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91. 发明授权

US07358269B2 2-((2-Thioxo-2,3-dihydro-1H-imidazol-4-yl)methyl)-3,4-dihydronapthalen-1(2H)-one 有权
标题翻译： 2 - （（2-硫代-2,3-二氢-1H-咪唑-4-基）甲基）-3,4-二氢萘-1-（2H） - 酮
公开(公告)号：US07358269B2
公开(公告)日：2008-04-15
申请号：US11368990
申请日：2006-03-06
申请人： Ken Chow , Todd M. Heidelbaugh , Daniel W. Gil , Michael E. Garst , Larry A. Wheeler
发明人： Ken Chow , Todd M. Heidelbaugh , Daniel W. Gil , Michael E. Garst , Larry A. Wheeler
IPC分类号： A61K31/4164 , C07D233/04
CPC分类号： C07D233/70 , A61K9/0019 , A61K31/4164 , C07D233/84 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/08
摘要： A compound of the formula or a pharmaceutically acceptable salt thereof, is disclosed herein. Methods and compositions related thereto are also disclosed.
摘要翻译：本文公开了下式的化合物或其药学上可接受的盐。还公开了与其相关的方法和组合物。

92. 发明授权

US06395878B1 Nucleic acid encoding a human EP prostaglandin receptor 失效
标题翻译：编码人EP前列腺素受体的核酸
公开(公告)号：US06395878B1
公开(公告)日：2002-05-28
申请号：US09267423
申请日：1999-03-12
申请人： John W. Regan , Daniel W. Gil , David F. Woodward
发明人： John W. Regan , Daniel W. Gil , David F. Woodward
IPC分类号： C07K100
CPC分类号： C07K14/72
摘要： A gene encoding the HP4 human prostaglandin receptor is disclosed. The protein encoded by this gene exhibits significant sequence identity with other prostaglandin receptors. The HP4 receptor, when expressed in eukaryotic cells, is capable of binding prostaglandins and their analogs and stimulating adenylate cyclase activity in response to prostaglandins. Also disclosed are antisense agents able to decrease or prevent translation of a human HP4 prostaglandin receptor.
摘要翻译：公开了编码HP4人前列腺素受体的基因。由该基因编码的蛋白质与其他前列腺素受体显示出显着的序列同一性。当在真核细胞中表达时，HP4受体能够结合前列腺素及其类似物并且响应于前列腺素刺激腺苷酸环化酶活性。还公开了能够减少或预防人HP4前列腺素受体翻译的反义剂。

93. 发明授权

US06329369B1 Methods of treating pain and other conditions 有权
标题翻译：治疗疼痛等症状的方法
公开(公告)号：US06329369B1
公开(公告)日：2001-12-11
申请号：US09679919
申请日：2000-10-05
申请人： Ken Chow , Daniel W. Gil , James A. Burke , Dale A. Harcourt , Michael E. Garst , Larry A. Wheeler , Stephen A. Munk
发明人： Ken Chow , Daniel W. Gil , James A. Burke , Dale A. Harcourt , Michael E. Garst , Larry A. Wheeler , Stephen A. Munk
IPC分类号： A61R314168
CPC分类号： C07D233/56 , C07D233/06 , C07D233/10 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04 , Y10S514/816 , Y10S514/913
摘要： Methods of treating glaucoma or elevated pressure and other diseases with reduced side effects by treating a mammal in need thereof an agonist of the alpha 2B or alpha 2B/2C adrenergic receptor(s). Also described are compounds having such selective agonist activity.
摘要翻译：通过用有需要的哺乳动物治疗α2B或α2B / 2C肾上腺素能受体的激动剂来治疗青光眼或升高压力的其它疾病及其副作用降低的方法。还描述了具有这种选择性激动剂活性的化合物。

