主权项 |
1. A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is H; F; Cl; Br; CN; CH3; CF3; or C(O)NH2; R is H; or C1-4 alkyl, wherein C1-4 alkyl is optionally substituted with one or more halogen, which are the same or different; T0A is phenyl, naphthyl, or aromatic 5 to 6 membered heterocyclyl, wherein T0A is optionally substituted with one or more R1; Each R1 is independently halogen; CN; C(O)OR2; OR2; C(O)R2; C(O)N(R2R2a); S(O)2N(R2R2a); S(O)N(R2R2a); S(O)2R2; S(O)R2; N(R2)S(O)2N(R2aR2b); N(R2)S(O)N(R2aR2b); SR2; N(R2R2a); NO2; OC(O)R2; N(R2)C(O)R2a; N(R2)S(O)2R2a; N(R2)S(O)R2a; N(R2)C(O)N(R2aR2b); N(R2)C(O)OR2a; OC(O)N(R2R2a); T1; 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 R3, which are the same or different; R2, R2a, R2b are independently selected from the group consisting of H; T1; 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 R3, which are the same or different; R3 is halogen; CN; C(O)OR4; OR4; C(O)R4; C(O)N(R4R4a); S(O)2N(R4R4a); S(O)N(R4R4a); S(O)2R4; S(O)R4; N(R4)S(O)2N(R4aR4b); N(R4)S(O)N(R4aR4b); SR4; N(R4R4a); NO2; OC(O)R4; N(R4)C(O)R4a; N(R4)S(O)2R4a; N(R4)S(O)R4a; N(R4)C(O)N(R4aR4b); N(R4)C(O)OR4a; OC(O)N(R4R4a); or T1; R4, R4a, R4b are independently selected from the group consisting of H; T1; 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; T1 is C3-7 cycloalkyl; saturated 4 to 7 membered heterocyclyl; or saturated 7 to 11 membered heterobicyclyl, wherein T1 is optionally substituted with one or more R10, which are the same or different; Y0 is C(R5R5a); R5, R5a are independently selected from the group consisting of H; and unsubstituted C1-6 alkyl; or jointly form oxo (═O); Optionally, R5, R5a are joined to form an unsubstituted C3-7 cycloalkyl; T0B is C3-7 cycloalkyl; or saturated 4 to 7 membered heterocyclyl, wherein T0B is optionally substituted with one or more R6, which are the same or different; R6 is halogen; CN; C(O)OR7; OR7; oxo (═O); C(O)R7; C(O)N(R7R7a); S(O)2N(R7R7a); S(O)N(R7R7a); S(O)2R7; S(O)R7; N(R7)S(O)2N(R7aR7b); N(R7)S(O)N(R7aR7b); SR7; N(R7R7a); NO2; OC(O)R7; N(R7)C(O)R7a; N(R7)S(O)2R7a; N(R7)S(O)R7a; N(R7)C(O)N(R7aR7b); N(R7)C(O)OR7a; OC(O)N(R7R7a); T2; 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 R11, which are the same or different; R7, R7a, R7b are independently selected from the group consisting of H; T2; 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 R8, which are the same or different; R8 is 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); N(R9)S(O)N(R9aR9b); SR9; N(R9R9a); NO2; OC(O)R9; N(R9)C(O)R9a; N(R9)S(O)2R9a; N(R9)S(O)R9a; N(R9)C(O)N(R9aR9b); N(R9)C(O)OR9a; OC(O)N(R9R9a); or T2; R9, R9a, R9b are independently selected from the group consisting of H; T2; 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 R12, which are the same or different; R10 is halogen; CN; C(O)OR13; OR13; oxo (═O), where the ring is at least partially saturated; 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(R13R13a); N(R13)S(O)N(R13aR13b); SR13; N(R13R13a); NO2; OC(O)R13; N(R13)C(O)R13a; N(R13)S(O)2R13a; N(R13)S(O)R13a; N(R13)C(O)N(R13aR13b); N(R13)C(O)OR13a; OC(O)N(R13R13a); 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 RH, which are the same or different; R13, R13a, 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 R14, which are the same or different; R11, R12 are independently selected from the group consisting of halogen; CN; C(O)OR15; OR15; C(O)R15; C(O)N(R15R15a); S(O)2N(R15R15a); S(O)N(R15R15a); S(O)2R15; S(O)R15; N(R15)S(O)2N(R15aR15b); N(R15)S(O)N(R15aR15b); SR15; N(R15R15a); NO2; OC(O)R15; N(R15)C(O)R15a; N(R15)S(O)2R15a; N(R15)S(O)R15a; N(R15)C(O)N(R15aR15b); N(R15)C(O)OR15a; OC(O)N(R15R15a); and T2; R15, R15a, R15b are independently selected from the group consisting of H; T2; 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 substituents selected from the group consisting of halogen and CN; R14 is halogen; CN; C(O)OR16; OR16; C(O)R16; C(O)N(R16R16a); S(O)2N(R16R16a); S(O)N(R16R16a); S(O)2R16; S(O)R16; N(R16)S(O)2N(R16aR16); N(R16)S(O)N(R16aR16b); SR16; N(R16R16a); NO2; OC(O)R16; N(R16)C(O)R16a; N(R16)S(O)2R16a; N(R16)S(O)R16a; N(R16)C(O)N(R16aR16b); N(R16)C(O)OR16a; or OC(O)N(R16R16a); R16, R16a, R16b 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; T2 is phenyl; naphthyl; indenyl; indanyl; C3-7 cycloalkyl; 4 to 7 membered heterocyclyl; or 7 to 11 membered heterobicyclyl, wherein T2 is optionally substituted with one or more R17, which are the same or different; R17 is halogen; CN; C(O)OR18; OR18; oxo (═O), where the ring is at least partially saturated; C(O)R18; C(O)N(R18R18a); S(O)2N(R18R18a); S(O)N(R18R18a); S(O)2R18; S(O)R18; N(R18)S(O)2N(R18aR18a); N(R18)S(O)N(R18aR18b); SR18; N(R18R18a); NO2, OC(O)R18; N(R18)C(O)R18a; N(R18)S(O)2R18a; N(R18)S(O)R18a; N(R18)C(O)N(R18aR18b); N(R18)C(O)OR18a; OC(O)N(R18R18a); 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 R19, which are the same or different; R18, R18a, R18b 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 R19, which are the same or different; R19 is halogen; CN; C(O)OR20; OR20; C(O)R20; C(O)N(R20R20a); S(O)2N(R20R20a); S(O)N(R20R20a); S(O)2R20; S(O)R20; N(R20)S(O)2N(R20aR20b); N(R20)S(O)N(R20aR20b); SR20; N(R20R20a); NO2; OC(O)R20; N(R20)C(O)R20a; N(R20)S(O)2R20a; N(R20)S(O)R20a; N(R20)C(O)N(R20aR20b); N(R20)C(O)OR20a; or OC(O)N(R20R20a); R20, R20a, R20b 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. |