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公开(公告)号：US09034910B2
公开(公告)日：2015-05-19
申请号：US13275029
申请日：2011-10-17
申请人： Daniel W. Gil , John E. Donello , Wenkui K. Fang , Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh , Dario G. Gomez , Michael E. Garst , Santosh C. Sinha
发明人： Daniel W. Gil , John E. Donello , Wenkui K. Fang , Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh , Dario G. Gomez , Michael E. Garst , Santosh C. Sinha
IPC分类号： A61K31/4174 , A61K31/4168 , C07D233/48 , C07D233/50
CPC分类号： A61K31/40 , A61K9/0053 , A61K31/4168 , A61K31/4174 , C07D233/48 , C07D233/50
摘要： Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an α-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, acute, neuropathic and chronic.
摘要翻译： 本文描述了通过向受试者施用含有有效量的α-肾上腺素能调节剂的药物组合物来治疗受试者的病症或疾病的化合物和方法。 化合物和方法也可用于缓解急性，神经性和慢性疼痛的类型。
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2.发明授权公开(公告)号：US08486985B2
公开(公告)日：2013-07-16
申请号：US12992535
申请日：2009-05-11
申请人： Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh
发明人： Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh
IPC分类号： A01N43/50
CPC分类号： A61K31/4168
摘要： The invention provides methods for treating disorders associated with selective subtype modulation of alpha 2 adrenergic receptors. In particular, the invention provides methods employing well-defined N-[1-(2 and/or 3-substituted-phenyl)-alkyl]-(4,5-dihydro-1H-imidazol-2-yl)-amines and pharmaceutical compositions thereof to treat disorders associated with selective subtype alpha 2 adrenergic receptor modulation, such as ocular disorders, pain and central nervous system (CNS) motor disorders.
摘要翻译： 本发明提供了治疗与α2肾上腺素能受体的选择性亚型调节相关的疾病的方法。 特别地，本发明提供使用明确定义的N- [1-（2和/或3-取代 - 苯基） - 烷基] - （4,5-二氢-1H-咪唑-2-基） - 胺和药物 用于治疗与选择性亚型α2肾上腺素能受体调节相关的疾病的组合物，例如眼部疾病，疼痛和中枢神经系统（CNS）运动障碍。
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3.发明授权公开(公告)号：US08383646B2
公开(公告)日：2013-02-26
申请号：US12600757
申请日：2008-05-21
申请人： Santosh C. Sinha , Todd M. Heidelbaugh , Ken Chow , Smita S. Bhat , Phong X. Nguyen , Michael E. Garst
发明人： Santosh C. Sinha , Todd M. Heidelbaugh , Ken Chow , Smita S. Bhat , Phong X. Nguyen , Michael E. Garst
IPC分类号： A61K31/47 , C07D401/14
CPC分类号： C07D409/12
摘要： Disclosed herein is a compound of the formula (I) therapeutic methods, compositions, and medicaments related thereto are also disclosed.
