主权项 |
1. A compound of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein: Y is NH or O; R1 is hydroxyl, fluoro, or —OCD3; R2 is hydrogen or deuterium; or R2 is C1-C6alkyl, allenyl, C2-C6alkenyl, or C2-C6alkynyl; each of which is optionally deuterated and optionally substituted; or R1 and R2 are joined to form a 3- to 6-membered cycloalkyl ring or a 3- to 6-membered heterocycloalkyl ring containing one heteroatom selected from N, O, and S, each of which is optionally substituted; R3 is hydrogen, deuterium, halogen, or —N3; or R3 is C1-C6alkyl, allenyl, C2-C6alkenyl, C2-C6alkynyl, (C3-C6cycloalkyl)C0-C4carbhydryl, (4- to 6-membered heterocycloalkyl)C0-C4carbhydryl, (aryl)C0-C4carbhydryl, or (heteroaryl)C0-C4carbhydryl, each or which is optionally deuterated and optionally substituted; and R3′ is hydroxyl; or R3 and R3′ are taken together to form a 3- to 6-membered ring optionally containing one heteroatom selected from N, O, and S, which is optionally substituted with one or more substituents independently selected from halogen, hydroxyl, C1-C2alkyl, and C1-C2alkoxy; R4 is hydrogen, deuterium, halogen, C1-C2haloalkyl, or C1-C2haloalkoxy; or R4 is C1-C6alkyl, allenyl, C2-C6alkenyl, C2-C6alkynyl, or C1-C6alkoxy, each of which is optionally deuterated and optionally substituted; R5 is hydrogen, deuterium, or halogen; or R5 is C1-C6alkyl, allenyl, C2-C6alkenyl, C2-C6alkynyl, or C1-C6alkoxy, each of which is optionally deuterated and optionally substituted; or R4 and R5 are taken together to form a 3- to 6-membered ring optionally containing one heteroatom selected from N, O, and S, which ring is optionally substituted with one or more substituents independently selected from halogen, hydroxyl, C1-C2alkyl, and C1-C2alkoxy; R6 is C1-C6alkyl, allenyl, C2-C6alkenyl, C2-C6alkynyl, (aryl)C0-C2alkyl, or 5- to 6-membered monocyclic heteroaryl containing 1 to 3 heteroatoms independently chosen from N, O, and S, or 8- to 10-membered bicyclic heteroaryl containing 1 to 4 heteroatoms independently chosen from N, O, and S; each of which R6 is optionally substituted; R7 is hydrogen, halogen, C1-C2haloalkyl, or C1-C2haloalkoxy; or R7 is C1-C6alkyl, allenyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkoxy, (C3-C6cycloalkyl)C0-C4alkyl, or (aryl)C0-C2alkyl; each of which is optionally substituted; R8 is hydrogen, halogen, C1-C2haloalkyl, or C1-C2haloalkoxy; or R8 is C1-C6alkyl, allenyl, C2-C6alkenyl, C2-C6alkynyl, or C1-C6alkoxy, each of which is optionally substituted; or R7 and R8 are taken together to form a 3- to 6-membered cycloalkyl ring or 3- to 6-membered heterocycloalkyl ring containing one heteroatom chosen from N, O, and S; each of which is optionally substituted; R9 is C1-C6alkyl, allenyl, C2-C6alkenyl, C2-C6alkynyl, (C3-C7cycloalkyl)C0-C4carbhydryl, (aryl)C0-C4carbhydryl, (3- to 6-membered hetero cycloalkyl)C0-C4carbhydryl, or (heteroaryl)C0-C4carbhydryl, each of which is optionally substituted; B1 is a base selected from R10 and R11 are independently hydrogen and deuterium; R12, R13, and R13′ are independently hydrogen, deuterium, methyl, and —CD3; R14 is hydrogen, deuterium, hydroxyl, amino, C1-C4alkoxy, deuterated C1-C4alkoxy, C1-C4alkylester, or mono- or di-C1-C4alkylcarbamate;wherein each position represented by D has a deuterium enrichment of at least 50%; andone or both of R4 and R5 is deuterium with a deuterium enrichment of at least 50%; and one or more of R1, R2, R10, R11, R12, R13, R13′, and R14 is optionally deuterium with a deuterium enrichment of at least 50% or a deuterated substituent with at least one position of the substituent having a deuterium enrichment of at least 50%. |