# US 5,707,973 A · Sulfated polysaccharids for treatment or prevention of thromboses

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- Number: US 5,707,973 A
- Document ID: US5707973A
- Status: Granted
- Kind: A
- Application number: 08/353,161
- Filed: 1994-12-09
- Granted: 1998-01-13
- Earliest claimed: 1991-04-23
- Assignees: Rhone-Poulenc Rorer S.A.
- Inventors: Jean-Pierre Baron; Andre Brun; Hendrik Hemker; Andre Uzan
- Web page: https://patentgrep.com/patent/US5707973A

## CPC

- A61K 31/702: Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
- A61K 31/70: Carbohydrates; Sugars; Derivatives thereof (sorbitol A61K31/047)
- A61K 31/715: Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
- A61K 31/727: Heparin; Heparan
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- C08B 37/0078: {Degradation products}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C08B: POLYSACCHARIDES; DERIVATIVES THEREOF (polysaccharides containing less than six saccharide radicals attached to each other by glycosidic linkages C07H; fermentation or enzyme-using processes C12P19/00; sugar industry C13; production of cellulose D21)

## Abstract

The invention relates to new mixtures of sulfated oligosaccharides having the general structure of heparin constitutive oligosaccharides, having an average molecular mass of 6.+-.0.6 kD, a polydispersiveness close to 1 and the capacity of inhibiting the production of thrombin. The invention also relates to their preparation and to pharmaceutical compositions containing them.

## Claims

### Claim 1

A mixture of sulfated oligosaccharides having the structure of constituent oligosaccharides of heparin, that has a mean molecular mass of 6.+-.0.6 kD and a polydispersity of 1 to 1.029, and that possesses a capacity to inhibit the generation of thrombin.

### Claim 2 (depends on 1)

The mixture according to claim 1, wherein the heparin is a depolymerized heparin fraction.

### Claim 3 (depends on 2)

The mixture according to claim 2, consisting of constituent oligosaccharides having a 2-O-sulpho-4-enopyranosuronic acid at one of their ends.

### Claim 4 (depends on 3)

The mixture according to claim 3, wherein the heparin is a depolymerized heparin that is depolymerized by the action of a base on an ester of the heparin.

### Claim 5 (depends on 1)

The mixture according to claim 1, having the capacity, in a test on plasma low in platelets stimulated by human thromboplastin or by contact, to inhibit the generation of thrombin by 25% at concentrations less than 400 ng/ml.

### Claim 6 (depends on 1)

A composition comprising the mixture of oligosaccharides according to claim 1 and a buffer.

### Claim 7 (depends on 1)

A method of treating or preventing venous or arterial thromboses comprising administering the mixture according to claim 1 to a patient.

### Claim 8 (depends on 7)

A method according to claim 7 wherein the arterial thromboses is an arterial thrombotic accident.

### Claim 9 (depends on 8)

The method according to claim 8 wherein the arterial thrombotic accident is myocardial infarction.

### Claim 10 (depends on 7)

The method according to claim 7 wherein the preventing of the venous thromboses is in a post-operative regime on a surgical patient.

### Claim 11 (depends on 1)

A method of inhibiting the generation of thrombin comprising administering the mixture of oligosaccharides according to claim 1 to a patient.

### Claim 12 (depends on 1)

A method of preventing thromboses in a surgical material comprising contacting the material with the mixture of claim 1.