FLUORINATED DIAMINOALKYNE DERIVATIVES

摘要

Alkyne derivs. of formula (I) and their pharmaceutically acceptable salts are new. R=H or C1-4 alkyl. (I) inhibit ornithine decarboxylase vitro and vivo and produce a decrease in putrescine and spermidine concn. in cells in which polyamine biosynthesis occurs. Thus (I) are useful for controlling undersirable cell growth or proliferation (e.g. tumour growth and benign protastic hypertrophy). (I) can also be used to control the growth of pathogenic protozoa (e.g. Tb, brucei, Tb rhodesiense, Eimeria tenella and Plasmodium falciparum) in mammals including man. Dose is 5-50 mg/kg/day. Specific cpd. is 1, 4- diamino-2,2-difluoro-hex-5-yne.