituted with one or more halogen, —CN, —OH, or —NH 2 .
[0497] In some embodiments, R9 is —(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl).
[0498] In some embodiments, R9 is —(CH2) u-(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is optionally substituted with one or more halogen, -CN, -OH, or -NH.
[0499] In some embodiments, R9 is —(CH2) u In some embodiments, R is -(5-membered heteroaryl), wherein the heteroaryl is optionally substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(6-membered heteroaryl), wherein the heteroaryl is optionally substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(7-membered heteroaryl), wherein the heteroaryl is optionally substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(8-membered heteroaryl), wherein the heteroaryl is optionally substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(9-membered heteroaryl), wherein the heteroaryl is optionally substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u -(10-membered heteroaryl), wherein the heteroaryl is optionally substituted with one or more halogen, -CN, -OH, or -NH2.
[0500] In some embodiments, R9 is —(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one or more halogen, -CN, -OH, or -NH.
[0501] In some embodiments, R9 is —(CH2) uIn some embodiments, R is -(5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one or more halogens, -CN, -OH, or -NH. In some embodiments, R is -(CH). u -(10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one or more halogen, -CN, -OH, or -NH.
[0502] In some embodiments, R9 is —(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one halogen, -CN, -OH, or -NH.
[0503] In some embodiments, R9 is —(CH2) uIn some embodiments, R is -(5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one halogen, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one halogen, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one halogen, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one halogen, -CN, -OH, or -NH. In some embodiments, R is -(CH). u In some embodiments, R is -(9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one halogen, -CN, -OH, or -NH. In some embodiments, R is -(CH). u -(10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S), wherein the heteroaryl is substituted with one halogen, -CN, -OH, or -NH2.
[0504] In some embodiments, R9 is —(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S).
[0505] In some embodiments, R9 is —(CH2) u In some embodiments, R is -(5-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R is -(CH). uIn some embodiments, R is -(6-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R is -(CH). u In some embodiments, R is -(7-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R is -(CH) u In some embodiments, R is -(8-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R is -(CH). u -(9-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S). In some embodiments, R9 is -(CH2) u -(10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S).
[0506] In some embodiments, R9 is —(CH2) u -(C 6~10 In some embodiments, R is -(CH) u -(C 6~8 In some embodiments, R is -(CH) u -(phenyl), wherein the phenyl is optionally substituted with one or more halogens, -CN, -OH, or -NH2.
[0507] In some embodiments, R9 is —(CH2) u -(C 6~10 In some embodiments, R is -(CH) u -(C 6~8 In some embodiments, R is -(CH) u-(phenyl), wherein the phenyl is substituted with one or more halogen, -CN, -OH, or -NH2.
[0508] In some embodiments, R9 is —(CH2) u -(C 6~10 In some embodiments, R is -(CH) u -(C 6~8 In some embodiments, R is -(CH) u -(phenyl), wherein the phenyl is substituted with one halogen, -CN, -OH, or -NH2.
[0509] In some embodiments, R9 is —(CH2) u -(C 6~10 In some embodiments, R is —(CH) u -(C 6~8 In some embodiments, R is —(CH) u -(phenyl).
[0510] In some embodiments, R9 is —(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein said heteroaryl or aryl may be optionally substituted with one or more halogen or —OH.
[0511] In some embodiments, R9 is —(CH2) u -(5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S) or -(CH2) u -(C 6~10 aryl), wherein the heteroaryl or aryl is substituted with one or more halogen or —OH.
[0512] In some embodiments, each R 10 are independently halogen, -OH, -NH2, -CN, C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C 1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0513] In some embodiments, R 10 is a halogen, -OH, -NH2, or -CN.
[0514] In some embodiments, R 10 is a halogen.
[0515] In some embodiments, R 10 is F, Cl, Br, or I. In some embodiments, R 10 is F, Cl, or Br.
[0516] In some embodiments, R 10 is F. In some embodiments, R 10 is Cl. In some embodiments, R 10 is Br. In some embodiments, R 10 is I.
[0517] In some embodiments, R 10 is —OH. In some embodiments, R 10 is -NH2. In some embodiments, R 10 is -CN.
[0518] In some embodiments, R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, C1~6 Haloalkyl, C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0519] In some embodiments, R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 Alkynyl, or C 1~6 It is haloalkyl.
[0520] In some embodiments, R 10 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 It is alkynyl.
