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公开(公告)号：US08557853B2
公开(公告)日：2013-10-15
申请号：US11950667
申请日：2007-12-05
申请人： Ken Chow , Wenkui K. Fang , Evelyn G. Corpuz , Daniel W. Gil , Michael E. Garst
发明人： Ken Chow , Wenkui K. Fang , Evelyn G. Corpuz , Daniel W. Gil , Michael E. Garst
IPC分类号： A61K31/44 , C07D213/62 , C07D211/82
CPC分类号： C07C275/24 , C07C275/28 , C07C275/30 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D231/12 , C07D307/52 , C07D307/79 , C07D317/58 , C07D333/20
摘要： The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.
摘要翻译： 本发明提供了可用作选择性α2肾上腺素能激动剂的明确定义的芳基氟乙基脲。 因此，本文所述的化合物可用于治疗与调节α2肾上腺素能受体相关的多种疾病。
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![Ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl] methanol for lowering intraocular pressure](/abs-image/US/2013/08/06/US08501796B2/abs.jpg.150x150.jpg)
102.发明授权Ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl] methanol for lowering intraocular pressure 有权用于降低眼内压的[3-（1-（1H-咪唑-4-基）乙基）-2-甲基苯基]甲酯的酯前体药物公开(公告)号：US08501796B2
公开(公告)日：2013-08-06
申请号：US13233844
申请日：2011-09-15
申请人： Mohammad I. Dibas , Daniel W. Gil , John E. Donello , Ken Chow , Liming Wang , Michael E. Garst
发明人： Mohammad I. Dibas , Daniel W. Gil , John E. Donello , Ken Chow , Liming Wang , Michael E. Garst
IPC分类号： A61K31/415
CPC分类号： A61K31/4174 , A61K9/0014 , A61K31/4164 , C07D233/64 , Y10S514/912
摘要： The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, of enantiomers thereof, of tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译： 本发明涉及降低需要这种治疗的受试者的眼内压的方法，其包括施用治疗有效量的包含[3-（1-（1H-咪唑-4-基） ）乙基）-2-甲基苯基]甲醇，其对映异构体，其互变异构体，含有它们的药物组合物及其作为药物的用途。
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![ESTER PRO-DRUGS OF [3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL] METHANOL FOR LOWERING INTRAOCULAR PRESSURE](/abs-image/US/2012/06/07/US20120142746A1/abs.jpg.150x150.jpg)
103.发明申请ESTER PRO-DRUGS OF [3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL] METHANOL FOR LOWERING INTRAOCULAR PRESSURE 有权[3-（1-（1H-咪唑-4-基）乙基）-2-甲基苯基]甲醇用于降低内压的ESTER制剂公开(公告)号：US20120142746A1
公开(公告)日：2012-06-07
申请号：US13233844
申请日：2011-09-15
申请人： Mohammed I. Dibas , Daniel W. Gil , John E. Donello , Ken Chow , Liming Wang , Michael E. Garst
发明人： Mohammed I. Dibas , Daniel W. Gil , John E. Donello , Ken Chow , Liming Wang , Michael E. Garst
IPC分类号： A61K31/4174 , A61P27/02 , C07D233/64
CPC分类号： A61K31/4174 , A61K9/0014 , A61K31/4164 , C07D233/64 , Y10S514/912
摘要： The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, of enantiomers thereof, of tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译： 本发明涉及降低需要这种治疗的受试者的眼内压的方法，其包括施用治疗有效量的包含[3-（1-（1H-咪唑-4-基） ）乙基）-2-甲基苯基]甲醇，其对映异构体，其互变异构体，含有它们的药物组合物及其作为药物的用途。
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![ESTER PRO-DRUGS OF [3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL] METHANOL FOR TREATING SKIN DISEASES AND CONDITIONS](/abs-image/US/2012/05/31/US20120136036A1/abs.jpg.150x150.jpg)
104.发明申请ESTER PRO-DRUGS OF [3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL] METHANOL FOR TREATING SKIN DISEASES AND CONDITIONS 有权用于治疗皮肤疾病和病症的[3-（1-（1H-咪唑-4-基）乙基）-2-甲基苯基]甲醇的酯类药物公开(公告)号：US20120136036A1
公开(公告)日：2012-05-31
申请号：US13233665
申请日：2011-09-15
申请人： Mohammed I. Dibas , Ken Chow , Liming Wang , Michael E. Garst , John E. Donello , Daniel W. Gil
发明人： Mohammed I. Dibas , Ken Chow , Liming Wang , Michael E. Garst , John E. Donello , Daniel W. Gil
IPC分类号： A61K31/4174 , A61P17/00 , A61P27/02 , A61P15/12 , A61P17/08 , A61P17/10 , C07D233/64 , A61P17/06
CPC分类号： A61K31/4174 , A61K9/0014 , A61K31/4164 , C07D233/64 , Y10S514/912
摘要： The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.
