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41. 发明申请

US20080255230A1 THERAPEUTIC FLUOROETHYLCYANO GUANIDINES 有权
标题翻译：治疗性氟代乙酰胆碱
公开(公告)号：US20080255230A1
公开(公告)日：2008-10-16
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： A61K31/155 , A61P25/00 , C07C255/61 , C07D307/81 , A61K31/343
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。

42. 发明授权

US07399868B2 4-(Heteroaryl-methyl and substituted heteroaryl-methyl)-imidazole-2-thiones acting as alpha2 adrenergic agonists 失效
标题翻译：作为α2肾上腺素能激动剂的4-（杂芳基 - 甲基和取代的杂芳基 - 甲基） - 咪唑-2-硫酮
公开(公告)号：US07399868B2
公开(公告)日：2008-07-15
申请号：US11232323
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： C07D233/42 , C07D403/06 , C07D209/04 , C07D209/02 , C07D487/04
CPC分类号： C07D471/04 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06
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 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。本公开内容的若干化合物优先于α2A2肾上腺素能受体是特异性或选择性的α2B2和/或α2C2N2肾上腺素能受体。另外一些所要求保护的化合物没有或只有最小的血管内和/或镇静作用。式1的化合物可用作哺乳动物（包括人）中用作治疗疾病的药物和/或缓解通过α2肾上腺素能受体的激动剂治疗的病症。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。

43. 发明申请

US20080146635A1 2-((2-THIOXO-2,3-DIHYDRO-1H-IMIDAZOL-4-YL)METHYL)-3,4-DIHYDRONAPHTHALEN-1(2H)-ONE 失效
标题翻译： 2 - （（2-噻唑-2,3-二氢-1H-咪唑-4-基）甲基）-3,4-二氢萘-1（2H） - 酮
公开(公告)号：US20080146635A1
公开(公告)日：2008-06-19
申请号：US12034303
申请日：2008-02-20
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 , C07D233/42 , A61P25/00 , A61P21/00 , A61P27/06
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。

44. 发明授权

US07183310B2 Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
标题翻译：环戊烷庚（烯）酸，2-杂芳基烯基衍生物作为治疗剂
公开(公告)号：US07183310B2
公开(公告)日：2007-02-27
申请号：US10915933
申请日：2004-08-10
申请人： Yariv Donde , Robert M. Burk , Michael E. Garst
发明人： Yariv Donde , Robert M. Burk , Michael E. Garst
IPC分类号： A61K31/38 , C07D333/16
CPC分类号： C07D333/28
摘要： A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, having the groups described in detail herein is disclosed. Also disclosed herein are compounds comprising or derivatives thereof, or pharmaceutically acceptable salts, tetrazoles, or prodrugs of compounds of the structure or derivatives thereof, said derivatives being described in detail herein. Also disclosed herein are methods of treating diseases or conditions, including glaucoma and elevated intraocular pressure. Compositions and methods of manufacturing medicaments related thereto are also disclosed.
摘要翻译：公开了具有本文详细描述的基团的化合物或其药学上可接受的盐或其前药。本文还公开了包含其衍生物或其衍生物的化合物或其结构或衍生物的化合物的药学上可接受的盐，四唑或前药，所述衍生物在此详细描述。本文还公开了治疗疾病或病症的方法，包括青光眼和眼内压升高。还公开了与其相关的药物制备的组合物和方法。

45. 发明授权

US07101904B2 Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents 有权
标题翻译：环戊烷庚烷（ENE）OIC酸，2-杂芳基烯基衍生物作为治疗剂
公开(公告)号：US07101904B2
公开(公告)日：2006-09-05
申请号：US10915987
申请日：2004-08-10
申请人： Yariv Donde , Robert M. Burk , Michael E. Garst
发明人： Yariv Donde , Robert M. Burk , Michael E. Garst
IPC分类号： C07D333/10 , A61K31/381 , C07D333/28 , C07D333/32
CPC分类号： C07D333/16 , C07D333/28
摘要： A compound or a pharmaceutically acceptable salt or a prodrug thereof, wherein A, B, R1, R2, D, and E are defined herein. Use of the diseases for the treatment of diseases, and compositions and medicaments related thereto are also disclosed.
摘要翻译：其中A，B，R 1，R 2，D和E的化合物或其药学上可接受的盐或前体药物在本文中定义。还公开了用于治疗疾病的疾病的使用，以及与其相关的组合物和药物。

46. 发明授权

US06350442B2 Ocular treatment using cyclosporin-A derivatives 有权
标题翻译：使用环孢菌素A衍生物进行眼部治疗
公开(公告)号：US06350442B2
公开(公告)日：2002-02-26
申请号：US09870256
申请日：2001-05-30
申请人： Michael E. Garst
发明人： Michael E. Garst
IPC分类号： A61K3174
CPC分类号： A61K38/13 , A61K9/0048
摘要： A method of treating a disorder in an eye, for example, an aqueous deficient dry eye state, phacoanaphylactic endophthalmitis, or uveitis, is provided. The method generally includes administering a therapeutically effective amount of a certain cyclosporin A derivative topically to the affected eye. The derivative may be administered as a solution, suspension or ointment in a pharmaceutically acceptable excipient.
摘要翻译：提供了治疗眼睛疾病的方法，例如水性缺血性干眼症，超声乳内镜眼内炎或葡萄膜炎。该方法通常包括向受影响的眼部局部施用治疗有效量的某种环孢菌素A衍生物。衍生物可以作为药学上可接受的赋形剂中的溶液，悬浮液或软膏施用。

47. 发明授权

US06294563B1 Combinations of prostaglandins and brimonidine or derivatives thereof 有权
标题翻译：前列腺素和溴莫尼定或其衍生物的组合
公开(公告)号：US06294563B1
公开(公告)日：2001-09-25
申请号：US09440379
申请日：1999-11-15
申请人： Michael E. Garst
发明人： Michael E. Garst
IPC分类号： A61K31415
CPC分类号： A61K31/5575 , A61K31/557 , A61K31/5585 , Y10S514/912 , Y10S514/913 , A61K2300/00
摘要： The invention concerns combinations of alpha adrenergic agents such as brimonidine and its derivatives as represented by formula (I) below wherein each Y is independently selected from the group consisting of N, N—CH3, O, S and C—R1; R1 is hydrogen, lower alkyl or oxo; R2, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, lower alkyl and lower alkenyl; n is an integer from 1 to 3; and a broken line beside a solid line indicates either a single or a double bond with the proviso that when n=1, both bonds from Y to C—R1 cannot be double bonds, and prostaglandins known in the art to cause lowering of intraocular pressure which are useful in compositions, methods of treatment and articles of manufacture for the treatment of glaucoma and alleviation of elevated intraocular pressure and providing neuroprotection.
摘要翻译：本发明涉及α型肾上腺素能药物的组合，例如由下式（I）表示的溴莫尼定及其衍生物，其中每个Y独立地选自N，N-CH 3，O，S和C-R 1; R1是氢，低级烷基或氧代; R2，R3和R4独立地选自氢，卤素，低级烷基和低级烯基; n为1〜3的整数，而实线旁边的虚线表示单键或双键，条件是当n = 1时，Y到C-R1的两个键都不能是双键，而本领域已知的引起眼压降低的前列腺素可用于治疗青光眼的组合物，治疗方法和制品，并且降低眼内压升高并提供神经保护作用。

48. 发明授权

US6093734A Prodrugs of proton pump inhibitors 失效
标题翻译：质子泵抑制剂的前药
公开(公告)号：US6093734A
公开(公告)日：2000-07-25
申请号：US131481
申请日：1998-08-10
申请人： Michael E. Garst , George Sachs , Jai Moo Shin
发明人： Michael E. Garst , George Sachs , Jai Moo Shin
IPC分类号： C07D235/28 , C07D401/12 , C07D401/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07F9/6558 , A61K31/4439 , A61K31/445 , C07D413/12
CPC分类号： C07D401/12 , C07D235/28 , C07D401/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07F9/65583
摘要： Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable sulfinyl or arylsulfonyl group attached to the benzimidazole nitrogen, or include a group that forms a Mannich base with the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs. The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion.
摘要翻译：吡啶基甲基亚磺酰基苯并咪唑型质子泵抑制剂药物的前药具有与苯并咪唑氮连接的可水解亚磺酰基或芳基磺酰基，或包括与苯并咪唑氮形成曼尼希碱的基团。本发明的前药在生理条件下水解以提供质子泵抑制剂，其半衰期可在几小时内测量，并且能够提供质子泵抑制剂药物的持续血浆浓度比目前使用的药物更长时间。在生理条件下从本发明前药产生的质子泵抑制剂药物可以更有效地治疗由胃酸分泌引起的几种疾病和病症。

49. 发明授权

US5773654A 7-(5-substituted cyclopentyl) and (5-substituted cyclopentenyl) heptyl alcohols, heptylamines and heptanoic acid amides, and method of lowering intraocular pressure in the eye of a mammal by administration of these compounds 失效
公开(公告)号：US5773654A
公开(公告)日：1998-06-30
申请号：US899972
申请日：1997-07-24
申请人： Michael E. Garst , Robert M. Burk
发明人： Michael E. Garst , Robert M. Burk
IPC分类号： A61K31/557 , A61K31/5575 , A61P27/02 , C07C405/00 , C07C403/00
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0041
摘要： Compounds of the formula ##STR1## where the dotted line represents a bond or the absence of a bond, the wavy lines represent bonds which are either in cis or trans configuration; R.sub.1 represents H, or CO-R.sub.2 where R.sub.2 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group; X represents CO-NR.sub.3 R.sub.4, CH.sub.2 OH, CH.sub.2 OR.sub.5, CH.sub.2 O-COR.sub.6, and CH.sub.2 -NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 independently are H or lower alkyl, R.sub.5 is lower alkyl of 1 to 6 carbons, and R.sub.6 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group, and n is an integer between 0 and 8 are capable of lowering intraocular pressure in the eye of a mammal.

50. 发明授权

US5675019A Process for making piloloctam and derivatives thereof 失效
标题翻译：吡罗克定及其衍生物的制备方法
公开(公告)号：US5675019A
公开(公告)日：1997-10-07
申请号：US685897
申请日：1996-07-18
申请人： Lloyd J. Dolby , Nestor A. Fedoruk , Shervin Esfandiari , Michael E. Garst
发明人： Lloyd J. Dolby , Nestor A. Fedoruk , Shervin Esfandiari , Michael E. Garst
IPC分类号： C07D207/26 , C07D207/267
CPC分类号： C07D207/26
摘要： A process of preparing lactam derivatives of pilocarpine is disclosed. The process involves condensation of a dihydroxybutene and alkyl orthoester to form a lactone intermediate which is oxidized to trans-pilopic acid. This lactone ring is reacted with a benzylamine and the benzyl group removed with a novel dissolving metal reduction mixture to yield the key intermediate IV ##STR1## which can be elaborated to pilolactam through a known sequence of steps.
摘要翻译：公开了制备毛果芸香碱内酰胺衍生物的方法。该方法涉及二羟基丁烯和烷基原酸酯的缩合形成内酯中间体，其被氧化成反式吡啶酸。该内酯环与苄胺反应，并用新的溶解金属还原混合物除去苄基，得到关键的中间体式IV，其可以通过已知的步骤顺序制备成吡咯酰胺。

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