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公开(公告)号:US20080032950A1
公开(公告)日:2008-02-07
申请号:US11630707
申请日:2005-06-24
申请人: Mary Chebib , Rohan Kumar , Graham Johnston , Hane Hanrahan
发明人: Mary Chebib , Rohan Kumar , Graham Johnston , Hane Hanrahan
CPC分类号: C07F9/303
摘要: The invention provides a compound of the formula I: wherein R is methyl, ethyl, propyl, isopropyl, butyl, pentyl, neo-pentyl or cyclohexyl, or a salt or solvate thereof. These compounds are selective GABAC receptor antagonists. The invention also provides pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt or solvate thereof. The invention also provides methods of enhancing the cognitive activity of an animal and methods of stimulating memory capacity in an animal, comprising the step of administering to the animal an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof.
摘要翻译: 本发明提供式I化合物或其盐或溶剂合物:其中R是甲基,乙基,丙基,异丙基,丁基,戊基,新戊基或环己基。 这些化合物是选择性GABA C受体拮抗剂。 本发明还提供包含式I化合物或其药学上可接受的盐或溶剂化物的药物组合物。 本发明还提供增强动物的认知活动的方法和刺激动物记忆能力的方法,其包括向动物施用有效量的式I化合物或其药学上可接受的盐或溶剂合物的步骤。
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公开(公告)号:US20050004083A1
公开(公告)日:2005-01-06
申请号:US10496904
申请日:2002-11-29
申请人: Mary Chebib , Jane Hanrahan , Graham Johnston
发明人: Mary Chebib , Jane Hanrahan , Graham Johnston
CPC分类号: C07F9/303
摘要: The invention provides compounds of the formula II: wherein R represents propyl, butyl, pentyl, neo-pentyl or cyclohexyl, and salts thereof. These compounds are selective GABAC receptor antagonists. The invention also provides a method of enhancing the cognitive activity of an animal and a method of stimulating memory capacity in an animal, comprising administering to the animal an effective amount of a compound of formula II or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供式II化合物:其中R代表丙基,丁基,戊基,新戊基或环己基,及其盐。 这些化合物是选择性GABAC受体拮抗剂。 本发明还提供了增强动物的认知活性的方法和刺激动物记忆能力的方法,其包括向动物施用有效量的式II化合物或其药学上可接受的盐。
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3.
公开(公告)号:US5227485A
公开(公告)日:1993-07-13
申请号:US717202
申请日:1991-06-19
IPC分类号: C07D487/04
CPC分类号: C07D487/04
摘要: The A21 receptor extracelluar site and the A2 receptor extracellular site of adenosine analogues are structurally different and that binding orientations of adenosine or adenosine analogues are different at these sites and this may be used to determine their structure. Novel pyrimidine compounds are described.
摘要翻译: 腺苷类似物的A21受体胞外位点和A2受体胞外位点在结构上是不同的,并且腺苷或腺苷类似物的结合取向在这些位点是不同的,并且这可以用于确定其结构。 描述了新的嘧啶化合物。
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公开(公告)号:US06962907B2
公开(公告)日:2005-11-08
申请号:US10496904
申请日:2002-11-29
IPC分类号: A61P25/28 , C07F9/30 , A61K31/662
CPC分类号: C07F9/303
摘要: The invention provides compounds of the formula II: wherein R represents propyl, butyl, pentyl, neo-pentyl or cyclohexyl, and salts thereof. These compounds are selective GABAC receptor antagonists. The invention also provides a method of enhancing the cognitive activity of an animal and a method of stimulating memory capacity in an animal, comprising administering to the animal an effective amount of a compound of formula II or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供式II化合物:其中R代表丙基,丁基,戊基,新戊基或环己基,及其盐。 这些化合物是选择性GABA C受体拮抗剂。 本发明还提供了增强动物的认知活性的方法和刺激动物记忆能力的方法,其包括向动物施用有效量的式II化合物或其药学上可接受的盐。
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公开(公告)号:US06632806B1
公开(公告)日:2003-10-14
申请号:US09446721
申请日:1999-12-22
IPC分类号: A61K31675
CPC分类号: A61K31/675 , C07F9/59
摘要: The invention provides methods for enhancing cognitive activity and stimulating memory capacity, comprising the step of administering an effective amount of a compound with GABAC receptor antagonist activity to an animal in need of such treatment. Preferably the compound has selective GABAc receptor antagonist activity, and more preferably comprises a phosphinic acid group. The invention also provides novel compounds and compositions. The methods of the invention are useful in the treatment of dementias and conditions involving cognitive deficit, or memory impairment.
摘要翻译: 本发明提供了增强认知活动和刺激记忆能力的方法,包括向有需要的动物施用有效量的具有GABA u> PDA受体拮抗剂活性的化合物的步骤 治疗。 优选地,化合物具有选择性GABA u> PDAT>受体拮抗剂活性,更优选包含次膦酸基团。 本发明还提供新的化合物和组合物。 本发明的方法可用于治疗痴呆和涉及认知缺陷或记忆障碍的病症。 PTEXT>
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