主权项 |
1. A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein: X, X1, X2 and X3 are C or N with the proviso that no more than one of X, X1, X2 and X3 is N; R1, R2, R3 and R4 are independently do not exist, hydrogen, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, —CN, —OR7, —SR7, —NR7R8, —CF3, —OCF3, —NO2, —C(O)R7, —C(O)OR7, —C(O)NR7R8, —NR7C(O)R8, —S(O)1-2R7, —NR7S(O)1-2R8, —S(O)1-2NR7R8, C3-C6 cycloalkyl, 3-10-membered heterocyclyl or 6-10 membered aryl, wherein R1, R2, R3 and R4 are independently optionally substituted by R9; R5 is does not exist, C1-C6 alkylene, C2-C6 alkenylene, C2-C6 alkynylene, wherein said alkylene, alkenylene and alkynylene are independently optionally substituted by halogen, oxo, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, —OR16, —SR16, —NR16R17, —CN, —C(O)R16, —C(O)OR16, —NR16C(O)R17, —NR16S(O)1-2R17, —CF3, —OCF3, 3-10-membered heterocyclyl or 6-10 membered aryl, and wherein said alkyl, alkenyl, alkynyl, heterocyclyl and phenyl are independently optionally substituted with R9; R6 is hydrogen, C3-C10 cycloalkyl, 3-10-membered heterocyclyl or 6-10-membered aryl, wherein R6 is independently optionally substituted by R9; each R7 and R8 are independently hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, 3-6-membered heterocyclyl or phenyl, wherein said alkyl, cycloalkyl, heterocyclyl and phenyl are independently optionally substituted by halogen, —CN, —CF3, —OCF3, oxo or C1-C6 alkyl optionally substituted by halogen or oxo; or R7 and R8 are independently taken together with the atom to which they are attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C1-C6 alkyl optionally substituted by halogen or oxo; each R9 is independently hydrogen, oxo, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, —(C0-C6 alkylene)CN, —(C0-C6 alkylene)OR10, —(C0-C6 alkylene)SR10, —(C0-C6 alkylene)NR10R11, —(C0-C6 alkylene)CF3, —(C0-C6 alkylene)NO2, —(C0-C6 alkylene)C(O)R10, —(C0-C6 alkylene)C(O)OR10, —(C0-C6 alkylene)C(O)NR10R11, —(C0-C6 alkylene)NR10C(O)R11, —(C0-C6 alkylene)S(O)1-2R10, —(C0-C6 alkylene)NR10S(O)1-2R11, —(C0-C6 alkylene)S(O)1-2NR10R11, —(C0-C6 alkylene)(C3-C6 cycloalkyl), —(C0-C6 alkylene)(3-10-membered heterocyclyl), —(C0-C6 alkylene)C(O)(3-10-membered heterocyclyl), or —(C0-C6 alkylene)(6-10 membered aryl), wherein each R9 is independently optionally substituted by halogen, oxo, —CF3, —CN, —OR12, —SR12, —NR12R13, —C(O)R12, —S(O)1-2R12, C1-C6 alkyl optionally substituted by oxo or halogen, C2-C6 alkenyl optionally substituted by oxo or halogen, or C2-C6 alkynyl optionally substituted by oxo or halogen; each R10 and R11 are independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, 3-6-membered heterocyclyl, phenyl or C3-C6 cycloalkyl, wherein said alkyl, alkenyl, alkynyl, heterocyclyl, phenyl and cycloalkyl are independently optionally substituted by halogen, oxo, —CF3, —OCF3, —OR14, —SR14, —NR14R15, —CN, 3-6-membered heterocyclyl, phenyl, C3-C6 cycloalkyl or C1-C6 alkyl optionally substituted by halogen or oxo; or R10 and R11 are independently taken together with the atom to which they are attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C1-C6 alkyl optionally substituted by halogen or oxo; each R12 and R13 are independently hydrogen or C1-C6 alkyl optionally substituted by halogen or oxo; or R12 and R13 are independently taken together with the atom to which they are attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C1-C6 alkyl optionally substituted by halogen; each R14 and R15 are independently hydrogen or C1-C6 alkyl optionally substituted by halogen or oxo; or R14 and R15 are independently taken together with the atom to which they are attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C1-C6 alkyl optionally substituted by halogen; each R16 and R17 are independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, 3-6-membered heterocyclyl, phenyl or C3-C6 cycloalkyl, wherein said alkyl, alkenyl, alkynyl, heterocyclyl, phenyl and cycloalkyl are independently optionally substituted by halogen, oxo, —CF3, —OCF3, —OR18, —SR18, —NR18R19, —CN, 3-6-membered heterocyclyl, phenyl, C3-C6 cycloalkyl or C1-C6 alkyl optionally substituted by halogen, —OR20, —NR20R21, or oxo; or R16 and R17 are independently taken together with the atom to which they are attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C1-C6 alkyl optionally substituted by halogen or oxo; each R18 and R19 are independently hydrogen or C1-C6 alkyl optionally substituted by halogen or oxo; or R18 and R19 are independently taken together with the atom to which they are attached to form a 3-6 membered heterocyclyl optionally substituted by halogen, oxo or C1-C6 alkyl optionally substituted by halogen; and each R20 and R21 are independently hydrogen or C1-C6 alkyl optionally substituted by halogen or oxo; other than N-(1-ethyl-1H-pyrazol-4-yl)-1H-indazole-3-carboxamide; 5-amino-N-(1-ethyl-1H-pyrazol-4-yl)-1H-indazole-3-carboxamide; 5-amino-N-(1-methyl-1H-pyrazol-4-yl)-1H-Indazole-3-carboxamide; N-[1-(imidazo[1,2-a]pyridin-2-ylmethyl)-1H-pyrazol-4-yl]-1H-Indazole-3-carboxamide; N-[1-[2-(diethylamino)ethyl]-1H-pyrazol-4-yl]-1H-Indazole-3-carboxamide; N-(1-methyl-1H-pyrazol-4-yl)-5-nitro-1H-Indazole-3-carboxamide; N-[1-[2-(3,4-dimethoxyphenyl)ethyl]-1H-pyrazol-4-yl]-1H-Indazole-3-carboxamide; 4-[(2H-indazol-3-ylcarbonyl)amino]-1H-Pyrazole-1-acetic acid; N-[1-[2-(phenylmethoxy)ethyl]-1H-pyrazol-4-yl]-1H-Indazole-3-carboxamide; N-[1-(4-cyanobutyl)-1H-pyrazol-4-yl]-1H-Indazole-3-carboxamide; or N-[1-[(3-cyanophenyl)methyl]-1H-pyrazol-4-yl]-1H-Indazole-3-carboxamide. |