Glaxosmithkline Intellectual Property (no.2) Limited

Glaxosmithkline Intellectual Property Development Limited

Glaxosmithkline LLC

Guosen Ye

Carl A Brooks

Hilary Schenck Eidam

Mark A Hilfiker

Jaclyn R Patterson

Mui Cheung

Brian Griffin Lawhorn

Edward J Brnardic

Marlys Hammond

Patrick Stoy

Krista B Goodman

Robert Sanchez

Joseph E Pero

Brian W Budzik

Ryan Michael Fox

Matthew Robert Sender

Jay M Matthews

John Jeffrey McAtee

Yue Li

David J Behm

Lamont Roscoe Terrell

Tram H Hoang

James V Thomas

Linda S Barton

Rodolfo Cadilla

Joshi M Ramanjulu

Joseph J Romano

Gren Z Wang

Adam Kenneth Charnley

John F Mehlmann

Lara Kallander

Yiqian Lian

Xiaoyang Dong

Jianxing Kang

Terry V Hughes

Lara Kathryn Leister

Daohua Zhang

Michael Jonathan Bury

Barry George Shearer

David G Washburn

Eric Steven Manas

Christie Schulte

Jason W Dodson

Joanne Philp

Neysa Nevins

Michael G Darcy

Yu Guo

Sharada Manns

Millard Hurst Lambert, Iii

Jon Collins

Huichang Zhang

Daniel Paone

Huijie Li

Anthony Handlon

Maben Ying

Sarah E Dowdell

Mark Elban

Brandon Turunen

Craig Leach

Yuehu Li

Peiling Chen

Cunyu Zhang

Beth A Knapp-reed

Joseph Paul Marino Jr

Hilary S Eidam

Eric S Manas

This invention relates to novel compounds according to Formula (I) which are antagonists of MrgX2, to pharmaceutical compositions containing them, and to their use in therapy for the treatment of MrgX2-mediated diseases and disorders.

MrgX2 antagonists

Disclosed are compounds having the formula:

Heterocyclic amides useful as protein modulators

The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

TRPV4 antagonists

The present invention relates to a novel compound useful as a TRPV4 antagonist, specifically the compound 1-(((5S,7R)-3-(5-cyclopropylpyrazin-2-yl)-7-hydroxy-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl)methyl)-1H-benzo[d]imidazole-6-carbonitrile, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compound. The compound of the invention can be useful in the treatment of a disease state selected from: atherosclerosis, disorders related to vasogenic edema, postsurgical abdominal edema, ocular edema, cerebral edema, local and systemic edema, fluid retention, sepsis, hypertension, inflammation, bone related dysfunctions and congestive heart failure, pulmonary disorders, chronic obstructive pulmonary disorder, ventilator induced lung injury, high altitude induced pulmonary edema, acute respiratory distress syndrome, acute lung injury, pulmonary fibrosis, sinusitis/rhinitis, asthma, cough; including acute cough, sub-acute cough and chronic cough, pulmonary hypertension, overactive bladder, cystitis, pain, motor neuron disorders, genetic gain of function disorders, cardiovascular disease, renal dysfunction, stroke, glaucoma, retinopathy, endometriosis, pre-term labor, dermatitis, pruritus, pruritus in liver disease, diabetes, metabolic disorder, obesity, migraine, pancreatitis, tumor suppression, immunosuppression, osteoarthritis, crohn's disease, colitis, diarrhea, intestinal irregularity (hyperreactivity/hyporeactivity), fecal incontinence, irritable bowel syndrome (IBS), constipation, intestinal pain and cramping, celiac disease, lactose intolerance, and flatulence.

TRPV4 antagonist

Disclosed are compounds having the formula: wherein R1, R2 and R3 are as defined herein, and methods of making and using the same, including use as inhibitors of BMP1, TLL1 and/or TLL2 and in treatment of diseases associated with BMP1, TLL1 and/or TLL2 activity.

Hydroxy formamide derivatives and their use

The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.

The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

Growing community of inventors

King of Prussia, PA, United States of America

Guosen Ye