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US4248889A
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3,5-Dihydroxypentanoic ester derivatives having antihyperlipaemic activity
Assignee: Sankyo Co Ltd
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Filing: 1979-10-26
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Granted: 1981-02-03
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Expires: 1999-10-26
Abstract
Abstract 3,5-Dihydroxypentanoic ester derivatives of formula (I): ##STR1## wherein: A represents an alkylene group which is optionally substituted by one or more alkyl groups, or an alkenylene group; Z represents a substituted or unsubstituted aryl or aryloxy group; and R represents a C 1 -C 4 alkyl group) may be prepared by reacting a dianion of an acetoacetic ester with an aldehyde of formula Z-A-CHO (wherein A and Z are as defined above) and then reducing the resulting compound. These 3,5-dihydroxypentanoic ester derivatives have antihyperlipaemic activity and are thus valuable pharmaceuticals.
Inventors
- 👤 Hidehiko Oka
- 👤 Akira Terahara
- 👤 Akira Endo
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 19:01
CPC Classifications
C; C07; C07C; C07C67/00; C07C67/30; A; A61; A61P; A61P3/00; A61P3/06
Claims Analysis
Total Claims: 30
Claim 1
Independent Claim
49 words
3,5-Dihydroxypentanoic ester derivatives of formula (I): ##STR4## wherein: A represents an alkylene group an alkylene group having one or more alkyl substituents, or an alkenylene group; Z represents a halo or alkyl substituted or unsubstituted aryl or aryloxy group; and R represents a C 1 -C 4 alkyl group.
Claim 2
Dependent Claim
49 words
3,5-Dihydroxypentanoic ester derivatives of formula (I): ##STR4## wherein: A represents an alkylene group an alkylene group having one or more alkyl substituents, or an alkenylene group; Z represents a halo or alkyl substituted or unsubstituted aryl or aryloxy group; and R represents a C 1 -C 4 alkyl group.
Claim 3
Dependent Claim
27 words
Compounds as claimed in claim 1, wherein A represents a C 1 or C 2 alkylene group optionally substituted with a C 1 -C 3 alkyl group.
Claim 4
Dependent Claim
16 words
Compounds as claimed in claim 2, wherein A represents a methylene, ethylene, methylethylene or dimethylmethylene group.
Claim 5
Dependent Claim
17 words
Compounds as claimed in claim 1, wherein A represents a C 2 or C 3 alkylene group.
Claim 6
Dependent Claim
14 words
Compounds as claimed in claim 4, wherein A represents a vinylene or propenylene group.
Claim 7
Dependent Claim
33 words
Compounds as claimed in claim 1, wherein Z represents a phenyl group, a naphthyl group or a tetrahydronaphthyl group optionally substituted by a halogen atom or a C 1 -C 3 alkyl group.
Claim 8
Dependent Claim
25 words
Compounds as claimed in claim 6, wherein Z represents a phenyl, naphthyl or tetrahydronaphthyl group optionally substituted with a chlorine atom or a methyl group.
Claim 9
Dependent Claim
20 words
Compounds as claimed in claim 7, wherein Z represents an o-chlorophenyl, m-chlorophenyl, p-chlorophenyl, 2,4-dichlorophenyl, 3,5-dichlorophenyl, 2,6-dichlorophenyl, 2-methyl-1-naphthyl, or 2-methyl-5,6,7,8-tetrahydro-1-naphthyl group.
Claim 10
Dependent Claim
22 words
Compounds as claimed in claim 1, wherein Z represents a phenoxy group or a naphthoxy group optionally substituted with a halogen atom.
Claim 11
Dependent Claim
18 words
Compounds as claimed in claim 9 wherein Z represents a o-chlorophenoxy, m-chlorophenoxy, p-chlorophenoxy, 2,4-dichlorophenoxy, 3,5-dichlorophenoxy or 2,6-dichlorophenoxy group.
Claim 12
Dependent Claim
8 words
Ethyl, 3,5-dihydroxy-7-phenylheptanoate of the formula of claim 1.
Claim 13
Dependent Claim
8 words
Ethyl 7-p-chlorophenyl-3,5-dihydroxyheptaoate of the formula of claim 1.
Claim 14
Dependent Claim
8 words
Ethyl 3,5-dihydroxy-7-(1-naphthyl)heptanoate of the formula of claim 1.
