substituted 5 - ((2 - chloro - 4 - chinolinyl) amino) - 3 (aminomethyl) - (1,1 '- biphenyl) - 2 - ol compounds methods for their preparation and pharmaceutical compositions containing the compounds;.

摘要

Substituted-5-[(7-chloro-4-quinolinyl)amino]-3-(aminomethyl)-[(1,1 min -biphenyl]-2-ol compounds and salts thereof; and processes for their production are disclosed. In addition, antimalarial pharmaceutical compositions including such compounds and methods of treatment employing the compositions are taught. Also disclosed are intermediates for use in producing the substituted compounds. The substituted compounds are those of the formula:- CHEM wherein X is a hydrogen, fluorine, bromine or chlorine atom or a lower alkyl radical; Y is a chlorine, fluorine or bromine atom or a trifluoromethyl, lower alkoxy, cyano, hydroxy, nitro, lower alkylthio, amino, lower alkyl amino, di(lower alkyl) amino, pyrrolidino or piperidino radical; R1 and R2, which are the same or different, are each a hydrogen atom or a lower alkyl radical, or R1R2N taken together is a pyrrolidino, piperidino or homopiperidino radical of which the heterocyclic ring is unsubstituted or substituted by from one to four lower alkyl radicals; Z is zero or one.