Arena Pharmaceuticals, Inc.

Boehringer Ingelheim International Gmbh

Pipeline Therapeutics, Inc.

Aries Associates, Inc.

Contineum Therapeutics, Inc.

Arena Pharmeceuticals, Inc.

Yifeng Xiong

Robert M Jones

Sonja Strah-Pleynet

Jin Sun Karoline Choi

Graeme Semple

Sangdon Han

Xiuwen Zhu

Albert S Ren

Jae-Kyu Jung

Lars Thoresen

Dawei Yue

Imelda Calderon

Beatriz Fioravanti

Juerg Lehmann

Anthony C Blackburn

Bradley Teegarden

Jaimie Karyn Rueter

Antonio Garrido Montalban

Young-Jun Shin

Peter Ian Dosa

Biman B Pal

Brett Ullman

Konrad Feichtinger

Yalda Mostofi Bravo

Honnappa Jayakumar

Brian Christopher Smith

Kai Gerlach

Marco Ferrara

Michael J Conrad

Ram S Bhatt

Mihai Azimioara

Thomas O Schrader

Scott Hobson

Thuy-Anh Tran

Austin Chih-Yu Chen

Viktor Vintonyak

Uta Friederike Lessel

Austin Chen

Giacomo Fossati

Barbara Bertani

Jonathan A Covel

Wei Zheng

Jayant Thatte

David J Unett

Carleton R Sage

Marc A Bruce

Martin Casper

Martin C Cherrier

Jill Melissa Baccei

Ursula Mueller-Vieira

Jane Laguerta Uy

Thomas Schrader

Jeffrey Roger Roppe

Azzouz Bencheikh

Guilherme Pereira

Vibha Dave

Kameshwari Duvvuri

Peter I Dosa

Didier Jc Bagnol

Andrew J Grottick

Daniela Berta

Julian Wippich

Brian M Smith

Jeffrey Roppe

Frank Runge

Kirsten Gutsche

Jin Sun Choi

Graem Semple

Henry Korman

Zheng Wei

Daniela Gavina Berta

Bret Ullman

Brett Ulmann

Provided herein are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M(mAChR M); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

Muscarinic acetylcholine M1 receptor antagonists

The invention relates to 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) for use as a medicament, pharmaceutical compositions comprising at least a compound of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives and the use thereof as medicament

Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CBreceptor;

Cannabinoid receptor modulators

Provided, inter alia, are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

Muscarinic acetylcholine Mreceptor antagonists

The invention relates to substituted 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) for use as a medicament, pharmaceutical compositions comprising the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

Substituted 3-phenoxyazetidin-1-yl-pyrazines

Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CBreceptor;

The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

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

Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CBreceptor; 

Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HTreceptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, 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 symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related 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. 

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rmidazo[1,2-&#x3b1;]pyridine 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 insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic- related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HTserotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together. 

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San Diego, CA, United States of America

Yifeng Xiong