摘要翻译： 本文公开了式（I）的化合物，还公开了与其相关的治疗方法，组合物和药物。
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4.发明申请公开(公告)号：US20120328661A1
公开(公告)日：2012-12-27
申请号：US13502980
申请日：2010-10-20
IPC分类号： A61K31/37 , A61K31/501 , A61K31/453 , A61K31/4433 , A61K31/4025 , C07F5/02 , C07D405/02 , C07D311/18 , A61P27/02 , A61P29/00 , A61P35/04 , A61P9/10 , A61P11/00 , A61P19/02 , A61P1/00 , A61P25/00 , A61P17/06 , A61P17/00 , A61P41/00 , A61P37/08 , A61P11/06 , A61P9/00 , A61P17/02 , A61P19/00 , A61P19/10 , A61P27/06 , A61P37/06
CPC分类号： A61K31/37 , A61K31/365 , A61K31/366 , A61K31/4025 , A61K31/4433 , A61K31/453 , A61K31/501 , C07D311/16 , C07D311/18 , C07D405/12
摘要： The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
摘要翻译： 本发明涉及新的2-氧代-2H-色烯-3-甲酰胺衍生物，其制备方法，含有它们的药物组合物及其作为药物作为鞘氨醇-1-磷酸受体调节剂的用途。
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公开(公告)号：US20120129813A1
公开(公告)日：2012-05-24
申请号：US13300537
申请日：2011-11-18
IPC分类号： A61K31/67 , C07F9/655 , C07F9/6558 , A61K31/665 , A61K31/675 , A61K31/443 , A61K31/4439 , A61P27/02 , A61P27/06 , A61P25/00 , A61P29/00 , A61P35/04 , A61P11/00 , A61P9/10 , A61P19/02 , A61P17/06 , A61P37/06 , A61P37/00 , A61P1/00 , A61P11/06 , A61P19/10 , A61P37/08 , A61P17/18 , A61P17/02 , A61P25/28 , C07D405/04 , C07D405/14 , A61P19/08 , A61P19/04 , C07D409/10 , A61K31/4178 , C07D405/10 , C07F9/6553
CPC分类号： C07F9/655345 , C07D307/42 , C07D307/52 , C07D333/12 , C07D333/20 , C07F9/6506 , C07F9/65515 , C07F9/65744
摘要： The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
摘要翻译： 本发明涉及新型衍生物，其制备方法，含有它们的药物组合物及其作为药物作为鞘氨醇-1-磷酸受体调节剂的用途。
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6.发明授权N-(1-phenyl-2-arylethyl)-4,5-dihydro-2H-pyrrol-5-amine compounds as subtype selective modulators of ALPHA2B or ALPHA2B and ALPHA2C adrenoceptors 失效作为ALPHA2B或ALPHA2B和ALPHA2C肾上腺素受体的亚型选择性调节剂的N-（1-苯基-2-芳基乙基）-4,5-二氢-2H-吡咯-5-胺化合物公开(公告)号：US08183414B2
公开(公告)日：2012-05-22
申请号：US12632494
申请日：2009-12-07
申请人： Ken Chow , Janet A. Takeuchi , Ling Li , Todd M. Heidelbaugh , Phong X. Nguyen , Evelyn G. Corpuz , Wenkui K Fang , Santosh C. Sinha , Michael E. Garst
发明人： Ken Chow , Janet A. Takeuchi , Ling Li , Todd M. Heidelbaugh , Phong X. Nguyen , Evelyn G. Corpuz , Wenkui K Fang , Santosh C. Sinha , Michael E. Garst
IPC分类号： C07C257/00 , A61K31/155
CPC分类号： C07D207/22 , C07D401/12
摘要： The present invention provides compounds which are N-(1-phenyl-2-arylethyl)-4,5-dihydro-2H-pyrrol-5-amine compounds and are subtype selective modulators of alpha 2B or alpha 2B and alpha 2C adrenoreceptors and are selected from the group of compounds represented by the formula
摘要翻译： 本发明提供了N-（1-苯基-2-芳基乙基）-4,5-二氢-2H-吡咯-5-胺化合物的化合物，并且是α2B或α2B和α2C肾上腺素受体的亚型选择性调节剂，并且是 选自由式表示的化合物组
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7.发明申请公开(公告)号：US20120035235A1
公开(公告)日：2012-02-09
申请号：US13274471
申请日：2011-10-17
申请人： Wenkui K. Fang , Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh , Dario G. Gomez , Michael E. Garst , Santosh C. Sinha , Daniel W. Gil , John E. Donello
发明人： Wenkui K. Fang , Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh , Dario G. Gomez , Michael E. Garst , Santosh C. Sinha , Daniel W. Gil , John E. Donello
IPC分类号： A61K31/4168 , A61P29/00 , A61P25/00 , C07D233/44
CPC分类号： A61K31/4168
摘要： Described herein are compounds for and methods of treating conditions or diseases in a subject by administering to the subject a pharmaceutical composition containing an effective amount of an α-adrenergic modulator. The compounds and methods are also useful for alleviating types of pain, both acute and chronic.
