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Claims for Patent: 4,444,784

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Claims for Patent: 4,444,784

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. (DE)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:06/217,640
Patent Claims: 1. A compound of the formula: ##STR68## wherein R' is H or CH.sub.3 ; R is

(1) 1,1-dimethylpropyl,

(2) C.sub.3-10 cycloalkyl,

(3) C.sub.2-10 alkenyl,

(4) C.sub.1-10 CF.sub.3 -substituted alkyl,

(5) phenyl,

(6) halophenyl,

(7) phenyl-C.sub.1-3 alkyl,

(8) substituted phenyl-C.sub.1-3 alkyl in which the substituent is halo, C.sub.1-3 alkyl or C.sub.1-3 alkoxy;

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: ##STR69## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid or a phenyl-, dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester of said acid.

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

3. The compound of claim 1 wherein R is 1,1-dimethylpropyl.

4. The compound of claim 2 wherein R is 1,1-dimethylpropyl.

5. The compound of claim 1 wherein none of X, Y or Z is a double bond.

6. A pharmaceutical antihypercholesterolemic composition comprising a pharmaceutical carrier and an antihypercholesterolemic effective amount of a compound of structural formula: ##STR70## in which R' is H or CH.sub.3 ; R is

(1) 1,1-dimethylpropyl,

(2) C.sub.3-10 cycloalkyl,

(3) C.sub.2-10 alkenyl,

(4) C.sub.1-10 CF.sub.3 -substituted alkyl,

(5) phenyl,

(6) halophenyl,

(7) phenyl-C.sub.1-3 alkyl,

(8) substituted phenyl-C.sub.1-3 alkyl in which the substituent is halo, C.sub.1-3 alkyl or C.sub.1-3 alkoxy;

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: ##STR71## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid or a phenyl-, dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester of said acid.

7. The composition of claim 6 wherein R' is CH.sub.3.

8. The composition of claim 6 wherein R is 1,1-dimethylpropyl.

9. The composition of claim 7 wherein R is 1,1-dimethylpropyl.

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

11. A method of treating hypercholesterolemia in a patient in need of such treatment which comprises administration of an antihypercholesterolemic effective amount of a compound of structural formula: ##STR72## in which R' is H or CH.sub.3 ; R is

(1) 1,1-dimethylpropyl,

(2) C.sub.3-10 cycloalkyl,

(3) C.sub.2-10 alkenyl,

(4) C.sub.1-10 CF.sub.3 -substituted alkyl,

(5) phenyl,

(6) halophenyl,

(7) phenyl-C.sub.1-3 alkyl,

(8) substituted phenyl-C.sub.1-3 alkyl in which the substituent is halo, C.sub.1-3 alkyl or C.sub.1-3 alkoxy;

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: ##STR73## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid or a phenyl-, dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester of said acid.

12. The method of claim 11 wherein R' is CH.sub.3.

13. The method of claim 11 wherein R is 1,1-dimethylpropyl.

14. The method of claim 12 wherein R is 1,1-dimethylpropyl.

15. The method of claim 11 wherein none of X, Y or Z is a double bond.

16. A compound of the formula: ##STR74## wherein R' is H or CH.sub.3 ; R is

(1) C.sub.3-10 cycloalkyl,

(2) C.sub.2-10 alkenyl,

(3) C.sub.1-10 CF.sub.3 -substituted alkyl,

(4) phenyl,

(5) halophenyl,

(6) phenyl-C.sub.1-3 alkyl

(7) substituted phenyl-C.sub.1-3 alkyl in which the substituent is halo, C.sub.1-3 alkyl or C.sub.1-3 alkoxy;

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: ##STR75## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid or a phenyl-, dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester of said acid.

17. A pharmaceutical antihypercholesterolemic composition comprising a pharmaceutical carrier and an antihypercholesterolemic effective amount of a compound of structural formula: ##STR76## in which R' is H or CH.sub.3 ; R is

(1) C.sub.3-10 cycloalkyl,

(2) C.sub.2-10 alkenyl,

(3) C.sub.1-10 CF.sub.3 -substituted alkyl,

(4) phenyl,

(5) halophenyl,

(6) phenyl-C.sub.1-3 alkyl,

(7) substituted phenyl-C.sub.1-3 alkyl in which the substituent is halo, C.sub.1-3 alkyl or C.sub.1-3 alkoxy;

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: ##STR77## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid or a phenyl-, dimethylamino-, or acetylamino-substituted-C.sub.1-4 alkyl ester of said acid.

18. A method of treating hypercholesterolemia in a patient in need of such treatment which comprises administration of an antihypercholesterolemic effective amount of a compound of structural formula: ##STR78## in which R' is H or CH.sub.3 ; R is

(1) C.sub.3-10 cycloalkyl,

(2) C.sub.2-10 alkenyl,

(3) C.sub.1-10 CF.sub.3 -substituted alkyl,

(4) phenyl,

(5) halophenyl,

(6) phenyl-C.sub.1-3 alkyl,

(7) substituted phenyl-C.sub.1-3 alkyl in which the substituent is halo, C.sub.1-3 alkyl or C.sub.1-3 alkoxy;

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: ##STR79## or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid or a phenyl-, dimethylamino-, or acetylamino-substituted C.sub.1-4 alkyl ester of said acid.
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