公开(公告)号：US10017480B2

公开(公告)日：2018-07-10

申请号：US15119034

申请日：2015-02-10

申请人： UNIVERSITÂ DEGLI STUDI DI GENOVA ,  THE TRUSTEES OF COLUMBIA UNIVERSITY ,  MAASTRICHT UNIVERSITY

发明人： Olga Bruno ,  Chiara Brullo ,  Alessia Romussi ,  Ernesto Fedele ,  Roberta Ricciarelli ,  Ottavio Arancio ,  Jos Prickaerts

IPC分类号： C07D207/34 ,  C07D207/337 ,  C07D231/12 ,  C07D261/04 ,  C07D261/08 ,  C07D261/18 ,  C07D401/06 ,  C07D413/06 ,  C07D403/06

CPC分类号： C07D261/04 ,  C07D207/337 ,  C07D207/34 ,  C07D231/12 ,  C07D261/08 ,  C07D261/18 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06

摘要： Compounds of formula (I), wherein Z=cyclopentyl. cyclopropylmethyl, —CH3; R′═—CH3, CHF2, X=formula (II) (III) (IV) (V) Y=—CO; —C═O(CH2), —CH(OH)—CH2, —CH2—C═O, —CH2—CH2—C═O; —CH2—CH(OH)—CH2, —CH2—CH(OCOR1)—CH2 NR2═ —N(CH2—CH2OH)2, formula (VI) (VII) (VIII) (IX) (X) (XI) R1=optionally substituted C1-C8 alkyl, optionally substituted aryl; optionally substituted aralkyl, preferably C1-C3 alkyl, more preferably CH3; and enantiomers, diastereoisomers and pharmaceutically acceptable salts thereof; these compounds have a PDE4D inhibiting activity and can be used as a medicament for treating dementia, in particular Alzheimer disease, and for improving memory.