首页> 外国专利> Pyrazolo (1,5-a) pyrimidine derivatives (PYRAZOLO 1,5-a PYRIMIDINE DERIVATIVE)

Pyrazolo (1,5-a) pyrimidine derivatives (PYRAZOLO 1,5-a PYRIMIDINE DERIVATIVE)

机译:吡唑并(1,5-a)嘧啶衍生物(吡唑并[1,5-a]嘧啶衍生物)

摘要

The present invention provides pyrazolo [1,5-a] pyrimidine derivatives of the general formula:;Wherein R 1 is hydrogen, lower alkyl, cycloalkyl, thienyl, furyl, lower alkenyl, or lower alkyl, lower alkoxy, which may have thienyl, lower alkoxy, lower alkylthio, oxo or hydroxyl as substituents Phenyl which may have from 1 to 3 substituents selected from the group consisting of phenylthio and halogen; R 2 is naphthyl, cycloalkyl, furyl, thienyl, optionally halogen-substituted pyridyl, optionally halogen-substituted phenoxy, or lower alkyl, lower alkoxy, halogen, nitro, halogen-substituted lower alkyl, 1 to 3 selected from halogen-substituted lower alkoxy, lower alkoxycarbonyl, hydroxyl, phenyl (lower) alkoxy, amino, cyano, lower alkanoyloxy, phenyl and di (lower) alkoxyphosphoryl (lower) alkyl Phenyl which may have a substituent; R 3 is hydrogen, phenyl or lower alkyl; R 4 is hydrogen, lower alkyl, lower alkoxycarbonyl, phenyl (lower) alkyl, optionally phenylthio-substituted phenyl, or halogen; R 5 is hydrogen or lower alkyl; R 6 is benzoyl having 1 to 3 substituents selected from the group consisting of hydrogen, lower alkyl, phenyl (lower) alkyl, or lower alkoxy, halogen-substituted lower alkyl and halogen; R 1 and R 5 may together form a lower alkylene; Q is carbonyl or sulfonyl; A is a single bond, lower alkylene or lower alkenylene; n is 0 or 1;;Such derivatives are useful as analgesics.
机译:本发明提供了具有以下通式的吡唑并[1,5-a]嘧啶衍生物:其中R 1 为氢,低级烷基,环烷基,噻吩基,呋喃基,低级烯基或低级烷基,低级可以具有噻吩基,低级烷氧基,低级烷硫基,氧代或羟基作为取代基的烷氧基,可以具有1-3个选自苯硫基和卤素的取代基; R 2 是萘基,环烷基,呋喃基,噻吩基,任选被卤素取代的吡啶基,任选被卤素取代的苯氧基或低级烷基,低级烷氧基,卤素,硝基,卤素取代的低级烷基,为1至3选自卤素取代的低级烷氧基,低级烷氧基羰基,羟基,苯基(低级)烷氧基,氨基,氰基,低级烷酰氧基,苯基和可具有取代基的二(低级)烷氧基磷酰基(低级)烷基苯基; R 3 为氢,苯基或低级烷基; R 4 为氢,低级烷基,低级烷氧羰基,苯基(低级)烷基,苯硫基取代的苯基或卤素; R 5 为氢或低级烷基; R 6 是具有1至3个选自氢,低级烷基,苯基(低级)烷基或低级烷氧基,卤素取代的低级烷基和卤素的取代基的苯甲酰基; R 1 和R 5 可以一起形成低级亚烷基。 Q是羰基或磺酰基; A是单键,低级亚烷基或低级亚烯基; n为0或1;这类衍生物可用作止痛药。

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