4-Benzamido-biphenyl-4'-oxy-propionic acids and related cpds. - have hypocholesterolemic and hypotriglyceremic activity

Biphenyloxy cpds of formula (I) and their salts with mineral or org. bases when R3=carboxy. (where R1=opt. branched 1-6C alkyl, 3-6C cycloalkyl or phenyl (opt. substd. alkyl), phenylalkyl, phenylalkenyl or pyridyl, R2=H or 1-4C alkyl, R3= hydroxymethyl, carboxy, 2-7C alkoxycarbonyl or 4-8C cycloalko...

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Main Authors GRISS,GERHARD,.DR, KAUBISCH,NIKOLAUS,.DR, LEITOLD,MATYAS,DR, HURNAUS,RUDOLF,.DR, SAUTER,ROBERT,.DR, EISELE,BERNHARD,.DR, GRELL,WOLFGANG,.DR
Format Patent
LanguageEnglish
German
Published 05.05.1977
Edition2
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:Biphenyloxy cpds of formula (I) and their salts with mineral or org. bases when R3=carboxy. (where R1=opt. branched 1-6C alkyl, 3-6C cycloalkyl or phenyl (opt. substd. alkyl), phenylalkyl, phenylalkenyl or pyridyl, R2=H or 1-4C alkyl, R3= hydroxymethyl, carboxy, 2-7C alkoxycarbonyl or 4-8C cycloalkoxycarbonyl, A=-CONH- or -NHCO-, n=1,2 or 3) have superior hypocholesterolemic and hypotriglyceremic activity to cpds. described in DT 2149070, GB 860303 and GB 112172. They are generally administered orally or rectally as unit doses of 5-100 mg (pref. 5-30 mg) to give a daily dose of 10-300 mg (pref. 15-90 mg). Tests show ED to lower serum cholesteral by 20%, compare favourably with known cpds.
Bibliography:Application Number: DE19752547872