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1. 发明公开

EP0317953A2 N-(1-thienylcycloalkyl)alkenylamines for treatment of neurotoxic injury 失效
标题翻译： N-（1-噻吩基环烷基）烯基胺zur Behandlung von neurotoxischen Krankheiten。
公开(公告)号：EP0317953A2
公开(公告)日：1989-05-31
申请号：EP88119410.4
申请日：1988-11-22
申请人： G.D. Searle & Co.
发明人： Rice, Kenner C. , Jacobson, Arthur E. , Thurkauf, Andrew , Mattson, Mariena V. , O'Donohue, Thomas L. , Contreras, Patricia C. , Gray, Nancy M.
IPC分类号： C07D333/20 , C07D409/06 , A61K31/38 , A61K31/44
CPC分类号： C07D409/06 , C07D333/20
摘要： Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an N-(1-thienylcycloalkyl)alkenylamine compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula
wherein R¹ is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; wherein each of R² is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl, oxo and alkoxy; wherein R⁵ is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; and wherein the broken line within the N-containing ring represents a double bond between any two adjacent carbon atoms involving the 3-, 4- and 5-positions of the N-containing ring.
摘要翻译：描述了治疗的化合物，组合物和方法以控制与缺氧或缺血相关的脑损伤，其通常在中风，心脏骤停或围产期窒息之后。该治疗包括施用N-（1-噻吩基环烷基）链烯基胺化合物作为拮抗剂以抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用。最感兴趣的化合物是式CHEM的化合物，其中R 1是一个或多个选自氢化物，1至约5个碳原子的烷基，3至约5个碳原子的环烷基，2至约5个的烯基碳原子，羟基和烷氧基; 其中R 2为选自氢化物，1至约5个碳原子的烷基，3至约5个碳原子的环烷基，2至约5个碳原子的链烯基，羟基，氧代和烷氧基的一个或多个基团; 其中R 5为一个或多个选自氢化物，一至约五个碳原子的烷基，三至五个碳原子的环烷基，二至五个碳原子的烯基，羟基和烷氧基; 并且其中所述含N环的虚线表示涉及所述含N环的3-，4-和5-位的任何两个相邻碳原子之间的双键。

2. 发明公开

EP0317953A3 N-(1-thienylcycloalkyl)alkenylamines for treatment of neurotoxic injury 失效
标题翻译：用于治疗神经毒性损伤的N-（1-三烯基二甲基）亚苄基胺
公开(公告)号：EP0317953A3
公开(公告)日：1990-12-05
申请号：EP88119410.4
申请日：1988-11-22
申请人： G.D. Searle & Co.
发明人： Rice, Kenner C. , Jacobson, Arthur E. , Thurkauf, Andrew , Mattson, Mariena V. , O'Donohue, Thomas L. , Contreras, Patricia C. , Gray, Nancy M.
IPC分类号： C07D333/20 , C07D409/06 , A61K31/38 , A61K31/44
CPC分类号： C07D409/06 , C07D333/20
摘要： Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an N-(1-thienylcycloalkyl)alkenylamine compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula
wherein R¹ is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; wherein each of R² is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl, oxo and alkoxy; wherein R⁵ is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; and wherein the broken line within the N-containing ring represents a double bond between any two adjacent carbon atoms involving the 3-, 4- and 5-positions of the N-containing ring.
摘要翻译：描述了治疗的化合物，组合物和方法以控制与缺氧或缺血相关的脑损伤，其通常在中风，心脏骤停或围产期窒息之后。该治疗包括施用N-（1-噻吩基环烷基）链烯基胺化合物作为拮抗剂以抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用。最感兴趣的化合物是式CHEM的化合物，其中R 1是一个或多个选自氢化物，1至约5个碳原子的烷基，3至约5个碳原子的环烷基，2至约5个的烯基碳原子，羟基和烷氧基; 其中R 2为选自氢化物，1至约5个碳原子的烷基，3至约5个碳原子的环烷基，2至约5个碳原子的链烯基，羟基，氧代和烷氧基的一个或多个基团; 其中R 5为一个或多个选自氢化物，一至约五个碳原子的烷基，三至五个碳原子的环烷基，二至五个碳原子的烯基，羟基和烷氧基; 并且其中所述含N环的虚线表示涉及所述含N环的3-，4-和5-位的任何两个相邻碳原子之间的双键。

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