Arena Pharmaceuticals, Inc.

Other

University of Utah Research Foundation

Cognetix, Inc.

Blackthorn Therapeutics, Inc.

The Scripps Research Institute

University of Minnesota

Neumora Therapeutics, Inc.

Xenome Limited

Jones, Robert M.

Composite Motors, Inc.

Brandt, Gary

Knight, Chris

Hardick, David

Urbano, Mariangela

Robert M Jones

Yifeng Xiong

Baldomero M Olivera

Sangdon Han

Xiuwen Zhu

Juerg Lehmann

J Michael McIntosh

Sonja Strah-Pleynet

Maren Watkins

Lars Thoresen

David R Hillyard

James N Leonard

Zhi-Liang Chu

Anthony C Blackburn

Jaimie Karyn Rueter

Antonio Garrido Montalban

Jae-Kyu Jung

Biman B Pal

Dawei Yue

Jin Sun Karoline Choi

Imelda Calderon

Beatriz Fioravanti

Graeme Semple

Mariangela Urbano

Daniel J Buzard

Sun Hee Kim

Lourdes J Cruz

Young-Jun Shin

Albert S Ren

Joseph M Lisiecki

Richard T Layer

Jayant Thatte

Hussien A Al-Shamma

Chris Knight

James E Garrett

David Hardick

Gary Brandt

Jason Tierney

John D Wagstaff

Eric Douglas Turtle

Bradley Teegarden

Brett Ullman

Konrad Feichtinger

Honnappa Jayakumar

Edward Roberts

Hugh Rosen

Peter Ian Dosa

Miguel A Guerrero

R Tyler McCabe

Scott Stirn

David J Unett

Craig S Walker

Julita S Imperial

A Grey Craig

Jeanne V Moody

Reshma Shetty

Carleton R Sage

Marc A Bruce

Martin Casper

Candace Mae Laxamana

Xianrui Zhao

Andrew Mamoru Kawasaki

Philip S Portoghese

Mihai Azimioara

David M Hooper

Richard Jacobsen

G Edward Cartier

Don E Johnson

David Griffen

Kameshwari Duvvuri

Vibha Dave

Gloria P Corpuz

Chris Lock

Guilherme Pereira

Jane Laguerta Uy

Mark Stewart Chambers

Tawfik Gharbaoui

Mark Stuart Chambers

Weichao George Chen

Thomas O Schrader

Gregory S Shen

Abu J M Sadeque

Elsie C Jimenez

Jeffrey Edwards

Cheryl Geraldine Lassen

Michelle Kasem

Ronald J Christopher

Michael E Morgan

Benjamin R Johnson

Que Liu

Jin Sun Choi

Glen Marquez

Hussein A Al-Shamma

Graem Semple

Doug Steel

Shiv K Sharma

Jacob Scott Nielsen

Doug Steele

David Griffin

Robert Schoenfeld

Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof: wherein Q, Q, Q, R, R, Rand X are as defined herein.

Vasopressin receptor antagonists and products and methods 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;

Cannabinoid receptor modulators

Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R, R, R, R, R, R, Rand Rare as defined herein.

Kappa opioid receptor antagonists and products and methods related thereto

Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof: wherein A, B, G, R, R, R, Rand X are as defined herein.

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 crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CBreceptor and are therefore useful in the treatment of CBreceptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; 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.

Crystalline forms and processes for the preparation of cannabinoid receptor modulators

The present invention relates to, inter alia, methods of treatment and combinations of (R)-2-(7-(4-cyclopentyl-3-(tri-fluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1) useful for the treatment of primary biliary cholangitis (PBC). In some embodiments, the methods further comprise administering Compound 1, or a pharmaceutically salt, solvate, or hydrate thereof, in combination with a compound selected from the group consisting of: an antihistamine (diphenhydramine), cholestyramine (questran, prevalite), rifampin, an opioid antagonist (naloxone), pilocarpine (isopto carpine, salagen), cevimeline (evoxac), calcium and/or vitamin D supplement, and vitamin A, D, E and/or K supplement. Other embodiments, relate to titration packages for enabling compliance with a regimen of changing dosage of a medication over a period of time for the treatment of primary biliary cholangitis (PBC).

Compounds and methods for treatment of primary biliary cholangitis

Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R, R, R, RR, R, Rand Rare as defined herein.

The present invention relates to the GPR119 receptor agonists: 3-fluoro-4-(5-fluoro-6-(4-3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N,N-imethylbenzamide; 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)-N-methylbenzamide; and 3-fluoro-4-(5-fluoro-6-(4-(3-(2-fluoropropan-2-yl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)pyrimidin-4-ylamino)benzamide, and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single pharmaceutical agent or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of, for example, a disorder selected from: a GPRI19-receptor-related disorder; a condition ameliorated by increasing secretion of an incretin; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

Modulators of the GPR119 receptor and the treatment of disorders related thereto

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

Growing community of inventors

San Diego, CA, United States of America

Robert M Jones