A NEW DIPHENYLAZETIDININE WITH IMPROVED PHYSIOLOGICAL PROPERTIES, METHODS OF ITS PRODUCTION CONTAINING THESE COMPOUNDS MEDICINES AND THEIR APPLICATION

摘要

Dodecanedioic acid 4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-(4-methoxyphenyl)-4-oxo-azetidin-1-yl)-benzylamide ((2R,3R,4R,5R)-2,3,4,5,6-pentahydroxyhexyl)-amide (I) and its salts are new. Dodecanedioic acid 4-((2S,3R)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-(4-methoxyphenyl)-4-oxo-azetidin-1-yl)-benzylamide ((2R,3R,4R,5R)-2,3,4,5,6-pentahydroxyhexyl)-amide of formula (I) and its salts are new. [Image] Independent claims are also included for the following: (1) intermediates of formula (III) and (IV); (2) pharmaceutical compositions comprising (I) optionally in combination with further active ingredients (X). [Image] [Image] R : acetyl, benzoyl, (1-12C) alkylaryl or 1-12C alkyl; and Q : Cl or OH. ACTIVITY : Antilipemic; antiarteriosclerotic; antidiabetic. In cholesterol absorption tests in mice, (I) had an oral ED 5 0 value of 0.005 mg (per mouse) for inhibition of cholesterol uptake in the liver. MECHANISM OF ACTION : None given in the source material.