Todd K. Jones - Solana Beach CA Mark E. Goldman - San Diego CA Charlotte L. F. Pooley - San Diego CA David T. Winn - San Diego CA James P. Edwards - San Diego CA Sarah J. West - San Diego CA Christopher M. Tegley - San Diego CA Lin Zhi - San Diego CA Lawrence G. Hamann - San Diego CA Luc J. Farmer - La Jolla CA Robert L. Davis - Santee CA
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
Pyrrolidine Compounds And Methods For Selective Inhibition Of Dipeptidyl Peptidase-Iv
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.
Pyrrolidine Compounds And Methods For Selective Inhibition Of Dipeptidyl Peptidase-Iv
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.
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.
Methyl And Ethyl Substituted Pyrrolidine Compounds And Methods For Selective Inhibition Of Dipeptidyl Peptidase-Iv
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.
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.
Methods Of Preparing Heterocyclic Boronic Acids And Derivatives Thereof
David Alan Campbell - San Diego CA, US David T. Winn - San Diego CA, US
Assignee:
Phenomix Corporation - San Diego CA
International Classification:
C07F 5/02
US Classification:
548408, 548558
Abstract:
In the context of synthesizing heterocyclic boronic acid compounds, a convergent synthetic methodology is particularly efficient for preparing boropyrrolidines and derivatives of boropyrrolidines.
Compounds And Methods For Selective Inhibition Of Dipeptidyl Peptidase-Iv
Sharp Memorial Hospital 7901 Frost Street, San Diego, CA 92123
Education:
Medical School George Washington University / School of Medicine And Health Sciences Graduated: 1992 Medical School The George Washington U Hosp Graduated: 1992
Dr. Winn graduated from the Eastern Virginia Medical School Medical College in 1983. He works in Columbia, SC and specializes in Urgent Care Medicine. Dr. Winn is affiliated with Lexington Medical Center.
Dr. Winn graduated from the Northwestern University Feinberg School of Medicine in 1993. He works in San Diego, CA and specializes in Internal Medicine. Dr. Winn is affiliated with Kaiser Permanente Medical Center.