MITCHELL, IAN S.,BLAKE, JAMES F.,XU, RUI,KALLAN, NICHOLAS C.,XIAO, DENGMING,SPENCER, KEITH LEE,BENCSIK, JOSEF R.,LIANG, JUN,SAFINA, BRIAN,LI, JUN,CHABOT, CHRISTINE,BANKA, ANNA.L.,WALLACE, ELI. M.,SCHL
申请号:
ES07799329
公开号:
ES2372955T3
申请日:
2007.07.05
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of the Formula: and its enantiomers and salts, in which: R1 and R1a are independently selected from H, Me, Et, CH = CH2. CH2OH, CF3, CHF2 or CH2F; R2 and R2a are independently selected from H or F; R5 is H, Me, Et, or CF3; A is where G is phenyl optionally substituted with one to four R9 groups or a 5-6 membered monocyclic or 9-membered bicyclic heteroaryl optionally substituted by a halogen; R6 and R7 are independently H, (C3-C6 cycloalkyl) - (CH2), (C3-C6 cycloalkyl) - (CH2CH2), V- (CH2) 0-1 in which V is a 5-6 heteroaryl members, W- (CH2) 1-2 wherein W is phenyl optionally substituted with F, Cl, Br, I OMe, CF3 or Me, C3-C6 cycloalkyl, hydroxy- (C3-C6 cycloalkyl), fluoro- (cycloalkyl C3-C6), CH (CH3) CH (OH) phenyl, 4-6 membered heterocycle optionally substituted with F, OH, cyclopropylmethyl, C1-C3 alkyl or C (= O) (C1-C3 alkyl) or C1- alkyl C6 optionally substituted with one or more groups independently selected from OH, oxo, O (C1C6 alkyl), CN, F, NH2, NH (C1-C6 alkyl), N (C1-C6 alkyl) 2, tetrahydropyranyl, tetrahydrofuranyl , morpholinyl, oxetanyl, piperidinyl and pyrrolidinyl, or R6 and R7 together with the nitrogen to which they form form a 3-6 membered heterocyclic ring optionally substituted with one or more groups independently selected from OH, halogen, oxo, CF3 , CH2CF3, CH2CH2OH, C (= O) CH3 and alky yl (C1-C3); Ra and Rb are H, or Ra is H and Rb and R6 together with the atoms to which they bind form a 5-6 membered heterocyclic ring having one or two ring nitrogen atoms; Rc and Rd are H or Me, or Rc and Rd together with the atom to which they are attached form a cyclopropyl ring; or R8 is H, Me, or OH, or R8 and R6, together with the atoms to which they bind form a 5-6 membered heterocyclic ring having one or two ring atoms; each of R9 is independently halogen, C1-C6 alkyl, C3-C6 cycloalkyl, O- (C1-C6 alkyl), CF3, OCF3, S (C6C1 alkyl), CN, OCH2-phenyl, CH2O-phenyl, NH2, NO 5 2 NH- (C1-C6 alkyl), N- (C1-C6 alkyl) 2, piperidine, pyrrolidine,