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1. 发明授权

US5229413A Compositions containing indole-2-carboxylate compounds for treatment of CNS disorders 失效
标题翻译：含有吲哚-2-羧酸盐化合物的组合物，用于治疗中枢神经系统疾病
公开(公告)号：US5229413A
公开(公告)日：1993-07-20
申请号：US830108
申请日：1992-02-03
申请人： Nancy M. Gray , Brian K. Cheng , William F. Hood , Michael S. Dappen , Alex A. Cordi
发明人： Nancy M. Gray , Brian K. Cheng , William F. Hood , Michael S. Dappen , Alex A. Cordi
IPC分类号： A61K31/405
CPC分类号： A61K31/405
摘要： Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R.sup.5 and R.sup.6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R.sup.10 and R.sup.12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.
摘要翻译：含有某些吲哚-2-羧酸酯化合物和衍生物的组合物被描述为治疗由神经毒性损伤或神经变性疾病，特别是由缺血事件引起的CNS障碍引起的CNS障碍的治疗有效性。优选的化合物具有式“IMAGE”，其中R 5和R 6各自独立地选自氢，溴，氯和氟，并且其中R 10和R 12各自独立地选自氢和低级烷基及其药学上可接受的盐。

2. 发明授权

US5137910A Compositions containing indole-2-carboxylate compounds for treatment of CNS disorders 失效
标题翻译：含有吲哚-2-羧酸盐化合物的组合物，用于治疗中枢神经系统疾病
公开(公告)号：US5137910A
公开(公告)日：1992-08-11
申请号：US484530
申请日：1990-03-01
申请人： Nancy M. Gray , Brian K. Cheng , William F. Hood , Michael S. Dappen , Alex A. Cordi
发明人： Nancy M. Gray , Brian K. Cheng , William F. Hood , Michael S. Dappen , Alex A. Cordi
IPC分类号： A61K31/405
CPC分类号： A61K31/405
摘要： Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R.sup.5 and R.sup.6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R.sup.10 and R.sup.12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.
摘要翻译：含有某些吲哚-2-羧酸酯化合物和衍生物的组合物被描述为治疗由神经毒性损伤或神经变性疾病，特别是由缺血事件引起的CNS障碍引起的CNS障碍的治疗有效性。优选的化合物具有式“IMAGE”，其中R 5和R 6各自独立地选自氢，溴，氯和氟，并且其中R 10和R 12各自独立地选自氢和低级烷基及其药学上可接受的盐。

3. 发明授权

US5087633A Use of a glycine B partial agonist for memory and learning enhancement or treatment of a cognitive disorder 失效
标题翻译：使用甘氨酸B部分激动剂进行记忆和学习增强或治疗认知障碍
公开(公告)号：US5087633A
公开(公告)日：1992-02-11
申请号：US438494
申请日：1989-07-27
申请人： Alex A. Cordi , Gail E. Handelmann , Joseph B. Monahan
发明人： Alex A. Cordi , Gail E. Handelmann , Joseph B. Monahan
IPC分类号： A61K31/42
CPC分类号： A61K31/42
摘要： A class of Glycine B partial agonists is described for use in memory and learning enhancement or for treatment of a cognitive disorder. Preferred Glycine B partial agonists include the compound D-cycloserine and its prodrug compounds.
摘要翻译： PCT No.PCT / US88 / 04244 Sec。 371日期：1989年7月27日 102（e）日期1989年7月27日PCT提交1988年12月1日PCT公布。出版物WO89 / 05144 日期：1989年6月15日。一类甘氨酸B部分激动剂被用于记忆和学习增强或治疗认知障碍。优选的甘氨酸B部分激动剂包括化合物D-环丝氨酸及其前药化合物。

4. 发明授权

US5187171A Use of a Glycine B partial agonist as an antipsychotic 失效
标题翻译：使用糖苷B部分AGONIST作为抗生素
公开(公告)号：US5187171A
公开(公告)日：1993-02-16
申请号：US294851
申请日：1989-01-09
申请人： Alex A. Cordi
发明人： Alex A. Cordi
IPC分类号： C07D261/04 , A61K31/00 , A61K31/42 , A61P25/18
CPC分类号： A61K31/00 , A61K31/42
摘要： A class of Glycine B partial agonists is described for use for treatment of psychosis. Preferred Glycine B partial agonists include amino-isoxazolidone compounds such as D-cycloserine and its prodrugs.

