Merck Sharp + Dohme Corp.

Jiangsu Hengrui Medicine Company Ltd.

Shanghai Hengrui Pharmaceutical Co., Ltd.

Albany Molecular Research, Inc.

Heping Wu

Rongze Kuang

Amjad Ali

Pauline C Ting

Yeon-Hee Lim

Andrew William Stamford

Younong Yu

Michael Man-Chu Lo

Scott D Edmondson

Paul Tempest

Weiguo Liu

Nicolas Zorn

Sung-Sau So

Xianhai Huang

Dong Xiao

Michael Berlin

Zhuyan Guo

Ying-Duo Gao

Anthony K Ogawa

Rajan Anand

Timothy J Henderson

Qiaolin Deng

Robert G Aslanian

Christopher W Boyce

Santhosh Francis Neelamkavil

Wanying Sun

Tao Yu

Yu Jiang

Manuel De Lera Ruiz

Eric Mertz

Junying Zheng

Jayaram R Tagat

Feng He

Linghang Zhuang

Weikang Tao

Kevin D McCormick

Joseph Michael Kelly

Jian Liu

Purakkattle J Biju

Tin-Yau Chan

Alan W Hruza

Blaise S Lippa

Gang Zhou

Jae-Hun Kim

Edward Metzger

Jianhua Cao

Gioconda V Gallo

Walter Won

Joe F Lee

David Kim

Robert Jason Herr

Linda Brockunier

Wei Zhou

Tanweer A Khan

Rumin Zhang

Yonglian Zhang

Joseph Leslie Duffy

Jiayi Xu

Nancy J Kevin

Brent Whitehead

Tingting Yu

Deyou Sha

Chunsing Li

Xiaohong Zhu

Jan Antoinette C Romero

Yi Zang

Mary Ann Caplen

John H Schwerdt

Zahid Hussain

Jiafang He

Hongwu Wang

Hyunjin M Kim

Remond Moningka

Rudrajit Mal

Sylvia Joanna Degrado

Jie Wu

Suxing Liu

Liwu Hong

Anjan Chakrabarti

Gioconda V Gallo-Etienne

Jinhai Yang

Hiroki Sone

Jon Christian Baber

Puneet Kumar

David Won-Shik Kim

Andrew John Zych

Joseph L Duffy

Jing Zhang

Alexander L Tung

Dong Won-Shik Kim

Yushi Xiao

Ali Amjad

Andrew F Nolting

Bhuamik Pandya

Xin Zhang

Linda L Brockunier

This application discloses CD73 inhibitors represented by the general formula (I) and analogs thereof, pharmaceutical compositions containing these compounds, methods of preparing them, and use of these compounds as therapeutic agents for the treatment of diseases or conditions associated with CD73 activity, such as various cancers. 

CD73 inhibitors and therapeutic uses thereof

The present invention is directed to 2,2-difluorodioxolo compounds that are antagonists of Areceptor. The present invention is also directed to uses of the 2,2-difluorodioxolo compounds described herein in the potential treatment or prevention of neurological disorders and diseases in which Areceptor are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds and to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which Areceptors are involved.

2,2-difluorodioxolo Areceptor antagonists

The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A-receptor is involved. The invention further involves use of the compounds as an A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases. 

Substituted aminoquinazoline compounds as Aantagonist

Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein 'R', 'R', &#x201c;R&#x201d;, &#x201c;R&#x201d;, and &#x201c;Het&#x201d; are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease. 

Aminopyrazine compounds with A2A antagonist properties

The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. 

[object Object]

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more compounds of Formula (I), and methods for using the compounds of Formula (I) for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

Factor XIa inhibitors

The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 

Disclosed are compounds of Formula G1: where 'R'. 'R' to &#x201c;R&#x201d;, &#x201c;n&#x201d;, &#x201c;m&#x201d;, &#x201c;p&#x201d;, &#x201c;W&#x201d;, &#x201c;X&#x201d;, &#x201c;Y&#x201d;, and &#x201c;Z&#x201d; are defined herein, which compounds are antagonists of Areceptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which Areceptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Heterobicyclo-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A anatagonist properties

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 

The present invention provides a compound of Formula I (The chemical formula should be inserted here.) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 

Factor Xla inhibitors

Disclosed are compounds of Formula A: (structurally represented) where 'RG1', 'RG2a', &#x201c;RG4&#x201d;, &#x201c;RG5&#x201d;, &#x201c;MG1&#x201d;, &#x201c;n&#x201d; and &#x201c;m&#x201d; are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions. 

The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ('DGAT') inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: 

Inhibitors of diacylglycerol acyltransferase

Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.

Pyridazinone derivatives useful as glucan synthase inhibitors

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Edison, NJ, United States of America

Heping Wu