Pfizer Corporation

Janssen Pharmaceutica Nv

Wyeth

Janssen Sciences Ireland Unlimited Company

Zhao-Kui Wan

Eddine Saiah

Li Huang Xing

Qian Liu

Wing Shun Cheung

Ariamala Gopalsamy

Ivan Viktorovich Efremov

John Isidro Trujillo

Liying Zhang

Haibing Guo

Brian Stephen Gerstenberger

Andrew Fensome

Betsy Susan Pierce

Jean-Baptiste Telliez

Jinbo Lee

Steve Yikkai Tam

Luoheng Qin

Balekudru Devadas

Margaret Lanahan Grapperhaus

Susan Landis Hockerman

Shaun Raj Selness

Douglas Wilson

Mark E Schnute

Robert Owen Hughes

Christoph Wolfgang Zapf

Daniel Patrick Walker

Yimin Jiang

Seungil Han

John Robert Springer

Michael J Smith

Kenneth W Foreman

David V Erbe

Liqiang Fu

Xuedong Dai

Michelle Ann Schmidt

Eva Deanna Binnun

Gang Deng

Weixin Xu

Danny James Garland

Pierre Jean-Marie Bernard Raboisson

James Patrick Edwards

Patrick René Angibaud

Abdellah Tahri

Koen Vandyck

Virginie Sophie Poncelet

Wei Li

Olivier Alexis Georges Querolle

Bruce Follows

Tarek Suhayl Mansour

Wei Cai

Yanping Xu

Vineet Pande

Lihren Chen

John C McKew

Yan-Ling Zhang

Jason Shaoyun Xiang

Zhanling Cheng

Daniel Jason Krosky

Aaron Nathaniel Patrick

Yingtao Liu

Diane Marie Joseph-McCarthy

Chao Liang

Steven J Kirincich

Jianchang Li

Huan-Qiu Li

Manus Ipek

Vipin Suri

Yuchuan Wu

Jun-Jun Wu

Barbara Morschhäuser Geb Herkert

Alessandro Fabio Moretto

Linglong Kong

Mark Edward Schnute

Pyrazolopyridinone compounds, the pharmaceutical compositions comprising said compounds, and the use of said compounds as FGFR (fibroblast growth factor receptor) inhibitors and their use in the treatment of diseases, e.g. cancer.

Pyrazolopyridinone compounds

Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject, and the compound has the structure of Formula I including any possible deuterated isomers, stereoisomers or tautomeric forms thereof.

Heteroaryldihydropyrimidine derivatives and methods of treating hepatitis B infections

Provided are compounds of Formula (I), pharmaceutical compositions comprising such compounds, and their use as menin/MLL protein/protein interaction inhibitors, useful for treating diseases such as cancer, myelodysplastic syndrome (MDS) and diabetes. 

Exo-aza spiro inhibitors of menin-MLL interaction

The invention relates to new quinolinone compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds as FGFR (fibroblast growth factor receptor) inhibitors and to their use in the treatment of diseases, e.g. cancer.

