Boehringer Ingelheim International Gmbh

Dana-farber-cancer Institute Inc.

Syros Pharmaceuticals, Inc.

Patrick Deroy

Christiane Yoakim

Bruno Simoneau

Alexandre Gagnon

Martin Duplessis

Anne-Marie Faucher

Sebastien Morin

Clint A James

Claudio F Sturino

Bounkham Thavonekham

Jeffrey O'Meara

Serge R Landry

Jean-Eric Lacoste

Louis Morency

Martin Tremblay

Joannie Minville

Nathanael Schiander Gray

Tinghu Zhang

M Arshad Siddiqui

Pierre Louis Beaulieu

Stephane Ciblat

Teddy Halmos

Joel D Moore

Kevin Sprott

Jason J Marineau

Darby Schmidt

Nathanael S Gray

Michael Bradley

Anzhelika Kabro

Paul John Edwards

Sylvie Goulet

Melissa Leblanc

Stephanie Roy

Dana K Winter

Tom Miller

Serge Leger

Oliver Hucke

Eric Malenfant

Sébastien Morin

Simon Suprenant

Christopher Lemke

Pierre Bonneau

Jeffrey O′Meara

Claudio Sturino

Paul J Edwards

The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. 

Heteroaromatic compounds useful for the treatment of proliferative diseases

Compounds of formula (I) and pharmaceutical compositions thereof: wherein AAand Aare each independently selected from the group consisting of N and CR, wherein Ris an optionally substituted heterocyclyl or an optionally substituted &#x2014;(C)alkyl-heterocyclyl, Ris an optionally substituted aryl or an optionally subsisted heteroaryl, Ris an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inhibitor of HIV replication. 

Inhibitors of HIV replication

Compounds of formula (I): wherein R, R, A, A, A, A, X and Y are as defined herein, are useful as inhibitors of HIV replication.

Compounds of formula (I): wherein Ar, X, R, R, Rand Rare as defined herein. The compounds are useful as reverse transcriptase inhibitors against wild type and single or double mutant strains of HIV.

Non-nucleoside reverse transcriptase inhibitors

The present invention relates to compounds of formula (I) wherein R, R, Rand Rare as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of HIV replication, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HIV infection. 

Non nucleoside reverse transcriptase inhibitors

Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table 

Alkynyl compounds as non nucleoside reverse transcriptase inhibitors

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Blainville, Canada

Patrick Deroy