公开(公告)号：EP1033978A1

公开(公告)日：2000-09-13

申请号：EP99910359.1

申请日：1999-03-18

申请人： LTS Lohmann Therapie-Systeme AG ,  Discovery Therapeutics, Inc.

发明人： MÜLLER, Walter ,  PECK, James, V.

IPC分类号： A61K9/70

CPC分类号： A61K9/7061 ,  A61K9/7023 ,  A61K9/703 ,  A61K9/7038 ,  A61K9/7069 ,  A61K9/7084 ,  A61K9/7092 ,  A61K31/381

摘要： The invention relates to a transdermal therapeutic system comprising a back layer which is inert with respect to the constituents of the matrix, a self-adhesive matrix layer containing an effective quantity of (-)-5,6,7,8,-tetrahydro-6-[propyl[2-(2-thienyl)-ethyl]amino]-1-naphthol, and a protective film which is to be removed before use. The invention is characterized by a matrix based on a non-aqueous polymer adhesive system, said system being based on acrylate or silicon, with a solubility for (-)-5,6,7,8,-tetrahydro-6-[propyl[2-(2-thienyl)-ethyl]amino]-1-naphthol of ≥5 % g/g. Said matrix is essentially free of inorganic silicate particles.

公开(公告)号：EP1033978B1

公开(公告)日：2001-12-19

申请号：EP99910359.1

申请日：1999-03-18

申请人： LTS Lohmann Therapie-Systeme AG ,  Discovery Therapeutics, Inc.

发明人： MÜLLER, Walter ,  PECK, James, V.

IPC分类号： A61K9/70

CPC分类号： A61K9/7061 ,  A61K9/7023 ,  A61K9/703 ,  A61K9/7038 ,  A61K9/7069 ,  A61K9/7084 ,  A61K9/7092 ,  A61K31/381

摘要： The invention relates to a transdermal therapeutic system comprising a back layer which is inert with respect to the constituents of the matrix, a self-adhesive matrix layer containing an effective quantity of (-)-5,6,7,8,-tetrahydro-6-[propyl[2-(2-thienyl)-ethyl]amino]-1-naphthol, and a protective film which is to be removed before use. The invention is characterized by a matrix based on a non-aqueous polymer adhesive system, said system being based on acrylate or silicon, with a solubility for (-)-5,6,7,8,-tetrahydro-6-[propyl[2-(2-thienyl)-ethyl]amino]-1-naphthol of >/=5 % g/g. Said matrix is essentially free of inorganic silicate particles.

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.