5. 发明授权

US4918064A Phenyl glycines for use in reducing neurotoxic injury 失效
标题翻译：用于减少神经毒性损伤的苯基甘氨酸
公开(公告)号：US4918064A
公开(公告)日：1990-04-17
申请号：US111749
申请日：1987-10-21
申请人： Alex A. Cordi , Michael L. Vazquez
发明人： Alex A. Cordi , Michael L. Vazquez
IPC分类号： C07F9/44 , A61K31/66 , A61P9/10 , A61P25/04 , A61P25/08 , A61P25/28 , A61P39/02 , A61P43/00 , C07F9/38 , C07F9/40
CPC分类号： C07F9/3882 , C07F9/4056
摘要： A class of phenyl glycine compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phenyl glycine compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites.

6. 发明授权

US5075337A Alpha-deuterated 2-alkylaminoacetamide derivatives having reduced toxicity for treatment of CNS disorders 失效
标题翻译： α-氘代2-烷基氨基乙酰胺衍生物，对于治疗CNS障碍具有降低的毒性
公开(公告)号：US5075337A
公开(公告)日：1991-12-24
申请号：US385632
申请日：1989-07-26
申请人： Alex A. Cordi , Philippe Janssens de Varebeke , Hugo Gorissen
发明人： Alex A. Cordi , Philippe Janssens de Varebeke , Hugo Gorissen
IPC分类号： A61K31/16 , C07B59/00 , C07C237/06 , C07C275/50
CPC分类号： A61K31/16 , C07B59/001 , C07C237/06 , C07C275/50
摘要： Deuterated 2-alkylaminoacetamide compounds are described having the alpha carbon of the alkyl side chain of the compounds substituted by one or two deuterium atoms. These compounds have pharmacokinetic properties which enable treatment of CNS diseases with lower toxic effects. These compounds are also useful in evaluating the metabolic fate of non-deuterated counterpart compounds. Of particular interest are compounds of Formula I: ##STR1## wherein X is deutero or hydrido; wherein R.sup.1 is selected from alkyl and aralkenyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and alkyl; wherein each of R.sup.1, R.sup.2 and R.sup.3 having a substitutable position may be substituted with one or more halo radicals; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了具有被一个或两个氘原子取代的化合物的烷基侧链的α碳的氘代2-烷基氨基乙酰胺化合物。这些化合物具有药代动力学特性，能够治疗具有较低毒性作用的CNS疾病。这些化合物也可用于评估非氘化对应化合物的代谢命运。特别感兴趣的是式I的化合物：其中X是氘代或杂环的; 其中R1选自烷基和芳烯基; 其中R2和R3各自独立地选自氢和烷基; 其中具有可取代位置的R1，R2和R3中的每一个可以被一个或多个卤素基团取代; 或其药学上可接受的盐。

7. 发明授权

US5468763A Use of a glycine B partial agonist for memory and learning enhancement or treatment of a cognitive disorder 失效
标题翻译：使用甘氨酸B部分激动剂进行记忆和学习增强或治疗认知障碍
公开(公告)号：US5468763A
公开(公告)日：1995-11-21
申请号：US975298
申请日：1992-11-12
申请人： Alex A. Cordi , Gail E. Handelmann , Joseph B. Monahan
发明人： Alex A. Cordi , Gail E. Handelmann , Joseph B. Monahan
IPC分类号： A61K31/42 , A61K31/41
CPC分类号： A61K31/42 , Y10S514/879
摘要： A class of Glycine B partial agonists is described for use in memory and learning enhancement or for treatment of a cognitive disorder. Preferred Glycine B partial agonists include the compound D-cycloserine and its prodrug compounds.
摘要翻译：描述了一类用于记忆和学习增强或治疗认知障碍的甘氨酸B部分激动剂。优选的甘氨酸B部分激动剂包括化合物D-环丝氨酸及其前药化合物。

