Arena Pharmaceuticals, Inc.

Research Development Foundation

The Salk Institute

Arena Pharmacueticals, Inc.

Strang Cancer Prevention Center

James N Leonard

Zhi-Liang Chu

Robert M Jones

Ruoping Chen

Hussien A Al-Shamma

Derek T Chalmers

Chen Wang Liaw

Dominic P Behan

Juerg Lehmann

Marc R Montminy

Yaron Hakak

David J Unett

I-Lin Lin

Daniel T Connolly

Marc A Bruce

P Douglas Boatman

Zhi Liang Chu

Kevin P Lowitz

Huong T Dang

Jeremy G Richman

Bryan J Choi

Michael R Lerner

Dominique Maciejewski-Lenior

Daniel Ortuño

Hussein A Al-Shamma

The present invention concerns combination of an amount of a BRS-3 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the BRS-3 agonist alone and by the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing obesity and diabetes and conditions related thereto and conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.

Methods for identifying a GLP-1 secretagogue

The present invention relates to a method for identifying a metabolic stabilizing compound by: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is modulated, where a modulation in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound. In addition, the invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is increased, wherein an increase in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound. Further, the invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR43, and b) determining whether GPR43 functionality is decreased, wherein a decrease in GPR43 functionality is indicative of the candidate compound being a metabolic stabilizing compound.

Method of screening for compounds useful in the treatment of insulin resistance, impaired glucose tolerance or diabetes

The present invention relates to methods of using GPR119 receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY, such as conditions modulated by stimulation of NPY Y2 receptor (Y2R). Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition modulated by PYY, such as a condition modulated by stimulation of Y2R. Conditions modulated by PYY such as may be a condition modulated by stimulation of Y2R include bone-related conditions, metabolic disorders, angiogenesis-related conditions, ischemia-related conditions, convulsive disorders, malabsorptive disorders, cancers, and inflammatory disorders.

Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues

The present invention relates to methods of using GPR119 receptor to identify compounds useful for increasing bone mass in an individual. Agonists of GPR119 receptor are useful as therapeutic agents for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. Agonists of GPR119 receptor promote bone formation in an individual.

Methods of using GPR119 receptor to identify compounds which stimulate glucose-dependent insulinotropic peptide secretion

Methods of using a G protein-coupled receptor to identify peptide YY (PYY) secretagogues

The present invention concerns combination of an amount of a GPR119 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-1 level in a subject over that provided by the amount of the GPR119 agonist or the amount of the DPP-IV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-1 level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-1 secretagogues.

Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level

The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual.

GPR119 receptor agonists in methods of increasing bone mass and of treating osteoporosis and other conditions characterized by low bone mass, and combination therapy relating thereto

The invention disclosed in this patent document relates to transmembrane receptors, more particularly to endogenous, human orphan G protein-coupled receptors.

Human orphan G protein-coupled receptors

The present invention relates to a method for identifying a metabolic stabilizing compound, comprising: a) contacting a candidate compound with GPR35, and b) determining whether GPR35 functionality is increased, wherein an increase in GPR35 functionality is indicative of the candidate compound being a metabolic stabilizing compound. The invention further relates to a method for treating or preventing a metabolic-related disorder, comprising administering to an individual in need thereof an effective amount of a GPR35 modulator.

Method of using GPR35 to identify metabolic-stabilizing compounds

Methods for identifying GLP-1 secretagogues

Methods of preparing pharmaceutical compositions comprising GPR119 agonists having the effect of glucose-dependent insulinotropic peptide secretatgogues

Methods of using GPR119 to identify compounds useful for increasing bone mass in an individual

Methods of preparing pharmaceutical compositions comprising GPR119 agonists having the effect of glucose-dependent insulinotropic peptide secretagogues

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San Diego, CA, United States of America

James N Leonard