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US4348402A
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2-Hydroxyalkyl-3,4,5-trihydroxy-piperidine compounds, their production and their medicinal use
Assignee: Bayer AG
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Filing: 1980-10-02
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Granted: 1982-09-07
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Expires: 2000-10-02
Abstract
Abstract The invention relates to α-hydroxyalkyl-3,4,5-trihydroxypiperidines defined by Formula (I), infra, and pharmaceutical compositions and medicaments containing said compounds. Also included in the invention are methods for the use of said compounds, compositions and medicaments as inhibitors of α-glucoside hydrolases; and intermediates for the compounds of said Formula (I).
Inventors
- 👤 Gunther Kinast
- 👤 Lutz Muller
- 👤 Rudiger Sitt
- 👤 Walter Puls
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 22:51
CPC Classifications
C; C07; C07H; C07H9/00; C07H9/02; C07H9/04; A; A61; A61P; A61P1/00; A61P3/00; A61P3/06; A61P3/08; A61P3/10; A61P43/00; A61P9/00; A61P9/12; C07D; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/40; C07D211/44; C07D211/46; C07H7/00; C07H7/02
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
117 words
A compound which is 2-hydroxyalkyl-3,4,5-trihydroxypiperidine of the formula ##STR24## in which R 1 denotes a hydrogen atom R 2 denotes a C 1 to C 10 alkyl, C 2 to C 6 alkenyl or C 4 to C 10 alkadienyl radical which is optionally substituted by hydroxyl, C 1 to C 4 alkoxy or phenyl, which can in turn be substituted by C 1 to C 4 alkyl, C 1 to C 4 alkoxy, halogen, nitro or cyano, or denotes a phenyl radical which is optionally substituted by C 1 to C 4 alkyl, C 1 to C 4 alkoxy, halogen, nitro or cyano, and R 3 denotes a hydrogen atom or a sulpho or hydroxyl group.
Claim 2
Dependent Claim
117 words
A compound which is 2-hydroxyalkyl-3,4,5-trihydroxypiperidine of the formula ##STR24## in which R 1 denotes a hydrogen atom R 2 denotes a C 1 to C 10 alkyl, C 2 to C 6 alkenyl or C 4 to C 10 alkadienyl radical which is optionally substituted by hydroxyl, C 1 to C 4 alkoxy or phenyl, which can in turn be substituted by C 1 to C 4 alkyl, C 1 to C 4 alkoxy, halogen, nitro or cyano, or denotes a phenyl radical which is optionally substituted by C 1 to C 4 alkyl, C 1 to C 4 alkoxy, halogen, nitro or cyano, and R 3 denotes a hydrogen atom or a sulpho or hydroxyl group.
Claim 3
Dependent Claim
24 words
A compound according to claim 1, in which R 1 denotes a hydrogen atom R 3 has the same meaning as in claim 1.
Claim 4
Dependent Claim
14 words
A compound according to claim 2 in which R 1 denotes a hydrogen atom.
Claim 5
Dependent Claim
30 words
A compound according to claim 1, in which R 1 denotes a hydrogen atom, R 2 denotes a methyl or a ethyl radical and R 3 denotes a hydrogen atom.
Claim 6
Dependent Claim
29 words
A compound according to claim 1, in which R 1 denotes a hydrogen atom, R 2 denotes a methyl radical and R 3 denotes a sulpho or hydroxyl radical.
Claim 7
Dependent Claim
27 words
A compound according to claim 1, in which R 1 denotes a hydrogen atom, R 2 denotes a methyl radical and R 3 denotes a hydrogen atom.
Claim 8
Dependent Claim
9 words
A compound according to claim 1 which is 2-α-hydroxypropyl-3,4,5-trihydroxypiperidine.
Claim 9
Dependent Claim
9 words
A compound according to claim 1 which is 2-α-hydroxypentyl-3,4,5-trihydroxypiperidine.
Claim 10
Dependent Claim
9 words
A compound according to claim 1 which is 2-α-hydroxybenzyl-3,4,5-trihydroxypiperidine.
Claim 11
Dependent Claim
33 words
A pharmaceutical composition containing as an active ingredient an amount effective for the treatment of adiposity, diabetes or hyperlipoproteinaemia of a compound according to claim 1, in admixture with an inert pharmaceutical carrier.
Claim 12
Dependent Claim
17 words
A pharmaceutical composition of claim 10 in the form of a sterile or physiologically isotonic aqueous solution.
Claim 13
Dependent Claim
20 words
A composition according to claim 10 or 11 containing from 0.1 to 99.5% by weight of the said active ingredient.
Claim 14
Dependent Claim
31 words
A medicament in dosage unit form comprising an amount effective for the treatment of adiposity, diabetes or hyperlipoproteinaemia of a compound according to claim 1 together with an inert pharmaceutical carrier.
Claim 15
Dependent Claim
16 words
A medicament of claim 13 in the form of tablets, pills, dragees, capsules, ampoules, or suppositories.
Claim 16
Dependent Claim
43 words
A method of combating disorders of carbohydrate metabolism and/or lipid metabolism in warm-blooded animals which comprises administering to the animals an α-glucoside hydrolase inhibiting amount of an active compound according to claim 1 either alone or in admixture with an inert pharmaceutical carrier.
Claim 17
Dependent Claim
27 words
A method according to claim 15 in which the active compound is administered in an amount of 0.05 to 10 mg per kg body weight per day.
Claim 18
Dependent Claim
13 words
A pharmaceutical composition according to claim 11 containing as an active ingredient 2-α-hydroxypropyl-3,4,5-trihydroxypiperidine.
Claim 19
Dependent Claim
13 words
A pharmaceutical composition according to claim 11 containing as an active ingredient 2-α-hydroxypentyl-3,4,5-trihydroxypiperidine.
Claim 20
Dependent Claim
13 words
A pharmaceutical composition according to claim 11 containing as an active ingredient 2-α-hydroxybenzyl-3,4,5-trihydroxypiperidine.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-09-06 | 1986-03-08 | 1986-09-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-09-06 | 1990-03-08 | 1990-09-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-09-06 | 1994-03-08 | 1994-09-07 | $7700.00 | Window Closed / Lapsed |