Piperidyl ethers and thioethers as inhibitors of cholesterol biosynthesis
AssigneeMerrell Dow Pharmaceuticals Inc.
InventorsCharlotte L. Barney, James R. McCarthy, Marion W. Wannamaker
Life of this patent
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Abstract
The present invention relates to certain novel piperidyl ethers and thioethers which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.
Claims13
A method of inhibiting the biosynthesis of cholesterol in a patient in need thereof comprising administering to said patient an effective cholesterol biosynthesis inhibiting amount of a compound of the formula ##STR7## wherein Y is oxygen, sulfur, sulfinyl or sulfonyl;
- A is a C.sub.2 -C.sub.15 alkylene having 0 to 3 double bonds;
- B is a C.sub.2 -C.sub.15 alkyl having 0 to 3 double bonds;
- v is a integer 0, 1 or 2;
- and
- R is hydroxy, C.sub.1 -C.sub.4 alkyl or a radical of the formula ##STR8## wherein n is an integer 0, 1, 2 or 3;
- and
- R.sub.1 R.sub.2 and R.sub.3 are each independently hydrogen or a C.sub.1 -C.sub.4 alkyl.
A method of lowering plasma cholesterol in a patient in need thereof comprising administering to said patient an effective hypocholesterolemic amount of a compound of the formula ##STR9## wherein Y is oxygen, sulfur, sulfinyl or sulfonyl;
- A is a C.sub.2 -C.sub.15 alkylene having 0 to 3 double bonds;
- B is a C.sub.2 -C.sub.15 alkyl having 0 to 3 double bonds;
- v is an integer 0, 1 or 2;
- and
- R is hydroxy, C.sub.1 -C.sub.4 alkyl or a radical of the formula ##STR10## wherein n is an integer 0, 1, 2 or 3;
- and
- R.sub.1 R.sub.2 and R.sub.3 are each independently hydrogen or a C.sub.1 -C.sub.4 alkyl.
A method of treating a patient afflicted with hypercholesterolemia comprising administering to said patient an effective hypocholesterolemic amount of a compound of the formula ##STR11## wherein Y is oxygen, sulfur, sulfinyl or sulfonyl;
- A is a C.sub.2 -C.sub.15 alkylene having 0 to 3 double bonds;
- B is a C.sub.2 -C.sub.15 alkyl having 0 to 3 double bonds;
- v is an integer 0, 1 or 2;
- and
- R is hydroxy, C.sub.1 -C.sub.4 alkyl or a radical of the formula ##STR12## wherein n is an integer 0, 1, 2 or 3;
- and
- R.sub.1 R.sub.2 and R.sub.3 are each independently hydrogen or a C.sub.1 -C.sub.4 alkyl.
A pharmaceutical composition comprising an effective hypocholesterolemic amount of a compound of the formula ##STR13## wherein Y is oxygen, sulfur, sulfinyl or sulfonyl;
- A is a C.sub.2 -C.sub.15 alkylene having 0 to 3 double bonds;
- B is a C.sub.2 -C.sub.15 alkyl having 0 to 3 double bonds;
- v is an integer 0, 1 or 2;
- and
- R is hydroxy, C.sub.1 -C.sub.4 alkyl or a radical of the formula ##STR14## wherein n is an integer 0, 1, 2 or 3;
- and
- R.sub.1 R.sub.2 and R.sub.3 are each independently hydrogen or a C.sub.1 -C.sub.4 alkyl
- in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients.
A method of treating a patient afflicted with a fungal infection comprising administering an effective antifungal amount of a compound of the formula ##STR15## wherein Y is oxygen, sulfur, sulfinyl or sulfonyl;
- A is a C.sub.2 -C.sub.15 alkylene having 0 to 3 double bonds;
- B is a C.sub.2 -C.sub.15 alkyl having 0 to 3 double bonds;
- v is an integer 0, 1 or 2;
- and
- R is hydroxy, C.sub.1 -C.sub.4 alkyl or a radical of the formula ##STR16## wherein n is an integer 0, 1, 2 or 3;
- and
- R.sub.1 R.sub.2 and R.sub.3 are each independently hydrogen or a C.sub.1 -C.sub.4 alkyl.
Dependencies are inferred from the claim text.