HOCUTT, FRANCES MEREDITH,LEONARD, BARRY EASTMAN,PELTIER, HILLARY M.,PHUONG, VICTOR K.,RABINOWITZ, MICHAEL H.,ROSEN, MARK D.,TARANTINO, KYLE T.,VENKATESAN, HARIHARAN,ZHAO, LUCY XIUMIN
申请号：
ES09739552
公开号：
ES2523720T3
申请日:
2009.04.28
申请国别(地区):
ES
年份:
2014
代理人:
摘要：
A compound having PHD inhibitor activity of formula (I): ** ** Formula wherein: ~ n is 2-4 each R 1 is independently selected from H, halogen, -C1-4alkyl, -cycloalkyl C3- 8, -perhaloalkyl group C1-4, C1-4 trifluoroalkoxy, -OH, -NO2, -CN, CO2H, -O-C1-4alkyl, -S-C1-4 alkyl, -S (C1-4 alkyl) -Rc , -S (O) 2 (C1-4 alkyl) -R c, - S (O) -C1-4alkyl, -SO2-C1-4alkyl, -S-Rc, -S (O) -R c, -SO2 -Rc, -SO2-NH-Rc, -O-Rc, -CH2-O-Rc, -C (O) NH-Rc, NRaRb, benzyloxy optionally substituted with Rd, phenyl or monocyclic heteroaryl optionally substituted with Rd, - C3-8cycloalkyl optionally containing one or more O, S or N wherein said -C 3-8 cycloalkyl is optionally substituted with Rd, benzyloxy-phenyl optionally substituted with up to three halo, cyanobiphenyl-4- ilmetilsulfanilo, cyano-biphenyl- 4-ilmetanosulfonilo, -S- (CH2) 2-morpholine and -C (O) -NH-morpholine, and two adjacent R1 groups may be joined to form a 3-8 membered ring optionally substituted or pcionalmente containing one or more O, S or N Ra and Rb are each independently H, C1-4 alkyl, -C (O) C1-4alkyl, -C (O) -R c, -C (O) CH2-Re, Re-C1-4alkyl, - SO2 -Rc, -SO2-C1-4 alkyl, phenyl optionally substituted with Rd, benzyl optionally substituted with Rd or monocyclic heteroaryl ring optionally substituted with Rd or Ra and Rb may be taken together with the nitrogen to which they are attached to form a monocyclic heterocycloalkyl ring optionally substituted, optionally containing one or more heteroatoms Rc is C3-8 -cycloalkyl, phenyl optionally substituted with Rd, benzyl optionally substituted with Rd, or monocyclic heteroaryl ring optionally substituted with Rd Rd is independently -H, halogen, -OH, -C1-4alkyl or C1-4 -perhaloalkyl group, trifluoro C1-4, -OC 1-4 alkyl, - O-phenyl or -O-benzyl Re is C3-8 -heterocycloalkyl optionally containing one or more O, S or N R2 and R3 are both H, -CF3 or C1-3 alkyl each Z is C or each Z is C or N, provided that exactly two Z are N simultaneously and enantiomers, diastereomers, racemates,
