# US 5,346,921 A · Treatment of inflammation with 15-keto-prostaglandin compounds

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

- Number: US 5,346,921 A
- Document ID: US5346921A
- Status: Granted
- Kind: A
- Application number: 07/972,092
- Filed: 1992-11-05
- Granted: 1994-09-13
- Earliest claimed: 1990-07-10
- Assignees: R-Tech Ueno, Ltd.
- Inventors: Ryuji Ueno
- Web page: https://patentgrep.com/patent/US5346921A

## CPC

- A61K 31/557: Eicosanoids, e.g. leukotrienes {or prostaglandins}
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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 treatment of inflammatory diseases which comprises administering, to a subject in need of such treatment, an anti-inflammatorily effective amount of a 15-keto-prostaglandin compound.

## Claims

### Claim 1

A method of treatment of a patient having an inflammation characterized by lesions caused by a defensive reaction or an inflammatory reaction of the patient and having signs of redness, heat, pain, swelling and loss of function which comprises administering, to a subject in need of such treatment, an anti-inflammatorily effective amount of a 15-keto-prostaglandin compound having the formula: ##STR7## wherein X and Y are hydrogen, hydroxy, halo, lower alkyl, hydroxy(lower)alkyl, or oxo, with the proviso that at least one of X and Y is a group other than hydrogen, and the 5-membered ring may have at least one double bond, Z is hydrogen or halo, A is --CH.sub.2 OH, --COCH.sub.2 OH, --COOH or its functional derivative, B is --CH.sub.2 --CH.sub.2, --CH.dbd.CH-- or --C.dbd.C--, R.sub.1 is a bivalent saturated or unsaturated, lower or medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halo, oxo or aryl, R.sub.2 is a saturated or unsaturated, lower or medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halo, hydroxy, oxo, lower alkoxy, lower alkanoyloxy, cyclo(lower)alkyl, aryl or aryloxy, and a carbon atom of R.sub.2 adjacent to the "CO" is substituted by at least one halogen atom; or R.sub.2 is a saturated or unsaturated aliphatic hydrocarbon residue containing a 5 carbon atom chain attached to the "C" of the "CO" which is unsbustituted or substituted with halo, hydroxy, oxo, lower alkoxy, lower alkanoyloxy, cyclo(lower)alkyl, aryl or aryloxy, [and said carbon atom of R.sub.2 adjacent to the CO is substituted by at least one halogen atom or ] and the terminal carbon atom of R.sub.2 is substituted by a lower alkyl.

### Claim 2 (depends on 1)

The method according to claim 1, wherein said 15-keto-prostaglandin compound is a 16-mono- or di-halo-15-keto-prostaglandin compound.

### Claim 3 (depends on 1)

The method according to claim 1, wherein said 15-keto-prostaglandin compound is a 13,14-dihydro-16-mono- or di-halo-15-keto-prostaglandin compound.

### Claim 4 (depends on 1)

The method according to claim 1, wherein said 15-keto-prostaglandin compound is a 13,14-dihydro-16-mono- or di-fluoro-15-keto-prostaglandin compound.

### Claim 5 (depends on 1)

The method according to claim 1, wherein said 15-keto-prostaglandin compound is a 13,14-dihydro-6,15-diketo-prostaglandin compound.

### Claim 6 (depends on 1)

The method according to claim 1, wherein said 15-keto-prostaglandin compound is a 15-keto-20-alkylprostaglandin compound.

### Claim 7 (depends on 1)

The method according to claim 1, wherein said 15-keto-prostaglandin compound is a 13,14-dihydro-15-keto-20-alkyl-prostaglandin compound.

### Claim 8 (depends on 1)

The method according to claim 1, wherein said 15-keto-prostaglandin compound is a 13,14-dihydro-15-keto-20-ethyl-prostaglandin compound.

### Claim 9 (depends on 1)

The method according to claim 1, wherein said inflammation to be treated is conjunctivitis.

### Claim 10 (depends on 1)

The method according to claim 1, wherein said compound is 13, 14-dihydro-15-keto-16, 16-difluoro-PGE or its lower alkyl ester.

### Claim 11 (depends on 1)

The method according to claim 1, wherein said compound is 13, 14-dihydro-15-keto-20-ethyl-PGF or its lower alkyl ester.

### Claim 12 (depends on 1)

The method according to claim 1, wherein said inflammation affects the eye.