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NEW CLASS OF SPIROPIPERIDINS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES.
专利权人:
PFIZER INC.
发明人:
BRODNEY, MICHAEL,HELAL, CHRISTOPHER,O'NEILL, BRIAN
申请号:
ES09742523
公开号:
ES2375913T3
申请日:
2009.05.04
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A compound of formula I: wherein the stereochemistry shown in formula I in the carbon bonded to R2 and in the spirocyclic carbon is the absolute stereochemistry; B is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, in which B is optionally substituted with zero to three R4 groups; Z is (CH2) n-Op- (CH2) qo a cycloalkylene moiety, with the proviso that when Z is (CH2) n-Op- (CH2) q, the terminal methylene of the chain (CH2) n is attached to the piperidinyl ring nitrogen; A is independently aryl, cycloalkyl, heterocycloalkyl or heteroaryl, wherein said aryl, cycloalkyl, heterocycloalkyl, or heteroaryl group is optionally substituted with one to three R1; each R1 is independently alkyl, halogen, cyano, SO2NHR9, CON (R8) 2, N (R8) COR8, SO2N (R8) 2, N (R8) SO2R8, COR8, SO2R8, cycloalkyl- (CH2) r, heterocycloalkyl- ( CH2) t, aryl- (CH2) t, heteroaryl- (CH2) t, (CH2) tN (R9) 2 or (CH2) t-OR6 in which each R1 alkyl, cycloalkyl- (CH2) t, heterocycloalkyl- ( CH2) t, aryl- (CH2) to heteroaryl- (CH2) t is optionally substituted independently with cyano, alkyl, halogen or OR6; R2 is alkyl, cycloalkyl or alkenyl in which said alkyl, cycloalkyl or alkenyl is optionally substituted by halogen, hydroxyl or cyano; R3A and R3B are each independently hydrogen, aryl, heteroaryl or alkyl optionally substituted with R1; or R3A and R3B together with the carbon to which they are attached form a C = O, C = NR8, a cycloalkylene moiety or a heterocycloalkylene moiety; each R4 is independently halogen, hydroxyl, cyano, halo, O-alkyl, O-cycloalkyl, SO2R8, N (R8) 2, COR8, CON (R8) 2, alkyl, cycloalkyl- (CH2) t, heterocycloalkyl- (CH2) t, aryl- (CH2) to heteroaryl- (CH2) t, wherein said R4 alkyl, cycloalkyl- (CH2) t, heterocycloalkyl- (CH2) t, aryl- (CH2) to heteroaryl- (CH2) t is optionally substituted with R1; each R5 is independently hydrogen alkyl, alkenyl, cycloalkyl- (CH2) t, heterocycloalkyl- (CH2), aryl- (CH2) to heteroaryl- (CH2) t, wherein said substituent R5 alkyl, alkenyl, cycloalky
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