Claim 15
Dependent Claim
8 words
Ethyl 3,5-dihydroxy-7-(2-methyl-1-naphthyl)heptanoate of the formula of claim 1.
Claim 16
Dependent Claim
8 words
Ethyl 3,5-dihydroxy-7-(2-methyl-5,6,7,8-tetrahydro-1-naphthyl)heptanoate of the formula of claim 1.
Claim 17
Dependent Claim
9 words
Ethyl 3,5-dihydroxy-8-(1naphthyl) octanoate of the formula of claim 1.
Claim 18
Dependent Claim
8 words
Ethyl 3,5-dihydroxy-8-(2-methyl-1-naphthyl)octanoate of the formula of claim 1.
Claim 19
Dependent Claim
8 words
Ethyl 3,5-dihydroxy-7-phenylpent-6-enoate of the formula of claim 1.
Claim 20
Dependent Claim
8 words
Ethyl 3,5-dihydroxy-6-phenoxyheptanoate of the formula of claim 1.
Claim 21
Dependent Claim
8 words
Ethyl 6-(o-chlorophenoxy)-3,5-dihydroxyhexanoate of the formula of claim 1.
Claim 22
Dependent Claim
8 words
Ethyl 7-(2,6-dimethyl-1-naphthyl)-3,5-dihydroxyheptanoate of the formula of claim 1.
Claim 23
Dependent Claim
8 words
Ethyl 3,5-dihydroxy-7-(o-methylphenyl)heptanoate of the formula of claim 1.
Claim 24
Dependent Claim
8 words
Ethyl 7-(2,6-dimethylphenyl)-3,5-dihydroxyheptanoate of the formula of claim 1.
Claim 25
Dependent Claim
8 words
Ethyl 7-(o-chlorophenyl)-3,5-dihydroxyheptanoate of the formula of claim 1.
Claim 26
Dependent Claim
8 words
Ethyl 7-(2,6-dichlorophenyl)-3,5-dihydroxyheptanoate of the formula of claim 1.
Claim 27
Dependent Claim
65 words
A pharmaceutical preparation comprising as active ingredient, a 3,5-dihydroxypentanoic ester derivative of formula (I): ##STR5## (wherein: A represents an alkylene group, an alkylene group having one or more alkyl substituents, or an alkenylene group; Z represents a halo or alkyl substituted or unsubstituted aryl or aryloxy group; and R represents a C 1 -C 4 alkyl group), together with a pharmaceutically acceptable carrier or excipient.
Claim 28
Dependent Claim
65 words
A pharmaceutical preparation comprising as active ingredient, a 3,5-dihydroxypentanoic ester derivative of formula (I): ##STR5## (wherein: A represents an alkylene group, an alkylene group having one or more alkyl substituents, or an alkenylene group; Z represents a halo or alkyl substituted or unsubstituted aryl or aryloxy group; and R represents a C 1 -C 4 alkyl group), together with a pharmaceutically acceptable carrier or excipient.
Claim 29
Dependent Claim
17 words
A pharmaceutical preparation as claimed in claim 26, in a form suitable for oral or parenteral administration.
Claim 30
Dependent Claim
41 words
A pharmaceutical preparation as claimed in claim 26, wherein said 3,5-dihydroxypentanoic ester derivative is selected from the group consisting of: Ethyl 3,5-dihydroxy-7-phenylheptanoate; Ethyl 7-p-chlorophenyl-3,5-dihydroxyheptanoate; Ethyl 3,5-dihydroxy-7-(1-naphthyl)heptanoate; Ethyl 3,5-dihydroxy-7-(2-methyl-1-naphthyl)heptanoate; Ethyl 3,5-dihydroxy-7-(2-methyl-5,6,7,8-tetrahydro-1-naphthyl)heptanoate; Ethyl 3,5-dihydroxy-8-(1-naphthyl)octanoate; Ethyl 3,5-dihydroxy-8-(2-methyl-1-naphthyl)octanoate; Ethyl 3,5-dihydroxy-7-phenylhept-6-enoate; Ethyl 3,5-dihydroxy-6-phenoxyheptanoate; and Ethyl 6-(o-chlorophenoxy)-3,5-dihydroxyhexanoate.
References Cited (Backward Citations)
US2915532A
Cited
US4007217A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-02-03 | 1984-08-04 | 1985-02-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-02-03 | 1988-08-04 | 1989-02-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-02-03 | 1992-08-04 | 1993-02-03 | $7700.00 | Window Closed / Lapsed |