# US 5,708,030 A · Substituted kynurenines and process for their preparation

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

- Number: US 5,708,030 A
- Document ID: US5708030A
- Status: Granted
- Kind: A
- Application number: 08/463,895
- Filed: 1995-06-05
- Granted: 1998-01-13
- Earliest claimed: 1993-08-06
- Assignees: University of Maryland; Pharmacia & Upjohn Company
- Inventors: Robert Schwarcz; Mario Varasi; Arturo Della Torre; Carmela Speciale; Alberto Bianchetti
- Web page: https://patentgrep.com/patent/US5708030A

## CPC

- C07C 229/36: with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 31/195: having an amino group
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 31/215: of carboxylic acids
- A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate
- C07C 2601/08: the ring being saturated
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- 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

The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).

## Claims

### Claim 1

A method of treating age-related cognitive disorders and perinatal brain disorders comprising administering a therapeutically effective amount of an inhibitor of kynurenine aminotransferase (KAT) to a patient afflicted therewith.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the inhibitor is a compound of the formula (I) ##STR7## wherein R is a halogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.7 cycloalkyl group, a phenyl-C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a C.sub.6 -C.sub.10 aryloxy group, a phenyl-C.sub.1 -C.sub.4 alkoxy group or a trifluoromethyl group; and
R.sub.1 is a hydroxy group, a C.sub.1 -C.sub.6 alkoxy group, an amino group, a mono-C.sub.1 -C.sub.6 alkylamino group, a di-C.sub.1 -C.sub.6 alkylamino group, hydroxylamino group, a C.sub.1 -C.sub.4 alkoxyamino group or a benzyloxyamino group,
either as a single isomer or as a mixture of isomers, or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 2)

The method according to claim 2, wherein the inhibitor is a compound selected from the group consisting of:
2-amino-4-(2-amino-5-chlorophenyl)-4-oxo-butyric acid, and
2-amino-4-(2-amino-5-ethylphenyl)-4-oxo-butyric acid;
either as a single isomer or as a mixture of isomers, and the pharmaceutically acceptable salts thereof.