| 主权项 |
1. A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is H or C1-C3 alkyl; X is formula (a) or formula (b) wherein R2A, R2B, R2C, and R2D, are each independently hydrogen or halogen; R3, R4, R6, and R7, are each independently hydrogen, C1-C3 alkyl, or halogen; R5, at each occurrence, is independently hydrogen, C1-C3 alkyl, C2-C4 alkenyl, or C1-C3 haloalkyl; X1A is O or CH2; X1B is O or CH2; Y is -G1, or Y is formula (c), (d), (e), (f), or (g); wherein
G1 is phenyl or monocyclic heteroaryl, each of which is optionally substituted with 1, 2, or 3 independently selected Rp groups; wherein each Rp is independently C1-C6 alkyl, halogen, C1-C6 haloalkyl, G2, C1-C3 alkoxy, C1-C3 haloalkoxy, —C(O)-GA, —C(O)NRARB, or —NRARB; wherein
RA, at each occurrence, is independently hydrogen, C1-C6 alkyl, or C1-C6 haloalkyl;RB, at each occurrence, is independently hydrogen, C1-C6 haloalkyl, or C1-C6 alkyl which is optionally substituted with 1 or 2 —OH;GA is a C3-C6 cycloalkyl or a 4-6 membered monocyclic heterocycle; each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 haloalkyl, —OH, C1-C3 alkoxy, and C1-C3 haloalkoxy; andG2 is phenyl, heterocycle, or monocyclic heteroaryl; each of which is optionally substituted with 1, 2, or 3 independently selected Rq groups;X2 is O or N(R2x) wherein R2x is hydrogen, C1-C3 alkyl, or C1-C3 haloalkyl;X3 is N or CH;X4-X5 is N═C, C(R4x)═C, or C(R4x)2—C(R5x), wherein R4x and R5x, at each occurrence, are each independently hydrogen, halogen, C1-C3 alkyl, or C1-C3 haloalkyl;R8 groups are optional substituents on the benzo ring, and are each independently halogen, C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy, or C1-C3 haloalkoxy;m is 0, 1, 2, 3, or 4;G3 is —(C1-C3 alkylenyl)-ORg, —(C1-C3 alkylenyl)-GB, phenyl, cycloalkyl, 4-6 membered monocyclic heterocycle, or monocyclic heteroaryl; wherein the phenyl, the cycloalkyl, the 4-6 membered monocyclic heterocycle, and the monocyclic heteroaryl are each optionally substituted with 1, 2, or 3 independently selected Rs groups;GB is phenyl, cycloalkyl, 4-6 membered monocyclic heterocycle, or monocyclic heteroaryl; each of which is optionally substituted with 1, 2, or 3 independently selected Rs groups;R9 is C1-C3 alkyl, C3-C6 cycloalkyl, or phenyl; wherein the C3-C6 cycloalkyl and the phenyl are each optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, —OH, C1-C3 alkyl, C1-C3 haloalkyl, C1-C3 alkoxy, and C1-C3 haloalkoxy;n is 0, 1, 2, or 3;R10 is C1-C6 alkyl substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, OH, C1-C3 alkoxy, C1-C3 haloalkoxy, and 2,2-dimethyl-1,3-dioxolan-4-yl; or R10 is phenyl, C3-C6 cycloalkyl, or monocyclic heteroaryl, wherein the phenyl, C3-C6 cycloalkyl, and monocyclic heteroaryl are each optionally substituted with 1, 2, or 3 independently selected Rv groups;R11 is halogen, C1-C3 alkyl, or G4 wherein G4 is C3-C6 cycloalkyl, 4-6 membered monocyclic heterocycle, monocyclic heteroaryl, or phenyl; each G4 is optionally substituted with 1, 2, or 3 independently selected Rw groups;R12 are optional substituents of the benzo ring, and are each independently halogen, C1-C3 alkyl, or C1-C3 haloalkyl;p is 0, 1, 2, or 3;R13 is hydrogen or C1-C6 alkyl which is substituted with 1, 2, or 3 substituents independently selected from the group consisting of CN, 2,2-dimethyl-1,3-dioxolan-4-yl, —OR13a, —O-benzyl, —N(R13a)2, —N(R13a)S(O)2R13b, and —N(R13a)C(O)R13b, wherein R13a, at each occurrence, is independently hydrogen, C1-C6 alkyl, or C1-C6 haloalkyl, and R13b, at each occurrence, is independently C1-C6 alkyl or C1-C6 haloalkyl;R14 and R15 are each independently C1-C3 alkyl, orR14 and R15, together with the carbon atom to which they are attached, form a C3-C6 cycloalkyl or a 4-6 membered monocyclic heterocycle containing one heteroatom selected from the group consisting of oxygen and nitrogen; wherein the C3-C6 cycloalkyl and the 4-6 membered monocyclic heterocycle are each optionally substituted with 1 or 2 substituents independently selected from the group consisting of C1-C3 alkyl, halogen, C1-C3 haloalkyl, —OH, C1-C3 alkoxy, and C1-C3 haloalkoxy;R16 is —OH or C1-C6 alkyl optionally substituted with 1 or 2 substituents independently selected from the group consisting of —CN, —ORj, —O-benzyl, —OC(O)Rk, —OC(O)N(Rj)2, —SRj, —S(O)2Rj, —S(O)2N(Rj)2, —C(O)Rj, —C(O)ORj, —C(O)N(Rj)2, —C(O)N(Rj)S(O)2Rk, —N(Rj)2, —N(Rj)C(O)Rk, —N(Rj)S(O)2Rk, —N(Rj)C(O)O(Rk), and —N(Rj)C(O)N(Rj)2;Rq is C2-C6 alkenyl, C2-C6 alkynyl, halogen, C1-C6 haloalkyl, —CN, oxo, NO2, —ORx, —OC(O)Ry, —OC(O)N(Rx)2, —SRx, —S(O)2Rx, —S(O)2N(Rx)2, —C(O)Rx, —C(O)ORx, —C(O)N(Rx)2, —C(O)N(Rx)S(O)2Ry, —N(Rx)2, —N(Rx)C(O)Ry, —N(Rx)S(O)2Ry, —N(Rx)C(O)O(Ry), —N(Rx)C(O)N(Rx)2, G2A, or C1-C6 alkyl which is optionally substituted with 1 or 2 substituents independently selected from the group consisting of —CN, NO2, —ORx, —OC(O)Ry, —OC(O)N(Rx)2, —SRx, —S(O)2Rx, —S(O)2N(Rx)2, —C(O)Rx, —C(O)ORx, —C(O)N(Rx)2, —C(O)N(Rx)S(O)2Ry, —N(Rx)2, —N(Rx)C(O)Ry, —N(Rx)S(O)2Ry, —N(Rx)C(O)O(Ry), —N(Rx)C(O)N(Rx)2, and G2A;Rx, at each occurrence, is independently hydrogen, C1-C6 alkyl, G2A, C1-C6 haloalkyl, or —(C1-C6 alkylenyl)-G2A;Ry, at each occurrence, is independently C1-C6 alkyl, G2A, C1-C6 haloalkyl, or —(C1-C6 alkylenyl)-G2A;G2A, at each occurrence, is independently phenyl or C3-C6 cycloalkyl; each of which is optionally substituted with 1, 2, or 3 Rz groups;Rs, at each occurrence, is independently C2-C6 alkenyl, C2-C6 alkynyl, halogen, C1-C6 haloalkyl, —CN, oxo, NO2, —ORj, —ORh, —OC(O)Rk, —OC(O)N(Rj)2, —SRj, —S(O)2Rj, —S(O)2N(Rj)2, —C(O)Rj, —C(O)ORj, —C(O)O(benzyl), —C(O)N(Rj)2, —C(O)N(Rm)(Rn), —C(O)N(Rj)S(O)2Rk, —N(Rj)2, —N(Rj)C(O)Rk, —N(Rj)S(O)2Rk, —N(Rj)C(O)O(Rk), G3A, —N(Rj)C(O)N(Rj)2, or C1-C6 alkyl which is optionally substituted with 1 or 2 substituents independently selected from the group consisting of —CN, NO2, —ORj, —O-benzyl, —OC(O)Rk, —OC(O)N(Rj)2, —SRj, —S(O)2Rj, —S(O)2N(Rj)2, —C(O)Rj, —C(O)ORj, —C(O)N(Rj)2, —C(O)N(Rj)S(O)2Rk, —N(Rj)2, —N(Rj)C(O)Rk, —N(Rj)S(O)2Rk, —N(Rj)C(O)O(Rk), —N(Rj)C(O)N(Rj)2, and G3A;G3A, at each occurrence, is independently phenyl or 4-6 membered monocyclic heterocycle; each G3A is optionally substituted with 1, 2, 3, or 4 Rc groups;Rg is hydrogen or benzyl, or Rg is C2-C6 alkyl which is substituted with 1 or 2 —ORj;Rh is benzyl or Rh is C2-C6 alkyl which is substituted with 1 or 2 —ORj;Rm is G3B or C1-C6 alkyl which is substituted with 1 or 2 substituents independently selected from the group consisting of —ORj, —S(O)2Rj, —C(O)N(Rj)2, and G3B;Rn is hydrogen, C1-C6 alkyl, C1-C6 haloalkyl, benzyl, or —(C2-C6 alkylenyl)-ORj; orRm and Rn, together with the nitrogen atom to which they are attached, form a 4-7 membered monocyclic heterocycle, wherein the 4-7 membered monocyclic heterocycle is optionally substituted with 1, 2, 3, or 4 independently selected Rc groups;G3B, at each occurrence, is independently a phenyl, a 4-7 membered monocyclic heterocycle, or a 3-10 membered cycloalkyl, each of which is optionally substituted with 1, 2, 3, or 4 independently selected Rc groups;Rc, Ru, Rv, Rw, and Rz, at each occurrence, are each independently C2-C6 alkenyl, C2-C6 alkynyl, halogen, C1-C6 haloalkyl, —CN, oxo, NO2, —ORj, —OC(O)Rk, —OC(O)N(Rj)2, —SRj, —S(O)2Rj, —S(O)2N(Rj)2, —C(O)Rj, —C(O)ORj, —C(O)N(Rj)2, —C(O)N(Rj)S(O)2Rk, —N(Rj)2, —N(Rj)C(O)Rk, —N(Rj)S(O)2Rk, —N(Rj)C(O)O(Rk), —N(Rj)C(O)N(Rj)2, or C1-C6 alkyl which is optionally substituted with 1 or 2 substituents independently selected from the group consisting of —CN, NO2, —OC(O)Rk, —OC(O)N(Rj)2, —S(O)2Rj, —S(O)2N(Rj)2, —C(O)Rj, —C(O)ORj, —C(O)N(Rj)2, —C(O)N(Rj)S(O)2Rk, —N(Rj)2, —N(Rj)C(O)Rk, —N(Rj)S(O)2Rk, —N(Rj)C(O)O(Rk), and —N(Rj)C(O)N(Rj)2;R1, at each occurrence, is independently hydrogen, C1-C6 alkyl, or C1-C6 haloalkyl; andRk, at each occurrence, is independently C1-C6 alkyl or C1-C6 haloalkyl. |
