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Relevant academic research and scientific papers

Cholesterol-lowering phenoxyalkanoic acid esters

Compounds possessing pharmaceutical activity as substances able to lower the level of fatty substances in the blood possess the following general formula: STR1 wherein R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms; A1 and A2 which can be the same or different are hydrogen or alkyl containing from 1 to 9 carbon atoms such that A1 and A2 contain together not more than 10 carbon atoms, Y is oxygen, in which case X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiary aminoalkoxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, or X is hydrogen and Z is pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, or Y is oxygen, X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is alkoxy containing from 1 to 4 carbon atoms, hydroxy or O- M+, M being a metal cation of Main Groups I, II or III of the Periodic System of the Elements or an organic base cation or ammonium ion, A1 and A2 being the same and being as aforesaid or being different with one of A1 and A2 being hydrogen or both being hydrogen and X being a para substituent with respect to Y in the benzene ring in the same general formula, Y is oxygen, X is hydrogen and Z is amine, azacyclohydrocarbyloxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, Or Y is sulphur, in which case X is hydrogen, benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy, alkoxy containing from 1 to 4 carbon atoms, hydroxy, O- M+ wherein M is a metal cation of Main Groups I, II or III of the Periodic System of The Elements or an organic base cation or ammonium ion, cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiaryaminoalkoxy, pivaloyloxyalkoxy or pyridyl-C-alkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, and pharmacologically acceptable acid addition and quaternary ammonium salts of compounds containing basic groups, and optical isomers of said compounds when A1 and A2 are different.

Beclobrate and eniclobrate hydrochloride, new diphenylmethane derivatives as agents for lowering cholesterol and triglyceride levels. Part I: Synthesis and consideration of structure-activity relationships (author's transl)

Within the course of a research project for finding new lipid-lowering substances with better therapeutic indices than the standard agent in use, various diphenylmethane derivatives were synthesized and tested with respect to their activity and toxicity. On the basis of these results Sgd 24774 (beclobrate) and Sgd 33374 (eniclobrate-hydrochloride) were selected for further investigation and clinical studies.