Carboxyalkylethers, formulations, and treatment of vascular diseases
AssigneeWarner-Lambert Company
InventorsCharles Larry Bisgaier, Paul Leroy Creger, Alan Robert Saltiel, Sherrie Rae Tafuri
Life of this patent
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Abstract
Dialkyl ethers lower Lp(a) and triglycerides, and elevate HDL-cholesterol, and are thereby useful for treating vascular diseases and noninsulin-dependent diabetes mellitus.
Claims8
A method for lowering plasma Lp(a) comprising administering to a mammal an Lp(a) lowering amount of a compound of the formula ##STR13## wherein n and m independently are integers fom 2 to 9;
- R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently are C.sub.1 -C.sub.6 alklyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, and R.sub.1 and R.sub.2 together with the carbon to which they are attached, and R.sub.3 and R.sub.4 together with the carbon to which they are attached, independently can complete a carbocyclic ring having from 3 to 6 carbons;
- Y.sub.1 and Y.sub.2 independently are COOH, CHO, tetrazole and COOR.sub.5 where R.sub.5 is C.sub.1 -C.sub.6 alky, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl;
- and where the alkyl, alkenyl, and alkynyl groups may be substituted with one or two groups selected from halo, hydroxy, C.sub.1 -C.sub.6 alkoxy, and phenyl, and the pharmaceutically acceptable salts theref.
A method for lowering apolipoprotein B comprising administering to a mammal an effective amount of a compound of the formula ##STR14## wherein n and m independently are integers from 2 to 9;
- R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently are C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, and R.sub.1 and R.sub.2 together vith the carbon to which they are attached, and R.sub.3 and R4 together with the carbon to which they are attached, independently can complete a carbocyclic ring having from 3 to 6 carbons;
- Y.sub.1 and Y.sub.2 independently are COOH, CHO, tetrazole, and COOR.sub.5 where R.sub.5 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 aIkynyl;
- and where the alkyl, alkenyl, and alkynyl groups may be substituted with one or two groups selected from halo, hydroxy, C.sub.1 -C.sub.6 alkoxy, and phenyl, and the pharmaceutically acceptable salts thereof.
A method of elevating plasma apolipoprotein A-1 comprising administering to a mammal an effective amount of a compound of the formula ##STR15## wherein n and m independently are integers from 2 to 9;
- R.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently are C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, and R.sub.1 and R.sub.2 together with the carbon to which they are attached, and R.sub.3 and R.sub.4 together with the carbon to which they are attached, independently can complete a carbocyclic ring having from 3 to 6 carbons;
- Y.sub.1 and Y.sub.2 independently are COOH, CHO, tetrazole , and COOR.sub.5 where R.sub.5 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl;
- and where the alkyl, alkenyl, and alkynyl groups may be substituted with one or two groups selected from halo, hydroxy, C.sub.1 -C.sub.6 alkoxy, and phenyl, and the pharmaceutically acceptable salts thereof.
A method of elevating plasma apolipoprotein E comprising administering an effective amount of a compound of the formula ##STR16## wherein n and m independently are integers from 2 to 9;
- R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently are C.sub.1 -C.sub.6 alyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, and R.sub.1 and R.sub.2 together with the carbon to which they are attached and R.sub.3 and R.sub.4 together with the carbon to which they are attached, indeperdently can complete a carbocyclic ring having fom 3 to 6 carbons;
- Y.sub.1 and Y.sub.2 independently are COOH, CHO, tetrazole, and COOR.sub.5 where R.sub.5 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl , C.sub.2 -C.sub.6 alkynyl;
- and where the alkyl, alkeny, and alkynyl groups may be substituted with one or two groups selected from halo, hydroxy, C.sub.1 -C.sub.6 alkoxy, and phenyl, and the pharmaceuticaliy acceptable salts thereof.
Dependencies are inferred from the claim text.