# US 5,708,010 A · Methods of inhibiting myeloperoxidase activity

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- Number: US 5,708,010 A
- Document ID: US5708010A
- Status: Granted
- Kind: A
- Application number: 08/443,840
- Filed: 1995-05-18
- Granted: 1998-01-13
- Earliest claimed: 1993-12-21
- Assignees: Eli Lilly and Company
- Inventors: Andrew L. Glasebrook
- Web page: https://patentgrep.com/patent/US5708010A

## CPC

- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 31/4535: containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A method of inhibiting myeloperoxidase activity or a physiological condition associated with an excess thereof, comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

## Claims

### Claim 1

A method of inhibiting myeloperoxidase activity comprising prophylactically administering to a human in need thereof an effective amount of a compound having the formula ##STR5## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR6## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

### Claim 2 (depends on 1)

The method of claim 1 wherein said compound is the hydrochloride salt thereof.

### Claim 3 (depends on 1)

The method of claim 1 wherein said compound is ##STR7## or its hydrochloride salt.

### Claim 4 (depends on 1)

The method of claim 1 wherein said human is a post-menopausal woman.

### Claim 5

A method for the inhibition of a physiological disorder associated with an excess of myeloperoxidase, which method comprises prophylactically administering to a human in need thereof an effective amount of a compound of Formula I ##STR8## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR9## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamtehylenemino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

### Claim 6 (depends on 5)

The method of claim 5 wherein said compound is the hydrochloride salt thereof.

### Claim 7 (depends on 5)

The method of claim 5 wherein said compound is ##STR10## or its hydrochloride salt.

### Claim 8 (depends on 5)

The method of claim 5 wherein said disorder is selected from systemic lupus erythrematosas, Hashimoto's thyroidiris, myasthenia gravis, rheumatoid arthritis, multiple sclerosis, Guillan Barre syndrome, or glomerulonephritis.