| 主权项 |
1. A compound of formula (I):wherein:
one of A and B is a bond, O, CO, S(O)p, NCORb, NCONHRc, NSO2Rd, or CR8R9 and the other of A and B is a bond, NRa, or CR10R11, wherein p is 0, 1, or 2, Ra is hydrogen, C1-C6alkyl, C1-C6alkoxy, hydroxy or C3-C6cycloalkyl, Rb, Rc and Rd are independently C1-C6alkyl, C1-C6alkoxy, C3-C6cycloalkyl, mono or bicyclic heteroaryl, monocyclic heterocyclyl, or mono or bicyclic aryl (wherein aforementioned mono or bicyclic aryl, mono or bicyclic heteroaryl, and monocyclic heterocyclyl are optionally substituted with one, two, or three substituents independently selected from C1-C6alkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, and cyano) and R8, R9, R10 and R11 are independently hydrogen, OH, C1-C6alkoxy, C1-C6alkyl, or C3-C8cycloalkyl, and provided that both A and B are not bond or heteroatoms simultaneously; ring C is phenyl, monocyclic heteroaryl, monocyclic heterocyclyl, or C5-C6cycloalkyl, wherein ring C, in addition to —CR3R4—Z—X1—R1, is optionally substituted with one or two substituents independently selected from C1-C6alkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, amino, C1-C6alkyl-amino, diC1-C6alkylamino, and cyano; R3 and R4 are independently hydrogen, fluoro, or C1-C6alkyl, or R3 and R4 together with the carbon they are attached form C═O, C═NR12 (wherein R12 is hydrogen, C1-C6alkyl, C1-C6alkoxy, or hydroxy), or C3-C6cycloalkyl, provided that when R3 and R4 together form C═NR12 then Z is NR13; Z is a bond, NR13, or CR14R15, wherein R13, R14, and R15 are independently hydrogen or C1-C6alkyl; X1 is bond, C═NR8, CR16R17, O, or S(O)q, wherein q is 0, 1, or 2, R8 is as defined above, and R16 and R17 are independently hydrogen, deuterium, or C1-C6alkyl, or R16 and R17 together with the carbon they are attached form C3-C6cycloalkyl, C═NH, or C═O, provided that when R3 and R4 together form C═O then X1 is not O; R1 is mono or bicyclic aryl, mono or bicyclic heteroaryl, C3-C6cycloalkyl, monocyclic heterocyclyl, or fused heterocyclyl, wherein each of the aforementioned ring(s) is optionally substituted with Re, Rf or Rg independently selected from C1-C6alkyl, C2-C6alkenyl, C3-C6cycloalkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, amino, C1-C6alkylamino, diC1-C6alkylamino, aminoC-C6alkyl, aminocarbonyl, amidinoC-C6alkyl, —C(═NRh)NHRi (where Rh and Ri are independently hydrogen, hydroxy, C1-C6alkoxy, benzyloxy, acyl, —C(O)OC1-C6alkyl, a natural or an unnatural amino acid residue, a dipeptidic residue, —CO(ethylene)SO2Ru (where Ru is C1-C6alkyl, optionally substituted monocyclic heteroaryl, optionally substituted phenyl, or optionally substituted monocyclic heterocyclyl), or —CO(CH2)2-3ORv (where Rv is hydrogen, C1-C6alkoxyC1-3alkyl, or optionally substituted monocyclic heterocyclyl)), cyano, monocyclic heteroaryl (wherein the monocyclic heteroaryl is optionally substituted with one, two or three substituents independently selected from C1-C6alkyl, C3-C6cycloalkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, amino, C1-C6alkylamino, diC1-C6alkylamino, and cyano), and monocyclic heterocyclyl (wherein the monocyclic heterocyclyl is optionally substituted with one, two or three substituents independently selected from C1-C6alkyl, C3-C6cycloalkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, amino, C1-C6alkylamino, and diC1-C6alkylamino); R5 and R6 independently are hydrogen, C1-C6alkyl, C3-C6cycloalkyl, halo, hydroxy, carboxy, C1-C6alkoxycarbonyl, or C1-C6alkoxy; R2 and R7 are independently hydrogen, halo, C1-C6alkyl, haloC1-C6alkyl, haloC1-C6alkoxy, cyano, hydroxyC1-C6alkyl, C1-C6alkoxyC1-C6alkyl, C3-C6cycloalkyl, mono or bicyclic aryl, mono or bicyclic heteroaryl, monocyclic heterocyclyl, fused heterocyclyl, mono or bicyclic arylC1-C6alkyl, mono or bicyclic heteroarylC1-C6alkyl, monocyclic heterocyclylC1-C6alkyl (wherein the alkylene chain in