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

• US 7,906,658 B2
• Filed: 08/02/2007
• Issued: 03/15/2011
• 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:
  US11/833,063
• Publication Number:
  US 20070299036A1
• Time in Patent Office: 1,321 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 a method of treatment of a malcondition that can be regulated or normalized via inhibition of DPP-IV. The method involves administration of an effective amount of a pyrrolidine compound of the invention, such as would be present in a pharmaceutical composition of the invention, to mammals, especially humans, to affect a malcondition that can be regulated or normalized via inhibition of DPP-IV.

Claims

1. A method for treating a malcondition characterized by impaired glycemic control in a human wherein the malcondition is selected from the group consisting of Type 1 diabetes, Type 2 diabetes, gestational diabetes, MODY, impaired glucose tolerance, impaired fasting glucose, hyperglycemia, impaired glucose metabolism, insulin resistance and obesity, comprising administering to a human in need thereof an effective amount of a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of formula (I):

2. The method of claim 1, wherein the compound of formula (I) is:

3. The method of claim 2, wherein the malcondition is diabetes mellitus.

4. The method of claim 2, wherein the malcondition is type 2 diabetes.

5. The method of claim 2, wherein the pharmaceutical composition comprises about 10 mg to about 1000 mg of the compound of formula (I) or a pharmaceutically acceptable salt thereof.

6. The method of claim 2, wherein the pharmaceutical composition comprises about 50 mg to about 750 mg of the compound of formula (I) or a pharmaceutically acceptable salt thereof.

7. The method of claim 2, wherein the pharmaceutical composition also comprises a therapeutically effective amount of metformin.

8. The method of claim 1, wherein the compound of formula (I) is a selective inhibitor of DPP-IV.

9. The method of claim 2, wherein the compound of formula (I) is a selective inhibitor of DPP-IV.