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Azaindole derivatives as CFTR modulators
专利权人:
Vertex Pharmaceuticals Incorporated
发明人:
Hadida Ruah, Sara,Zhou, Jinglan,Miller, Mark,Bear, Brian
申请号:
ES14164892
公开号:
ES2646175T3
申请日:
2007.11.02
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound having the formula I: ** Formula ** or a pharmaceutically acceptable salt thereof; in which: ** Formula ** Ar1 is: ** Formula ** in which: each of G1, G2, G3 and G4 are independently selected from the group consisting of CH and nitrogen, in which one of G1, G2, G3 and G4 is nitrogen and the rest of G1, G2, G3 and G4 is each CH. Ar1 is linked to N (RN) through G2 or G3; Ar1 is unsubstituted or substituted with w occurrences of -WRW; RN is H, R2 or R3; ring A is a 3-7 membered monocyclic ring having 0-3 heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, wherein ring A is optionally substituted with q-Q-RQ occurrences; Ring B is optionally condensed with a 5-7 member ring selected from the group consisting of cycloaliphatic, aryl, heterocyclic and heteroaryl, wherein Ring B, together with said optionally condensed ring, is optionally substituted with x -XRX occurrences ; Q, W, or X is, independently, a bond or is, independently, an alkylidene chain (C1-C6) where up to two methylene units of Q, W, or X are optionally and independently substituted with -CO-, -CS-, -COCO-, -CONR'-, -CONR'NR'-, -CO2-, -OCO-, -NR'CO2-, -O-, -NR'CONR'-, - OCONR'-, -NR'NR ', - NR'NR'CO-, -NR'CO-, -S-, -SO, -SO2 -, - NR'-, -SO2NR'-, NR'SO2-, or -NR'SO2NR'-; each RQ, RW and RX is, independently, R1, R2, R3, R4 or R5; R 'is, independently, R2, R3 or R6; R1 is oxo,>; = NN (R6) 2,>; = NN (R7) 2,>; = NN (R6R7), R6, or (aliphatic (C1-C4)) n-Y; where n is 0 or 1; and Y is halo, CN, NO2, CF3, OCF3, OH, SR6, S (O) R6, SO2R6, NH2, NHR6, N (R6) 2, NR6R8, COOH, COOR6 or OR6; or two R1 in adjacent atoms, together, form ** Formula ** in which J is selected from the group consisting of CH2, CF2, C (CH3) 2, C (O), C (phenyl) 2, B (OH ) and CH (OEt); R2 is aliphatic, wherein each R2 is unsubstituted or substituted with up to 2 substituents independently selected from the group consisting of R1, R4 and R5; R3 is a cycloaliphatic, aryl, heterocyclic or heteroaryl ring
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