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Claims for Patent: 4,346,227

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Claims for Patent: 4,346,227

Title: ML-236B Derivatives and their preparation
Abstract:Compounds of formula (I): ##STR1## (wherein R represents a group of formula ##STR2## and the corresponding ring-closed lactones, salts (especially alkali metal salts) and esters (especially C.sub.1 -C.sub.5 alkyl esters) thereof may be prepared by subjecting ML-236B, or ML-236B carboxylic acid or a salt or ester thereof to enzymatic hydroxylation, which may be effected by means of microorganisms of the genera Mucor, Rhizopus, Zygorynchus, Circinella, Actinomucor, Gongronella, Phycomyces, Martierella, Pycnoporus, Rhizoctonia, Absidia, Cunninghamella, Syncephalastrum and Streptomyces, or cell-free, enzyme-containing extracts from said microorganisms. The compounds are capable of inhibiting biosynthesis of cholesterol and are thus useful in the treatment of hypercholesteraemia.
Inventor(s): Terahara; Akira (Hiromachi, JP), Tanaka; Minoru (Hiromachi, JP)
Assignee: Sankyo Company, Limited (Tokyo, JP)
Application Number:06/270,846
Patent Claims: 1. Compounds of formula (I): ##STR19## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group, and R represents a group of the formula ##STR20## and pharmaceutically acceptable salts of the acid when R.sup.1 represents a hydrogen atom.

2. Compounds as claimed in claim 1, having the formula (II) ##STR21## (in which R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group) and pharmaceutically acceptable salts of the acid wherein R.sup.1 represents a hydrogen atom.

3. Compounds as claimed in claim 2, wherein R.sup.1 represents a hydrogen atom.

4. Compounds as claimed in claim 2, wherein R.sup.1 represents a C.sub.1 -C.sub.5 alkyl group.

5. Compounds as claimed in claim 2, wherein R.sup.1 represents a methyl group.

6. Compounds as claimed in claim 2, in the form of alkali metal salts.

7. Compounds as claimed in claim 6, in the form of the sodium salt.

8. Compounds as claimed in claim 2, having the configuration shown in formula (IV): ##STR22## (wherein R.sup.1 is as defined in claim 2) and pharmaceutically acceptable salts thereof.

9. Compounds as claimed in claim 8, wherein R.sup.1 represents a hydrogen atom.

10. Compounds as claimed in claim 8, wherein R.sup.1 represents a C.sub.1 -C.sub.5 alkyl group.

11. Compounds as claimed in claim 8, wherein R.sup.1 represents a methyl group.

12. Compounds as claimed in claim 8, in the form of the alkali metal salts.

13. Compounds as claimed in claim 12, in the form of the sodium salt.

14. Compounds as claimed in claim 2, having the configuration shown in formula (VI): ##STR23## (wherein R.sup.1 is as defined in claim 2) and pharmaceutically acceptable salts thereof.

15. Compounds as claimed in claim 14, wherein R.sup.1 represents a hydrogen atom.

16. Compounds as claimed in claim 14, wherein R.sup.1 represents a C.sub.1 -C.sub.5 alkyl group.

17. Compounds as claimed in claim 14, wherein R.sup.1 represents a methyl group.

18. Compounds as claimed in claim 14, in the form of the alkali metal salts.

19. Compounds as claimed in claim 18, in the form of the sodium salt.

20. Compounds as claimed in claim 1, which have the formula (VIII): ##STR24## (in which R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.5 alkyl group) and pharmaceutically acceptable salts of the acid wherein R.sup.1 represents a hydrogen atom.

21. Compounds as claimed in claim 20, wherein R.sup.1 represents a hydrogen atom.

22. Compounds as claimed in claim 20, wherein R.sup.1 represents a C.sub.1 -C.sub.5 alkyl group.

23. Compounds as claimed in claim 20, wherein R.sup.1 represents a methyl group.

24. Compounds as claimed in claim 20, in the form of the alkali metal salts.

25. Compounds as claimed in claim 24, in the form of the sodium salt.
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