发明授权
EP2744798B1 PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE
有权
PIPERAZINTHIAZOLDERIVATE阿尔茨海默病作为Tau蛋白病的治疗
- 专利标题: PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE
- 专利标题(中): PIPERAZINTHIAZOLDERIVATE阿尔茨海默病作为Tau蛋白病的治疗
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申请号: EP12756402.9申请日: 2012-08-17
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公开(公告)号: EP2744798B1公开(公告)日: 2016-03-30
- 发明人: GRIFFIOEN, Gerard , CECERE, Giuseppe , NETTEKOVEN, Matthias , PRINCEN, Katrien , RATNI, Hasane , ROGERS-EVANS, Mark , VIFIAN, Walter
- 申请人: reMYND NV
- 申请人地址: Bio-Incubator Gaston Geenslaan 1 3001 Leuven - Heverlee BE
- 专利权人: reMYND NV
- 当前专利权人: reMYND NV
- 当前专利权人地址: Bio-Incubator Gaston Geenslaan 1 3001 Leuven - Heverlee BE
- 代理机构: Bounaga, Sakina
- 优先权: EP11177742 20110817
- 国际公布: WO2013024168 20130221
- 主分类号: C07D417/14
- IPC分类号: C07D417/14 ; C07D285/08 ; C07D417/04 ; C07D417/12 ; A61K31/433 ; A61P25/28
摘要:
The present invention relates to a compound of formula (IA), wherein G1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is —NR2R3; R2 is hydrogen or lower alkyl; R3 is lower alkyl; tetrahydropyran-4-yl; —CH2-cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is —CH2—or —(CH2)2—; Ar is phenyl or pyridinyl; R4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
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