94. 发明授权

US06197933B1 Human EP3, prostaglandin receptor 失效
标题翻译：人EP3，前列腺素受体
公开(公告)号：US06197933B1
公开(公告)日：2001-03-06
申请号：US09363783
申请日：1999-07-29
申请人： Daniel W. Gil , John W. Regan
发明人： Daniel W. Gil , John W. Regan
IPC分类号： C07K100
CPC分类号： G01N33/88 , C07K14/72 , C07K16/2869 , C07K16/2878
摘要： A gene encoding the human EP3 prostaglandin receptor has been cloned and sequenced. The protein encoded by this gene has seven transmembrane domains and is 81% homologous to the murine EP3 receptor. Two variants that differ in their carboxy terminal coding sequence, and one variant that differs in its 3′ untranslated sequence only, have also been cloned. The proteins, when expressed in eukaryotic cells, are capable of binding prostaglandins and their agonists and regulating adenylate cyclase activity in response to prostaglandins.
摘要翻译：编码人EP3前列腺素受体的基因已被克隆并测序。由该基因编码的蛋白具有7个跨膜结构域，与鼠EP3受体81％同源。它们的羧基末端编码序列不同的两个变体和仅在其3'非翻译序列中不同的一个变体也被克隆。当在真核细胞中表达时，蛋白质能够结合前列腺素及其激动剂并且响应于前列腺素调节腺苷酸环化酶活性。

95. 发明授权

US5677327A Method for identifying muscarinic agents lacking miotic side effects 失效
标题翻译：识别缺乏瞳孔副作用的毒蕈碱药的方法
公开(公告)号：US5677327A
公开(公告)日：1997-10-14
申请号：US493509
申请日：1995-06-22
申请人： Daniel W. Gil , Elizabeth Woldemussie
发明人： Daniel W. Gil , Elizabeth Woldemussie
IPC分类号： G01N33/50 , G01N33/94 , A61K31/415
CPC分类号： G01N33/5044 , G01N33/5008 , G01N33/502 , G01N33/5088 , G01N33/944 , G01N2500/10 , Y10S514/913
摘要： The present invention provides a method for identifying a compound having muscarinic agonist activity that will lower intraocular pressure without causing miosis which comprises measuring the activity of the compound at the m.sub.3 and m.sub.5 muscarinic receptors and determining from the activity measurement a compound having at least twice the agonist activity at the m.sub.5 receptor as compared to the m.sub.3 receptor. Preferably, the method of measuring said muscarinic agonist activity comprises eliciting phosphoinositide hydrolysis in CHO-K1 cells stably expressing the m.sub.3 and m.sub.5 muscarinic receptor subtypes. The present invention also provides a method of lowering the intraocular pressure in a mammal which comprises administering to said mammal a compound that has been determined to have at least twice the agonist activity at the m.sub.5 receptor as compared to the m.sub.3 receptor.
摘要翻译：本发明提供了一种用于鉴定具有毒蕈碱激动剂活性的化合物的方法，其将降低眼内压而不引起瞳孔缩小，其包括测量化合物在m3和m5毒蕈碱受体的活性，并从活性测定确定具有至少两倍与m3受体相比，m5受体的激动剂活性。优选地，测量所述毒蕈碱激动剂活性的方法包括在稳定表达m3和m5毒蕈碱受体亚型的CHO-K1细胞中引发磷酸肌醇水解。本发明还提供一种降低哺乳动物眼内压的方法，其包括向所述哺乳动物施用与m 3受体相比被确定具有m5受体的激动剂活性至少两倍的化合物。

96. 发明授权

US09018202B2 Methods for treating diseases of the retina 有权
标题翻译：治疗视网膜疾病的方法
公开(公告)号：US09018202B2
公开(公告)日：2015-04-28
申请号：US13298028
申请日：2011-11-16
申请人： Jyotirmoy Kusari , Sheila X. Zhou , Mingting Tian , Edwin U. Padillo , Sandhya S. Rao , Daniel W. Gil , Larry A. Wheeler
发明人： Jyotirmoy Kusari , Sheila X. Zhou , Mingting Tian , Edwin U. Padillo , Sandhya S. Rao , Daniel W. Gil , Larry A. Wheeler
IPC分类号： A61K31/55 , A61K31/5513
CPC分类号： A61K31/5513 , A61K31/551 , Y10S514/912
摘要： Disclosed herein is a method of treating disorders of the retina comprising administering to a patient in need of such treatment a compound selected from the group consisting of olanzapine, certain of its metabolites, clozapine, and n-desmethyl clozapine.
摘要翻译：本文公开了一种治疗视网膜疾病的方法，包括向需要这种治疗的患者施用选自奥氮平，其某些代谢物，氯氮平和去甲基氯氮平的化合物。

