公开(公告)号：EP1009399B1

公开(公告)日：2010-03-24

申请号：EP98945758.5

申请日：1998-08-18

申请人： Warner-Lambert Company LLC ,  The Board of Regents for the University of Oklahoma

发明人： GUGLIETTA, Antonio ,  TAYLOR, Charles, Price, Jr. ,  REN, Jiayuan ,  WATSON, W. P. ,  RAFFERTY, Michael, Francis ,  DIOP, Laurent ,  CHOVET, Maria ,  BUENO, Lionel ,  LITTLE, Hilary J.

IPC分类号： A61K31/195 ,  A61P1/00

CPC分类号： A61K31/42 ,  A61K31/195 ,  A61K31/197 ,  A61K31/40 ,  A61K31/405 ,  A61K31/54 ,  A61K31/60 ,  A61K45/06 ,  A61K31/19 ,  A61K2300/00

公开(公告)号：EP1320523A2

公开(公告)日：2003-06-25

申请号：EP01964182.8

申请日：2001-08-17

申请人： Warner-Lambert Company LLC

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.

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

申请人： Warner-Lambert Company LLC

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.

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

申请人： Warner-Lambert Company LLC ,  THE PENN STATE RESEARCH FOUNDATION ,  WAKE FOREST UNIVERSITY

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。