公开(公告)号：EP0778836A1

公开(公告)日：1997-06-18

申请号：EP95930252.0

申请日：1995-08-22

申请人： Discovery Therapeutics, Inc.

发明人： PECK, James, V. ,  WYSOCKI, Ronald, J. ,  UWAYDAH, Ibrahim, M. ,  CUSACK, Noel, J.

IPC分类号： A61K31 ,  A61P7 ,  A61P9 ,  A61P13 ,  A61P15 ,  A61P25 ,  C07D473

CPC分类号： C07D473/34

摘要： Compounds of formula (I) where R1 is C1-C4 alkyl; R2 is H, -OR1, -SR1, -NH(R1), -N(R4)(R5), aminocarbonyl, halogen, or -CN, where R4 and R5 are independently C1-C6 alkyl, or together form a 3- to 7-membered heterocycloalkyl, such heteroatom selected from oxygen, nitrogen, and sulfur, optionally including an additional heteroatom which is nitrogen, oxygen, or sulfur; R3 is cyclopentyl or (a) where R' and R'' are independently H=O, -OH, or -NH2 or R' and R'' can together form (b), R''' is -OH or -NH2; provided that when R3 is cylopentyl or norbonyl, R2 cannot be H or halogen; and pharmaceutically-acceptable salts thereof. These are diuretics; renal protectives against renal failure; agents to facilitate recovery from coma, to improve the therapeutic outcome resulting from defibrillation or cardiopulmonary resuscitation by preventing post-resuscitation bradycardia, bradyarrhythmia and cardioplegia, to restore cardiac function following a cardioplegia procedure, and to treat or prevent intermittent claudication.