US 4,904,692 A · Novel HMG-CoA reductase inhibitors

Abstract

Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof. Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.

Claims25

Dependent claims

A compound of the formula ##STR4## and the pharmaceutically acceptable salts thereof wherein Y is:

--CHR--,
--CHRCHR--,
--CHRCHRCHR--, or
--RC.dbd.CR--;
X, X.sub.1 and X.sub.2 are independently:
H, F, Cl, Br, OH, CF.sub.3 alkyl, alkoxy, aryl, NO.sub.2, NH(CO)R, N(R).sub.2, or S(O).sub.n R;
R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently:
H or lower alkyl;
m is:
1 or 2;
m' is:
0 or 1;
m" is:
0 or 1;
n=0, 1, 2;
and
the dotted lines in the bicyclic ring represent optional double bonds.

14 more elements

Dependencies are inferred from the claim text.

Facts

Application

07/283,111Filed 12 Dec 1988 · continuation in part

Priority

21 Dec 1987

Granted

27 Feb 1990

Term ends

Not estimatedThe source records don’t support an estimate.

Classification6 codes

C07C 59/56
Containing hydroxy or O-metal groups: containing halogen
C07C 59/54
Containing hydroxy or O-metal groups: containing six-membered aromatic rings and other rings
C07C 59/64
Containing ether groups, [IMAGE cpc-sch-C07C-0958.gif] groups,[IMAGE cpc-sch-C07C-0959.gif] groups, or[IMAGE cpc-sch-C07C-0960.gif] groups:…
C07D 309/30
With hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals,…:…

Novel HMG-CoA reductase inhibitors

Life of this patent

Abstract

Claims25

Novel HMG-CoA reductase inhibitors

Life of this patent

Abstract

Claims25