Juan M Betancort

US Patent:

7576121, Aug 18, 2009

Filed:

May 1, 2006

Appl. No.:

11/381082

Inventors:

David Alan Campbell - San Diego CA, US
David T. Winn - San Diego CA, US
Juan Manuel Betancort - San Diego CA, US

Assignee:

Phenomix Corporation - San Diego CA

International Classification:

A61K 31/4025
C07D 207/10

US Classification:

514422, 548405

Abstract:

The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV (DPP-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.

US Patent:

7674913, Mar 9, 2010

Filed:

Nov 12, 2004

Appl. No.:

10/514575

Inventors:

David A. Campbell - San Diego CA, US
David T. Winn - San Diego CA, US
Juan M. Betancort - San Diego CA, US

Assignee:

Phenomix Corporation - San Diego CA

International Classification:

A61K 31/69
C07D 403/12
C07F 5/02

US Classification:

548405, 514 64

Abstract:

Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CH; S; O; CFor C(CH); Z is H; halogen; hydroxyl; (C)alkoxy; (C)alkyl; (C)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CrR, R, R, R, Rand Rare as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.

US Patent:

7767828, Aug 3, 2010

Filed:

May 1, 2006

Appl. No.:

11/381090

Inventors:

David Alan Campbell - San Diego CA, US
David T. Winn - San Diego CA, US
Juan Manuel Betancort - San Diego CA, US

Assignee:

Phenomix Corporation - San Diego CA

International Classification:

A61K 31/69
C07D 403/12
C07F 5/02

US Classification:

548405, 514 64

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.

US Patent:

7786163, Aug 31, 2010

Filed:

Jul 12, 2005

Appl. No.:

11/179797

Inventors:

David Alan Campbell - San Diego CA, US
Juan Manuel Betancort - San Diego CA, US
David T. Winn - San Diego CA, US

International Classification:

A61K 31/407
C07D 513/04

US Classification:

514413, 548453

Abstract:

Certain constrained cyano compounds are useful as inhibitors of post-proline/alanine cleaving amino-dipeptidases. Accordingly, these compounds can be employed, alone or with another therapeutic agent, to treat diabetes (especially, Type II diabetes), hyperglycemia, Syndrome X, diabetic complications, hyperinsulinemia, obesity, atherosclerosis and related diseases, as well as various immunomodulatory diseases and chronic inflammatory bowel disease.

US Patent:

7825139, Nov 2, 2010

Filed:

May 25, 2006

Appl. No.:

11/420273

Inventors:

David Alan Campbell - Sand Diego CA, US
David T. Winn - San Diego CA, US
Juan Manuel Betancort - San Diego CA, US

International Classification:

A61K 31/445
C07D 401/14

US Classification:

514326, 546208

Abstract:

Compounds that selectively inhibit dipeptidyl peptidase-IV over closely related dipeptidyl peptidases are those of Formula (I):.

US Patent:

7884217, Feb 8, 2011

Filed:

Oct 31, 2007

Appl. No.:

11/930337

Inventors:

David Alan Campbell - San Diego CA, US
David T. Winn - San Diego CA, US
Juan Manuel Betancort - San Diego CA, US

Assignee:

Phenomix Corporation - San Diego CA

International Classification:

A61K 31/69
C07F 5/02

US Classification:

548405, 514 64

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.

US Patent:

7906658, Mar 15, 2011

Filed:

Aug 2, 2007

Appl. No.:

11/833063

Inventors:

David Alan Campbell - San Diego CA, US
David T. Winn - San Diego CA, US
Juan Manuel Betancort - San Diego CA, US

Assignee:

Phenomix Corporation - Encinitas CA

International Classification:

A61K 31/69
C07D 403/12

US Classification:

548405, 514 64

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.

US Patent:

8415295, Apr 9, 2013

Filed:

Jan 22, 2010

Appl. No.:

12/692276

Inventors:

David Alan Campbell - San Diego CA, US
David T. Winn - San Diego CA, US
Juan Manuel Betancort - San Diego CA, US

Assignee:

Phenomix Corporation - Encinitas CA

International Classification:

A61K 38/28
A61K 31/69
C07F 5/02
C12N 9/99
C07D 205/02
A61P 3/10

US Classification:

514 3, 514 64, 548405, 435184, 546 13, 540200, 544229

Abstract:

Dipeptidyl peptidase IV (DPP-IV)-inhibiting compounds are provided that have formula I: wherein n is 1 to 3; X is CHS; O; CFor C(CH); Z is H; halogen; hydroxyl; (C)alkoxy; (C)alkyl; (C)cycloalkyl; phenyl; or heteroaryl; where the phenyl and heteroaryl groups are optionally mono- or independently plurisubstituted with R7; optionally, X together with an adjacent ring carbon and Z form a fused cyclopropyl; and optionally, one of the bonds in the ring containing X is a double bond; and CrR, R, R, R, Rand Rare as described herein. Methods for preparing these compounds, and methods for treating diabetes, especially Type II diabetes, and other related diseases are described using the compounds of formula I in pharmaceutical compositions which contain these compounds. Pharmaceutical compositions which contain combinations of these compounds with other antidiabetic agents are also described herein.