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Isothiazolopyridinones useful for the treatment of (among others) cystic fibrosis
专利权人:
Vertex Pharmaceuticals Incorporated
发明人:
GALLARDO-GODOY, Alejandra
申请号:
ES08831883
公开号:
ES2578735T3
申请日:
2008.08.15
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of formula I ** Formula ** or a pharmaceutically acceptable salt thereof, in which: Ar1 is a 5-6 membered aromatic monocyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen or sulfur, in the that said ring is optionally condensed with a 5-12 membered ring, monocyclic or bicyclic, aromatic, partially unsaturated, or saturated, in which each ring contains 0-4 heteroatoms independently selected from nitrogen, oxygen or sulfur, in which Ar1 it has m substituents, each independently selected from -WRW; W is a bond or is an optionally substituted C1-C6 alkylidene chain in which up to two methylene units of W are optionally and independently substituted with O, -CO-, -CS-, -COCO-, -CONR'-, -CONR'NR'-, -CO2-, -OCO-, -NR'CO2-, -O-, -NR'CONR'-, -C (O) NR'-, -OCONR'-, -NR'NR ', -NR'NR'CO-, -NR'CO-, -S-, -SO, -SO2-, -NR'-, -SO2NR'-, NR'SO2- or -NR'SO2NR'-; RW is independently R ', halogen, cyano, CF3, CHF2, OCHF2, Me, Et, CH (Me) 2, CHMeEt, n-propyl, t-butyl, OH, OMe, OEt, OPh, O-fluorophenyl, O-difluorophenyl, O-methoxyphenyl, O-tolyl, O-benzyl, SMe, SCF3, SCHF2, SEt, CH2CN, NH2, NHMe, N (Me) 2, NHEt, N (Et) 2, C (O) CH3, C (O) Ph, C (O) NH2, SPh, SO2- (aminopyridyl), SO2NH2, SO2Ph, SO2NHPh, SO2-N-morpholino, SO2-N-pyrrolidyl, N-pyrrolyl, 2-methylpyrrolyl, 3-30 fluoropyrrolyl, 3,3 -difluoropyrrolyl, 3,3-dimethylpyrrolyl, 2,5-dimethylpyrrolyl, N-morpholino, 1-piperidyl, phenyl, benzyl, (cyclohexylmethylamino) methyl, 4-methyl-2,4-dihydro-pyrazol-3-on- 2-yl, benzimidazol-2-yl, furan-2-yl, 4-methyl-4H- [1,2,4] triazol-3-yl, 3- (4'-chlorophenyl) - [1,2,4 ] oxadiazol-5-yl, NHC (O) Me, NHC (O) Et, NHC (O) Ph, or NHSO2Me; m is 0-5; k is 0-1; each of R1 is independently -X-RX; X is a bond or is an optionally substituted C1-C6 alkylidene chain in which up to two methylene units of 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-, - N
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