Amira Pharmaceuticals, Inc.

Merck + Co., Inc.

Panmira Pharmaceuticals, LLC

Merck Sharp + Dohme Corp.

Bristol-Myers Squibb Compnay

Yale University

Orion Ophthalmology LLC

Brickell Biotech, Inc.

Jeffrey Roger Roppe

John Howard Hutchinson

Thomas Jon Seiders

Jeannie M Arruda

Bowei Wang

Nicholas Simon Stock

Timothy Andrew Parr

Nicholas D Smith

Brian Andrew Stearns

Dehua Huang

Deborah Volkots

Lida R Tehrani

Nicholas D P Cosford

Nicholas David Cosford

Brian Walter Eastman

Steve Fong Poon

Jean-Michel Andre Vernier

Joseph E Payne

Yen Truong

Petpiboon Peppi Prasit

Jill Melissa Scott

Xiumin Zhao

Chris King

Mustapha Haddach

Thomas S Reger

Chixu Chen

Mark Moran

Jillian Frances Evans

Yiwei Li

Jasmine Eleanor Zunic

Austin Chih-Yu Chen

David J Donnelly

Renata Marcella Oballa

David Andrew Powell

Robert Gomez

Samuel J Bonacorsi, Jr

Tao Sheng

Joonyoung Kim

Adrienne Pena

Tritin Tran

Richard E Carson

Nabeel Nabulsi

Yiyun Huang

Kai Cao

Jean-Dominique Gallezot

Yen Pham Truong

Nicholas D Cosford

Timothy Parr

Steven F Poon

This invention is directed to novel aliphatic prolinamide derivatives of Formula I, and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention. The compounds of the invention are inhibitors of HTRA1. Thus, the compounds of the invention are useful in the prevention and treatment of a wide range of diseases mediated (in whole or in part) by HTRA1. The compounds of the invention are also useful for inhibiting HTRA1 protease activity in an eye or locus of an arthritis or related condition. 

Aliphatic prolinamide derivatives

The present invention relates to radiolabeled LPA1 receptor antagonists or pharmaceutically acceptable salts thereof which are useful for the quantitative imaging of LPA1 receptors in mammals.

Radioligands for imaging the LPA-1 receptor

Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.

Autotaxin inhibitors and uses thereof

Heterocyclic autotaxin inhibitors and uses thereof

The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.

Thiazolyl mGluR5 antagonists and methods for their use

Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

Lysophosphatidic acid receptor antagonists

Described herein are antagonists of PGDreceptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGDreceptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD-dependent or PGD-mediated conditions or diseases.

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Antagonists of lysophosphatidic acid receptors

Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.

5-lipoxygenase-activating protein (FLAP) inhibitors

Described herein are heteroaryl compounds that are antagonists of PGDreceptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGDreceptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD-dependent or PGD-mediated conditions or diseases.

Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Described herein are compounds that are antagonists of PGDreceptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGDreceptors. Also described herein are methods of using such antagonists of PGDreceptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD-dependent or PGD-mediated conditions or diseases.

N,N-disubstituted aminoalkylbiphenyl antagonists of prostaglandin D2 receptors

Polycyclic antagonists of lysophosphatidic acid receptors

Growing community of inventors

Temecula, CA, United States of America

Jeffrey Roger Roppe