8-quinolinxanthine and 8-isoquinolinxanthine derivs. as PDE 5 inhibitors

游离的或盐形式的式(I)化合物,∴其中R#+[1]是氢或任选地被羟基、烷氧基或烷硫基取代的烷基,R#+[2]是氢、烷基、羟基烷基、烷基羰基氧基烷基、烷氧基烷基、烷硫基烷基、链烯基、环烷基烷基、杂环基烷基、芳烷基,所述芳烷基中的芳环可以任选地与一个5元杂环基团稠合或者任选地被一个或多个选自烷氧基、氨基、烷基氨基、二烷基氨基、酰基氨基、卤素、羟基、氨基磺酰基、烷基氨基磺酰基、二烷基氨基磺酰基、烷基磺酰基氨基或二烷基氨基磺酰基氨基的取代基所取代,R#+[3]是氢或任选地被羟基、烷氧基或烷硫基取代的烷基,R#+[4]是氢或烷基,R#+[5]是喹啉基、异喹啉基或氧代二氢异喹啉基,这些基团任选地与一个5元...

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Hauptverfasser: G. BHALAY, S.P. COLLINGWOOD, R.A. FAIRHURST
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:游离的或盐形式的式(I)化合物,∴其中R#+[1]是氢或任选地被羟基、烷氧基或烷硫基取代的烷基,R#+[2]是氢、烷基、羟基烷基、烷基羰基氧基烷基、烷氧基烷基、烷硫基烷基、链烯基、环烷基烷基、杂环基烷基、芳烷基,所述芳烷基中的芳环可以任选地与一个5元杂环基团稠合或者任选地被一个或多个选自烷氧基、氨基、烷基氨基、二烷基氨基、酰基氨基、卤素、羟基、氨基磺酰基、烷基氨基磺酰基、二烷基氨基磺酰基、烷基磺酰基氨基或二烷基氨基磺酰基氨基的取代基所取代,R#+[3]是氢或任选地被羟基、烷氧基或烷硫基取代的烷基,R#+[4]是氢或烷基,R#+[5]是喹啉基、异喹啉基或氧代二氢异喹啉基,这些基团任选地与一个5元杂环基团稠合并且任选地被一个或多个选自下列的取代基所取代:卤素、氰基、羟基、烷基、羟基烷基、烷氧基烷基、烷硫基烷基、烷氧基、烷硫基、链烯基、烷氧基羰基、链炔基、羧基、酰基、式-N(R#+[6])R#+[7]的基团、任选地被一个或多个选自卤素或烷氧基的取代基取代的芳基、或通过环碳原子与指定碳原子连接的含有5或6个环原子的杂芳基,R#+[6]和R#+[7]彼此独立地是氢或任选地被羟基或烷氧基取代的烷基,或者R#+[6]和R#+[7]中有一个是氢而另一个是酰基,或者R#+[6]和R#+[7]与它们所连接的氮原子合在一起表示5或6元的杂环基团。 A compound of formula (I) in free or salt form, where R is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R is hydrogen or alkyl, R is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula -N(R )R , aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R and R are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R and R is hydrogen and the other is acyl, or R and R together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.