US4273765A
Expired / Lapsed
US
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Amino sugar derivatives containing trehalose
Assignee: Hoffmann La Roche Inc
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Filing: 1979-02-09
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Granted: 1981-06-16
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Expires: 1999-02-09
Abstract
Abstract This invention relates to Trestatin A, Trestatin B and Trestatin C salts thereof and mixtures thereof as well as compositions containing at least one of the Trestatins A, B or C or a salt thereof. These compositions are useful for the inhibition of sucrase and inhibition of alpha-amylase.
Inventors
- 👤 Yasuji Suhara
- 👤 Kiyoshi Ogawa
- 👤 Kazuteru Yokose
- 👤 Kimihiro Watanabe
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-10 01:40
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/22; C12; C12N; C12N9/00; C12N9/99; C12P; C12P19/00; C12P19/26
Claims Analysis
Total Claims: 3
Claim 1
Independent Claim
262 words
The novel amino sugar derivatives Trestatin A, Trestatin B and Trestatin C and salts and mixtures thereof having trehalose as a common structural feature and having the following properties: (a) Elementary analysis: ______________________________________
C H N O
% % % %
______________________________________
Trestatin A:
46.72 7.13 2.08 43.28
Trestatin B:
46.27 7.04 1.65 44.69
Trestatin C:
47.55 7.15 2.29 42.66
______________________________________ (b) Molecular weight (Osmometry): Trestatin A: 1470 Trestatin B: 975 Trestatin C: 1890 (c) Melting point: Trestatin A: 221°-232° C. (dec.) Trestatin B: 209°-219° C. (dec.) Trestatin C: 230°-237° C. (dec.) (d) Specific rotation: Trestatin A: [α] D 24 =+177° (c=1.0, H 2 O) Trestatin B: [α] D 26 =+187° (c=1.0, H 2 O) Trestatin C: [α] D 23 =+169.5° (c=1.0, H 2 O) (e) Ulraviolet absorption spectrum (in water): Each of Trestatin A, Trestatin B and Trestatin C shows end absorption (f) Infrared absorption spectrum (in KBr): Trestatin A: as shown in FIG. 1 Trestatin B: as shown in FIG. 2 Trestatin C: as shown in FIG. 3 (g) 1 H NMR spectrum (in D 2 O at 100 MHz): Trestatin A: as shown in FIG. 4 Trestatin B: as shown in FIG. 5 Trestatin C: as shown in FIG. 6 (h) Solubility in solvents: Trestatin A, Trestatin B and Trestatin C and their hydrochlorides are easily soluble in water; soluble in dimethylsulfoxide; slightly soluble in ethanol and acetone; and insoluble in ethyl acetate and chloroform; (i) Color reaction: Each of Trestatin A, Trestatin B and Trestatin C is positive to permanganate and anthrone reactions, and negative to Sakaguchi reaction.
Claim 2
Dependent Claim
262 words
The novel amino sugar derivatives Trestatin A, Trestatin B and Trestatin C and salts and mixtures thereof having trehalose as a common structural feature and having the following properties: (a) Elementary analysis: ______________________________________
C H N O
% % % %
______________________________________
Trestatin A:
46.72 7.13 2.08 43.28
Trestatin B:
46.27 7.04 1.65 44.69
Trestatin C:
47.55 7.15 2.29 42.66
______________________________________ (b) Molecular weight (Osmometry): Trestatin A: 1470 Trestatin B: 975 Trestatin C: 1890 (c) Melting point: Trestatin A: 221°-232° C. (dec.) Trestatin B: 209°-219° C. (dec.) Trestatin C: 230°-237° C. (dec.) (d) Specific rotation: Trestatin A: [α] D 24 =+177° (c=1.0, H 2 O) Trestatin B: [α] D 26 =+187° (c=1.0, H 2 O) Trestatin C: [α] D 23 =+169.5° (c=1.0, H 2 O) (e) Ulraviolet absorption spectrum (in water): Each of Trestatin A, Trestatin B and Trestatin C shows end absorption (f) Infrared absorption spectrum (in KBr): Trestatin A: as shown in FIG. 1 Trestatin B: as shown in FIG. 2 Trestatin C: as shown in FIG. 3 (g) 1 H NMR spectrum (in D 2 O at 100 MHz): Trestatin A: as shown in FIG. 4 Trestatin B: as shown in FIG. 5 Trestatin C: as shown in FIG. 6 (h) Solubility in solvents: Trestatin A, Trestatin B and Trestatin C and their hydrochlorides are easily soluble in water; soluble in dimethylsulfoxide; slightly soluble in ethanol and acetone; and insoluble in ethyl acetate and chloroform; (i) Color reaction: Each of Trestatin A, Trestatin B and Trestatin C is positive to permanganate and anthrone reactions, and negative to Sakaguchi reaction.
Claim 3
Dependent Claim
36 words
Amylase inhibiting compositions containing Trestatin A, Trestatin B or Trestatin C as defined in claim 1, or a salt of mixtures thereof in admixture with an organic or inorganic inert carrier material suitable for enteral application.
References Cited (Backward Citations)
FR2120073A1
Cited
DE2347782A1
Cited
FR2244536A1
Cited
US4062950A
Cited
US4065557A
Cited
USRE29903E
Cited
FR2346368A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1984-06-15 | 1984-12-15 | 1985-06-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-06-15 | 1988-12-15 | 1989-06-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-06-15 | 1992-12-15 | 1993-06-16 | $7700.00 | Window Closed / Lapsed |