PROTEASOME INHIBITORS AND PROCESSES FOR THEIR PREPARATION, PURIFICATION AND USE

• US 20140121182A1
• Filed: 06/21/2012
• Published: 05/01/2014
• Est. Priority Date: 06/22/2011
• Status: Abandoned Application

• Current Assignee: Cephalon Incorporated (Teva Pharmaceutical Industries Limited)
• Original Assignee: Cephalon Incorporated (Teva Pharmaceutical Industries Limited)
• Inventors: Bakale, Roger P., Mallamo, John P., Roemmele, Renee Caroline
• Application Number:
  US14/127,511
• Publication Number:
  US 20140121182A1
• Time in Patent Office: Days
• US Class Current: 514/64
• CPC Class Codes: A61P 19/00 Drugs for skeletal disorders
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07F 5/025 Boronic and borinic acid compounds
• CPC Class Codes: C07F 5/04 Esters of boric acids

Abstract

The invention provides boronic esters of Formula (I) wherein R is H or methyl, and methods for the preparation and purification thereof.

Claims

1. A boronic ester of Formula I

2. The boronic ester of claim 1, wherein R is H.

3. The boronic ester of claim 1, wherein R is CH₃.

4. A process for preparing a pharmaceutical composition comprising the step of combining a boronic ester of claim 1 with a pharmaceutically acceptable excipient.

5. A process for preparing a pharmaceutical composition of Compound 1

6. A process for purifying Compound 1

7. A process for preparing Compound 1

8. Compound 1 having a chemical purity of at least 99.5%

9. A pharmaceutical composition comprising Compound 1 having a chemical purity of at least 99.5%