Enanta Pharmaceuticals, Inc.

Ironwood Pharmaceuticals, Inc.

Dana-farber-cancer Institute Inc.

Cyclerion Therapeutics, Inc.

Syros Pharmaceuticals, Inc.

Joel D Moore

Takashi Nakai

Yat Sun Or

Zhe Wang

Nicholas Robert Perl

Rajesh R Iyengar

Ara Mermerian

Thomas Wai-Ho Lee

G-Yoon Jamie Im

Paul A Renhowe

Timothy Claude Barden

Colleen Hudson

Mark G Currie

Xiang Y Yu

Glen Robert Rennie

James Edward Sheppeck

Joon Jung

Dong Liu

Karthik Iyer

Kimberly Kafadar Long

George Todd Milne

Deqiang Niu

Yonghua Gai

Charles Kim

James Jia

Guoyou Xu

Datong Tang

Angelika Fretzen

Kevin Sprott

Jason Matthew Rohde

Nathanael Schiander Gray

Tinghu Zhang

M Arshad Siddiqui

Ying Sun

Stephane Ciblat

Jason J Marineau

Darby Schmidt

Michael Bradley

Anzhelika Kabro

Melissa Leblanc

Tom Miller

Stephanie Roy

Dana K Winter

Lei Jia

Nathanael S Gray

Eric L Elliott

Daniel P Zimmer

Zhigang Chen

Patrick Deroy

Serge Leger

Bo Peng

Wilmin Bartolini

Regina Graul

Mark Currie

Paul Allen Renhowe

Paul Allan Renhowe

Compounds of Formulae I' and I are described, which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed. 

sGC stimulators

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)

Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed. 

SGC stimulators

The present patent application discloses at least the compounds according to Formula I or Formula Ib shown below, or pharmaceutically acceptable salts thereof, 

Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.

2-benzyl, 3-(pyrimidin-2-yl) substituted pyrazoles useful as sGC stimulators

Compounds of Formula IA and Formula IB are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed. 

The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.

Quinoxalinyl derivatives

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Somerville, MA, United States of America

Joel D Moore