申请人:LILLY S.A.
公开号:EP0371594A1
公开(公告)日:1990-06-06
A pharmaceutical compound of the formula
in which R¹, R² and R³ independently are hydrogen, hydroxy, halo, nitro, amino, C₂₋₅ acylamino, C₁₋₄ alkyl, -CHO, -CH₂OH, -CH₂OC₁₋₄ alkyl, -COOH, -COC₁₋₃ alkyl, -CH(OH)C₁₋₃ alkyl, C₁₋₄ alkoxy, C₂₋₄ alkenyloxy, C₁₋₄ alkylthio, C₁₋₄ alkylsulphinyl, C₁₋₄ alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R¹ and R² together form a C₁₋₅ alkylene bridge; provided that at least one of R² and R³ is C₁₋₄ alkoxy or C₂₋₄ alkenyloxy; and X is (i) -(CH₂)nN(R⁴)₂ where each R⁴ independently is C₁₋₄ alkyl, C₂₋₄ alkenyl or optionally substituted C₆H₅CH₂-, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C₁₋₃ alkylene chain; and salts and esters thereof.
一种药物化合物,其化学式为
其中 R¹、R² 和 R³ 独立地为氢、羟基、卤代、硝基、氨基、C₂₋₅酰氨基、C₁₋₄ 烷基、-CHO、-CH₂OH、-CH₂OC、-CH₂₁₋₄ 烷基、-COOH、-COC₁₋₃烷基、-CH(OH)C₁₋₃烷基、C₁₋₄ 烷氧基、C₂₋₄烯氧基、C₁₋₄ 烷硫基、C₁₋₄ 烷硫基、C₁₋₄烷基磺酰基、N-取代的杂环基、任选取代的苯基、任选取代的苯硫基、任选取代的苯基亚磺酰基、任选取代的苯基磺酰基或任选取代的苯基磺酰氨基,或 R¹ 和 R² 共同形成 C₁₋₅亚烷基桥;条件是 R² 和 R³ 中至少有一个是 C₁₋₄ 烷氧基或 C₂₋₄ 烯氧基;和 X 是 (i) -(CH₂)nN(R⁴)₂ 其中每个 R⁴ 独立地是 C₁₋₄ 烷基、C₂₋₄ 烯基或任选取代的 C₆H₅CH₂-,且 n 是 1、2 或 3、或 (ii) 直接连接到氨基氮或通过 C₁₋₃ 亚烷基链连接的含有一个或两个氮原子的 5 至 8 元脂环基团;及其盐类和酯类。