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Generated: February 20, 2018

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Title: Substituted pyridines heptenoic acid derivatives, useful for treating arterioscleros, lipopotaemia and the like
Abstract:Novel compounds for treating hyperproteinaemia, lipoproteinaemia or arteriosclerosis of the formula ##STR1## in which A, B, D and E can have varied meanings, X is --CH.sub.2 --CH.sub.2 or --CH.dbd.CH--, and R is ##STR2## wherein R.sup.21 --denotes hydrogen or alkyl and R.sup.22 --denotes hydrogen, denotes alkyl, aryl or aralkyl, or denotes a cation, and their oxidation products.
Inventor(s): Angerbauer; Rolf (Wuppertal, DE), Fey; Peter (Wuppertal, DE), Hubsch; Walter (Wuppertal, DE), Philipps; Thomas (Cologne, DE), Bischoff; Hilmar (Wuppertal, DE), Petzinna; Dieter (Duesseldorf, DE), Schmidt; Delf (Wuppertal, DE), Thomas; Gunter (Arese, IT)
Assignee: Bayer Aktiengesellschaft (Leverkusen, DE)
Filing Date:Jul 20, 1992
Application Number:07/916,928
Claims:1. A substituted pyridine of the formula: ##STR234## wherein A represents phenyl or phenyl which is monosubstituted or disubstituted by a substituent selected from the group consisting of methyl, hydroxymethyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert.-butyl, methoxy, ethoxy, propoxy, isopropoxy, phenoxy, benzyloxy, fluorine, chlorine or trifluoromethyl;

B represents cyclopropyl, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, or tert.-butyl;

E represents methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert.-butyl, pentyl, isopentyl, hexyl or isohexyl; and

R.sup.22 represents hydrogen, lower alkyl, phenyl, benzyl or a physiologically tolerable metal or ammonium cation.

2. A compound according to claim 1, wherein such compound is erythro-(E)-7-[2-(4-fluorophenyl)-5-hydroxymethyl-4-isopropyl-6-methyl-pyr id-3-yl]-3,5-dihydroxy-hept-6-enoate of the formula: ##STR235##

3. A compound according to claim 1, wherein such compound is erythro-(E)-7-[2-(4-fluorophenyl)-5-hydroxymethyl-4,6-diisopropyl-pyridin- 3-yl]-3,5-dihydroxy-hept-6-enoate of the formula: ##STR236##

4. A composition for inhibiting cholesterol biosynthesis and HMG-CoA reductase comprising an amount effective therefor of a compound according to claim 1 and a pharmaceutically acceptable diluent.

5. A method of treating a patient afflicted with hyperlipoproteinaemia, lipoproteinaemia or arteriosclerosis which comprises administering to such patient an amount effective therefor of a compound according to claim 1.
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Daiichi Sankyo
Cantor Fitzgerald
US Army
US Department of Justice
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