公开(公告)号：EP0342558B1

公开(公告)日：1994-02-02

申请号：EP89108637.3

申请日：1989-05-12

申请人： G.D. Searle & Co.

发明人： Cordi, Alexis A. ,  Marinozzi, Maura ,  Lanthorn, Thomas H. ,  Monahan, Joseph B. ,  Natalini, Benedetto ,  Pellicciari, Roberto

IPC分类号： C07C229/28 ,  C07C271/06 ,  C07C235/72 ,  A61K31/195 ,  A61K31/215 ,  A61K31/325

CPC分类号： C07C233/48 ,  C07C229/46 ,  C07C271/22 ,  C07C2601/02

公开(公告)号：EP0342558A3

公开(公告)日：1990-12-27

申请号：EP89108637.3

申请日：1989-05-12

申请人： G.D. Searle & Co.

发明人： Cordi, Alexis A. ,  Marinozzi, Maura ,  Lanthorn, Thomas H. ,  Monahan, Joseph B. ,  Natalini, Benedetto ,  Pellicciari, Roberto

IPC分类号： C07C229/28 ,  C07C271/06 ,  C07C235/72 ,  A61K31/195 ,  A61K31/215 ,  A61K31/325

CPC分类号： C07C233/48 ,  C07C229/46 ,  C07C271/22 ,  C07C2601/02

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.

摘要翻译： 描述了用于治疗诸如认知障碍，癫痫症，抑郁症，帕金森病，阿尔茨海默病，神经变性疾病或神经毒性损伤的CNS病症的化合物，组合物和方法。 化合物是2-氨基-4,5-亚甲基己二酸化合物和由式I定义的衍生物：其中R 1选自氢，烷基，环烷基，芳烷基，芳氧基烷基，芳硫基烷基， R 2，R 3，R 4和R 5各自独立地选自氢，烷基，环烷基，芳基和芳烷基; 其中X和Y各自独立地选自羟基，烷氧基，烷硫基，氨基和，每个R 6和R 7独立地选自氢，烷基，环烷基，芳基和芳烷基; 其中具有可取代位置的R 1至R 7中的任一个可以被一个或多个选自羟基，卤素，烷基，卤代烷基，氰基，烷氧基，烷硫基，亚磺酰基，磺酰基，亚磺基烷基，磺酰基烷基，氨基 ，酰基，酰氧基，烷氧基羰基和氨基羰基; 或其药学上可接受的盐。 这些化合物的2R，4S，5S异构体和2R，4R，5R异构体是优选的。

公开(公告)号：EP0342558A2

公开(公告)日：1989-11-23

申请号：EP89108637.3

申请日：1989-05-12

申请人： G.D. Searle & Co.

发明人： Cordi, Alexis A. ,  Marinozzi, Maura ,  Lanthorn, Thomas H. ,  Monahan, Joseph B. ,  Natalini, Benedetto ,  Pellicciari, Roberto

IPC分类号： C07C229/28 ,  C07C271/06 ,  C07C235/72 ,  A61K31/195 ,  A61K31/215 ,  A61K31/325

CPC分类号： C07C233/48 ,  C07C229/46 ,  C07C271/22 ,  C07C2601/02

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.