Use of new and known thiaza heterocyclic N-nitrosimine cpds. - as nitrogen mon:oxide mediating pharmaceuticals to treat and prevent e.g. hypertension, angina, thrombosis and erectile dysfunction

摘要

Use of thiazole, thiazoline and thiadiazole N-nitrosamines (I) as pharmacueticals with nitrogen monoxide-mediating activity is claimed. In the formula R1 is 1-6C alkyl opt. substd. by 4-8C cycloalkyl or aryl; 3-6C alkenyl opt. substd. by aryl; 3-6C alkynyl; 4-8C cycloalkyl; or aryl; A is -CH=CB-; -CR2=CB1-; -CHR2-CH(Ar)-; or -N=CR3; B is H; R2; CO2R2; Ar; or CH(Ar)2; B1 is R2; or Ar; R2 is 1-6C alkyl; R3 is H; 1-6C alkyl; or Ar; Ar is phenyl opt. mono- or di-substd. by 1-4C alkyl, 1-4C alkoxy, F, Cl, Br or NO2. Also claimed are cpds. (I) except N-nitroso-2(3H)-thiazolimines having 3-methyl, 3,4-dimethyl, 3-methyl-4-phenyl or 3,4-diphenyl substitution and N-nitroso-1,3,4-thiadiazol-5(2H)-imines having 3-methyl, 4-methyl or 4-methyl-3-phenyl substitution. USE - Cpds. (I) release nitrogen monoxide and are useful esp. in treating and preventing cardiovascular disorders, e.g. hypertension, angina and thromboses. They may also be used to treat erectile dysfunction. Admin. can be orally, ractally, parenterally or percutaneously in conventional formulations at daily dosage of 0.5-100 mg. pref. 1-20 mg.