New 1-(4-(2-sulfamoyl-3-thienyl)-imidazoles, are potent angiotensin (1-7) receptor agonists useful e.g. for treating hypertension, angina pectoris, cardiac infarction or thrombosis

摘要

1-(4-(2-Sulfamoyl-3-thienyl)-imidazoles (I) and (X) are new. Imidazoles of formula (I) and their stereoisomers (including mixtures in all ratios) and salts are new. R1 = halo, OH, alkoxy (optionally substituted by a saturated cyclic ether), 1-8C alkoxy having 1-6C replaced by O, NH or S, 2-4C alkenyloxy, arylalkoxy or phenoxy (optionally substituted by halo, 1-3C alkyl, 1-3C alkoxy or CF3); R2 = CHO, COOH or alkoxycarbonyl; R3 = alkyl or aryl; R4 = H, halo or alkyl; X = O or S; Y = O or NH; R5 = 1-6C alkyl or alkylaryl; or can also be H if Y = NH; R6 = 1-5C alkyl; alkyl moieties have 1-4C unless specified otherwise; compounds in which R1 = halo and R2 = COOH or alkoxycarbonyl are excluded. Independent claims are also included for: (1) new imidazole derivatives of formula (X) and their stereoisomers (including mixtures) and salts; (2) use of (I) (and their salts etc.), including the known compounds excluded by the proviso, for the preparation of a medicament for the treatment or prophylaxis of diseases primarily or secondarily caused, at least partially, by reduced production and/or release of the vasorelaxant, antithrombotic and cardioprotective messenger cyclic 3',5'-guanosine monophosphate (cGMP) and nitrogen monoxide (NO); and (3) use of angiotensin (1-7) receptor agonists in general for the production of a medicament as specified in (ii). R = H or 1-6C alkyl.