| 主权项 |
1. A compound of Formula (X):or a stereoisomer, a tautomer, a pharmaceutically acceptable salt thereof, wherein:
ring A is independently selected from a 6-membered aryl and a 5- to 6-membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S, wherein said aryl and heterocycle are optionally substituted with, where valence allows, one or more R4; ring B is a 6-membered aryl wherein said aryl is optionally substituted with, where valence allows, one or more R3; ring C is independently selected from - - - is an optional bond; G1 is independently selected from a C3-10 carbocycle and a 5- to 10-membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S, wherein said carbocycle and heterocycle are optionally substituted with, where valence allows, one or more R8; X is independently selected from C4-8 alkylene and C4-8 alkenylene, wherein said alkylene and alkenylene are substituted with R1 and R2; alternatively one or more of the carbon atoms of said alkylene and alkenylene may be replaced by 0, C═O, S(O)p, S(O)pNH, NH, and N(C1-4 alkyl); X1 is CR7; Y is —C(O)—NH—; R1 and R2 are independently selected from H, halogen, haloalkyl, C1-6 alkyl (optionally substituted with R6), hydroxyl, and alkoxy (optionally substituted with R6), and C3-6 cycloalkyl optionally substituted with R6; optionally, when R1 and R2 are attached to the same carbon atom, together they form an oxo group or C3-6cycloalkyl; optionally, when R1 and R2 are attached to carbon atoms adjacent to each other, together they form a bond or a carbocycle; R3 is independently selected from H, NO2, ═O, halogen, haloalkyl, C1-4alkyl (optionally substituted with R6), C2-4alkenyl (optionally substituted with R6), C2-4alkynyl (optionally substituted with R6), CN, —(CH2)n—OR5, —(CH2)n—NR5R5, —(CH2)n—C(O)OR5, —(CH2)n—NR9C(O)OR5, —(CH2)n—NR9C(O)R5, —(CH2)n—NR9C(N—CN)NHR5, —(CH2)n—NR9C(NH)NHR5, —(CH2)n—N═CR9NR5R5, —(CH2)n—NR9C(O)NR5R5, —(CH2)n—C(O)NR5R5, —(CH2)n—NR9C(S)NR9C(O)R5, —(CH2)n—S(O)pR12, —(CH2)n—S(O)pNR5R5, —(CH2)n—NR9S(O)pNR5R5, —(CH2)n—NR9S(O)pR12, —(CH2)n—C3-10 carbocycle and —(CH2)n-4- to 10-membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S, wherein said carbocycle and heterocycle are optionally substituted with R6; optionally, two adjacent R3 groups on the carbocycle and heterocycle may form a ring optionally substituted with R6; R4 is independently selected from H, OH, NH2, halogen, CN, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, —CH2OH, —CO2H, —CH2CO2H, —CO2(C1-4 alkyl), —C(O)NH2, —C(O)NH(C1-4 alkyl), —C(O)N(C1-4 alkyl)2, S(O)2NH2, C3-6 cycloalkyl, aryl, and 5- to 6-membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S, wherein said cycloalkyl, aryl and heterocycle are optionally substituted with R6; R5 is independently selected from H, C1-4 alkyl (optionally substituted with halogen, hydroxyl, alkoxy, carboxy, alkoxycarbonyl, amino, substituted amino), —(CH2)n—C3-10 carbocycle and —(CH2)n-4- to 10-membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S, wherein said carbocycle and heterocycle are optionally substituted with R6; alternatively, R5 and R5 together with the nitrogen atom to which they are both attached form a heterocyclic ring optionally substituted with R6; R6 is independently selected from H, —(CH2)n—OH, ═O, —(CH2)nNH2, —(CH2)nCN, halogen, C1-6 alkyl, —(CH2)n—C(═O)OH, —(CH2)n—C(═O)OC1-4 alkyl, —(CH2)n—OC1-4 alkyl, —(CH2)n—C3-10 carbocycle, —(CH2)n-4- to 10-membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S, and —O-4- to 10-membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S, wherein said carbocycle and heterocycle are optionally substituted with R10; R7 is independently selected from H, hydroxyl, alkoxy, halogen, C1-3 alkyl; R8 is independently selected from H, halogen, CN, NH2, C1-6 alkyl, haloalkyl, haloalkylcarbonylamine, alkylcarbonyl, alkoxy, haloalkoxy, —(CH2)n-aryl, —(CH2)n—C3-6 cycloalkyl, and —(CH2)n-4-6 membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S; optionally, two adjacent R8 groups on the carbocycle and heterocycle may form a ring optionally substituted with R10; R9 is H or C1-6 alkyl; R10 is independently selected from H, C1-6 alkyl (optionally substituted with R11), C2-6 alkenyl, C2-6 alkynyl, —(CH2)n—C3-6 cycloalkyl (optionally substituted with R11), —O-4- to 10-membered heterocycle containing carbon atoms and 1, 2, 3 or 4 heteroatoms independently selected from the group consisting of N, O and S (optionally substituted with R11), F, Cl, Br, CN, NO2, ═O, CO2H, —(CH2)n—OC1-5 alkyl, —(CH2)n—OR11, and —(CH2)n—NR11R11; R11, at each occurrence, is independently selected from H, C1-5 alkyl, —(CH2)n—OH, C3-6 cycloalkyl, and phenyl, or R11 and R11 together with the nitrogen atom to which they are both attached form a heterocyclic ring optionally substituted with C1-4alkyl; R12 is C1-6 alkyl optionally substituted with R11; m is an integer of 1; n, at each occurrence, is an integer independently selected from 0, 1, 2, 3, and 4; p, at each occurrence, is an integer independently selected from 0, 1, and 2;provided the following compounds are excluded: wherein ring A is independently selected from ---- is an optional bond; R1 is independently selected from H, hydroxyl, and C1-4alkyl; R2, at each occurrence, is independently selected from H and hydroxyl; R4 is independently selected from H, OH, F, OC1-4 alkyl, and CN; R8a is independently selected from H, F, Cl, and Br; R8b is independently selected from H and F; and R8c is independently selected from H, F, and Cl. |
