Boron-containing small molecules as anti-inflammatory agents

• US 9,012,431 B2
• Filed: 06/11/2013
• Issued: 04/21/2015
• Est. Priority Date: 03/06/2008
• Status: Active Grant

• Current Assignee: Anacor Pharmaceuticals, Inc. (Pfizer Inc.)
• Original Assignee: Anacor Pharmaceuticals, Inc. (Pfizer Inc.)
• Inventors: Akama, Tsutomu
• Primary Examiner(s): Aulakh, Charanjit
• Application Number:
  US13/915,494
• Publication Number:
  US 20140011768A1
• Time in Patent Office: 679 Days
• Field of Search: 514/64, 544/229, 544/330
• US Class Current: 514/64
• CPC Class Codes: A61K 31/69 Boron compounds
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 19/00 Drugs for skeletal disorders
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: C07F 5/025 Boronic and borinic acid compounds
• CPC Class Codes: C07F 5/04 Esters of boric acids
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Compounds and methods of treating anti-inflammatory conditions are disclosed.

Claims

1. A compound having a structure according to the formula:

2. The compound of claim 1, or a salt thereof, wherein R^b is OR⁴, and R⁴ is a member selected from —

CH₃, —

CH₂CH₃, —

(CH₂)₂CH₃, and —

CH(CH₃)₂.

3. The compound of claim 1, which is 2-(1-Hydroxy-1,3-dihydro-benzo[c][1,2]oxaborol-5-yloxy)-4-methoxy-pyrimidine-5-carbonitrile.

4. A pharmaceutical formulation comprising:

(a) the compound of claim 1, or a pharmaceutically acceptable salt thereof;

(b) a pharmaceutically acceptable excipient.

5. The formulation of claim 4, wherein the formulation is in a unit dosage form.

6. The formulation of claim 4, wherein the formulation is for oral or topical use.