Arena Pharmaceuticals, Inc.

David J Unett

Robert M Jones

Yifeng Xiong

Bradley Teegarden

Sonja Strah-Pleynet

Konrad Feichtinger

Juerg Lehmann

Honnappa Jayakumar

Peter Ian Dosa

Jin Sun Karoline Choi

Yaron Hakak

Martin Casper

Derek T Chalmers

Chen Wang Liaw

Dominic P Behan

Ruoping Chen

Daniel T Connolly

Jeremy G Richman

Joel Gatlin

James N Leonard

Kevin P Lowitz

Huong T Dang

Sonia Villegas

Jin Sun Choi

Bryan J Choi

Michael R Lerner

Gregory S Kelner

Peter I Dosa

The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HTserotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HTserotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

3-phenyl-pyrazole derivatives as modulators of the 5-HTserotonin receptor useful for the treatment of disorders related thereto

3-phenyl-pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

The present invention relates to methods of using a G protein-coupled receptor (GPCR) to identify whether a candidate compound is a modulator of atherogenesis. In certain embodiments, the GPCR couples to Gi. In certain embodiments, the GPCR is human. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of atherosclerosis and atherosclerotic disease, including coronary artery disease, myocardial infarction, peripheral arterial disease, and ischemic stroke. Agonists of the invention are additionally useful as therapeutic agents for the prevention or treatment of conditions related to MCP-1 expression, including but not limited to rheumatoid arthritis, Crohn's disease, and multiple sclerosis.

Methods of screening for a compound that reduces atherogenesis

The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HTserotonin receptor and are useful, optionally in combination with other pharmaceutical agents administered separately or together, in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. 

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The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.

Human G protein-coupled receptors for metabolic-related disorders

The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In certain embodiments, the GPCR is human. In certain embodiments, the GPCR is expressed endogenously by neuronal cells or muscle cells. In certain embodiments, the GPCR is neuroprotective or myoprotective. In certain embodiments, the GPCR is a Humanin receptor. The present invention also relates to methods of using a modulator of the GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of neurodegenerative diseases in general, including Alzheimer's disease, Parkinson's disease, prion-associated disease, stroke and motor-neuron disease in particular, peripheral neuropathy, cerebral amyloid beta-protein angiopathy, and ischemic heart disease, including myocardial infarction and congestive heart failure.

Human G protein-coupled receptor and modulators thereof for the treatment of cell death-related disorders

Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders

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San Diego, CA, United States of America

David J Unett