Patent DE-19931206-A1 (DE)
Title: Relaxing, or increasing cyclic adenosine monophosphate concentration in smooth muscular tissue, e.g. by administration of cAMP phosphodiesterase inhibitors, dipyridamole or sildenafil
Inventor: STIEF CHRISTIAN G
IPC: A61K31/00
Filed: 1999-07-07
Abstract: 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.