Schering Corporation

Merck Sharp + Dohme Corp.

Syros Pharmaceuticals, Inc.

Dana-farber-cancer Institute Inc.

Bantam Pharmaceutical, LLC

Other

M Arshad Siddiqui

Dansu Li

Lianyun Zhao

Neng-Yang Shih

Janeta Popovici-Muller

Joseph A Kozlowski

Wensheng Yu

Brian J Lavey

Vinay M Girijavallabhan

Guowei Zhou

Ling Tong

Gerald Wayne Shipps, Jr

Stephane Ciblat

Michael K C Wong

De-Yi Yang

Vincent Stewart Madison

Bandarpalle B Shankar

Umar Faruk Mansoor

Timothy J Guzi

Seong Heon Kim

Kevin Sprott

Jason J Marineau

Lei Chen

Darby Schmidt

Yongqi Deng

Alan B Cooper

Zhuyan Guo

Peter Orth

Amy Ripka

Nathanael Schiander Gray

Michael P Dwyer

Kamil Paruch

Tinghu Zhang

Joel D Moore

Alan W Hruza

Thierry Olivier Fischmann

Ronald J Doll

Joseph Michael Kelly

Sunil Paliwal

Li Xiao

Zhaoning Zhu

Brian Alexander McKittrick

Pauline C Ting

Robert D Mazzola, Jr

Tin-Yau Chan

Tong Wang

Chaoyang Dai

Panduranga Adulla P Reddy

Kristin E Rosner

Razia Rizvi

Anzhelika Kabro

Patrick J Curran

Melissa Leblanc

Stephanie Roy

Dana K Winter

Tom Miller

Panduranga Adulla Reddy

Zhaoyang Meng

Michael Bradley

David Benjamin Belanger

Shuyi Tang

Yang Nan

Duan Liu

Serge Leger

Praveen K Tadikonda

Binyuan Sun

Mehul F Patel

Liping Yang

Hongbo Zeng

Cliff C Cheng

Andrew J McRiner

Jose S Duca

Lea Constantineau-Forget

Chantal Grand-Maitre

Gerald W Shipps

Marc A Labroli

Rumin Zhang

Jagdish A Desai

William T Windsor

Robert Sun

James J-s Wang

Luis E Torres

Hugh Y Zhu

Xiaohua Huang

Youhao Dong

David Parry

Charles W McNemar

Matthew J Kostura

Xiaolei Gao

Kartik M Keertikar

Matthew H Daniels

Hon-Chung Tsui

Nathanael S Gray

Ahmed Abdi Samatar

Sobhana Babu Boga

Henry A Vaccaro

Iwona Wrona

Liang Zhu

Abdul-Basit Alhassan

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., 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

The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), 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), cyclin-dependent kinase 12 (CDK12), or cyclin-dependent kinase 13 (CDK13)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. 

Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)

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 cyclin-dependent kinase (e.g., CDK7), and therefore induce cellular apoptosis and/or inhibit transcription in the subject. 

Inhibitors of cyclin-dependent kinase 7 (CDK7)

Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts and/V-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. 

The present invention provides novel compounds of Formula (I) and Formula (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., 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 cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R, R, R, R, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.

Pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors

The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase. 

Anilinopiperazine derivatives and methods of use thereof

This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.

Fused tricyclic inhibitors of mammalian target of rapamycin

The present invention relates to certain pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine and dipyrazolopyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine or dipyrazolopyrimidine compounds.

Fused tricyclic compounds as mTOR inhibitors

The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.

Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors

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Newton, MA, United States of America

M Arshad Siddiqui