Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)

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 inventiv...

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Hauptverfasser: Siddiqui, M. Arshad, Schmidt, