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121. 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。

122. 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。

123. 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。

124. 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。

125. 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。

126. 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.

127. 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。

128. 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。

129. 发明授权

US5552434A 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
标题翻译： 7-（5-取代的环戊基）和（5-取代的环戊烯基）庚醇，庚胺和庚酸酰胺，以及通过施用这些化合物降低哺乳动物眼睛的眼内压的方法
公开(公告)号：US5552434A
公开(公告)日：1996-09-03
申请号：US355463
申请日：1994-12-14
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
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.
摘要翻译：其中虚线代表键或不存在键的式“IMAGE”的化合物，波浪线表示顺式或反式构型的键; R1表示H或CO-R2，其中R2是1至6个碳的低级烷基，碳环芳基或杂环芳基; 或碳环芳基或杂芳基取代的低级烷基; X表示CO-NR 3 R 4，CH 2 OH，CH 2 OR 5，CH 2 O-COR 6和CH 2 -NR 3 R 4，其中R 3和R 4独立地是H或低级烷基，R 5是1至6个碳的低级烷基，并且R 6是1至6个碳的低级烷基，碳环芳基或杂环芳基; 或碳环芳基或杂芳基取代的低级烷基，n是0至8之间的整数能够降低哺乳动物眼睛的眼内压。

130. 发明授权

US5468778A Method of lowering intraocular pressure by administering a pharmaceutical composition containing 7-(5-substituted cyclopentyl) and 7-(5-substituted-cyclopentenyl) 5-heptenoic acids and derivatives 失效
标题翻译：通过施用含有7-（5-取代的环戊基）和7-（5-取代的环戊烯基）-5-庚烯酸和衍生物的药物组合物来降低眼内压的方法
公开(公告)号：US5468778A
公开(公告)日：1995-11-21
申请号：US950855
申请日：1992-09-24
申请人： Michael E. Garst , Robert M. Burk , Ming F. Chan , Michael B. Roof
发明人： Michael E. Garst , Robert M. Burk , Ming F. Chan , Michael B. Roof
IPC分类号： A61K31/557 , A61K31/19 , A61K31/215
CPC分类号： A61K31/557 , Y10S514/913
摘要： Intraocular pressure is lowered in the eye of a mammal by administration of a pharmaceutical composition containing as active ingredient a compound of the formula ##STR1## where the dotted line represents a bond or the absence of a bond, wavy lines connected to the olefinic bond represent cis or trans configuration about the olefinic bond; R.sub.1 represents H, or CO-R.sub.3 where R.sub.3 is lower alkyl of 1 to 6 carbons, carbocyclic aryl or heterocyclic aryl; or carbocyclic aryl or heteroaryl substituted lower alkyl group; R.sub.2 represents H or lower alkyl of 1 to 6 carbons, and n is an integer between 0 and 8.
摘要翻译：通过给药含有作为活性成分的式“IMAGE”的化合物的药物组合物，在哺乳动物的眼睛中降低眼内压，其中虚线表示键或不存在键，与烯键连接的波浪线代表关于烯键的顺式或反式构型; R1表示H或CO-R3，其中R3是1至6个碳的低级烷基，碳环芳基或杂环芳基; 或碳环芳基或杂芳基取代的低级烷基; R2表示H或碳原子数为1〜6的低级烷基，n为0〜8的整数。

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