Piperidyl amides, sulfonamides and sulfoxamides as inhibitors of cholesterol biosynthesis
OwnerMarion W. Wannamaker, William A. VanSickle +1inventors
InventorsMarion W. Wannamaker, William A. VanSickle, William R. Moore
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Abstract
The present invention relates to piperidyl amides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.
Claims3
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 ##STR16## wherein A is a C.sub.2 -C.sub.14 alkylene;
- Y is a methylene, oxygen, sulfur, sulfinyl or sulfonyl;
- B is a C.sub.2 -C.sub.14 alkyl, ##STR17## m is an integer 0 or 1;
- 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 R is 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;
- provided that when R is a radical of the formula ##STR19## or when B is a C.sub.2 -C.sub.14 alkyl and v is 0, Y is not methylene.
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 ##STR20## wherein A is a C.sub.2 -C.sub.14 alkylene;
- Y is a methylene, oxygen, sulfur, sulfinyl or sulfonyl;
- B is a C.sub.2 -C.sub.14 alkyl, ##STR21## m is an integer 0 or 1;
- 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 R is a radical of the formula ##STR22## 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;
- provided that when R is a radical of the formula ##STR23## or when B is a C.sub.2 -C.sub.14 alkyl and v is 0, Y is not methylene.
A method of treating a patient afflicted with hypercholesterolemia comprising administering to said patient an effective hypocholesterolemic amount of a compound of the formula ##STR24## wherein A is a C.sub.2 -C.sub.14 alkylene;
- Y is a methylene, oxygen, sulfur, sulfinyl or sulfonyl;
- B is a C.sub.2 -C.sub.14 alkyl, ##STR25## m is an integer 0 or 1;
- 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 R is a radical of the formula ##STR26## 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;
- provided that when R is a radical of the formula ##STR27## or when B is a C.sub.2 -C.sub.14 alkyl and v is 0, Y is not methylene.
Dependencies are inferred from the claim text.