Global Blood Therapeutics, Inc.

Novartis Ag

Lina Quattrocchio Setti

Zhe Li

Yan Lou

Savithri Ramurthy

Matthew T Burger

Ming Yu

Benjamin R Taft

Gisele A Nishiguchi

Alice C Rico

Hing L Sham

Qing Xu

Aaron Matthew Smith

Sharadha Subramanian

Paul Andrew Barsanti

Calvin Wesley Yee

Lifeng Wan

Naeem Yusuff

Huw Roland Tanner

Robert John Aversa

Valery Rostislavovich Polyakov

Cheng Hu

Yue Pan

Manuel Zancanella

Chul Yu

Alan Dipesa

Brian Walter Metcalf

Martin Sendzik

Stephen L Gwaltney, Ii

Vivek Rauniyar

Shahul Nilar

Huw Rowland Tanner

Thomas A Dineen, Jr

Steven Richards

Matthew A Lardy

Alan DiPesa

Thomas A Dineen Jr

The present disclosure provides tricyclic compounds of formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. 

Tricyclic compounds as histone methyltransferase inhibitors

The subject matter described herein is directed to pyruvate kinase activating compounds of Formula I: and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for the treatment of diseases associated with PKR and/or PKM2, such as pyruvate kinase deficiency, sickle cell disease, and beta-thalassemia.

Substituted 2,6-dihydropyrrolo[3,4-c]pyrazoles as pyruvate kinase activators

The present disclosure provides certain compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinpathies such as beta-thalassemia and sickle cell disease. Also provided are pharmaceutical compositions containing such compounds as well as processes and intermediates for preparing such compounds.

Histone methyltransferase inhibitors

The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.

Biaryl amide compounds as kinase inhibitors

The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent. 

The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent. 

Compounds and compositions as RAF kinase inhibitors

Provided herein are kallikrein modulating compounds, pharmaceutical compositions comprising the same, and uses thereof.

Bridged bicyclic kallikrein inhibitors

In one aspect this invention relates generally to compounds of Formula: and sub-formulas thereof, or a tautomer of each thereof, a pharmaceutically acceptable salt of each thereof, or a pharmaceutically acceptable solvate of each of the foregoing, where X, L, L, and Rare described herein.

Pyrazolopyridine pyrazolopyrimidine and related compounds

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Fremont, CA, United States of America

Lina Quattrocchio Setti