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公开(公告)号：US09073888B2
公开(公告)日：2015-07-07
申请号：US13502980
申请日：2010-10-20
IPC分类号： C07D311/16 , C07D311/18 , C07D405/12
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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2.发明申请公开(公告)号：US20120190694A1
公开(公告)日：2012-07-26
申请号：US13437463
申请日：2012-04-02
IPC分类号： A61K31/501 , A61P27/02 , C07D401/12
CPC分类号： C07D213/81 , C07D405/12 , C07D409/12
摘要： Described herein are compounds useful as antagonists of sphingosine-1-phosphate receptors. Further described herein is the use of these compounds and related pharmaceutical compositions to treat disorders associated with sphingosine-1-phosphate-3 (S1P3) receptor modulation.
摘要翻译： 本文描述的是可用作鞘氨醇-1-磷酸受体拮抗剂的化合物。 本文进一步描述的是这些化合物和相关药物组合物用于治疗与鞘氨醇-1-磷酸-3（S1P3）受体调节相关的病症的用途。
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公开(公告)号：US08168795B2
公开(公告)日：2012-05-01
申请号：US12852768
申请日：2010-08-09
IPC分类号： A61K31/44 , C07D213/46
CPC分类号： C07D213/81 , C07D405/12 , C07D409/12
摘要： Described herein are compounds useful as antagonists of sphingosine-1-phosphate receptors. Further described herein is the use of these compounds and related pharmaceutical compositions to treat disorders associated with sphingosine-1-phosphate-3 (S1P3) receptor modulation.
摘要翻译： 本文描述的是可用作鞘氨醇-1-磷酸受体拮抗剂的化合物。 本文进一步描述的是这些化合物和相关药物组合物用于治疗与鞘氨醇-1-磷酸-3（S1P3）受体调节相关的病症的用途。
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公开(公告)号：US07868020B2
公开(公告)日：2011-01-11
申请号：US12522887
申请日：2008-01-04
IPC分类号： A61K31/47 , C07D215/12
CPC分类号： C07D401/06
摘要： Disclosed herein is a compound of the formula (I):(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：（I）。 还公开了与此相关的治疗方法，组合物和药物。
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5.发明授权4-(condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists 有权作为α2肾上腺素能激动剂的4-（缩合环状甲基） - 咪唑-2-硫酮公开(公告)号：US07838545B2
公开(公告)日：2010-11-23
申请号：US12166964
申请日：2008-07-02
申请人： Todd M. Heidelbaugh , Ken Chow , Phong X. Nguyen , Daniel W. Gill , John E. Donello , Michael E. Garst , Larry A. Wheeler
发明人： Todd M. Heidelbaugh , Ken Chow , Phong X. Nguyen , Daniel W. Gill , John E. Donello , Michael E. Garst , Larry A. Wheeler
IPC分类号： A61K31/4174 , C07D233/42
CPC分类号： C07D405/06 , C07D233/84 , C07D401/06 , C07D409/06 , C07D417/06
摘要： Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The 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 alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
摘要翻译： 变量具有本说明书中定义的含义的式1化合物是α2肾上腺素能受体的激动剂。 本公开的几种化合物优选α2B和/或α2C肾上腺素能受体是优于α2A肾上腺素能受体的特异性或选择性的。 另外一些要求保护的化合物没有或仅有最小的心血管和/或镇静活性。 式1的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α2肾上腺素能受体激动剂治疗有反应的病症。 没有明显的心血管和/或镇静作用的式1化合物可用于治疗疼痛和其他具有最小副作用的病症。
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6.发明授权4-(Phenylmethyl and substituted phenylmethyl)-imidazole-2-thiones acting as specific alpha2 adrenergic agonists 失效作为特定α2肾上腺素能激动剂的4-（苯基甲基和取代的苯基甲基） - 咪唑-2-硫酮公开(公告)号：US07683089B1
公开(公告)日：2010-03-23
申请号：US11232341
申请日：2005-09-20
申请人： Todd M. Heidelbaugh , Ken Chow , Phong X. Nguyen , Daniel W. Gil , John E. Donello , Michael E. Garst , Larry A. Wheeler
发明人： Todd M. Heidelbaugh , Ken Chow , Phong X. Nguyen , Daniel W. Gil , John E. Donello , Michael E. Garst , Larry A. Wheeler
IPC分类号： A61K31/4164 , C07D233/30
CPC分类号： C07D233/84
摘要： Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The 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 alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
摘要翻译： 变量具有本说明书中定义的含义的式1化合物是α2肾上腺素能受体的激动剂。 本公开的几种化合物优选α2B和/或α2C肾上腺素能受体是优于α2A肾上腺素能受体的特异性或选择性的。 另外一些要求保护的化合物没有或仅有最小的心血管和/或镇静活性。 式1的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α2肾上腺素能受体激动剂治疗有反应的病症。 没有明显的心血管和/或镇静作用的式1化合物可用于治疗疼痛和其他具有最小副作用的病症。
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公开(公告)号：US20090286829A1
公开(公告)日：2009-11-19
申请号：US12436837
申请日：2009-05-07
IPC分类号： A61K31/4709 , A61P25/00
CPC分类号： A61K31/4709
摘要： Disclosed herein are methods for treating a disorder associated with selective subtype modulation of alpha 2B and alpha 2C adrenergic receptors. Such methods can be performed, for example, by administering to a subject in need thereof a pharmaceutical composition containing a therapeutically effective amount of at least one compound having the structure: Compositions and medicaments related thereto are also disclosed.
