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11. 发明授权

US06194415B1 Method of using (2-imidazolin-2-ylamino) quinoxoalines in treating neural injury 有权
标题翻译：使用（2-咪唑啉-2-基氨基）喹喔啉在治疗神经损伤中的应用
公开(公告)号：US06194415B1
公开(公告)日：2001-02-27
申请号：US09225036
申请日：1999-01-04
申请人： Larry A. Wheeler , Elizabeth Woldemussie , Ronald K. Lai
发明人： Larry A. Wheeler , Elizabeth Woldemussie , Ronald K. Lai
IPC分类号： A61K31495
CPC分类号： A61K31/498 , A61K31/495 , Y10S514/912 , Y10S514/913
摘要： The present invention provides a method of protecting the optic or retinal nerve cells of a mammal comprising administering to said mammal suffering from or at risk of suffering a noxious action on said nerve cells an effective amount of a compound of formula I to inhibit or prevent nerve cell injury or death wherein the 2-imidazolin-2-ylamino group is in either the 5- or 6-position of the quinoxaline nucleus; x, y and z are in any of the remaining 5-, 6-, 7- or 8-positions and are selected from hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; and R is an optional substituent in either the 2- or 3-position of the quinoxaline nucleus and may be hydrogen, lower alkyl or lower alkoxy, or pharmaceutically acceptable salts thereof and mixtures thereof. Such noxious action may result from glaucomatous optic neuropathy, age related macular degeneration or retinitis pigmentosa.
摘要翻译：本发明提供一种保护哺乳动物视神经细胞或视网膜神经细胞的方法，其包括向所述神经细胞给患有或有风险的所述哺乳动物施用有效量的式I化合物以抑制或预防神经细胞损伤或死亡，其中2-咪唑啉-2-基氨基位于喹喔啉核的5-或6-位; x，y和z在剩余的5-，6-，7-或8-位中的任一个中，并且选自氢，卤素，低级烷基，低级烷氧基或三氟甲基; 并且R是喹喔啉核的2-或3-位任选的取代基，并且可以是氢，低级烷基或低级烷氧基，或其药学上可接受的盐及其混合物。这种有害作用可能由青光眼性视神经病变，年龄相关性黄斑变性或色素性视网膜炎引起。

12. 发明授权

US5756503A Methods for using (2-imidazolin-2-ylamino) Quinoxaline derivatives 失效
标题翻译：使用（2-咪唑啉-2-基氨基）喹喔啉衍生物的方法
公开(公告)号：US5756503A
公开(公告)日：1998-05-26
申请号：US636740
申请日：1996-04-19
申请人： James A. Burke , Michael E. Garst , Larry A. Wheeler
发明人： James A. Burke , Michael E. Garst , Larry A. Wheeler
IPC分类号： C07D401/12 , A61K31/495 , A61K31/498 , A61P1/12 , A61P1/14 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P13/12 , A61P15/00 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P27/16 , A61P29/00 , C07D403/12
CPC分类号： A61K31/498 , A61K31/495
摘要： A method of treating a mammal is disclosed comprising administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain.
摘要翻译：公开了一种治疗哺乳动物的方法，其包括向哺乳动物施用有效量以在哺乳动物中提供期望的治疗效果，所述化合物选自具有下式的那些化合物及其药学上可接受的酸加成盐，以及其混合物，其中R 1和R 2各自选自含有1至4个碳原子的烷基和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以是5- 喹喔啉核的6-，7-或8-位，并且R3，R4和R5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并且独立地选自由Cl，Br，H组成的组和含有1至3个碳原子的烷基。当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少外周疼痛。

13. 发明授权

US4524063A Ophthalmic compositions 失效
标题翻译：眼用组合物
公开(公告)号：US4524063A
公开(公告)日：1985-06-18
申请号：US564156
申请日：1983-12-22
申请人： Larry A. Wheeler
发明人： Larry A. Wheeler
IPC分类号： A61K9/00 , A61K31/765 , A61K47/32 , A61K31/74 , A61K31/275
CPC分类号： A61K47/32 , A61K31/765 , A61K9/0048 , Y10S514/912
摘要： A topical lodoxamide composition having enhanced efficacy for treatment of ocular allergic diseases. The composition comprises the addition of polyvinyl alcohol to an aqueous solution containing lodoxamide tromethamine.
摘要翻译：一种具有增强的用于治疗眼部过敏性疾病的功效的局部氯化物组合物。组合物包括将聚乙烯醇加入到含有脱氧酰胺氨丁三醇的水溶液中。

14. 发明授权

US08425929B2 Sustained release intraocular implants and methods for preventing retinal dysfunction 有权
公开(公告)号：US08425929B2
公开(公告)日：2013-04-23
申请号：US10837143
申请日：2004-04-30
申请人： Glenn T. Huang , James Burke , Patrick M. Hughes , Kai-Ming Zhang , Ton Lin , Larry A. Wheeler , Rosy Sheng Donn
发明人： Glenn T. Huang , James Burke , Patrick M. Hughes , Kai-Ming Zhang , Ton Lin , Larry A. Wheeler , Rosy Sheng Donn
IPC分类号： A61F2/02
CPC分类号： A61K31/498 , A61K9/0051 , A61K47/34
摘要： Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to prevent the occurrence of one or more ocular conditions, or to reduce one or more symptoms of an ocular condition, such as an ocular neurosensory disorder and the like.

15. 发明授权

US08293741B2 Intraocular implants and methods for improving vision 有权
标题翻译：眼内植入物和改善视力的方法
公开(公告)号：US08293741B2
公开(公告)日：2012-10-23
申请号：US11119021
申请日：2005-04-29
申请人： James A. Burke , Patrick M. Hughes , Kai-Ming Zhang , Ton Lin , Glenn Huang , Brittany A. Jackson , Larry A. Wheeler , Rosy S. Donn
发明人： James A. Burke , Patrick M. Hughes , Kai-Ming Zhang , Ton Lin , Glenn Huang , Brittany A. Jackson , Larry A. Wheeler , Rosy S. Donn
IPC分类号： A61K31/495
CPC分类号： A61L31/148 , A61K9/0051 , A61K9/204 , A61K31/498 , A61K47/34 , A61L27/58 , A61L31/06 , A61L31/16 , A61L2300/436 , A61L2300/604 , C08L67/04 , Y02A50/401
摘要： Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants can be placed in an eye to treat one or more ocular conditions, such as an ocular vasculopathy or glaucoma, among others or to improve vision in a normal eye.
摘要翻译：生物相容性眼内植入物包括α-2肾上腺素能受体激动剂和与α-2肾上腺素能受体激动剂相关的聚合物，以促进α-2肾上腺素能受体激动剂延长一段时间的眼睛释放。 α-2肾上腺素能受体激动剂可以与可生物降解的聚合物基质例如两种可生物降解的聚合物的基质相关联。植入物可以放置在眼睛中以治疗一种或多种眼部病症，例如眼睛血管病变或青光眼等，或改善正常眼睛的视力。

16. 发明申请

US20120136011A1 COMPOUNDS AND METHODS FOR SKIN REPAIR 审中-公开
标题翻译：化合物和方法进行皮肤修复
公开(公告)号：US20120136011A1
公开(公告)日：2012-05-31
申请号：US13194078
申请日：2011-07-29
申请人： Guang L. Jiang , Wha-Bin Im , Frederick C. Beddingfield , Larry A. Wheeler , Scott M. Whitcup , Robert M. Burk
发明人： Guang L. Jiang , Wha-Bin Im , Frederick C. Beddingfield , Larry A. Wheeler , Scott M. Whitcup , Robert M. Burk
IPC分类号： A61K31/519 , A61K31/343 , A61K31/4015 , A61P17/02 , A61K31/216 , A61K31/4025 , A61K31/421 , A61K31/381 , A61K31/192
CPC分类号： A61K31/381 , A61K8/49 , A61K2800/91 , A61Q19/08
摘要： The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles.
摘要翻译：本公开提供了治疗皮肤瑕疵的组合物和方法。组合物包含治疗有效量的用于治疗皮肤瑕疵如化合物，伤口，皱纹和皱纹的化合物。

17. 发明申请

US20110318303A1 IL-10 AND METHODS OF TREATING OCULAR AND OTHER DISEASES 有权
标题翻译： IL-10和治疗其他疾病的方法
公开(公告)号：US20110318303A1
公开(公告)日：2011-12-29
申请号：US13161964
申请日：2011-06-16
申请人： Michael E. Stern , Christopher S. Schaumburg , Karyn F. Siemasko , Larry A. Wheeler
发明人： Michael E. Stern , Christopher S. Schaumburg , Karyn F. Siemasko , Larry A. Wheeler
IPC分类号： A61K38/20 , A61P17/00 , A61P37/00 , A61P27/02
CPC分类号： C07K14/005 , A61K9/0048 , A61K38/162 , A61K38/2066 , C12N2710/24033
摘要： Disclosed herein TPV1 is a method of treating ocular and systemic conditions by administering IL-10 and TPV134R polypeptides.
摘要翻译：本文公开了TPV1是通过施用IL-10和TPV134R多肽来治疗眼部和全身病症的方法。

18. 发明授权

US07838545B2 4-(condensed cyclicmethyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists 有权
标题翻译：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。

19. 发明授权

US07683089B1 4-(Phenylmethyl and substituted phenylmethyl)-imidazole-2-thiones acting as specific alpha2 adrenergic agonists 失效
标题翻译：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。

20. 发明申请

US20080319013A1 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
标题翻译： 4-（取代的环己基甲基）咪唑-2-酮，4-（取代的环己基甲基）咪唑-2-酮，4-（取代的环己基甲基）咪唑-2-酮和4-（取代的环己基甲基）咪唑-2-酮和相关化合物
公开(公告)号：US20080319013A1
公开(公告)日：2008-12-25
申请号：US12180162
申请日：2008-07-25
申请人： Ken Chow , Todd Heidelbaugh , Daniel Gil , Michael Garst , Larry A. Wheeler , Phong X. Nguyen , Dario G. Gomez
发明人： Ken Chow , Todd Heidelbaugh , Daniel Gil , Michael Garst , Larry A. Wheeler , Phong X. Nguyen , Dario G. Gomez
IPC分类号： A61K31/4709 , A61K31/4164 , A61K31/4166 , A61P25/00 , A61P9/10
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 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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