摘要翻译： 本文描述了通过向受试者施用含有有效量的α-肾上腺素能调节剂的药物组合物来治疗受试者的病症或疾病的化合物和方法。 化合物和方法也可用于缓解急性和慢性疼痛的类型。
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公开(公告)号：US08063231B2
公开(公告)日：2011-11-22
申请号：US12479256
申请日：2009-06-05
申请人： Wenkui K. Fang , Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh , Dario G. Gomez , Michael E. Garst , Santosh C. Sinha
发明人： Wenkui K. Fang , Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh , Dario G. Gomez , Michael E. Garst , Santosh C. Sinha
IPC分类号： C07D233/48
CPC分类号： A61K31/4168 , C07D233/48
摘要： Described herein are novel N-(2 and/or 3-substituted benzyl)-4,5-dihydro-1H-imidazol-2-amine derivatives processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals modulators of subtype α2B and/or α2C adrenergic receptors.
摘要翻译： 本文描述的是新型的N-（2和/或3-取代的苄基）-4,5-二氢-1H-咪唑-2-胺衍生物的制备方法，含有它们的药物组合物及其作为α2B亚型的药物调节剂的用途 /或α2C肾上腺素能受体。
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9.发明授权4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazole-2-ones and, 4-(substituted cycloalkylmethyl) imidazole-2-ones and related compounds 失效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-酮和4-（取代的环烷基甲基）咪唑-2-酮和相关的 化合物公开(公告)号：US08063087B2
公开(公告)日：2011-11-22
申请号：US12180162
申请日：2008-07-25
申请人： Ken Chow , Todd Heidelbaugh , Daniel Gill , Michael Garst , Larry A. Wheeler , Phong X. Nguyen , Dario G. Gomez
发明人： Ken Chow , Todd Heidelbaugh , Daniel Gill , Michael Garst , Larry A. Wheeler , Phong X. Nguyen , Dario G. Gomez
IPC分类号： A61K31/4164 , C07D233/30
CPC分类号： C07D401/06 , C07D233/70 , C07D233/84 , 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 cardiovascular 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 cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular 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，优先选择α2B和/或α2C肾上腺素能受体，优于α2A肾上腺素能受体，因此没有或只有最小的心血管和/或镇静剂 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为O的式1的化合物也具有它们没有或只有最小的心血管和/或镇静活性的有利特性，并且可用于治疗没有或仅有最小的心血管和/或镇静活性的疼痛和其它状况。
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10.发明申请SELECTIVE SUBTYPE ALPHA 2 ADRENERGIC AGENTS AND METHODS FOR USE THEREOF 有权选择性亚型ALPHA 2 ADRENERGIC AGENTS及其使用方法公开(公告)号：US20110136884A1
公开(公告)日：2011-06-09
申请号：US12992535
申请日：2009-05-11
申请人： Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh
发明人： Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh
IPC分类号： A61K31/4168 , A61P27/02 , A61P27/06 , A61P9/10 , A61P29/00 , A61P25/28 , A61P25/00 , A61P25/22 , A61P25/24 , A61P1/00 , A61P19/02 , A61P1/04
CPC分类号： A61K31/4168
摘要： The invention provides methods for treating disorders associated with selective subtype modulation of alpha 2 adrenergic receptors. In particular, the invention provides methods employing well-defined N-[1-(2 and/or 3-substituted-phenyl)-alkyl]-(4,5-dihydro-1H-imidazol-2-yl)-amines and pharmaceutical compositions thereof to treat disorders associated with selective subtype alpha 2 adrenergic receptor modulation, such as ocular disorders, pain and central nervous system (CNS) motor disorders.
摘要翻译： 本发明提供了治疗与α2肾上腺素能受体的选择性亚型调节相关的疾病的方法。 特别地，本发明提供使用明确定义的N- [1-（2和/或3-取代 - 苯基） - 烷基] - （4,5-二氢-1H-咪唑-2-基） - 胺和药物 用于治疗与选择性亚型α2肾上腺素能受体调节相关的疾病的组合物，例如眼部疾病，疼痛和中枢神经系统（CNS）运动障碍。
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