Syros Pharmaceuticals, Inc.

Bantam Pharmaceutical, LLC

Dana-farber-cancer Institute Inc.

Bellus Health Inc.

Pyramid Biosciences, Inc

Oric Pharmaceuticals, Inc.

Bhi Limited Partnership

Other

Aduro Biotech Inc.

Biohaven Therapeutics Ltd.

Stephane Ciblat

Nathanael Schiander Gray

Robert Zahler

Jason J Marineau

Kevin Sprott

Anzhelika Kabro

M Arshad Siddiqui

Michael Bradley

Darby Schmidt

Melissa Leblanc

Stephanie Roy

Dana K Winter

Xianqi Kong

Lea Constantineau-Forget

Dansu Li

Amy Ripka

Yi Zhang

Abderrahim Bouzide

Claudio Edmundo Chuaqui

Alan B Cooper

Daniel Delorme

David Migneault

Xinfu Wu

Benoit Bachand

Robin Larouche-Gauthier

Sophie Levesque

Chantal Grand-Maitre

Francis Beaumier

Luce Lépissier

Isabelle Valade

Gerald W Shipps

Tinghu Zhang

Joel D Moore

Kollol Pal

Peter B Rahl

Xiaohui Du

F Anthony Romero

Paul Gibbons

Jared Moore

Kejia Wu

Hiroyuki Kawai

Chudi Obioma Ndubaku

Richard Frenette

Clint A James

Matthew J Kostura

Yeeman K Ramtohul

Franck Raeppel

Nathanael S Gray

Tom Miller

Serge Leger

Nicolas Bruneau-Latour

Mohamed Atfani

Lauren Berstler

Christopher Roberts

Boubacar Sow

Martin Dery

Vincent Albert

Vu Linh Ly

Xiangyu Guo

Sanjay Srivastava

Jonathan Boudreault

Joanne Tan

Michael Luther

Guoli Zhang

Amit Nayyar

Jedd Levine

Nigel Levens

Jae Hyuk Chang

Chudi Ndubaku

Hong Wang

Henri Piras

Dilan Emine Polat

Kenneth Matthew Whitmore

Hugo De Almeida Silva

Daniel Gordon Michael Shore

Kate-Lyn Lund

Vibha Oza

David C Moebius

Huiping Amy Guan

Leonard Sung

Arshad Siddiqui

Patrick Deroy

Serge Lamothe

Goran Malojcic

George Edwin Katibah

William Sinko

Mariam Zaky

Sylvain Bernard

Tucker Curran Roberts

Taras Rybak

Laura Gillard

Hossein Ismaili

Mohammed Atfani

Johanne Renaud

Amandine Xolin

Malay Doshi

Arshad M Siddiqui

Matthew W Kostura

Peter B Rahi

The application relates to pyrazolo[1,5-a]pyrimidine derivatives of formula (IV) as Trk kinase inhibitors for treating cancer and inflammatory diseases.

5-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-(1H-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine derivatives and related compounds as Trk kinase inhibitors for treating cancer

Disclosed herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, that are inhibitors of Polo Like Kinase 4 (PLK4). Also disclosed herein are pharmaceutical compositions comprising the compounds of Formula (I), or pharmaceutically acceptable salts thereof, and one or more pharmaceutically acceptable excipients. Further disclosed herein are methods of treating cancer in a subject in need thereof, comprising administering to the subject an amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

Polo like kinase 4 inhibitors

The present invention provides various compositions, including compounds of Formula (I) or (Ia), or a species thereof, and pharmaceutically acceptable salts, solvates (e.g., hydrates), stereoisomer, tautomers, isotopic and other specified forms thereof. Also provided are methods (or uses) and kits involving the compounds or pharmaceutically acceptable compositions containing them for treating or preventing a disease (e.g., a proliferative disease such as cancer) in a subject. Administration of a compound or pharmaceutical composition described herein is expected to inhibit cyclin-dependent kinase 7 (CDK7), and thereby, induce apoptosis in tumor cells in the subject.

Inhibitors of cyclin-dependent kinase 7 (CDK7)

Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X, X, Z, Z, the ring system denoted by 'a', R, L, L, Q, L, R, L, R, L, and Rare as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.

Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases

The present invention provides, inter alia, compounds having the structures of formulas described herein; pharmaceutically acceptable salts, solvates, hydrates, tautomers, and isotopic forms thereof; and compositions (e.g., pharmaceutical compositions and kits) containing one or more of the foregoing. Also provided are methods of administering and uses involving the compounds and/or pharmaceutical compositions for treating or preventing disease. The disease can be a proliferative disease, such as a cancer (e.g., a blood cancer (e.g., a leukemia or lymphoma), a brain cancer, a breast cancer, melanoma, multiple myeloma, or an ovarian cancer) a benign neoplasm, pathologic angiogenesis, or a fibrotic disease. While no aspect of the invention is limited by the biological events that may transpire, administering a compound or other composition described herein may selectively inhibit the aberrant expression or activity of cyclin-dependent kinase 7 (CDK7) and, thereby, induce cellular apoptosis and/or inhibit the transcription of disease-related genes in the patient (or in a biological sample).

Inhibitors of cyclin dependent kinase 7 (CDK7)

The present invention provides novel compounds of Formulas (I) and (II) 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., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject.

Compounds for the modulation of Myc activity

5-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-(1H-pyrazol-1-yl)pyrazolo [1,5-A]pyrimidine derivatives and related compounds as Trk kinase inhibitors for treating cancer

Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts and N-oxides thereof, wherein X, X, Z, Z, the ring system denoted by 'a', R, A, L, A, L, L, Q, L, R, A, L, A, L, R, L, and Rare as described herein. In certain embodiments, compounds disclosed herein disrupt the eIF4E/eiF4G interaction, and can be used to treat hyperproliferative disorder, a neurological disease or disorder, or autism.

Substituted pyrazole and pyrrole compounds and methods for using them for inhibition of initiation of translation and treatment of diseases and disorders relating thereto

Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formulae (Ia), (Ib), (Ic), (Id) and (Ie), in which R, L, L, Q, L, R, L, R, L, and Rare as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene. 

Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases

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., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angiogenesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject. 

Compounds for the modulation of MYC activity

The application relates to inhibitors of Trk kinases useful in the treatment of Trk kinase associated diseases and disorders, having the Formula: wherein A, L, X, X, and Y are described herein.

5-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-(1h-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine derivatives and related compounds as Trk kinase inhibitors for treating cancer

The present invention provides novel compounds of Formulas (I) and (II) 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., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject. 

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

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Montreal, Canada

Stephane Ciblat