.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 4,450,171

« Back to Dashboard

Details for Patent: 4,450,171

Title: Antihypercholesterolemic compounds
Abstract:6(R)-[2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H- pyran-2-ones are prepared by acylation of the corresponding 8'-hydroxy compounds. The products are strong inhibitors of the biosynthesis of cholesterol.
Inventor(s): Hoffman; William F. (Lansdale, PA), Smith; Robert L. (Lansdale, PA), Willard; Alvin K. (Wilmington, DE)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Filing Date:Jun 14, 1982
Application Number:06/388,372
Claims:1. A compound of the formula: ##STR81## wherein R' is H or CH.sub.3 ;

R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl,

the dotted lines at X, Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone; or

the corresponding dihydroxy acid of the formula: ##STR82## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester or .alpha.-monoglyceride of said acid.

2. The compound of claim 1 wherein R' is CH.sub.3.

3. The compound of claims 1 or 2, wherein none of X, Y or Z is a double bond.

4. A pharmaceutical antihypercholesterolemic composition comprising a pharmaceutical carrier and an antihypercholesterolemic effective amount of a compound of structural formula: ##STR83## in which R' is H, or CH.sub.3 ;

R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl,

the dotted lines at X, Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone; or

the corresponding dihydroxy acid of the formula: ##STR84## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester or .alpha.-monoglyceride of said acid.

5. The composition of claim 4 wherein R' is CH.sub.3.

6. The composition of claim 4 or 5, wherein none of X, Y or Z is a double bond.

7. A method of treating hypercholesterolemia in a patient in need of such treatment which comprises administration of an antihyperchloesterolemic effective amount of a compound of structural formula: ##STR85## wherein R' is H or CH.sub.3 ;

R is 1-ethyl-1-methylpropyl, 1,1-diethylpropyl, 1,1-dimethyethyl, or 1,1-diethylbutyl,

the dotted lines at X, Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone; or

the corresponding dihydroxy acid of the formula: ##STR86## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, a phenyl- dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester or .alpha.-monoglyceride of said acid.

8. The method of claim 7 wherein R' is CH.sub.3.

9. The method of claim 7 or 8, wherein none of X, Y or Z is a double bond.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc