| abstract |
Disclosed as thromboxane synthetase inhibitors are the compounds of formula <IMAGE> (I) wherein R1 represents hydrogen or lower alkyl; Ar represents 3-pyridyl or 1-imidazolyl, each unsubstituted or substituted by lower alkyl, carboxy, lower alkoxycarbonyl or carbamoyl; R2 and R3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, carboxy lower alkyl, lower alkoxycarbonyl lower alkyl, carboxy, lower alkoxycarbonyl, or lower alkyl-(thio, sulfinyl or sulfonyl), or R2 and R3 together on adjacent carbon atoms represent lower alkylenedioxy; A represents straight chain or branched alkylene of 3 to 12 carbon atoms in which the number of the carbon atoms separating the indole nucleus from group B is 3 to 12, straight chain or branched alkenylene of 2 to 12 carbon atoms, straight chain or branched alkynylene of 2 to 12 carbon atoms, lower alkylenephenylene-lower (alkylene or alkenylene), lower alkylenephenylene, lower alkylene-(thio or oxy)-lower alkylene, lower alkylene-(thio or oxy)-phenylene, or lower alkylene-phenylene-(thio or oxy)-lower alkylene; B represents carboxy, esterified carboxy, carbamoyl, mono- or di-lower alkylcarbamoyl, hydroxymethyl, cyano, hydroxycarbamoyl, 5-tetrazolyl or formyl; the imidazolyl and pyridyl N-oxide thereof; or a pharmaceutically acceptable salt thereof; as well as their synthesis, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds. |