[0521] In some embodiments, R 10 is C 1~6 In some embodiments, R 10 is methyl. In some embodiments, R 10 is ethyl. In some embodiments, R 10 is propyl. In some embodiments, R 10 is butyl. In some embodiments, R 10 is pentyl. In some embodiments, R 10 is hexyl. In some embodiments, R 10 is isopropyl. In some embodiments, R 10 is isobutyl. In some embodiments, R 10 is isopentyl. In some embodiments, R 10 is isohexyl. In some embodiments, R 10 is sec butyl. In some embodiments, R 10 is sec pentyl. In some embodiments, R 10 is sec hexyl. In some embodiments, R 10 is tert butyl.
[0522] In some embodiments, R 10 is C 2~6 In some embodiments, R is alkenyl. 10 is C alkenyl. In some embodiments, R 10 is C alkenyl. In some embodiments, R 10 is C4 alkenyl. In some embodiments, R 10 is C5 alkenyl. In some embodiments, R 10 is a C6 alkenyl.
[0523] In some embodiments, R 10 is C 2~6 In some embodiments, R is alkynyl. 10 is C alkynyl. In some embodiments, R 10 is C alkynyl. In some embodiments, R 10 is C4 alkynyl. In some embodiments, R 10 is C5 alkynyl. In some embodiments, R 10 is a C6 alkynyl.
[0524] In some embodiments, R 10 is C 1~6 In some embodiments, R 10 is halomethyl. In some embodiments, R 10 is haloethyl. In some embodiments, R 10 is halopropyl. In some embodiments, R 10 is halobutyl. In some embodiments, R 10 is halopentyl. In some embodiments, R 10 is halohexyl.
[0525] In some embodiments, R 10 is C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0526] In some embodiments, R 10 is C 3~10 cycloalkyl, or a 3- to 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0527] In some embodiments, R 10 is C 3~10 It is cycloalkyl.
[0528] In some embodiments, R 10 is C cycloalkyl. In some embodiments, R 10 is C4 cycloalkyl. In some embodiments, R 10 is C5 cycloalkyl. In some embodiments, R 10 is C6 cycloalkyl. In some embodiments, R 10 is C7 cycloalkyl. In some embodiments, R 10 is C cycloalkyl. In some embodiments, R 10 is C cycloalkyl. In some embodiments, R 10 is C 10 It is cycloalkyl.
[0529] In some embodiments, R 10 is a C3-C7 monocyclic cycloalkyl. In some embodiments, R 10 is a C3-C7 monocyclic saturated cycloalkyl. In some embodiments, R 10 is a C3-C7 monocyclic partially saturated cycloalkyl. In some embodiments, R 10 is C9~C 10 In some embodiments, R is a bicyclic cycloalkyl. 10 is C9~C 10 In some embodiments, R is a bicyclic saturated cycloalkyl. 10 is C9~C 10 In some embodiments, R is a bicyclic partially saturated cycloalkyl.10 is C8~C 10 It is a polycyclic cycloalkyl.
[0530] In some embodiments, R 10 is a 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 3-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 4-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 5-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 6-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 7-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is an 8-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 9-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 10-membered heterocyclyl containing 1 to 4 heteroatoms selected from N, O, and S.
[0531] In some embodiments, R 10 is C 6~10 aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0532] In some embodiments, R 10 is C 6~10 It is aryl.
[0533] In some embodiments, R 10 is C 6~8In some embodiments, R 10 is phenyl.
[0534] In some embodiments, R 10 is a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 5-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 6-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 7-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is an 8-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 9-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S. In some embodiments, R 10 is a 10-membered heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S.
[0535] In some embodiments, R 10 is C 1~6 Alkyl, C 1~6 haloalkyl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S.
[0536] In some embodiments, each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 optionally substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2; 2 R's 11 together with the atom to which they are attached form a 4- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, or a 5- to 10-membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the heterocyclyl or heteroaryl is selected from one or more C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, halogen, -CN, -OH, or -NH2.
[0537] In some embodiments, each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2.
[0538] In some embodiments, each R 11 are independently H, C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 It may be substituted with aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O and S.
[0539] In some embodiments, R 11 is H.
[0540] In some embodiments, R 11 is C 1~6 Alkyl, C 2~6 Alkenyl, or C 2~6 alkynyl, wherein the alkyl, alkenyl, or alkynyl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2.
