发明公开
EP0342558A3 2-amino-4,5-methyleneadipic acid compounds for treatment of CNS disorders
失效
用于治疗CNS疾病的2-氨基-4,5-甲亚胺酸化合物
- 专利标题: 2-amino-4,5-methyleneadipic acid compounds for treatment of CNS disorders
- 专利标题(中): 用于治疗CNS疾病的2-氨基-4,5-甲亚胺酸化合物
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申请号: EP89108637.3申请日: 1989-05-12
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公开(公告)号: EP0342558A3公开(公告)日: 1990-12-27
- 发明人: Cordi, Alexis A. , Marinozzi, Maura , Lanthorn, Thomas H. , Monahan, Joseph B. , Natalini, Benedetto , Pellicciari, Roberto
- 申请人: G.D. Searle & Co.
- 申请人地址: P.O. Box 5110 Chicago Illinois 60680 US
- 专利权人: G.D. Searle & Co.
- 当前专利权人: G.D. Searle & Co.
- 当前专利权人地址: P.O. Box 5110 Chicago Illinois 60680 US
- 代理机构: Beil, Hans Chr., Dr.
- 优先权: US194361 19880516
- 主分类号: C07C229/28
- IPC分类号: C07C229/28 ; C07C271/06 ; C07C235/72 ; A61K31/195 ; A61K31/215 ; A61K31/325
摘要:
Compounds, compositions and methods are described for treating a CNS disorder such as a cognitive disorder, epilepsy, depression, Parkinson's disease, Alzheimer's disease, a neurodegenerative disease or neurotoxic injury. Compound of interest are 2-amino-4,5-methyleneadipic acid compounds and derivatives defined by the formula I:
wherein R¹ is selected from hydrido, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl,
with each of R², R³, R⁴ and R⁵ being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein each of X and Y is independently selected from hydroxyl, alkoxy, alkylthio, amino and
with each of R⁶ and R⁷ being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein any of R¹ through R⁷ groups having a substitutable position may be substituted with one or more substituents selected from hydroxyl, halo, alkyl, haloalkyl, cyano, alkoxy, alkylthio, sulfinyl, sulfonyl, sulfinylalkyl, sulfonylalkyl, amino, acyl, acyloxy, alkoxycarbonyl and aminocarbonyl; or a pharmaceutically-acceptable salt thereof. The 2R,4S,5S isomers and the 2R,4R,5R isomers of these compounds are preferred.
wherein R¹ is selected from hydrido, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl,
with each of R², R³, R⁴ and R⁵ being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein each of X and Y is independently selected from hydroxyl, alkoxy, alkylthio, amino and
with each of R⁶ and R⁷ being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein any of R¹ through R⁷ groups having a substitutable position may be substituted with one or more substituents selected from hydroxyl, halo, alkyl, haloalkyl, cyano, alkoxy, alkylthio, sulfinyl, sulfonyl, sulfinylalkyl, sulfonylalkyl, amino, acyl, acyloxy, alkoxycarbonyl and aminocarbonyl; or a pharmaceutically-acceptable salt thereof. The 2R,4S,5S isomers and the 2R,4R,5R isomers of these compounds are preferred.
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