Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-IV

• US 7,884,217 B2
• Filed: 10/31/2007
• Issued: 02/08/2011
• Est. Priority Date: 11/12/2003
• Status: Active Grant

• Current Assignee: Sino-Med International Alliance Inc.
• Original Assignee: Phenomix Corporation
• Inventors: Winn, David T., Campbell, David Alan, Betancort, Juan Manuel
• Primary Examiner(s): STOCKTON, LAURA LYNNE
• Application Number:
  US11/930,337
• Publication Number:
  US 20080182995A1
• Time in Patent Office: 1,196 Days
• Field of Search: 548/405
• US Class Current: 548/405
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: C07F 5/025 Boronic and borinic acid compounds

Abstract

The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.

Claims

1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of formula (I)

2. The pharmaceutical composition of claim 1, wherein R² and R³ are both —

OH and wherein the compound of formula (I) is;

3. The pharmaceutical composition of claim 1 or 2, wherein the composition is an oral dosage form.

4. The pharmaceutical composition of claim 1 or 2 wherein the therapeutically effective amount is about 50 mg to about 750 mg.