BOYS, MARK LAURENCE,DELISLE, ROBERT KIRK,HICKEN, ERIK JAMES,KENNEDY, APRIL L.,MARESKA, DAVID A.,MARMSATER, FREDRIK P.,MUNSON, MARK C.,NEWHOUSE, BRAD,RAST, BRYSON,RIZZI, JAMES P.,RODRIGUEZ, MARTHA E.,T
申请号:
ES11808427
公开号:
ES2540996T3
申请日:
2011.12.13
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound with the general formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is hetAr1 (CH2) m-, hetAr2CH2-, hetAr3CH2-, (C3-6 cycloalkyl) -CH2-, hetCyc1CH2-, Ar1 ( CH2) n- or (N-C1-3alkyl) pyridinonyl-CH2-; hetAr1 is a 6-membered heteroaryl that has 1-2 N ring atoms and is optionally substituted with one or more substituents independently selected from: (C1-6) alkyl, (C1-4) alkoxy, halogen, CF3 or (C3) cycloalkyl -6); m is 0, 1 or 2; hetAr2 is a 5-membered heteroaryl ring having 2-3 ring heteroatoms independently selected from N and S where at least one of said heteroatoms is N, wherein said ring is optionally substituted with one or more substituents independently selected from alkyl ( C1-6); hetAr3 is a 5,6-fused, bicyclic heteroaryl ring having two ring nitrogen atoms; hetCyc1 is a 6-membered saturated heterocyclic ring having 1-2 ring heteroatoms independently selected from N and O and optionally substituted with -C (>; = O) (C1-6 alkyl) or - C (>; = O) O ( C1-6 alkyl); Ar1 is phenyl optionally substituted with one or more substituents independently selected from: halogen, (C1-6) alkyl, CN, CF3, OH, (C1-6) alkoxy, -C (>; = O) OH, -C (>; = O) O ((C1-6) alkyl, - C (>; = O) NRaRb or benzyloxy; Ra and Rb are independently H or (C1-6) alkyl; n is 0, 1 or 2; R2 is H, F, Cl or CH3; R3 is H, F or Cl; R4 is H, CN, F, Cl, Br, -OMe, -OCF3, -CF3, -CH (OH) CH2OH or -C (>; = O) NH2; R5 is selected from: H, halogen, CN, OH, hetAr4, hetAr5, hetCyc2, hetCyc3 (C1-4 alkyl) -, hetCyc4alkoxy (C1-4), hetCyc5alkoxy (C1-4), (C1-3 alkoxy) alkoxy (C1 -4), hydroxyalkoxy (C1-6), dihydroxyalkoxy (C2-6), alkoxy (C1-6), [hydroxyalkyl (C2-4)) amino] -alkyl (C1-4), [(C1-4 alkoxy) (C1-4 alkyl) amino] (C1-4) alkyl, [di (C1-4 alkyl) amino] (C1-4) alkyl, (C1-4 alkyl) C (>; = O) -, (C1-) hydroxyalkyl 6), dihydroxyalkyl (C2-6), [di (C1-3 alkyl) amino] (C1-4) alkoxy, N- (C1-3 alkyl) pyridinone, hetAr6, hetCyc6C (>; = O) -, (hetCyc7) -O-, hetCyc8alkoxy (C1-4), difl