Bristol-myers Squibb Compnay

Centocor, Inc.

University of Oklahoma

Douglas James Riexinger

Claudio Mapelli

Michael G Kornacker

Ving G Lee

William R Ewing

Richard B Sulsky

Yeheng Zhu

George A Heavner

Tasir Shamsul Haque

Miljenko Mervic

Rogelio L Martinez

Rodger P McEver

Vijay H Naringrekar

Robert A Copeland

Marian Kruszynski

Leon A Epps

Feng Qian

Lori S Burton

Jian-Guo Geng

Jovita Marcinkeviciene

Mark Richard Witmer

Zhihong Lai

Joseph Hendrick

Nina Ni

William Metzler

Protease activated receptor 4 (PAR4) agonist peptides are disclosed. These peptides are useful for developing robust PAR4 receptor assays.

PAR4 agonist peptides

The present invention provides PAR4 agonist peptides. These peptides are useful for developing robust PAR4 receptor assays.

PAR4 agonist peptides are disclosed. These peptides are useful for developing robust PAR4 receptor assays.

The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that may stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

N-terminally modified GLP-1 receptor modulators

The present invention provides novel pharmaceutical compositions comprising a human glucagon-like peptide-1 (GLP-1)-receptor modulator as an active ingredient in a sustained release formulation.

Sustained release GLP-1 receptor modulators

The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

Human glucagon-like-peptide-1 modulators and their use in treatment of diabetes and related conditions

The present invention provides peptides that specifically bind to BACE at a newly discovered exosite. The invention also provides methods for identifying peptides that bind to a BACE exosite. The invention further provides methods for identifying compounds that bind to a BACE exosite and modulate BACE activity. In another aspect, the invention provides methods for treating or preventing neurodegenerative disorders such as Alzheimer's disease by administering compounds that bind to a BACE exosite and modulate BACE activity.

Beta secretase exosite binding peptides and methods for identifying beta secretase modulators

Peptides derived from three regions of the lectin domain of GMP-140 (P-selectin) and the related selectins, ELAM-1 (E-selectin) and the lymphocyte homing receptor (L-selectin), have been found to inhibit neutrophil adhesion to GMP-140. These and additional peptides have been synthesized, having as their core region portions of the 74-76 amino acid sequence of GMP-140, with residue 1 defined as the N-terminus of the mature protein after the cleavage of the signal peptide. Examples demonstrate the inhibition of the binding of neutrophils to GMP-140 of peptides in concentrations ranging from 30 to 1500 .mu.mol. It has been found that alterations within the core sequence, as well as N-terminal and C-terminal flanking regions, do not result in loss of biological activity. The peptides are useful as diagnostics and, in combination with a suitable pharmaceutical carrier, for clinical applications in the modulation or inhibition of coagulation processes or inflammatory processes.

Peptide inhibitors of inflammation mediated by selectins

The present invention provides peptides comprising portions of the amino acid sequence at positions 58-61 of P-selectin. The invention also provides pharmacuetical compositions comprising the peptides of the invention, diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention, and method of preparing the peptides and pharmacuetical compositions.

Growing community of inventors

Flemington, NJ, United States of America

Douglas James Riexinger