# US 5,352,682 A · Compositions containing salts of bile acid-aminosalicylate conjugates

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- Number: US 5,352,682 A
- Document ID: US5352682A
- Status: Granted
- Kind: A
- Application number: 08/027,693
- Filed: 1993-03-08
- Granted: 1994-10-04
- Earliest claimed: 1993-03-08
- Assignees: Digestive Care Inc.
- Inventors: Tibor Sipos
- Web page: https://patentgrep.com/patent/US5352682A

## CPC

- A61K 31/60: Salicylic acid; Derivatives 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)

## Abstract

Disclosed are compositions containing bile acid-aminosalicylate conjugates having the formula, or a pharmaceutically acceptable salt thereof ##STR1## wherein R.sub.1 is OH either the .alpha. or the .beta. position; R.sub.2 is OH; R.sub.3 is H or OH; and R.sub.4 is H or acetyl, the process for their preparation and method of treating/preventing gastrointestinal disorders, impaired liver function, autoimmune diseases of the liver and biliary tract, colon cancer, inflammatory bowel diseases, Crohn's disease, cystic fibrosis, dissolving gallstones, and regulating dietary cholesterol absorption by administering said compositions to a mammal in need of such treatment.

## Claims

### Claim 1

A method of treating/preventing bile acid deficiency condition and inflammatory disease in a patient comprising the administration to said patient in need of such treatment/prevention an effective amount of a pharmaceutically acceptable bile acid-aminosalicylic acid conjugate of the formula (I) or a pharmaceutically acceptable salt thereof ##STR4## wherein R.sub.1 is OH either in the .alpha. or in the .beta. position;
R.sub.2 is OH;
R.sub.3 is H or OH; and
R.sub.4 is H or acetyl.

### Claim 2 (depends on 1)

A method of treating/preventing bile acid deficiency condition and inflammatory disease in a patient comprising the administration to said patient in need of such treatment/prevention an effective amount of a salt according to claim 1 wherein said pharmaceutically acceptable salt is selected from the group consisting of sodiums potassium and tromethamine.

### Claim 3 (depends on 1)

A method of treating/preventing bile acid deficiency condition and inflammatory disease in a patient comprising the administration to said patient in need of such treatment/prevention an effective amount of a conjugate according to claim 1 wherein said bile acid-aminosalicylic acid conjugate is selected from the group consisting of ursodeoxycholic acid-3-aminosalicylic acid amide, ursodeoxycholic acid-4-aminosalicylic acid amide, ursodeoxycholic acid-5-aminosalicylic acid amide, chenodeoxycholic acid-3-aminosalicylic acid amide, chenodeoxycholic acid-4-aminosalicylic acid amide and chenodeoxycholic acid-5-aminosalicylic acid amide.

### Claim 4 (depends on 1)

A method of treating/preventing bile acid deficiency condition and inflammatory disease in a patient comprising the administration to said patient in need of such treatment/prevention an effective amount of a conjugate according to claim 1 wherein said bile acid-aminosalicylic acid conjugate is selected from the group consisting of cholic acid-3-aminosalicylic acid amide, cholic acid-4-aminosalicylic acid amide, cholic acid-5-aminosalicylic acid amide, deoxycholic acid-3-acetylaminosalicylic acid amide, deoxycholic acid-4-acetylaminosalicylic acid amide and deoxycholic acid-5-acetylaminosalicylic acid amide.