摘要翻译： 本发明涉及治疗需要这种治疗的受试者皮肤疾病和皮肤病症的方法，其包括给予治疗有效量的包含[3-（1-（1H-咪唑-4-基） - 基）乙基）-2-甲基苯基]甲醇或其对映体，含有它们的药物组合物及其作为药物的用途。
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公开(公告)号：US07884244B2
公开(公告)日：2011-02-08
申请号：US12058037
申请日：2008-03-28
申请人： Ken Chow , Wenkui K. Fang , Evelyn G. Corpuz , Daniel W. Gil , Michael E. Garst
发明人： Ken Chow , Wenkui K. Fang , Evelyn G. Corpuz , Daniel W. Gil , Michael E. Garst
IPC分类号： C07C277/00
CPC分类号： C07D307/81 , C07C279/28 , C07C323/44 , C07C2601/08 , C07C2602/08 , C07C2602/10 , C07C2603/16
摘要： Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
摘要翻译： 本文公开的是具有本文所述的式的化合物。 还公开了与之相关的治疗方法，组合物和药物。
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公开(公告)号：US20080194650A1
公开(公告)日：2008-08-14
申请号：US11950667
申请日：2007-12-05
申请人： Ken Chow , Wenkui K. Fang , Evelyn G. Corpuz , Daniel W. Gil , Michael E. Garst
发明人： Ken Chow , Wenkui K. Fang , Evelyn G. Corpuz , Daniel W. Gil , Michael E. Garst
IPC分类号： A61K31/44 , C07C275/00 , A61K31/17 , A61K31/38 , A61K31/357 , C07D315/00 , C07D231/10 , A61P25/04 , A61P25/00 , A61K31/415 , C07D317/44 , A61K31/343 , A61K31/351 , C07D333/02 , C07D211/04
CPC分类号： C07C275/24 , C07C275/28 , C07C275/30 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D231/12 , C07D307/52 , C07D307/79 , C07D317/58 , C07D333/20
摘要： The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.
摘要翻译： 本发明提供了可用作选择性α2肾上腺素能激动剂的明确定义的芳基氟乙基脲。 因此，本文所述的化合物可用于治疗与调节α2肾上腺素能受体相关的多种疾病。
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107.发明申请METHODS AND COMPOSITIONS FOR MODULATING ALPHA ADRENERGIC RECEPTOR ACTIVITY 失效调节ALPHA ADRENERGIC受体活性的方法和组合物公开(公告)号：US20080132576A1
公开(公告)日：2008-06-05
申请号：US12024609
申请日：2008-02-01
申请人： Ken Chow , Daniel W. Gil , Wenkui Ken Fang , Michael E. Garst , Larry A. Wheeler
发明人： Ken Chow , Daniel W. Gil , Wenkui Ken Fang , Michael E. Garst , Larry A. Wheeler
CPC分类号： A61K31/17 , Y10S514/913
摘要： Methods and compositions for the treatment of pain and intraocular pressure. Particularly disclosed are new compositions for the treatment of chronic pain, glaucoma and methods for their use.
摘要翻译： 用于治疗疼痛和眼内压的方法和组合物。 特别公开了用于治疗慢性疼痛，青光眼的新组合物及其使用方法。
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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。
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109.发明授权4-(2-methyl-5,6,7,8-tetrahydro-quinolin-7-ylmethyl)-1,3-dihydro-imidazole-2-thione as specific alpha2b agonist and methods of using the same 失效4-（2-甲基-5,6,7,8-四氢 - 喹啉-7-基甲基）-1,3-二氢 - 咪唑-2-硫酮作为特异性α2b激动剂及其使用方法公开(公告)号：US07569584B2
公开(公告)日：2009-08-04
申请号：US11858191
申请日：2007-09-20
申请人： Todd M. Heidelbaugh , Ken Chow , Phong Nguyen , Daniel Gil , John E. Donello
发明人： Todd M. Heidelbaugh , Ken Chow , Phong Nguyen , Daniel Gil , John E. Donello
IPC分类号： A61K31/4709 , C07D401/06 , C07D215/00
CPC分类号： C07D233/70 , C07D233/84 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/08
摘要： The compound of the formula wherein the * indicates an asymmetric carbon, is specific to alpha2B adrenergic receptors in preference over alpha2A and alpha2C adrenergic receptors, and as such has no or only minimal cardivascular and/or sedatory activity. The compound is useful as medicament in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors.
摘要翻译： 下式的化合物，其中*表示不对称碳，优先于α2A和α2C肾上腺素能受体的α2B肾上腺素能受体特异性，因此没有或仅有最小的血管内和/或镇静作用。 该化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或缓解对α2B肾上腺素能受体激动剂治疗有反应的病症。
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110.发明授权4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones, 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds 有权4-（取代的环烷基甲基）咪唑-2-硫酮，4-（取代的环烯基甲基）咪唑-2-硫酮，4-（取代的环烷基甲基）咪唑-2-酮，4-（取代的环烯基甲基）咪唑-2-酮和相关化合物公开(公告)号：US07276522B2
公开(公告)日：2007-10-02
申请号：US10950376
申请日：2004-09-24
申请人： Todd M. Heidelbaugh , Ken Chow , Phong Nguyen , Daniel Gil , John E. Donello
发明人： Todd M. Heidelbaugh , Ken Chow , Phong Nguyen , Daniel Gil , John E. Donello
IPC分类号： C07D401/06 , C07D215/00 , A61K31/4709
CPC分类号： C07D233/70 , C07D233/84 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/08
摘要： The compound of the formula wherein the * indicates an asymmetric carbon, is specific to alpha2B adrenergic receptors in preference over alpha2A and alpha2C adrenergic receptors, and as such has no or only minimal cardivascular and/or sedatory activity. The compound is useful as medicament in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors.
摘要翻译： 下式的化合物，其中*表示不对称碳，优选α2 B 2肾上腺素能受体比α2A和α2 N 2肾上腺素能 受体，因此没有或仅有最小的血管内和/或镇静作用。 该化合物可用作哺乳动物（包括人）中的药物，用于治疗疾病和/或缓解对α2B2肾上腺素能受体的激动剂治疗有反应的病症。
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