Venenum Biodesign, LLC

Schering Corporation

Pharmacopeia Inc.

Merck Sharp + Dohme Corp.

Cephalon, Inc.

Pharmacopeia Drug Discovery, Inc.

Schering-plough Corporation

Scheeing Corporation

Chia-Yu Huang

Robert G Aslanian

Kevin D McCormick

Christopher W Boyce

Pietro Mangiaracina

Bo Liang

Neng-Yang Shih

Younong Yu

Brian F McGuinness

Manuel De Lera Ruiz

Jeffrey John Letourneau

Rong-qiang Liu

Lisa Guise-Zawacki

John J Baldwin

Viyyoor Moopil Girijavallabhan

Ronald J Doll

Ge Li

Alan B Cooper

Junying Zheng

Salem Fevrier

Ruiyan Liu

Steven G Kultgen

Venugopalareddy Bommireddy Venkata

Kiruthika Selvarangan Elamparuthi

James R Beasley

Ashit K Ganguly

F George Njoroge

Arthur G Taveras

Robert L Hudkins

Edward R Bacon

Timothy J Guzi

Tao Guo

Michael Berlin

Allison L Zulli

Philip D Stein

Purakkattle J Biju

Dinanath F Rane

Patrick A Pinto

Ming Tao

Nadine C Becknell

Kartik M Keertikar

Carmen S Alvarez

Steven David Paget

Reddeppa Reddy Dandu

Ray Anthony James

David J Diller

Jagdish A Desai

Jianping Chao

Bancha Vibulbhan

James J-s Wang

Hugh Y Zhu

Axel Metzger

Babu G Sundar

Huagang Lu

Johan A Ferreira

Dongchuan Shi

Keith P Minor

Bama Santhanam

Audrey Hospital

Andrew G Cole

Minglang Wu

Reddeppareddy Dandu

Xiaoqing Xu

David E Kaelin, Jr

William Ronald Solvibile, Jr

Ellen Sieber McMaster

Stephanie Louise Ciesla

Brian F Mcguiness

Audrey Julie Hospital

Pietro Mangiarcina

The present invention provides compounds of Formula I: wherein X, R, R, Rand Rare as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.

Substituted pyrrolo[1,2-a]pyrazines and pyrrolo[1,2-a][1,4]diazepines as TREX1 inhibitors

The present invention provides compounds of Formula I wherein X, R, R, Rand Rare as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.

The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs. 

Non-systemic TGR5 agonists

The present invention provides compounds of Formula I': wherein, W, X, Y, Z, Z, Z, R, R, R, Rand Rare as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

Sting agonists

The present invention relates to tricyclic compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present tricyclic compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing tricyclic compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs.

The present invention provides compounds of Formula (I): their use as Hantagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.

Substituted spirocyclic piperidine derivatives as histamine-3 (H3) receptor ligands

In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of &#xff;2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the &#xff;2C adrenergic receptors using such compounds or pharmaceutical compositions.

Functionally selective alpha2C adrenoreceptor agonists

In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as &#x3b1;2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the &#x3b1;2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

ALPHA2C adrenoreceptor agonists

In its many embodiments, the present invention provides a novel class of indolines as inhibitors of &#x3b1;2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the &#x3b1;2C adrenergic receptors using such compounds or pharmaceutical compositions.

&#x3b1;2C adrenoreceptor agonists

Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

Farnesyl protein transferase inhibitors as antitumor agents

Novel compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel aminooxyamide compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.

Inhibitors of farnesyl-protein transferase

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Princeton Junction, NJ, United States of America

Chia-Yu Huang