[0541] In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C optionally substituted with aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 1~6 alkyl, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 methyl, optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or ethyl, optionally substituted with a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 propyl, optionally substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 butyl, optionally substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 pentyl, optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 cycloalkyl, heterocyclyl, aryl, or heteroaryl optionally substituted with one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 isopropyl, optionally substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10isobutyl, optionally substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 isopentyl, optionally substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10isohexyl, optionally substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 sec-butyl, optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10secpentyl, optionally substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 cycloalkyl, heterocyclyl, aryl, or sechexyl optionally substituted with 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, or tertbutyl optionally substituted with a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2.
[0542] In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C substituted with aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S 1~6 alkyl, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10methyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or ethyl substituted with a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10propyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 butyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10pentyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 cycloalkyl, heterocyclyl, aryl, or heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S; 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10isopropyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 isobutyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10isopentyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 isohexyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10sec-butyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 secpentyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10cycloalkyl, heterocyclyl, aryl, or heteroaryl containing 1 to 4 heteroatoms selected from N, O, and S; 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, or tertbutyl substituted with a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2.
[0543] In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C optionally substituted with aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S;2~6 alkenyl, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C2 alkenyl optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C alkenyl optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C4 alkenyl optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C alkenyl optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C6 alkenyl optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2.
[0544] In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C substituted with aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S 2~6 alkenyl, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C alkenyl substituted with aryl, or a 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C alkenyl substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C4 alkenyl substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C alkenyl substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C6 alkenyl substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2.
[0545] In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C optionally substituted with aryl or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; 2~6 alkynyl, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C6~10 C alkynyl optionally substituted with aryl, or 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl is selected from one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 aryl, 5-10 membered heteroaryl containing 1-4 heteroatoms selected from N, O, and S; C 1~6 Alkyl, C 2~6 Alkenyl, C 2~6 It may be substituted with alkynyl, oxo, halogen, -CN, -OH, or -NH2. In some embodiments, R 11 is one or more C 3~10 cycloalkyl, 3- to 10-membered heterocyclyl containing 1-4 heteroatoms selected from N, O, and S, C 6~10 C alkynyl optionally subs...
Claims
1. The following compounds 1 to 88, 90 to 97, 99 to 108, 110, 111, 115 to 128, 130 to 214, 216 to 235, 237, 239 to 242, 244, 245, 247 to 255, 257, 258, 260, 262 to 266, 268 to 270, and 272 to 283: or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, selected from the group consisting of:
2. Compounds 16 and 48 below:
2. The compound of claim 1, or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, selected from:
3. 10. A pharmaceutical composition comprising the compound of claim 1, or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, and a pharmaceutically acceptable diluent or carrier.
4. 4. The pharmaceutical composition of claim 3 for use in treating cancer sensitive to modulation of P-glycoprotein activity and / or cytochrome P450 activity.
5. 4. The pharmaceutical composition of claim 3 for use in modulating P-glycoprotein activity and / or cytochrome P450 activity.
6. 4. The pharmaceutical composition of claim 3 for use in the treatment or prevention of a disease or disorder sensitive to modulation of P-glycoprotein activity and / or cytochrome P450 activity.
7. 4. The pharmaceutical composition of claim 3 for use in treating or preventing cancer.
8. Use of the compound of claim 1, or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, or the pharmaceutical composition of claim 3, in the manufacture of a medicament for treating cancer sensitive to modulation of P-glycoprotein activity and / or cytochrome P450 activity.
9. Use of a compound of claim 1, or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, or a pharmaceutical composition of claim 3, in the manufacture of a medicament for treating or preventing a disease or disorder sensitive to modulation of P-glycoprotein activity and / or cytochrome P450 activity.
10. 10. Use of a compound of claim 1, or a pharmaceutically acceptable solvate, enantiomer, stereoisomer, tautomer, or salt thereof, or a pharmaceutical composition of claim 3, in the manufacture of a medicament for treating or preventing cancer.
Citation Information
Patent Citations
Anthranilic Acid Derivatives as Multidrug Resistance Modulators
JP2001502683A
Method for producing hydrate of anthranilic acid derivative
JP2005538051A
Novel anthranilic acid derivatives
JP2017530141A
Novel p-glycoprotein inhibitor, method for the preparation thereof and pharmaceutical composition comprising the same
WO2005033101A1
Neurotrypsin inhibitors
WO2012059442A2