Genentech, Inc.

Gilead Connecticut, Inc.

Isis Pharmaceuticals, Inc.

F. Hoffmann-la Roche Ag

Genetech, Inc.

Inotek Pharmaceuticals Corporation

Cgi Pharmaceuticals, Inc.

Ionis Pharmaceuticals, Inc.

Xiaojing Wang

Daniel Fred Ortwine

Jun Liang

Kevin S Currie

Jason R Zbieg

Nicholas Charles Ray

Wendy B Young

Sharada Shenvi Labadie

Birong Zhang

Simon Charles Goodacre

Eric E Swayze

Richard Holmes Griffey

Scott A Mitchell

Peter A Blomgren

Jeffrey E Kropf

Jianjun Xu

Seung H Lee

Zhongdong Zhao

Aaron C Schmitt

Michael T Migawa

Pavel E Zhichkin

Andrew Sharpe

Minghua Sun

Vickie H Tsui

Alastair James Hodges

Antonio J M Barbosa

Honglu Zhang

Ravi Krishnamoorthy

Steven Huy Do

Aleksandr Kolesnikov

Stephen Hanessian

Jun M Li

Susanta Sekhar Adhikari

Huiyong Hu

Janek Szychowski

Kandasamy Pachamuthu

Tao Wang

Nicholas D Smith

Mehmet Kahraman

Steven P Govek

Wendy Lee

Wesley Peter Blackaby

Johnny Yasuo Nagasawa

Jason Burch

Zhaoyang Wen

Mizio Matteucci

Antonio J Barbosa

Jiangpeng Liao

Bing-Yan Zhu

Huifen Chen

Allen J Ebens

Prakash Jagtap

Frederick Cohen

Georgette M Castanedo

Vickie Hsiao-Wei Tsui

David R Brittelli

Andiliy Gokching Lai

Robin Larouche-Gauthier

Zhiguo Liu

Malcolm Huestis

John Wai

Jason David Burch

Jun Li

Lisa Marie Barton

Ciara Metcalfe

Tommy Lai

Duy-Phong Pham-Huu

Wei Zhou

Michael John Lambrecht

Araz Jakalian

Fabio Broccatelli

Man Un Ung

Arun Yadav

Maia Vinogradova

Jason Zbieg

John Sui-Man Wai

Kwong Wah Lai

Jr Allen J Ebens

Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure:

Tetrahydro-pyrido[3,4-b]indole estrogen receptor modulators and uses thereof

A compound, of formula (I): suitable for treating a cancer wherein the cancer is susceptible to inhibition of Cbl-B.

Lactams as CBL-B inhibitors selective over C-CBL

Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure:  and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: and

Heteroaryl estrogen receptor modulators and uses thereof

Described herein are tetrahydronaphthalene compounds with estrogen receptor modulation activity or function having the Formula I structure: 

Tetrahydronaphthalene estrogen receptor modulators and uses thereof

Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Pyridone and aza-pyridone compounds and methods of use

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

Heterocyclic estrogen receptor modulators and uses thereof

Described herein are tetrahydro-pyrido[3,4-b]indol-1-yl compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Described herein are tetrahydroisoquinoline compounds with estrogen receptor modulation activity or function having the Formula I structure: 

Tetrahydroisoquinoline estrogen receptor modulators and uses thereof

Oxepan-2-yl pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Oxepan-2-yl-pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use

Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein Ris a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use

Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein Rand Rare as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Pyrazolo[3,4-c]pyridine compounds and methods of use

Described herein are compounds that are estrogen receptor modulators of Formula (I): 

Estrogen receptor modulators and uses thereof

Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use

Growing community of inventors

Foster City, CA, United States of America

Xiaojing Wang