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3-SUBSTITUTED-1,5-DIARLY-2-ALKYL-PYRROLES HIGHLY SELECTIVE AND ORALLY EFFECTIVE COX-2 INHIBITORS

机译:3-取代-1,5-二芳基-2-烷基-吡咯类高效选择性和口头有效的COX-2抑制剂

摘要

This invention relates to 3-substituted-1,5-diaryl-2-alkyl-pyrroles of Formula I, pharmaceutical compositions containing them, and to their use for the pharmacological treatment of pain and COX-2 over-activation associated disorders. Compounds of this invention are new pyrrole derivatives bearing in position -3 of the pyrrole ring, several variously functionalized, not aliphatic, side chains which confer to the compounds a relevant COX-2 potency and selectivity along with a remarkable oral efficacy. Phenyl rings in position -1 and -5 are variously substituted, but compounds of particular interest are those substituted in position -5 with 4-methylsulphonyl-phenyl or with 4-aminosulphonyl-phenyl groups.
机译:本发明涉及式Ⅰ的3-取代的1,5-二芳基-2-烷基-吡咯,含有它们的药物组合物,及其在疼痛和COX-2过度活化相关疾病的药理学治疗中的用途。本发明的化合物是在吡咯环的-3位上带有几个不同官能的非脂族侧链的新型吡咯衍生物,这些化合物赋予化合物相关的COX-2效力和选择性以及显着的口服功效。在-1和-5位上的苯环被各种取代,但特别令人感兴趣的化合物是在-5位上被4-甲基磺酰基-苯基或4-氨基磺酰基-苯基取代的那些。

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