# US 5,707,974 A · Method of synthesis of 2-O-desulfated heparin and use thereof for inhibition of elastase and cathepsin G

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 5,707,974 A
- Document ID: US5707974A
- Status: Granted
- Kind: A
- Application number: 08/478,199
- Filed: 1995-06-07
- Granted: 1998-01-13
- Earliest claimed: 1992-07-24
- Assignees: Cavalier Pharmaceuticals
- Inventors: Thomas P. Kennedy
- Web page: https://patentgrep.com/patent/US5707974A

## CPC

- 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
- C08B 37/0075: {Heparin; Heparan sulfate; Derivatives thereof, e.g. heparosan; Purification or extraction methods thereof}
- 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

A method and medicament for the inhibition of neutrophil elastase and cathepsin G in mammals comprising administering a treatment effective amount of 2-O-desulfated heparin to a mammal in need thereof. The medicament preferably is administered by aerosolization or by intravenous (IV) injection. Preferably, the 2-O-desulfated heparin medicament includes a physiologically acceptable carrier which may be selected from the group consisting of physiologically buffered saline, normal saline, and distilled water. Additionally provided is a method of synthesizing 2-O-desulfated heparin.

## Claims

### Claim 1

A medicament comprising a partially desulfated heparin made by the process comprising alkalinizing a solution containing heparin to pH 13.

### Claim 2 (depends on 1)

The medicament of claim 1, wherein the process further comprises, after the solution is alkalinized, lyophilizing the solution.

### Claim 3 (depends on 1)

The medicament of claim 1, wherein the solution is alkalinized with sodium hydroxide.

### Claim 4 (depends on 1)

The medicament of claim 1, further comprising a physiologically acceptable carrier.

### Claim 5 (depends on 4)

The medicament of claim 4, wherein said carrier is selected from the group consisting of physiologically buffered saline, normal saline and distilled water.

### Claim 6 (depends on 1)

The medicament of claim 1, wherein the heparin has a weight ranging from 2.5 mg/kg to 5.0 mg/kg.

### Claim 7 (depends on 1)

The medicament of claim 1, wherein the heparin has a weight ranging from about 10 mg to about 100 mg.

### Claim 8 (depends on 1)

The medicament of claim 1, wherein the heparin has a weight ranging from 0.5 mg/kg to 10 mg/kg.

### Claim 9 (depends on 1)

The medicament of claim 1 in the form of aerosol particles.

### Claim 10 (depends on 7)

The medicament of claim 7 in the form of aerosol particles.

### Claim 11 (depends on 1)

The medicament of claim 1 in the form of an IV solution.

### Claim 12 (depends on 6)

The medicament of claim 6 in the form of an IV solution.

### Claim 13 (depends on 1)

The medicament of claim 1 for inhibiting neutrophil elastase or cathepsin G in a mammal, wherein the partially desulfated heparin is in an inhibiting effective amount.

### Claim 14 (depends on 1)

The medicament of claim 1 for treating emphysema, chronic bronchitis, adult respiratory distress syndrome, cystic fibrosis, or an ischemia-reperfusion related condition, wherein the partially desulfated heparin is in a treatment effective amount.

### Claim 15 (depends on 14)

The method of claim 14, wherein the ischemia-reperfusion related condition arises from a myocardial infarction or a stroke.

### Claim 16 (depends on 13)

The medicament of claim 13, wherein the mammal is a human.

### Claim 17 (depends on 13)

The medicament of claim 13, wherein the process further comprises, after the solution is alkalinized, lyophilizing the solution.

### Claim 18 (depends on 13)

The medicament of claim 13, wherein the solution is alkalinized with sodium hydroxide.

### Claim 19 (depends on 13)

The medicament of claim 13, further comprising a physiologically acceptable carrier.

### Claim 20 (depends on 19)

The medicament of claim 19, wherein said carrier is selected from the group consisting of physiologically buffered saline, normal saline and distilled water.

### Claim 21 (depends on 13)

The medicament of claim 13, wherein the heparin has a weight ranging from 2.5 mg/kg to 5.0 mg/kg.

### Claim 22 (depends on 13)

The medicament of claim 13, wherein the heparin has a weight ranging from about 10 mg to about 100 mg.

### Claim 23 (depends on 13)

The medicament of claim 13, wherein the heparin has a weight ranging from 0.5 mg/kg to 10 mg/kg.

### Claim 24 (depends on 13)

The medicament of claim 13 in the form of aerosol particles.

### Claim 25 (depends on 22)

The medicament of claim 22 in the form of aerosol particles.

### Claim 26 (depends on 13)

The medicament of claim 13 in the form of an IV solution.

### Claim 27 (depends on 21)

The medicament of claim 21 in the form of an IV solution.

### Claim 28 (depends on 1)

The medicament of claim 1 further comprising a physiologically acceptable carrier, wherein the heparin has a weight ranging from 2.5 mg/kg to 5.0 mg/kg.

### Claim 29 (depends on 1)

The medicament of claim 1, further comprising a physiologically acceptable carrier, wherein the heparin has a weight ranging from about 10 mg to about 100 mg.

### Claim 30 (depends on 1)

The medicament of claim 1, further comprising a physiologically acceptable carrier, wherein the heparin has a weight ranging from 0.5 mg/kg to 10 mg/kg.

### Claim 31 (depends on 13)

The medicament of claim 13, further comprising a physiologically acceptable carrier, wherein the heparin has a weight ranging from 2.5 mg/kg to 5.0 mg/kg.

### Claim 32 (depends on 13)

The medicament of claim 13, further comprising a physiologically acceptable carrier, wherein the heparin has a weight ranging from about 10 mg to about 100 mg.

### Claim 33 (depends on 13)

The medicament of claim 13, further comprising a physiologically acceptable carrier, wherein the heparin has a weight ranging from 0.5 mg/kg to 10 mg/kg.