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1.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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2.发明公开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：EP1157000A1
公开(公告)日：2001-11-28
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.
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3.发明授权BRANCHED CHAIN AMINO ACID-DEPENDENT AMINOTRANSFERASE INHIBITORS AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES 有权支链氨基酸依赖性氨基转移酶的抑制剂，它们在神经退行性疾病的治疗
公开(公告)号：EP1320523B1
公开(公告)日：2005-06-22
申请号：EP01964182.8
申请日：2001-08-17
发明人： BORA, Keenan, Martin , HU, Lain-Yen , KESTEN, Suzanne, Ross , LEI, Huanyshu , MORELAND, David, Winslow , RAFFERTY, Michael, Francis , RYDER, Todd, Robert , SCHOLTEN, Jeffrey, David , WUSTROW, David, Juergen
IPC分类号： C07D209/18
CPC分类号： C07D307/79 , C07C311/49 , C07D209/08 , C07D209/30 , C07D209/88 , C07D215/48 , C07D215/50 , C07D307/84 , C07D307/91 , C07D307/92
摘要： The invention relates to BCAT inhibitor compounds of formula (I) and use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
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4.发明公开4(3)SUBSTITUTED-4(3)-AMINOMETHYL-(THIO)PYRAN OR -PIPERIDINE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS 审中-公开4（3） - 取代-4（3）氨基甲基（硫代）OR PYRAN - 哌啶衍生物（=加巴喷丁类似物），它们的制备和它们在神经系统病症的治疗
公开(公告)号：EP1045834A1
公开(公告)日：2000-10-25
申请号：EP98958528.6
申请日：1998-11-10
发明人： BRYANS, Justin Stephen , HORWELL, David Christopher , KNEEN, Clare Octavia , WUSTROW, David, Juergen
IPC分类号： C07D211/26 , A61K31/445 , C07D211/34 , C07F9/38 , A61K31/66 , C07D413/06 , C07D401/06 , C07D417/06 , C07D419/06 , C07D309/04 , A61K31/35 , A61K31/41 , C07D407/06 , C07D335/02 , A61K31/38
CPC分类号： C07F9/655363 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D257/04 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/592 , C07F9/6552
摘要： Novel amines of formulas 1D and 1Eare disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 公式一维和1Eare盘的新cardamines游离缺失的，且与癫痫，昏厥发作，运动机能减退，颅异常，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理疾病，炎性疾病和胃肠功能紊乱，爱尤其是肠易激综合征的治疗剂 ， 因此用于制备和中间体在制备有用的方法是游离缺失盘。
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5.发明授权1-SUBSTITUTED-1-AMINOMETHYL-CYCLOALKANE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS 有权1-取代的1氨基甲基CYCLO的烷衍生物（=加巴喷丁类似物），生产和它们在神经系统病症的治疗
公开(公告)号：EP1047678B1
公开(公告)日：2004-09-08
申请号：EP98957745.7
申请日：1998-11-10
发明人： BRYANS, Justin Stephen , CAPIRIS, Thomas , HORWELL, David Christopher , KNEEN, Clare Octavia , WUSTROW, David, Juergen
IPC分类号： C07D257/04 , A61K31/41 , C07D271/06 , C07F9/38 , A61K31/66 , C07D291/04 , C07C311/10 , A61K31/18 , C07C311/07 , C07C239/14 , A61K31/16 , C07C309/25 , A61K31/255
CPC分类号： C07D257/04 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/592 , C07F9/6552 , C07F9/655363
摘要： Novel amines of formulas 1, 1C, 1F, 1G and 1H or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, heterocycle, sulfonic acid, or hydroxamic acid; A' is a bridged ring selected from wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.
摘要翻译： 式（1），（1C），（1F），（1G）和（1个H）或其药学上可接受的盐，其中n是从0至2的整数的新颖胺; m是从0至3的整数; R是磺酰胺，酰胺，膦酸基，杂环，磺酸，或异羟肟酸; A“是由式（1），（2），（3），（4），（5）是worin连接点中选择的桥连的环; Z1到Z4是选自氢和甲基中选择的每个unabhängig; o是1至4的整数; 且p是上述R为0〜2。在式（1）的整数不能磺酸当m为2和n为1的盘游离缺失和是有用的，如癫痫，昏厥发作，运动机能减退，颅异常的治疗剂 ，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理症状，特别是肠易激综合征。
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6.发明授权1,3-SUBSTITUTED CYCLOALKENES AND CYCLOALKANES AS CENTRAL NERVOUS SYSTEM AGENTS 失效1,3-取代的环烯烃和环烷烃WITH中枢神经系统影响
公开(公告)号：EP0613465B1
公开(公告)日：2001-10-04
申请号：EP92925105.6
申请日：1992-11-05
发明人： CAPRATHE, Bradley, William , DOWNING, Dennis, Michael , JAEN, Juan, Carlos , JOHNSON, Stephen, Joseph , SMITH, William, John, III , WISE, Lawrence, David , WRIGHT, Jonathan , WUSTROW, David, Juergen
IPC分类号： C07D211/70 , C07D213/74 , A61K31/435 , A61K31/495 , C07D239/42 , C07D295/02 , C07D401/08 , C07D405/08
CPC分类号： C07D213/74 , C07D211/70 , C07D295/03 , C07D401/08 , C07D405/08 , C07D409/04 , C07D409/08
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7.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：EP1032555B1
公开(公告)日：2006-04-12
申请号：EP98950649.8
申请日：1998-09-23
发明人： BRYANS, Justin Stephen , HORWELL, David Christopher , THORPE, Andrew, John , WUSTROW, David, Juergen , YUEN, Po-Wai
IPC分类号： C07C229/28 , C07C229/34 , A61K31/195
CPC分类号： C07D221/20 , C07C49/417 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/28 , C07C229/34 , C07C2601/04 , C07C2601/08 , C07C2602/50 , C07D209/96 , C07D307/94 , C07D311/96
摘要： The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
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公开(公告)号：EP0906294B1
公开(公告)日：2003-01-29
申请号：EP97925651.8
申请日：1997-05-20
IPC分类号： C07D265/36 , C07D413/12 , C07D413/06 , C07D417/12 , A61K31/535
CPC分类号： C07D413/06 , C07D265/36 , C07D413/12 , C07D417/12
摘要： Compounds having formulae (I) or (II) wherein R?1 and R2¿ are independently hydrogen or C¿1?-C6 alkyl; X is N or CH; and R?3¿ is phenyl, naphthyl, heteroaryl, substituted phenyl, substituted naphthyl or substituted heteroaryl, wherein each substituent is independently selected from halogen, C¿1?-C6 alkoxy, C1-C6 alkyl, -CN, -CF3, or sulphonamido, and the pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, are antagonists of dopamine D4 receptors.
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公开(公告)号：EP1192125A2
公开(公告)日：2002-04-03
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, Jacop, 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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