UN PROCEDIMIENTO PARA LA PREPARACION DE 3-OR7- O 3-SR7- PIRAZINAMIDOGUANIDINAS.

摘要

1,181,034. Diuretics. MERCK & CO. Inc. 22 April, 1968 [27 April, 1967], No. 18933/68. Heading A5B. [Also in Division C2] Pharmaceutical compositions, in the form of pills tablets, capsules, elixirs and injectionable preparations, a novel pyrazinamidoguanidine or a pharmaceutically acceptable acid addition salt thereof of the formula: wherein Z is OR7, wherein R7 is H, C 1-5 alkyl or phenyl C 1-5 alkyl, or SR8 wherein R8 is H, C 1-5 alkyl, aralkyl or mononuclear aryl X is H, halogen, C 1-5 alkyl, C 3-6 cycloalkyl, mononuclear aryl, halo-mononuclear aryl; Y is H, OH, C 1-5 alkoxy, C 1-3 alkylthio, C 1-5 alkyl, W, W, W-trifluoro-C 1-5 alkyl, C 3-6 cycloalkyl, mononuclear aryl or -N(R5)R6, wherein R5 is H or C 1-5 alkyl and R6 is H, C 1-5 alkyl, hydroxy-C 1-5 alkyl, W, W, W-trifluoro-C 1-5 alkyl, (C 3-6 cycloalkyl)-(C 1-5 alkyl), C 1-5 alkylmononuclear aryl-C 1-5 alkyl, halomononuclear aryl C 1-5 alkyl C 2-5 alkenyl, C 3-5 alkynyl, C 3-6 cycloalkyl, C 1-3 alkoxy-C 1-5 alkyl, mononuclear aryl, or heterocyclic C 1-5 alkyl, or R5 and R6 together with N atom to which they are attached may form a 5-8 membered heterocyclic ring, optionally containing a further N atom optionally substituted by an alkyl radical; or X and Y when linked together form with the pyrazine ring or quinoxaline or tetrahydroquinaline R3 is H, C 1-5 alkyl or C 3-6 cycloalkyl, either unsubstituted or substituted by one or more hydroxyl or mononuclear aryl substituents, mononuclear aryl, C 2-5 alkenyl or amino; and R4 is H, C 1-5 alkyl or C 2-5 alkenyl, and, if desired, other diuretic agents as the active ingredients. The above compositions may be used in the treatment of adema, hypertension and other diseases known to be responsive to diuretic therapy.