8. 发明授权

US4904681A D-cycloserine and its prodrugs as cognitive enhancers 失效
标题翻译： D-环丝氨酸及其前药作为认知增强剂
公开(公告)号：US4904681A
公开(公告)日：1990-02-27
申请号：US127121
申请日：1987-12-01
申请人： Alex A. Cordi , Gail E. Handelmann , Joseph B. Monahan
发明人： Alex A. Cordi , Gail E. Handelmann , Joseph B. Monahan
IPC分类号： C07D261/04 , A61K31/42 , A61P25/28
CPC分类号： A61K31/42
摘要： The compound D-4-amino-3-isoxazolidone, its pharmaceutically-acceptable salts and its prodrug compounds are described as having cognitive-enhancing activity.

9. 发明授权

US4882343A Biarylalkylimidazole derivatives as anti-depressants 失效
标题翻译：二芳基烷基咪唑衍生物作为抗抑郁剂
公开(公告)号：US4882343A
公开(公告)日：1989-11-21
申请号：US90890
申请日：1987-08-28
申请人： Alex A. Cordi , Hugo J. Gorissen
发明人： Alex A. Cordi , Hugo J. Gorissen
IPC分类号： A61K31/44 , A61K31/415 , A61K31/4427 , A61K31/4433 , A61P25/02 , A61P25/24 , A61P25/26 , C07D233/54 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06
CPC分类号： C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06
摘要： Certain 4(5)-(biarylethyl)imidazole derivatives are selectiv3 .alpha..sub.2 -adrenergic receptor blockers and are useful as anti-depressant agents.

10. 发明授权

US5288905A Glycyl urea derivatives as anti-convulsants 失效
标题翻译：甘氨酰脲衍生物作为抗惊厥药
公开(公告)号：US5288905A
公开(公告)日：1994-02-22
申请号：US761111
申请日：1991-09-17
申请人： Alex A. Cordi , Claude L. Gillet
发明人： Alex A. Cordi , Claude L. Gillet
IPC分类号： C07C275/50 , C07C275/48
CPC分类号： C07C275/50
摘要： A class of glycyl urea derivatives is described having use in treatment of CNS dysfunctions such as epilepsy and convulsive disorders. Compounds of interest are those of the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is a group independently selected from hydrido, alkyl, aralkyl, aryloxyalkyl and arylthioalkyl, any one of which groups having a substitutable position may be substituted with one or more radicals selected from halo, alkyl of one to about ten carbon atoms, alkenyl of two to about ten carbon atoms, alkynyl of two to about ten carbon atoms, haloalkyl, alkoxy, alkylthio, alkylsulfinyl and alkylsulfonyl; or a pharmaceutically-acceptable salt thereof; with the proviso that when each of R.sup.1 and R.sup.2 is ethyl, then R.sup.3 and R.sup.4 cannot be hydrido simultaneously.
摘要翻译：描述了一类甘氨酰脲衍生物用于治疗CNS功能障碍如癫痫和惊厥性疾病。感兴趣的化合物是式（*化学结构*）的化合物，其中R 1，R 2，R 3和R 4各自独立地选自氢，烷基，芳烷基，芳氧基烷基和芳硫基烷基，其中任何一个具有可取代位置的基团被一个或多个选自卤素，1至约10个碳原子的烷基，2至约10个碳原子的烯基，2至约10个碳原子的炔基，卤代烷基，烷氧基，烷硫基，烷基亚磺酰基和烷基磺酰基取代; 或其药学上可接受的盐; 条件是当R 1和R 2各自为乙基时，则R 3和R 4不能同时氢化。

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