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1.发明授权METHOD FOR THE STEREOSELECTIVE SYNTHESIS OF CYCLIC AMINO ACIDS 有权VERFAHREN ZUR STEREOSELEKTIVEN SYNTHESE ZYKLISCHERAMINOSÄUREN
公开(公告)号：EP1237847B1
公开(公告)日：2006-05-17
申请号：EP00980881.7
申请日：2000-11-30
IPC分类号： C07C227/32 , C07C229/28 , C07C57/46 , C07C255/31 , C07C255/41 , C07C265/08 , C07C271/12 , C07C69/616
CPC分类号： C07C271/12 , C07B2200/07 , C07C51/08 , C07C51/412 , C07C51/43 , C07C69/608 , C07C69/616 , C07C227/32 , C07C229/28 , C07C255/31 , C07C255/41 , C07C265/08 , C07C2601/08 , C07C57/46
摘要： The instant invention is a route to stereospecific 3-substituted 5-membered ring isomers of Formula (A). The final products are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), inflammation especially arthritis, sleep disorders, premenstrual syndrome, and hot flashes. The invention provides novel routes to synthesize stereoselectively analogs of gabapentin (Neurontin®) of Formulas (I), (II), (III) and (IV) wherein R is C1-C10 alkyl or C3-C10 cycloalkyl and pharmaceutically acceptable salts thereof.
摘要翻译： 本发明是式（A）的立体特异性3-取代的5元环异构体的途径。 最终产品可用作治疗癫痫，微弱攻击，运动不良，颅内疾病，神经退行性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，胃肠道疾病如肠易激综合征（IBS），炎症尤其是关节炎， 睡眠障碍，经前期综合征和潮热。 本发明提供了合成式（I），（II），（III）和（IV）的加巴喷丁（Neurontin3）的立体选择性类似物的新途径，其中R是C 1 -C 10烷基或C 3 -C 10环烷基及其药学上可接受的盐。
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2.发明授权MONO-SUBSTITUTED 3-PROPYL GAMMA-AMINOBUTYRIC ACIDS 有权MONO-SUBSTITUIERTE 3-PROPYL-GAMMA-AMINOBUTTERSÄURE
公开(公告)号：EP1192125B9
公开(公告)日：2009-09-16
申请号：EP00938022.1
申请日：2000-05-31
发明人： BELLIOTTI, Thomas, Richard , BRYANS, Justin, Stephen , EKHATO, Ihoezo, Victor , OSUMA, Augustine, Tobi , SCHELKUN, Robert, Michael , THORPE, Andrew, John , WISE, Lawrence, David , WUSTROW, David, Juergen , YUEN, Po-Wai , SCHWARZ, Jacob,Bradley
IPC分类号： C07C229/08 , A61K31/197 , C07C229/30 , C07C229/22 , C07C229/34 , C07C229/32 , C07C229/20 , A61P25/00 , A61P1/00
CPC分类号： C07C229/34 , C07B2200/07 , C07C229/08 , C07C229/20 , C07C229/22 , C07C229/30 , C07C229/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula (I). The compounds are useful as therapeutic agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, arthritis, sleep disorders, IBS, and gastric damage. Methods of preparing the compounds and useful intermediates are also part of the invention.
摘要翻译： 本发明是一系列式（I）的新颖的单取代和二取代的3-丙基γ-氨基丁酸。 这些化合物可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，关节炎，睡眠障碍，IBS和胃损伤的治疗剂。 制备化合物和有用的中间体的方法也是本发明的一部分。
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公开(公告)号：EP1192125B1
公开(公告)日：2008-12-31
申请号：EP00938022.1
申请日：2000-05-31
发明人： BELLIOTTI, Thomas, Richard , BRYANS, Justin, Stephen , EKHATO, Ihoezo, Victor , OSUMA, Augustine, Tobi , SCHELKUN, Robert, Michael , THORPE, Andrew, John , WISE, Lawrence, David , WUSTROW, David, Juergen , YUEN, Po-Wai , SCHWARZ, Jacob,Bradley
IPC分类号： C07C229/08 , A61K31/197 , C07C229/30 , C07C229/22 , C07C229/34 , C07C229/32 , C07C229/20 , A61P25/00 , A61P1/00
CPC分类号： C07C229/34 , C07B2200/07 , C07C229/08 , C07C229/20 , C07C229/22 , C07C229/30 , C07C229/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula (I). The compounds are useful as therapeutic agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, arthritis, sleep disorders, IBS, and gastric damage. Methods of preparing the compounds and useful intermediates are also part of the invention.
