HETEROCYCLIC AMIDES PROCESSES FOR THEIR PREPARATION AND PHARMA CEUTICAL COMPOSITIONS CONTAINING THEM

摘要

1428493 Nicotinamides and pyrimidinecarboxamides SCIENCE UNION ET CIE SOC FRANCAISE DE RECHERCHE MEDICALE 2 May 1974 [2 May 1973] 20842/73 Heading C2C The invention comprises nicotinamides and pyrimidinecarboxamides of the formula wherein X is N or CH; n is 0 or 1; and R is -CH(R 1 )CH 2 NR 2 R 3 , -CH(NR 2 R 3 )CH 2 R 1 or a 1-R 4 -pyrrolidin-2(or 3)-yl radical, wherein R 1 is H or CH 3 , R 2 and R 3 each are C 1 -C 6 alkyl, or R 2 and R 3 together are C 4 -C 7 polymethylene, which is optionally interrupted by an oxygen atom, and R 4 is C 1 -C 20 acyclic hydrocarbon, C 3 -C 7 cycloalkyl or Ar-A or wherein A is a single bond or C 1 -C 6 acyclic hydrocarbon, and Ar and R11 each are phenyl optionally substituted by alkoxy, methylenodioxy, ethylenedioxy or trimethylenedioxy radicals; and acid addition salts thereof. The compounds are prepared by either reacting acid halides of the Formula IV wherein Z is Cl, Br or OCOOY, where Y is C 1 -C 6 alkyl with amines of the formula and deacetylating the resulting amides of the formula or by reacting the appropriate aminonicotinic acids or aminopyrimidinecarboxylic acids with compounds of the formula 6 - Acetamidonicotinoyl chloride is obtained by reacting 6-acetamidonictonic acid with thionyl chloride. Pharmaceutical compositions suitable for oral, parenteral or rectal administration, contains the above novel compound or acid addition salts thereof and pharmaceutically acceptable carriers. The compounds possess gastric antisecretory, antiulcerous, gastro-intestinal motility and central nervous system acting properties.