Disclosed are the pyrrolylphenyl-substituted hydroxamic acid derivatives of the formula
wherein R represents hydrogen, lower alkyl, halogen or lower alkoxy; R₁ and R₂ independently represent hydrogen, lower alkyl or aryl; Y represents a direct bond, lower alkylene, lower alkenylene, lower alkadienylene, (thio, sulfinyl or sulfonyl)-lower alkylene or oxy-lower alkylene; Z represents
wherein R₃ represents hydrogen or acyl; R₄ represents lower alkyl, C₃-C₇-cycloalkyl, aryl or aryl-lower alkyl; or Z represents
wherein R₃ represents hydrogen or acyl; R₅ represents lower alkyl, C₃-C₇-cycloalkyl, aryl, aryl-lower alkyl, amino or N-(mono- or di-lower alkyl)-amino; R₆ and R₇ represent hydrogen or lower alkyl; and pharmaceutically acceptable salts thereof provided that R₃ represents hydrogen; which are useful as selective lipoxygenase inhibitors, methods for preparation thereof, pharmaceutical compositions comprising said compounds, and a method of inhibiting lipoxygenase and of treating diseases in mammals which are responsive to lipoxygenase inhibition using said compounds and pharmaceutical compositions comprising said compounds of the invention.
所公开的是式中的
吡咯基苯基取代的羟
肟酸衍
生物
其中 R 代表氢、低级烷基、卤素或低级烷氧基;R₁ 和 R₂ 独立地代表氢、低级烷基或芳基;Y 代表直接键、低级亚烷基、低级亚烯基、低级亚烷基二烯基、(
硫代、亚砜基或磺酰基)-低级亚烷基或氧基-低级亚烷基;Z 代表
其中 R₃ 代表氢或酰基; R₄ 代表低级烷基、C₃-C₇-环烷基、芳基或芳基-低级烷基;或 Z 代表
其中 R₃ 代表氢或酰基;R₅ 代表低级烷基、C₃-C₇-环烷基、芳基、芳基-低级烷基、
氨基或 N-(单-或二-低级烷基)-
氨基;R₆ 和 R₇ 代表氢或低级烷基;及其药学上可接受的盐,条件是 R₃ 代表氢;可用作选择性脂氧合酶
抑制剂、其制备方法、包含所述化合物的药物组合物,以及使用所述化合物和包含本发明所述化合物的药物组合物抑制脂氧合酶和治疗对脂氧合酶抑制有反应的哺乳动物疾病的方法。