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4.发明授权BRANCHED CHAIN AMINO ACID-DEPENDENT AMINOTRANSFERASE INHIBITORS AND THEIR USE IN THE TREATMENT OF DIABETIC RETINOPATHY 有权支链氨基酸依赖性转氨酶INHIBITORE及其用途糖ILL视网膜病
公开(公告)号：EP1157000B1
公开(公告)日：2005-11-02
申请号：EP00977094.2
申请日：2000-11-08
发明人： BRYANS, Justin, Stephen , HU, Lain-Yen , HUTSON, Susan, M. , LANOUE, Kathryn, Foley , LIETH, Erich , RAFFERTY, Michael, Francis , RYDER, Todd, Robert , SU, Ti-Zhi , WELTY, Devin, Franklin , WUSTROW, David, Juergen
IPC分类号： C07C229/28 , C07C59/11 , C07C59/62 , A61K31/19 , A61P27/02
CPC分类号： C07C271/22 , C07C59/11 , C07C229/28 , C07C229/34 , C07C233/47 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： The present invention is directed to a method for the prophylactic and therapeutic treatment of diabetic retinopathy. The method involves the administration of an inhibitor of formulae (I), (II) and (III) of the branch chain amino acid-dependent aminotransferase (BCAT) pathway to an animal, such as a mammal, in particular a human, in an amount sufficient to treat the retina for diabetic retinopathy prophylactically or therapeutically. The present invention is also directed to several novel inhibitors of formula (IV) of the BCAT pathway. In formulae (I-IV), n, m, X and R1-R13 have the meanings given in the description.
摘要翻译： 本发明涉及一种用于糖尿病性视网膜病的预防和治疗的方法。 该方法涉及式餐饮（I）的抑制剂的给药，（II）和（III）的支链氨基酸依赖性酸氨基转移酶的（BCAT）途径给动物，求为哺乳动物，特别是人，在 足量的预防性或治疗性治疗糖尿病视网膜病变视网膜。 因此，本发明涉及式的若干新颖抑制剂BCAT通路（IV）。 在式（I-IV）中，n，M，X和R1-R13具有说明书中给出的含义。
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公开(公告)号：EP1112253B1
公开(公告)日：2004-10-20
申请号：EP99941063.2
申请日：1999-08-11
发明人： BRYANS, Justin, Stephen , EKHATO, Ihoezo, Victor , HORWELL, David, Christopher , LING, Rong , RECEVEUR, Jean-Marie, Residence Chenes-Colombiere , WUSTROW, David, Juergen
IPC分类号： C07D207/16 , A61K31/40
CPC分类号： C07D207/16
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6.发明授权NOVEL STEREOSELECTIVE PROCESSES FOR THE PREPARATION OF GABAPENTIN ANALOGUES 有权STEREOSELEKTIVE VERFAHREN ZUR HERSTELLUNG VON GABAPENTINANALOGEN
公开(公告)号：EP1015415B1
公开(公告)日：2003-05-07
申请号：EP98939340.0
申请日：1998-08-11
IPC分类号： C07C227/22 , C07B53/00
CPC分类号： C07C227/32 , C07C227/22 , C07C2601/14 , C07C229/28
摘要： This invention is novel processes for the stereoselective preparation of gabapentin analogues.
摘要翻译： 本发明是立体选择性制备加巴喷丁类似物的新方法。
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