| CPC C07D 413/14 (2013.01) [C07D 413/04 (2013.01)] | 31 Claims |
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1. A compound of formula (I)
 or a pharmaceutically acceptable salt, solvate, hydrate, tautomer or stereoisomer thereof, wherein
X1 is N(Ra1);
X1a is a covalent single bond or CH(Ra3);
Ra1 is H, C(O)OC1-4 alkyl, or C1-4 alkyl, wherein C(O)OC1-4 alkyl and C1-4 alkyl are optionally substituted with one or more substituents selected from the group consisting of halogen, OH, and O—C1-3 alkyl, wherein the substituents are the same or different;
Ra2 and Ra3 are independently selected from the group consisting of H, OH, OC1-4 alkyl, halogen, C1-4 alkyl, and A2a; and
Ra4, Ra5, Ra6, and Ra7 are independently selected from the group consisting of H, halogen, C1-4 alkyl, and A2a,
provided that only one of Ra2, Ra3, Ra4, Ra5, Ra6, and Ra7 is A2a;
or Ra1 and one of Ra2 and Ra3 form a methylene or ethylene group;
or Ra1 and Ra6 form an ethylene group;
or Ra2 and Ra5 form a covalent single bond;
or Ra5, Ra7 are joined to form an oxo group;
A1 is C5 cycloalkylene, C5 cycloalkenylene, or a nitrogen ring atom containing 5-membered heterocyclene, wherein A1 is optionally substituted with one or more R4, which are the same or different;
each R4 is independently oxo (=O) where the ring is at least partially saturated, thiooxo (═S) where the ring is at least partially saturated, halogen, CN, OR5, or C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with one or more halogen, which are the same or different;
R5 is H or C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with one or more halogen, which are the same or different;
A2 is R6a or A2a;
R6a is OR6a1, SR6a1, N(R6a1R6a2), C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted with one or more substituents selected from the group consisting of halogen, OR6a3, CN, and A2a, wherein the substituents are the same or different;
R6a1 and R6a2 are independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and A2a, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted with one or more substituents selected from the group consisting of halogen, CN, OR6a3, OA2a and A2a, wherein the substituents are the same or different;
R6a3 is H, or C1-4 alkyl, wherein C1-4 alkyl is optionally substituted with one or more halogen, which are the same or different;
A2a is phenyl, C3-7 cycloalkyl, C4-12 bicycloalkyl, or 3- to 7-membered heterocyclyl, wherein A2a is optionally substituted with one or more R6, which are the same or different;
each R6 is independently R6b, OH, OR6b, halogen, or CN, wherein R6b is cyclopropyl, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, wherein R6b is optionally substituted with one or more halogen, which are the same or different; or
two R6 are joined to form together with the atoms to which they are attached a ring A2b;
A2b is phenyl, C3-7 cycloalkyl; or 3 to 7 membered heterocyclyl, wherein A2b is optionally substituted with one or more R7, which are the same or different;
each R7 is independently C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted with one or more halogen, which are the same or different;
R1 is H or C1-4 alkyl, preferably H, wherein C1-4 alkyl is optionally substituted with one or more halogen, which are the same or different;
R2 is H, F, or C1-4 alkyl, wherein C1-4 alkyl is optionally substituted with one or more halogen, which are the same or different; and
R3 is A3, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted with one or more R8, which are the same or different; or
R2 and R3 are joined to form together with the oxygen atom and carbon atom to which they are attached a ring A3a, wherein A3a is a 7 to 12 membered heterobicyclyl, wherein 7 to 12 membered heterobicyclyl is optionally substituted with one or more R10, which are the same or different;
R2a is H or F;
each R8 is independently halogen; CN, C(O)OR9, OR9, C(O)R9, C(O)N(R9R9a) S(O)2N(R9R9a), S(O)N(R9R9a), S(O)2R9, S(O)R9, N(R9)S(O)2N(R9aR9b), SR9, N(R9R9a), NO2, OC(O)R9, N(R9)C(O)R9a, N(R9)SO2R9a, N(R9)S(O)R9a, N(R9)C(O)N(R9aR9b), N(R9)C(O)OR9a, OC(O)N(R9R9a), or A3;
R9, R9a, and R9b are independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted with one or more halogen, which are the same or different, or one OH, or one OC1-4 alkyl, or one A3;
each A3 is independently phenyl, naphthyl, C3-7 cycloalkyl, 3 to 7 membered heterocyclyl, or 7 to 12 membered heterobicyclyl, wherein A3 is optionally substituted with one or more R10, which are the same or different;
each R10 is independently halogen, CN, C(O)OR11, OR11, C(O)R11, C(O)N(R11R11a) S(O)2N(R11R11a), S(O)N(R11R11a), S(O)2R11, S(O)R11, N(R11)S(O)2N(R11aR11b), SR11, N(R11R11a), NO2, OC(O)R11, N(R11)C(O)R11a, N(R11)S(O)2R11a, N(R11)S(O)R11a, N(R11)C(O)OR11a, N(R11)C(O)N(R11aR11b) OC(O)N(R11R11a), oxo (=O) where the ring is at least partially saturated, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted with one or more R12, which are the same or different;
R11, R11a, and R11b are independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted with one or more halogen, which are the same or different;
each R12 is independently halogen, CN, C(O)OR13, OR13, C(O)R13, C(O)N(R13R13a), S(O)2N(R13R13a), S(O)N(R13R13a), S(O)2R13, S(O)R13, N(R13)S(O)2N(R13aR13b), SR13, N(R13R13a), NO2, OC(O)R13, N(R13)C(O)R13a, N(R13)SO2R13a, N(R13)S(O)R13a, N(R13)C(O)N(R13aR13b), N(R13)C(O)OR13a, or OC(O)N(R13R13a);
R13, R13a, and R13b are independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl, wherein C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl are optionally substituted with one or more halogen, which are the same or different,
provided that the following compounds or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof are excluded:
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