| abstract |
A compound having PHD inhibitor activity of formula (I): ** Formula ** in which: ~ n is 2-4 each R1 is independently selected from H, halogen, -C 1-4 alkyl, -C3 -cycloalkyl- 8, -C 1-4 alkylhaloalkyl, C 1-4 trifluoroalkoxy, -OH, -NO2, -CN, CO2H, -O-C 1-4 alkyl, -S-C 1-4 alkyl, -S (C 1-4 alkyl) -Rc , -S (O) 2 (C1-4 alkyl) -Rc, - S (O) -C1-4 alkyl, -SO2-C1-4 alkyl, -S-Rc, -S (O) -Rc, -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, - C3-8 cycloalkyl which optionally contains one or more O, S or N in which said C3-8 cycloalkyl is optionally substituted with Rd, benzyloxy-phenyl optionally substituted with up to three halogen, cyanobiphenyl-4-ylmethylsulfanyl, cyano-biphenyl- 4-ylmethanesulfonyl, -S- (CH2) 2-morpholine and -C (O) -NH-morpholine, and two adjacent R1 groups can be joined to form an optionally substituted 3-8 membered ring that or it optionally contains one or more O, S or N; Ra and Rb are each independently H, C1-4 alkyl, -C (O) C1-4 alkyl, -C (O) -Rc, -C (O) CH2-Re, C1-4 alkyl, - 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 can be taken together with the nitrogen to which they are attached to form an optionally substituted monocyclic heterocycloalkyl ring that optionally contains one or more heteroatoms; Rc is C3-8 -cycloalkyl, phenyl optionally substituted with Rd, benzyl optionally substituted with Rd, or a monocyclic heteroaryl ring optionally substituted with Rd; Rd is independently -H, halogen, -OH, -C 1-4 alkyl or -C 1-4 alkylhalo, C 1-4 trifluoroalkoxy, -O-C 1-4 alkyl, -O-phenyl or -O-benzyl; Re is C 3-8 heterocycloalkyl which optionally contains 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 simultaneously N; and enantiomers, diastereomers, racemates and pharmaceutically acceptable salts thereof. |