Invention Grant
US09376387B2 Oxidisable pyridine derivatives, their preparation and use as anti-alzheimer agents
有权
可氧化吡啶衍生物,其制备和用作抗阿尔茨海默病药物
- Patent Title: Oxidisable pyridine derivatives, their preparation and use as anti-alzheimer agents
- Patent Title (中): 可氧化吡啶衍生物,其制备和用作抗阿尔茨海默病药物
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Application No.: US14763222Application Date: 2014-01-24
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Publication No.: US09376387B2Publication Date: 2016-06-28
- Inventor: Francis Marsais , Vincent Levacher , Cyril Papamicael , Pierre Bohn , Ludovic Peauger , Vincent Gembus , Nicolas Le Fur , Marie-Laurence Dumartin-Lepine
- Applicant: INSA (INSTITUT NATIONAL DES SCIENCES APPLIQUEES) DE ROUEN , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) , UNIVERSITE DE ROUEN , VFP THERAPIES
- Agency: Duane Morris LLP
- Priority: EP13305088 20130125
- International Application: PCT/EP2014/051392 WO 20140124
- International Announcement: WO2014/114742 WO 20140731
- Main IPC: C07D211/84
- IPC: C07D211/84 ; C07D213/61 ; C07D401/06 ; C07D405/06 ; C07D213/50 ; C07D213/56 ; C07D213/80 ; C07D213/803 ; C07D213/71 ; C07D213/70 ; C07D213/57 ; C07D213/82 ; C07D213/85 ; C07D211/82 ; C07D211/90

Abstract:
A compound of formula (I) in which the dotted lines indicate the presence of at least one double bond; n=0 to 4; R3 and R4 are H, or when n=1, R3 and R4 can also form together a double bond between the carbon atoms, and m=0, 1 or 2, Z is CH or N or Z is C and —CHR3— is ═CH— linked by the double bond to cyclopentanone; or −(−)m- is absent, and Z is NH, >N-alkyl, >N-phenyl, >N-benzyl or >N heteroaryl; R8 is alkyl, aryl or heteroaryl which can be optionally substituted; EWG represents an electron withdrawing group selected from the group comprising COOR, COSR, CONRR′, CN, COR, CF3, SOR, SO2R, SONRR′, SO2NRR′, NO2, halogen, heteroaryl; and the pharmaceutical salts and stereisomers thereof. The compounds of formula (I) are potent in the treatment of neurodegenerative diseases such as Alzheimer's disease.
Public/Granted literature
- US20150353493A1 OXIDISABLE PYRIDINE DERIVATIVES, THEIR PREPARATION AND USE AS ANTI-ALZHEIMER AGENTS Public/Granted day:2015-12-10
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