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US 5,294,627 AGranted
Directed biosynthesis of biologically active compounds
AssigneeMerck & Co., Inc.
InventorsBryon H. Arison, Shieh-Shung T. Chen, Raymond F. White, Brian R. Petuch
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Abstract
Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.
Claims14
A compound of structural formula (I) ##STR6## wherein R.sup.1 is ##STR7## wherein X is:
- (a) hydrogen,
- (b) halogen,
- (c) hydroxy, or
- (d) methyl;
- wherein Z.sub.1, Z.sub.2 and Z.sub.3 are each independently:
- (a) hydrogen,
- (b) C.sub.1-5 alkyl,
- (c) C.sub.1-5 alkyl substituted with
- (i) phenyl,
- (ii) phenyl substituted with methyl, methoxy, halogen or hydroxy,
- (iii) C.sub.1-5 alkylcarbonyloxy, or
- (iv) C.sub.1-5 alkoxycarbonyloxy, or
- (d) a pharmaceutically acceptable cation;
- and wherein halogen is Cl, Br, I, or F.
11 more elements
Dependencies are inferred from the claim text.