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1. 发明申请

US20120276196A1 Pharmaceutical Compositions of a Neuroactive Steroid and Methods of Use Thereof 审中-公开
标题翻译：神经活性类固醇的药物组合物及其使用方法
公开(公告)号：US20120276196A1
公开(公告)日：2012-11-01
申请号：US13464369
申请日：2012-05-04
申请人： Richard M. WOODWARD
发明人： Richard M. WOODWARD
IPC分类号： A61K31/58 , A61P15/00 , A61P25/24 , A61P25/32 , A61K9/48 , A61P25/22
CPC分类号： A61K9/1635 , A61K9/1617 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/5026 , A61K9/5078 , A61K31/58
摘要： The present invention relates to pharmaceutical compositions of the neuroactive steroid 3α-hydroxy-3β-methoxymethyl-21-(1′-imidazolyl)-5α-pregnan-20-one or a pharmaceutically-acceptable salt or solvate thereof, with properties desirable for use in treating mood disorders and the like. The pharmaceutical compositions provide sustained therapeutic plasma levels of 3α-hydroxy-3β-methoxymethyl-21-(1′-imidazolyl)-5α-pregnan-20-one. The present invention also relates to methods of treating these disorders by administering the pharmaceutical compositions.
摘要翻译：本发明涉及神经活性甾族化合物3α-羟基-3β-甲氧基甲基-21-（1'-咪唑基）-5α-孕烷-20-酮或其药学上可接受的盐或溶剂合物的药物组合物，用于治疗情绪障碍等。药物组合物提供3α-羟基-3β-甲氧基甲基-21-（1'-咪唑基）-5α-孕烷-20酮的持续治疗血浆水平。本发明还涉及通过施用药物组合物来治疗这些疾病的方法。

2. 发明申请

US20090131383A1 Pharmaceutical compositions of a neuroactive steriod and methods of use thereof 审中-公开
标题翻译：神经活性抑制剂的药物组合物及其使用方法
公开(公告)号：US20090131383A1
公开(公告)日：2009-05-21
申请号：US11921889
申请日：2006-06-09
申请人： Richard M. Woodward
发明人： Richard M. Woodward
IPC分类号： A61K31/58 , A61P25/22
CPC分类号： A61K9/1635 , A61K9/1617 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/5026 , A61K9/5078 , A61K31/58
摘要： The present invention relates to pharmaceutical compositions of the neuroactive steroid 3α-hydroxy-3β-methoxymethyl-21-(1′-imidazolyl)-5α-pregnan-20-one or a pharmaceutically-acceptable salt or solvate thereof, with properties desirable for use in treating mood disorders and the like. The pharmaceutical compositions provide sustained therapeutic plasma levels of 3α-hydroxy-3β-methoxymethyl-21-(1′-imidazolyl)-5α-pregnan-20-one. The present invention also relates to methods of treating these disorders by administering the pharmaceutical compositions.
摘要翻译：本发明涉及神经活性类固醇3α-羟基-3β-甲氧基甲基-21-（1'-咪唑基）-5α-孕烷-20-酮或其药学上可接受的盐或溶剂合物的药物组合物，其性质适合使用治疗情绪障碍等。药物组合物提供3α-羟基-3β-甲氧基甲基-21-（1'-咪唑基）-5α-孕烷-20酮的持续治疗血浆水平。本发明还涉及通过施用药物组合物来治疗这些疾病的方法。

3. 发明授权

US5637617A Methods for use of GABA.sub.a receptor GABAergic compounds 失效
标题翻译：使用GABAa受体GABA能化合物的方法
公开(公告)号：US5637617A
公开(公告)日：1997-06-10
申请号：US221883
申请日：1994-04-01
申请人： Richard M. Woodward , Ricardo Miledi
发明人： Richard M. Woodward , Ricardo Miledi
IPC分类号： A61K31/196 , A61K31/19
CPC分类号： A61K31/603 , A61K31/196
摘要： A method is disclosed for potentiating mammalian GABA.sub.A receptor responses to GABA. The receptor responses are potentiated according to the invention by contacting GABA.sub.A receptors with GABA and an effective amount of non-steroidal anti-inflammatory agents, in particular, fenamates and structurally related compounds.
摘要翻译：公开了一种增强哺乳动物GABA A受体对GABA的反应的方法。通过使GABA A受体与GABA和有效量的非甾体抗炎剂，特别是与其结构相关的化合物接触，根据本发明增强受体反应。

4. 发明申请

US20110071163A1 USE OF AN OPIOID RECEPTOR ANTAGONIST FOR THE TREATMENT OR PREVENTION OF GASTROINTESTINAL TRACT DISORDERS 审中-公开
标题翻译：使用阿片受体拮抗剂治疗或预防胃肠疾病
公开(公告)号：US20110071163A1
公开(公告)日：2011-03-24
申请号：US12884985
申请日：2010-09-17
申请人： Richard M. WOODWARD
发明人： Richard M. WOODWARD
IPC分类号： A61K31/497 , C07D403/12 , A61P1/00
CPC分类号： A61K31/497
摘要： The disclosure relates to a method of treating or preventing a condition in a subject associated with the activation of an opioid receptor in the periphery by administering an effective amount of 5-(2-methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl}-phenoxy)-pyrazine-2-carboxamide (Compound I). In particular, the disclosure relates to a method of treating or preventing opioid-induced constipation or opioid-induced bowel dysfunction in a human without reducing centrally-mediated opioid analgesia or producing central opioid withdrawal symptoms by administering an effective amount of Compound I. The disclosure further relates to the use of Compound I for the preparation of a medicament for the treatment or prevention of a condition in a subject associated with the activation of an opioid receptor in the periphery.
摘要翻译：本公开内容涉及通过施用有效量的5-（2-甲氧基-4 - {[2-（四氢 - 吡喃-2-基） - 哌嗪-1-基）吡啶-4-基） - 乙基氨基] - 甲基} - 苯氧基） - 吡嗪-2-甲酰胺（化合物I）。特别地，本公开涉及一种治疗或预防人类阿片样物质诱发的便秘或阿片样物质诱导的肠功能障碍的方法，而不会通过施用有效量的化合物I而减少中枢介导的阿片样镇痛或产生中枢阿片样物质戒断症状。进一步涉及化合物I用于制备用于治疗或预防与周围阿片受体活化相关的受试者中的病症的药物的用途。

5. 发明授权

US5627169A Selective antagonists for GABA.sub.rho receptor 失效
标题翻译： GABArho受体的选择性拮抗剂
公开(公告)号：US5627169A
公开(公告)日：1997-05-06
申请号：US277735
申请日：1994-07-20
申请人： Ricardo Miledi , Larry E. Overman , Yoshinori Murata , Richard M. Woodward
发明人： Ricardo Miledi , Larry E. Overman , Yoshinori Murata , Richard M. Woodward
IPC分类号： C07F9/553 , C07F9/572 , C07F9/59 , C07F9/58 , A61K31/675
CPC分类号： C07F9/5532 , C07F9/5726 , C07F9/597
摘要： Novel phosphinic and phosphonic acid derivatives of pyridine, pyrrole and azepine with utility as antagonists of the GABA.sub.rho receptor are disclosed. These compounds have utility as modulators of the excitability of the central nervous system as mediated by their ability to specifically act on closed-channel binding sites of GABA.sub.rho receptors.
摘要翻译：公开了作为GABArho受体的拮抗剂的吡啶，吡咯和氮杂的新的次膦酸和膦酸衍生物。这些化合物具有作为中枢神经系统兴奋性的调节剂的作用，其作用是通过其特异性作用于GABAho受体的闭合通道结合位点的能力来介导。

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