Quinolinone compounds

A compound compound having the structure: or a pharmaceutically acceptable salt thereof, wherein X is N or CR, where R is hydrogen, deuterium, C-Calkyl, C-Calkoxy, C-Ccycloalkyl, aryl, heteroaryl, aryl(C-Calkyl), CN, amino, alkylamino, dialkylamino, CF, or hydroxyl; A is selected from the group consisting of a bond, C&#x2550;O, &#x2014;SO&#x2014;, &#x2014;(C&#x2550;O)NR&#x2014;, and &#x2014;(CRR)&#x2014;, where Ris H or C-Calkyl, and Rand Rare independently hydrogen, deuterium, C-Calkyl, C-Ccycloalkyl, aryl, aryl(C-Calkyl), heteroaryl, (C-Calkyl)heteroaryl, etc.; A' is selected from the group consisting of a bond, C&#x2550;O, &#x2014;SO&#x2014;, &#x2014;(C&#x2550;O)NR&#x2032;, &#x2014;NR&#x2032;(C&#x2550;O)&#x2014;, and &#x2014;(CR&#x2032;R&#x2032;)&#x2014;, where R&#x2032; is H or C-Calkyl, and R&#x2032; and R&#x2032; are independently hydrogen, deuterium, C-Calkyl, C-Ccycloalkyl, aryl, aryl(C-Calkyl), heteroaryl, (C-Calkyl)heteroaryl, heteroaryl(C-Calkyl), and heterocyclic(C-Calkyl); Z is &#x2014;(CH)&#x2014; or a bond, where one or more methylene units are optionally substituted by one or more C-Calkyl, CN, OH, methoxy, or halo, and where said alkyl may be substituted by one or more fluorine atoms; Rand R&#x2032; are independently selected from the group consisting of hydrogen, deuterium, C-Calkyl, C-Ccycloalkyl, aryl, heteroaryl, aryl(C-Calkyl), CN, etc., wherein said alkyl, aryl, cycloalkyl, heterocyclic, or heteroaryl is further optionally substituted with one or more substituents selected from the group consisting of C-Calkyl, halo, CN, C-Calkylamino, C-Ccycloalkyl, etc.; Ris selected from the group consisting of hydrogen, deuterium, C-Calkyl, C-Ccycloalkyl, halo, and cyano, where said alkyl may be substituted by one or more fluorine atoms; Ris selected from the group consisting of hydrogen, deuterium, and amino; Ris monocyclic or bicyclic aryl or monocyclic or bicyclic heteroaryl wherein said aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of C-Calkyl, heterocycloalkyl, halo, C-Ccycloalkyl, etc., where said alkyl, cycloalkyl, alkoxy, or heterocycloalkyl may be substituted by one or more C-Calkyl, halo, CN, OH, alkoxy, amino, &#x2014;COH, &#x2014;(CO)NH, &#x2014;(CO)NH(C-Calkyl), or &#x2014;(CO)N(C-Calkyl), and where said alkyl may be further substituted by one or more fluorine atoms; Ris independently selected from the group consisting of hydrogen, C-Calkyl, C-Calkoxy, and hydroxyl; h is 1, 2 or 3; j and k are independently 0, 1, 2, or 3; m and n are independently 0, 1 or 2; and, q is 0, 1 or 2. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

Aminopyrimidinyl compounds

The application describes dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.

Substituted 1,4-dihydropyrimidines for the treatment of HBV infection or HBV-induced diseases

A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C&#x2550;O, &#x2014;SO&#x2014;, etc.; A' is selected from the group consisting of a bond, C&#x2550;O, etc.; Z is &#x2014;(CH)&#x2014; or a bond, etc.; Rand Rare independently selected from the group consisting of hydrogen, alkyl, etc.; Ris selected from hydrogen, alkyl, etc.; Ris selected from the group consisting of hydrogen, and amino; Ris monocyclic or bicyclic, etc.; Ris independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. (Formula I) 

Bruton's tyrosine kinase inhibitors

Potent 5-HT2B antagonist of Formula (A), including stereochemically isomeric forms, and salts, hydrates, solvates thereof and their use wherein R1 to R4 and Ar have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them, alone or in combination with other drugs, in fibrosis and/or cirrhosis prevention or therapy. 

Sulphamoylaryl derivatives and use thereof as medicaments for the treatment of liver fibrosis

A compound having the structure: or an acceptable salt thereof, wherein X is N or CR, where R is hydrogen, alkyl, etc.; A is selected from the group consisting of a bond, C&#x2550;O, &#x2014;SO&#x2014;, etc.; A' is selected from the group consisting of a bond, C&#x2550;O, etc.; Z is &#x2014;(CH)&#x2014; or a bond, etc.; Rand R&#x2032; are independently selected from the group consisting of hydrogen, alkyl, etc.; Ris selected from hydrogen, alkyl, etc.; Ris selected from the group consisting of hydrogen, and amino; Ris monocyclic or bicyclic, etc.; Ris independently selected from hydrogen, alkyl, etc.; h, j, k, m, n and q are integers as defined in the specification. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations with other therapeutic agents.

Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (BTK). Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the BTK inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseeases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. 

This invention relates to modulating (e.g., inhibiting) protein tyrosine phosphatase 1B (PTP1B).

PTP1b inhibitors

This invention relates to inhibiting 11&#x3b2;HSD1.

11-beta HSD1 inhibitors

Growing community of inventors

Lexington, MA, United States of America

Zhao-Kui Wan