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US4346227A
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ML-236B Derivatives and their preparation
Assignee: Sankyo Co Ltd
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Filing: 1981-06-05
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Granted: 1982-08-24
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Expires: 2001-06-05
Abstract
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 1 -C 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.
Inventors
- 👤 Akira Terahara
- 👤 Minoru Tanaka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:15
CPC Classifications
C; C07; C07D; C07D309/00; C07D309/16; C07D309/28; C07D309/30; C12; C12N; C12N1/00; C12N1/20; C12N1/205; C12N1/14; C12N1/145; C12P; C12P17/00; C12P17/02; C12P17/06; C12P7/00; C12P7/62; C12R; C12R2001/00; C12R2001/01; C12R2001/465; C12R2001/645; C12R2001/65; C12R2001/785; C12R2001/845; Y; Y10; Y10S; Y10S435/00; Y10S435/8215; Y10S435/822; Y10S435/886
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
43 words
Compounds of formula (I): ##STR19## wherein R 1 represents a hydrogen atom or a C 1 -C 5 alkyl group, and R represents a group of the formula ##STR20## and pharmaceutically acceptable salts of the acid when R 1 represents a hydrogen atom.
Claim 2
Dependent Claim
43 words
Compounds of formula (I): ##STR19## wherein R 1 represents a hydrogen atom or a C 1 -C 5 alkyl group, and R represents a group of the formula ##STR20## and pharmaceutically acceptable salts of the acid when R 1 represents a hydrogen atom.
Claim 3
Dependent Claim
41 words
Compounds as claimed in claim 1, having the formula (II) ##STR21## (in which R 1 represents a hydrogen atom or a C 1 -C 5 alkyl group) and pharmaceutically acceptable salts of the acid wherein R 1 represents a hydrogen atom.
Claim 4
Dependent Claim
13 words
Compounds as claimed in claim 2, wherein R 1 represents a hydrogen atom.
Claim 5
Dependent Claim
17 words
Compounds as claimed in claim 2, wherein R 1 represents a C 1 -C 5 alkyl group.
Claim 6
Dependent Claim
13 words
Compounds as claimed in claim 2, wherein R 1 represents a methyl group.
Claim 7
Dependent Claim
13 words
Compounds as claimed in claim 2, in the form of alkali metal salts.
Claim 8
Dependent Claim
13 words
Compounds as claimed in claim 6, in the form of the sodium salt.
Claim 9
Dependent Claim
28 words
Compounds as claimed in claim 2, having the configuration shown in formula (IV): ##STR22## (wherein R 1 is as defined in claim 2) and pharmaceutically acceptable salts thereof.
Claim 10
Dependent Claim
13 words
Compounds as claimed in claim 8, wherein R 1 represents a hydrogen atom.
Claim 11
Dependent Claim
17 words
Compounds as claimed in claim 8, wherein R 1 represents a C 1 -C 5 alkyl group.
Claim 12
Dependent Claim
13 words
Compounds as claimed in claim 8, wherein R 1 represents a methyl group.
Claim 13
Dependent Claim
14 words
Compounds as claimed in claim 8, in the form of the alkali metal salts.
Claim 14
Dependent Claim
13 words
Compounds as claimed in claim 12, in the form of the sodium salt.
Claim 15
Dependent Claim
28 words
Compounds as claimed in claim 2, having the configuration shown in formula (VI): ##STR23## (wherein R 1 is as defined in claim 2) and pharmaceutically acceptable salts thereof.
Claim 16
Dependent Claim
13 words
Compounds as claimed in claim 14, wherein R 1 represents a hydrogen atom.
Claim 17
Dependent Claim
17 words
Compounds as claimed in claim 14, wherein R 1 represents a C 1 -C 5 alkyl group.
Claim 18
Dependent Claim
13 words
Compounds as claimed in claim 14, wherein R 1 represents a methyl group.
Claim 19
Dependent Claim
14 words
Compounds as claimed in claim 14, in the form of the alkali metal salts.
Claim 20
Dependent Claim
13 words
Compounds as claimed in claim 18, in the form of the sodium salt.
Claim 21
Dependent Claim
42 words
Compounds as claimed in claim 1, which have the formula (VIII): ##STR24## (in which R 1 represents a hydrogen atom or a C 1 -C 5 alkyl group) and pharmaceutically acceptable salts of the acid wherein R 1 represents a hydrogen atom.
Claim 22
Dependent Claim
13 words
Compounds as claimed in claim 20, wherein R 1 represents a hydrogen atom.
Claim 23
Dependent Claim
17 words
Compounds as claimed in claim 20, wherein R 1 represents a C 1 -C 5 alkyl group.
Claim 24
Dependent Claim
13 words
Compounds as claimed in claim 20, wherein R 1 represents a methyl group.
Claim 25
Dependent Claim
14 words
Compounds as claimed in claim 20, in the form of the alkali metal salts.
Claim 26
Dependent Claim
13 words
Compounds as claimed in claim 24, in the form of the sodium salt.
References Cited (Backward Citations)
US4137322A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-08-23 | 1986-02-22 | 1986-08-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-08-23 | 1990-02-22 | 1990-08-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-08-23 | 1994-02-22 | 1994-08-24 | $7700.00 | Window Closed / Lapsed |