mono or bicyclic arylC1-C6alkyl, mono or bicyclic heteroarylC1-C6alkyl or monocyclic heterocyclylC1-C6alkyl is optionally substituted with deuterium), spiroheterocycloamino, bridged heterocycloamino, —NR18R19, —OR20, —CHFR21, —CF2R22, SR23, SOR24, SO2R25, —C(═O)R26; —C(═O)NR27R28, or —NR18C(═O)R29 wherein R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, and R29 are independently hydrogen, C1-C6alkyl, C3-C6cycloalkyl, C3-C6cycloalkylC1-C6alkyl, mono or bicyclic aryl, mono or bicyclic heteroaryl, or monocyclic heterocyclyl; or R18 and R19 or R27 and R28 together with the nitrogen atom they are attached form heterocycloamino or mono or bicyclic heteroaryl, and wherein each of the aforementioned ring in R2 and R7, by itself or as part of another group, is optionally substituted with Rj, Rk or Rl independently selected from C1-C6alkyl, C2-C6alkenyl, C3-C6cycloalkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, C1-C6alkylthio, C1-C6alkylsulfonyl, amino, C1-C6alkyl-amino, diC1-C6alkylamino, aminoC1-C6alkyl, cyano, monocyclic heteroaryl (wherein the monocyclic heteroaryl is optionally substituted with one, two or three substituents independently selected from C1-C6alkyl, C3-C6cycloalkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, amino, C1-C6alkylamino, diC1-C6alkylamino, and cyano), and monocyclic heterocyclyl (wherein the monocyclic heterocyclyl is optionally substituted with one, two or three substituents independently selected from C1-C6alkyl, C3-C6cycloalkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, amino, C1-C6alkylamino, and diC1-C6alkylamino); or R2 and R7 together with the atoms they are attached form ring D: where ring D is phenyl, mono or bicyclic heteroaryl, monocyclic heterocyclyl, fused heterocyclyl, or C5-C6cycloalkyl; and R30 and R31 are independently hydrogen, halo, C1-C6alkyl, haloC1-C6alkyl, haloC1-C6alkoxy, cyano, hydroxyC1-C6alkyl, C1-C6alkoxyC1-C6alkyl, C3-C6cycloalkyl, mono or bicyclic aryl, mono or bicyclic heteroaryl, monocyclic heterocyclyl, fused heterocyclyl, mono or bicyclic arylC1-C6alkyl, mono or bicyclic heteroarylC1-C6alkyl monocyclic heterocyclylC1-C6alkyl (wherein the alkylene chain in mono or bicyclic arylC1-C6alkyl, mono or bicyclic heteroarylC1-C6alkyl or monocyclic heterocyclylC1-C6alkyl is optionally substituted with deuterium), spiro heterocycloamino, bridged heterocycloamino, —NR32R33, —OR34, —CHFR35, —CF2R36, SR37, SOR38, SO2R39, —C(═O)R40, —C(═O)NR41R42, or —NR43C(═O)R44, wherein R32, R33, R34, R35, R36, R37, R38, R39, R40, R41, R42, R43, and R44 are independently hydrogen, C1-C6alkyl, mono or bicyclic aryl, mono or bicyclic heteroaryl, or monocyclic heterocyclyl; or R32 and R33 or R41 and R42 together with the nitrogen atom they are attached form heterocycloamino or mono or bicyclic heteroaryl, and wherein each of the aforementioned ring in R30 and R31, whether by itself or part of another group, is optionally substituted with Rm, Rn or Ro independently selected from C1-C6alkyl, C2-C6alkenyl, C3-C6cycloalkyl, C3-C6cycloalkylC1-6alkoxy, C3-C6cycloalkylC1-6alkoxy, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, C1-C6alkylthio, C1-C6alkylsulfonyl, amino, C1-C6alkylamino, diC1-C6alkylamino, aminocarbonyl, acyl, aminoC1-C6alkyl, cyano, monocyclic heteroaryl (wherein the monocyclic heteroaryl is optionally substituted with one, two or three substituents independently selected from C1-C6alkyl, C3-C6cycloalkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, amino, C1-C6alkylamino, diC1-C6alkylamino, and cyano), and monocyclic heterocyclyl (wherein the monocyclic heterocyclyl is optionally substituted with one, two or three substituents independently selected from C1-C6alkyl, C3-C6cycloalkyl, C1-C6alkoxy, hydroxy, halo, haloC1-C6alkyl, haloC1-C6alkoxy, amino, C1-C6alkylamino, and diC1-C6alkylamino); or a pharmaceutically acceptable salt thereof. |
