# US 2012/0238528 A1 · Novel phosphonic acid compounds as inhibitors of serine proteases

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

- Number: US 2012/0238528 A1
- Document ID: US20120238528A1
- Status: Published application
- Kind: A1
- Application number: 13/471,876
- Filed: 2012-05-15
- Published: 2012-09-20
- Earliest claimed: 2001-10-19
- Assignees: Ortho-McNeil Pharmaceutical, Inc.
- Inventors: Michael N. Greco; Harold R. Almond, JR.; Lawrence de Garavilla; Michael J. Hawkins; Michael J. Humora; Yun Qian; Donald Gilmore Walker; Sergio Cesco-Cancian; Christopher Norman Nilsen; Mitul N. Patel; Kirk Leonard Sorgi; Eugene Powell
- Web page: https://patentgrep.com/patent/US20120238528A1

## CPC

- C07F 9/65586: {at least one of the hetero rings does not contain nitrogen as ring hetero atom}
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 11/08: Bronchodilators
- A61P 13/12: of the kidneys
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 27/02: Ophthalmic agents
- A61P 27/16: Otologicals
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/12: Antivirals
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- C07F 9/3882: {Arylalkanephosphonic acids (C07F9/3839 takes precedence)}
- C07F 9/572: Five-membered rings
- C07F 9/59: Hydrogenated pyridine rings
- C07F 9/650952: {having the nitrogen atoms in the positions 1 and 4}
- C07F 9/65517: {condensed with carbocyclic rings or carbocyclic ring systems}
- C07F 9/65583: {each of the hetero rings containing nitrogen as ring hetero atom}
- C07F 9/6561: containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.

## Claims

### Claim 1

A compound 35 having the structure:

### Claim 2 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

### Claim 3 (depends on 1)

A cationic salt of a compound of claim 1 wherein the cation is selected from the group consisting of, t-butylamine, calcium, choline, lithium, NH4+, potassium, sodium and tromethane.

### Claim 4 (depends on 3)

A cationic salt of claim 3 wherein the cation is selected from t-butylamine, NH4OH and tromethane.

### Claim 5 (depends on 4)

A cationic salt of claim 4 wherein the cation is tromethane.