# US 5,350,758 A · Piperidyl sulfonamides and sulfoxamides as inhibitors of cholesterol biosynthesis

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- Number: US 5,350,758 A
- Document ID: US5350758A
- Status: Granted
- Kind: A
- Application number: 07/993,497
- Filed: 1992-12-18
- Granted: 1994-09-27
- Earliest claimed: 1992-07-08
- Assignees: Merrell Dow Pharmaceuticals Inc.
- Inventors: Marion W. Wannamaker; William A. VanSickle; William R. Moore
- Web page: https://patentgrep.com/patent/US5350758A

## CPC

- C07D 211/96: Sulfur atom
- A61P 3/06: Antihyperlipidemics
- A61P 31/04: Antibacterial agents
- C07D 211/22: by oxygen atoms
- C07D 211/42: attached in position 3 or 5
- C07D 211/46: having a hydrogen atom as the second substituent in position 4
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to piperidyl sulfonamides and sulfoxamides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.

## Claims

### Claim 1

A compound of the formula ##STR16## wherein B is a C.sub.5 -C.sub.14 alkyl, ##STR17## m is an integer 0 or 1; x is an integer 1 or 2;
v is an integer 0, 1 or 2; and
R is -(CH.sub.2).sub.m OH, with the proviso that when m is 0, R cannot be in the 2-position of the piperidine ring or a radical of the formula ##STR18## wherein n is an integer 0, 1, 2 or 3; and R.sub.1 is hydrogen, phenyl, vinyl or a C.sub.1 -C.sub.4 alkyl.

### Claim 2 (depends on 1)

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 claim 1.

### Claim 3 (depends on 1)

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 claim 1.

### Claim 4 (depends on 1)

A method of treating a patient afflicted with hypercholesterolemia comprising administering to said patient an effective hypocholesterolemic amount of a compound of claim 1.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising an effective hypocholesterolemic amount of a compound of claim 1 in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients.

### Claim 6 (depends on 1)

A compound of claim 1 wherein the compound is 1-(1-Sulfonododecyl)-4-piperidine.

### Claim 7 (depends on 1)

A compound of claim 1 wherein the compound is 1-(1-Sulfonododecyl)-4-piperidine.