申请人:American Home Products Corporation
公开号:US05605918A1
公开(公告)日:1997-02-25
This invention relates to novel 5-[3-aryl-prop-2-ynyl]-5-(arylsulfonyl)thiazolidine-2,4-diones and 5-[3-aryl-prop-2-ynyl]-5-(arylsulfanyl)thiazolidine-2,4-diones characterized by the general formula (I), seen below, wherein Ar is phenyl, 2-naphthyl, alkyl substituted phenyl, alkoxy substituted phenyl, halogen substituted phenyl, 2-pyridinyl, substituted 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 2-quinolinyl, 2-pyrimidinyl, 2-benzoxazolyl, 2-benzthiazolyl, 2-benzimidazolyl, 2-furanyl, 2-benzo-[b]-furanyl, 2-thienyl, or 2-benzo-[b]-thienyl; n is 0 or 2; and Ar' is phenyl, alkyl substituted phenyl, perfluoroalkyl substituted phenyl, halogen substituted phenyl, alkoxy substituted phenyl, perfluoroalkoxy substituted phenyl or alkylthio substituted phenyl: ##STR1## This invention also relates to the use of the abovementioned compounds in lowering the blood glucose levels in hyperglycemic mammals and pharmaceutical compositions containing the same.
本发明涉及新颖的5-[3-芳基-丙-2-炔基]-5-(芳基磺酰基)
噻唑烷-2,4-二酮和5-[3-芳基-丙-2-炔基]-5-(芳基
硫基)
噻唑烷-2,4-二酮,其特征是具有下面的通式(I),其中Ar是苯基、2-
萘基、烷基取代的苯基、烷氧基取代的苯基、卤素取代的苯基、2-
吡啶基、取代的2-
吡啶基、3-
吡啶基、4-
吡啶基、2-
喹啉基、2-
嘧啶基、2-苯并
噁唑基、2-
苯并噻唑基、2-
苯并咪唑基、2-
呋喃基、2-苯并[b]-
呋喃基、2-
噻吩基或2-苯并[b]-
噻吩基;n为0或2;Ar'是苯基、烷基取代的苯基、
全氟烷基取代的苯基、卤素取代的苯基、烷氧基取代的苯基、
全氟烷氧基取代的苯基或烷基
硫基取代的苯基: ##STR1## 本发明还涉及上述化合物在降低高血糖哺乳动物的血糖
水平和含有它们的制药组合物中的用途。