97. 发明申请

US20120238615A1 Alpha adrenergic receptor modulators 审中-公开
标题翻译： α肾上腺素能受体调节剂
公开(公告)号：US20120238615A1
公开(公告)日：2012-09-20
申请号：US13502871
申请日：2010-10-20
申请人： Ken Chow , Liming Wang , Wenkui K. Fang , Evelyn G. Corpuz , Daniel W. Gil
发明人： Ken Chow , Liming Wang , Wenkui K. Fang , Evelyn G. Corpuz , Daniel W. Gil
IPC分类号： A61K31/40 , A61P11/02 , A61P25/00 , A61P9/10 , A61P25/18 , A61P17/00 , A61P29/00 , A61P17/10 , A61P17/06 , A61P25/24 , C07D207/22 , A61P25/06
CPC分类号： C07D207/22
摘要： Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor, in particular the alpha 2C receptor. The compounds can include N-(2,3-substituted phenyl)-3,4-dihydro-2H-pyrrol-5-amine derivatives. Methods of making, using and formulating these compounds are described
摘要翻译：本文描述的化合物可用于通过调节一种或多种α-肾上腺素能受体，特别是α2C受体来治疗疾病和病症。该化合物可以包括N-（2,3-取代的苯基）-3,4-二氢-2H-吡咯-5-胺衍生物。描述制备，使用和配制这些化合物的方法

98. 发明申请

US20120142675A1 Methods for Treating Diseases of the Retina 有权
标题翻译：治疗视网膜疾病的方法
公开(公告)号：US20120142675A1
公开(公告)日：2012-06-07
申请号：US13298028
申请日：2011-11-16
申请人： Jyotirmoy Kusari , Sheila X. Zhou , Mingting Tian , Edwin U. Padillo , Sandhya S. Rao , Daniel W. Gil , Larry A. Wheeler
发明人： Jyotirmoy Kusari , Sheila X. Zhou , Mingting Tian , Edwin U. Padillo , Sandhya S. Rao , Daniel W. Gil , Larry A. Wheeler
IPC分类号： A61K31/5513 , A61P35/00 , A61P27/02
CPC分类号： A61K31/5513 , A61K31/551 , Y10S514/912
摘要： Disclosed herein is a method of treating disorders of the retina comprising administering to a patient in need of such treatment a compound selected from the group consisting of olanzapine, certain of its metabolites, clozapine, and n-desmethyl clozapine.
摘要翻译：本文公开了一种治疗视网膜疾病的方法，包括向需要这种治疗的患者施用选自奥氮平，其某些代谢物，氯氮平和去甲基氯氮平的化合物。

99. 发明申请

US20110301214A1 PHARMACEUTICAL COMPOSITIONS COMPRISING (3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL)METHANOL 审中-公开
标题翻译：包含（3-（1-（1H-咪唑-4-基）乙基）-2-甲基苯基）甲醇的药物组合物
公开(公告)号：US20110301214A1
公开(公告)日：2011-12-08
申请号：US13147760
申请日：2010-02-12
申请人： Daniel W. Gil
发明人： Daniel W. Gil
IPC分类号： A61K31/4174 , A61P25/06 , A61P29/00 , C07D233/64
CPC分类号： A61K31/4164 , A61K31/4174 , C07D233/64
摘要： Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain.
摘要翻译：本文公开了包含（3-（1-（1H-咪唑-4-基）乙基）-2-甲基苯基）甲醇的药物组合物和使用该组合物治疗慢性疼痛的方法。

100. 发明授权

US07960423B2 Imidazole-2-thiones 有权
标题翻译：咪唑-2-硫酮
公开(公告)号：US07960423B2
公开(公告)日：2011-06-14
申请号：US11873537
申请日：2007-10-17
申请人： Ken Chow , Todd M. Heidelbaugh , Daniel W. Gil , Michael E. Garst , Larry A. Wheeler
发明人： Ken Chow , Todd M. Heidelbaugh , Daniel W. Gil , Michael E. Garst , Larry A. Wheeler
IPC分类号： A61K31/4164 , C07D233/30
CPC分类号： C07D233/84 , C07D233/70 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/08
摘要： Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.
摘要翻译：式1的化合物，其中X为S且变量具有本说明书中定义的含义，优先于α2B肾上腺素能受体，对α2B和/或α2C肾上腺素能受体是特异性或选择性的，因此没有或仅有最小的血管内和/或镇静活动。式1的这些化合物可用作哺乳动物（包括人）中用于治疗疾病的药物和/或缓解对α2B肾上腺素能受体的激动剂治疗有反应的病症。其中X是O的式1化合物也具有它们没有或只有最小的血管内和/或镇静作用的有利性质，并且可用于治疗没有或仅有最小血管和/或镇静作用的疼痛和其它病症。

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