Hadida Ruah, Sarah S.,Hazlewood, Anna R.,Grootenhuis, Peter D. J.,Van Goor, Fredrick F.,Singh, Ashvani K.,Zhou, Jinglan,McCartney, Jason
申请号:
ES12152225
公开号:
ES2628026T3
申请日:
2005.06.24
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula VA-1: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein each of WRW2 and WRW4 is independently selected from hydrogen, CN, CF3, halogen, linear or branched C1-C6 alkyl, 3-12 membered cycloaliphatic, phenyl, C5-C10 heteroaryl or C3-C7 heterocyclic, wherein said heteroaryl or heterocyclic has up to 3 heteroatoms selected from O, S or N, wherein said WRW2 and WRW4 are independently and optionally substituted with up to three substituents selected from -OR ', -CF3, -OCF3, SR', S (O) R ', SO2R', -SCF3, halogen, CN, -COOR ', - COR', -O (CH2) 2N (R ') (R'), -O (CH2) N (R ') (R'), -CON (R ') (R'), - (CH2) 2OR ', - (CH2) OR', CH2CN , optionally substituted phenyl or phenoxy, -N (R ') (R'), -NR'C (O) OR ', -NR'C (O) R', - (CH2) 2N (R ') (R' ) or - (CH2) N (R ') (R'); and WRW5 is selected from hydrogen, -OH, NH2, CN, CHF2, NHR ', N (R') 2, -NHC (O) R ', -NHC (O) OR', NHSO2R ', -OR', CH2OH , CH2N (R ') 2, C (O) OR', SO2NHR 'SO2N (R') 2, CH2O (C1-C6 alkyl) or CH2NHC (O) OR '; and X is an RX bond is hydrogen; R 'is independently selected from hydrogen or an optionally substituted group selected from a C1-C8 aliphatic group, a saturated, partially unsaturated, or completely unsaturated 3-8 membered monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered saturated, partially unsaturated, or completely unsaturated bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or two occurrences of R 'taken together with the atoms to which they are attached to form an optionally substituted 3-12 membered saturated or partially unsaturated monocyclic or bicyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen , or sulfur; provided that: ** Formula ** of formula VA-1 is not phenyl, 2-methylphenyl, 2,4-dichlorophenyl, 2-bromophenyl, 4-bromophenyl, 2,4-dimethylphenyl, 2-ethylphenyl, 3-carboxylic acid phenyl, 2-fluorophenyl, 3-