发明名称 Relaxing, or increasing cyclic adenosine monophosphate concentration in smooth muscular tissue, e.g. by administration of cAMP phosphodiesterase inhibitors, dipyridamole or sildenafil
摘要 The use of cyclic adenosine monophosphate (cAMP) phosphodiesterase (PDE) inhibitors (I) is claimed in the production of medicaments for the relaxation of smooth muscular tissue or for increasing the cAMP concentration in smooth muscular tissue. Independent claims are included for the following: (i) the use of the following compounds (II) as for (I) above: (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-2,5-dimethyl-3-benzyl-cyclopenta (4,5)-imidazo (2,1-b) purin-4(3H)-one; (6aR,9aS)-benzyl-5,6a,7,8,9,9a-hexahydro-5-methyl-3-benzyl-cyclopenta (4,5)-imidazo (2,1-b) purin-4(3H)-one; rac-(6aR asterisk ,9aS asterisk )-5,6a,7,8,9,9a-hexahydro-5-methyl-1-benzyl-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; (6aR,9aS)-3,5-dimethyl-5,6a,7,8,9,9a-hexahydro-1-benzyl-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; rac-(6a asterisk R,9aS asterisk )-5,6a,7,8,9,9a-hexahydro-1,5-dimethyl-3-benzyl-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; rac-(6a asterisk R,9aS asterisk )-1,3-dibenzyl-5,6a,7,8,9,9a-hexahydro-5-methyl-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; rac-(6a asterisk R,9aS asterisk )-5,6a,7,8,9,9a-hexahydro-2,5-dimethyl-3-benzyl-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one;(6aR,9aS)-5,6a,7,8,9,9a-hexahydro-2,5-dimethyl-3-b enzyl-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; 2',5'-dimethyl-3'-benzyl-spiro-(cyclopentane-1,7'(8'H)-(2H) imidazo (1,2-a) pyrazolo (4,3-e) pyrimidine)-4'(5'H)-one; 7,8-dihydro-3-benzyl-2,5,7,7-tetramethyl-(2H)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; (7R)-7,8-dihydro-2,5-dimethyl-7-isopropyl-3-benzyl-(2H)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-phenyl-2-benzyl-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; rac-(6aR asterisk ,9aS asterisk )-5,6a,7,8,9,9a-hexahydro-5-methyl-3-benzyl-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; (6aR,9aS)-3,5-dimethyl-5,6a,7,8,9,9a-hexahydro-cyclopenta (4,5)-imidazo (1,2-a) pyrazolo (4,3-e) pyrimidin-4(1H)-one; 2-(2-propoxyphenyl)-8-azapurin-6-one (zaprinast); dipyridamole; 1-(3-chlorophenylamino)-4-phenylphthalazine; 2-(N-(4-carboxypiperidine)-6-chloro-4-(3,4-methylenedioxy)-benzyl)-ami no)-quinazoline; 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxin-2-methanol; 4-((3,4-methylenedioxy)-benzyl)-amino)-6,7,8-trimethoxy-quinazoline; 1-methyl-3'-propyl-6-(5-(N-(4-methylmorpholino)-sulfonyl)-2-ethoxyphen yl)-pyrazolo (4,5) pyrimidin-4(5H)-one (sildenafil); 2-n-butyl-5-chloro-1-(2-chlorobenzyl)-4-methylacetate-imidazole; 1-cyclopentyl-3-methyl-6-(4-pyridinyl)-pyrazolo (3,4-d) pyrimidin-4(5H)-one; 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxypropoxy)-2-carboxy -2,3-didehydro-chroman-4-one; quinazolines or their trimethoxy derivatives; or pyrazolopyrimidines and (ii) the use of sildenafil, IC 351 or BAY-9456 for the production of medicaments for the treatment of diseases in which an increase of the cAMP concentration in smooth muscular tissue.
申请公布号 DE19931206(A1) 申请公布日期 2001.01.11
申请号 DE19991031206 申请日期 1999.07.07
申请人 STIEF, CHRISTIAN 发明人 STIEF, CHRISTIAN G.;UECKERT, STEFAN;BECKER, ARMIN;JONAS, UDO;FORSSMANN, WOLF-GEORG
分类号 A61K31/00;A61K31/352;A61K31/357;A61K31/502;A61K31/517;A61K31/519;(IPC1-7):A61K31/505 主分类号 A61K31/00
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