申请人:LILLY INDUSTRIES LIMITED
公开号:EP0455356A1
公开(公告)日:1991-11-06
Pharmaceutical compounds of the following formula are described:
in which R¹ is hydrogen, C₁₋₄ alkyl, C₁₋₄ alkoxy-C₁₋₄ alkyl, hydroxy-C₁₋₄ alkyl, optionally substituted phenyl, optionally substituted phenyl-C₁₋₄ alkyl or a heterocycle selected from:
where R³ is hydrogen, C₁₋₄ alkyl, C₁₋₄ alkoxy, nitro, halo, cyano, trifluoromethyl, carboxyl or -CONH₂, and R⁴ is C₁₋₄ alkyl; and R² is hydrogen, C₁₋₄ alkyl, phenyl or thienyl substituted with a carboxyl or C₁₋₄ alkoxy-carbonyl group, an acyl group of the formula R⁵CO- where R⁵ is hydrogen, C₁₋₄ alkyl, C₁₋₄ alkoxy-C₁₋₄ alkyl, halo C₁₋₄ alkyl, C₁₋₄ alkoxy, halo-C₁₋₄ alkoxy, phenyl, phenyl-C₁₋₄ alkyl, -NHC₁₋₄ alkyl, -NH phenyl or
where R⁶ is C₁₋₄ alkyl, or a group of the formula -CH=C(COC₁₋₄ alkoxy)₂; or a salt thereof.
以下是描述的具有以下结构的药物化合物:
其中R¹为
氢、C₁₋₄烷基、C₁₋₄烷
氧基-C₁₋₄烷基、羟基-C₁₋₄烷基、可选择取代的
苯基、可选择取代的
苯基-C₁₋₄烷基或从以下选取的杂环:
其中R³为
氢、C₁₋₄烷基、C₁₋₄烷
氧基、硝基、卤素、
氰基、三
氟甲基、羧基或-CONH₂,R⁴为C₁₋₄烷基;而R²为
氢、C₁₋₄烷基、
苯基或经羧基或C₁₋₄烷
氧基羰基取代的
噻吩基,具有R⁵CO-式的酰基,其中R⁵为
氢、C₁₋₄烷基、C₁₋₄烷
氧基-C₁₋₄烷基、卤素C₁₋₄烷基、C₁₋₄烷
氧基、卤素-C₁₋₄烷
氧基、
苯基、
苯基-C₁₋₄烷基、-NHC₁₋₄烷基、-NH
苯基或
其中R⁶为C₁₋₄烷基,或具有-CH=C(COC₁₋₄烷
氧基)₂式的基团;或其盐。