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Oligosaccharides having selective anticoagulation activity

Assignee: Pfizer Health AB
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Filing: 1981-09-11
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Granted: 1985-01-29
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Expires: 2001-09-11
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Abstract

Abstract The invention relates to an oligosaccharide which contains 4-8 monosaccharide units and which is characterized in that it contains at least one glucosamine unit which is 3-0-sulfated, and at least one additional glucosamine unit, whereby these units are linked via an intermediate monosaccharide unit, which is bound to the reducing end of the 3-0-sulfated glucosamine unit. The invention further relates to a pharmaceutical composition containing one or more such oligosaccharides, and to a process for the preparation of these oligosaccharides.

Inventors

  • 👤 Ulf P. F. Lindahl
  • 👤 Gudrun E. Backstrom
  • 👤 John Y. L. Thunberg

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 23:48
CPC Classifications
C; C08; C08B; C08B37/00; C08B37/006; C08B37/0063; C08B37/0075; C07; C07H; C07H11/00

Claims Analysis

Total Claims: 20
Claim 1
Independent Claim 49 words
Oligosaccharide comprising 4-8 monosaccharide units, characterized in that it contains at least one glucosamine unit which is 3-O-sulfated, and at least one further glucosamine unit, whereby these units are connected by an iduronic unit linking monosaccharide unit, which is bound to the reducing end of the 3-O-sulfated glucosamine unit.
Claim 2
Dependent Claim 49 words
Oligosaccharide comprising 4-8 monosaccharide units, characterized in that it contains at least one glucosamine unit which is 3-O-sulfated, and at least one further glucosamine unit, whereby these units are connected by an iduronic unit linking monosaccharide unit, which is bound to the reducing end of the 3-O-sulfated glucosamine unit.
Claim 3
Dependent Claim 15 words
Oligosaccharide according to claim 1, characterized in that the 3-O-sulfated glucosamine unit also is 2-N-sulfated.
Claim 4
Dependent Claim 21 words
Oligosaccharide according to claim 1 or claim 2, characterized in that the said at least one further glucosamine unit is 2-N-sulfated.
Claim 5
Dependent Claim 18 words
Oligosaccharide according to claim 1, characterized in that the intermediate monosaccharide unit is a sulfated iduronic acid unit.
Claim 6
Dependent Claim 30 words
Oligosaccharide according to claim 1, characterized in that it contains a non-sulfated iduronic acid unit linked to position C 4 of the 3-O-sulfated glucosamine unit via two linking monosaccharide units.
Claim 7
Dependent Claim 21 words
Oligosaccharide according to claim 1, characterized in that its last unit is a 2,5-anhydro-D-mannose unit, which can be sulfated or non-sulfated.
Claim 8
Dependent Claim 26 words
Oligosaccharide according to claim 1, characterized in that it exhibits selective coagulation activity by affinity to antithrombine and increases the reactivity of antithrombine towards factor X.
Claim 9
Dependent Claim 18 words
Oligosaccharide according to claim 1, characterized in that it is a tetrasaccharide, pentasaccharide, hexasaccharide, heptasaccharide or an octasaccharide.
Claim 10
Dependent Claim 23 words
A pharmaceutical preparation, characterized in that it contains one or more oligosaccharides according to claim 1 in an amount sufficient for anticoagulation activity.
Claim 11
Dependent Claim 32 words
The oligosaccharide of claim 5 wherein one of the two linking monosaccharide units is an acetylated glucosamine unit, and the other of the two linking monosaccharide units is a glucuronic acid unit.
Claim 12
Dependent Claim 12 words
The oligosaccharide of claim 10 wherein said acetylated glucosamine unit is 6-O-sulfated.
Claim 13
Dependent Claim 21 words
Oligosaccharide according to claim 11 characterized in that its last unit is a 2,5-anhydro-D-mannose unit, which can be sulfated or non-sulfated.
Claim 14
Dependent Claim 11 words
The oligosaccharide of claim 12 wherein said 2,5-anhydro-D-mannose unit is sulfated.
Claim 15
Dependent Claim 18 words
Oligosaccharide according to claim 2 characterized in that the intermediate monosaccharide unit is a sulfated iduronic acid unit.
Claim 16
Dependent Claim 18 words
Oligosaccharide according to claim 14 characterized in that the said at least one further glucosamine unit is 2-N-sulfated.
Claim 17
Dependent Claim 30 words
Oligosaccharide according to claim 15 characterized in that it contains a non-sulfated iduronic acid unit linked to position C 4 of the 3-O-sulfated glucosamine unit via two linking monosaccharide units.
Claim 18
Dependent Claim 32 words
Oligosaccharide according to claim 16 wherein one of the two linking monosaccharide units is an acetylated glucosamine unit and the other of the two linking monosaccharide units is a glucuronic acid unit.
Claim 19
Dependent Claim 12 words
Oligosaccharide according to claim 17 wherein said acetylated glucosamine unit is 6-O-sulfated.
Claim 20
Dependent Claim 21 words
Oligosaccharide according to claim 18 characterized in that its last unit is a 2,5-anhydro-D-mannose unit, which can be sulfated or non-sulfated.

References Cited (Backward Citations)

GB2002406A Cited
GB2035349A Cited
EP0014184A2 Cited
US4303651A Cited
EP0027089A1 Cited
US4401758A Cited
US4401662A Cited
US4281108A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-01-29 1988-07-30 1989-01-29 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-01-29 1992-07-30 1993-01-29 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-01-29 1996-07-30 1997-01-29 $7700.00 Window Closed / Lapsed

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