摘要翻译： 本文公开了治疗与α2B和α2C肾上腺素能受体的选择性亚型调节相关的病症的方法。 这样的方法可以例如通过向有需要的受试者施用含有治疗有效量的至少一种具有以下结构的化合物的药物组合物：还公开了与其有关的组合物和药物。
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8.发明授权公开(公告)号：US08809379B2
公开(公告)日：2014-08-19
申请号：US12353406
申请日：2009-01-14
申请人： Todd M. Heidelbaugh , Ken Chow , Santosh C. Sinha , Phong X. Nguyen , Ling Li , Wenkui K. Fang , Janet A. Takeuchi , Smita Bhat
发明人： Todd M. Heidelbaugh , Ken Chow , Santosh C. Sinha , Phong X. Nguyen , Ling Li , Wenkui K. Fang , Janet A. Takeuchi , Smita Bhat
IPC分类号： A61K31/53 , A61K31/50 , A61K31/44 , A61K31/497 , A61K31/4439
CPC分类号： A61K31/4439 , A61K31/497
摘要： The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.
摘要翻译： 本发明提供了明确定义的杂环化合物，其可用作亚型选择性α2肾上腺素能激动剂。 因此，本文所述的化合物可用于治疗与α2肾上腺素能受体的选择性亚型调节相关的多种疾病。
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9.发明授权公开(公告)号：US08735399B2
公开(公告)日：2014-05-27
申请号：US12863386
申请日：2009-01-14
申请人： Todd M. Heidelbaugh , Ken Chow , Santosh C. Sinha , Phong X. Nguyen , Wenkui K. Fang , Ling Li , Janet A. Takeuchi , Smita S. Bhat
发明人： Todd M. Heidelbaugh , Ken Chow , Santosh C. Sinha , Phong X. Nguyen , Wenkui K. Fang , Ling Li , Janet A. Takeuchi , Smita S. Bhat
IPC分类号： A61K31/422 , A61K31/497 , C07D241/12 , C07D263/12 , C07D413/12 , C07D213/18
CPC分类号： C07D401/12 , A61K31/422 , A61K31/497 , C07D213/18 , C07D241/12 , C07D263/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The invention provides oxazolidine and thiazolidine derivatives that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.
摘要翻译： 本发明提供可用作亚型选择性α2肾上腺素能激动剂的恶唑烷和噻唑烷衍生物。 因此，本文所述的化合物可用于治疗与α2肾上腺素能受体的选择性亚型调节相关的多种病症。
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公开(公告)号：US08329918B2
公开(公告)日：2012-12-11
申请号：US12828429
申请日：2010-07-01
申请人： Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh , Dario G. Gomez , Wenkui K. Fang , Santosh C. Sinha , Michael E. Garst , Daniel W. Gil
发明人： Phong X. Nguyen , Ken Chow , Todd M. Heidelbaugh , Dario G. Gomez , Wenkui K. Fang , Santosh C. Sinha , Michael E. Garst , Daniel W. Gil
IPC分类号： C07D263/28 , A61K31/42
CPC分类号： C07D277/18 , C07D263/28
摘要： Described herein are compounds useful as agonists of alpha 2B/2C receptors. Pharmaceutical compositions including the presently described compounds and methods of treatment of diseases and conditions with the presently described compounds also are disclosed.
摘要翻译： 本文描述的是可用作α2B / 2C受体激动剂的化合物。 还公开了包括目前描述的化合物的药物组合物和用目前描述的化合物治疗疾病和病症的方法。
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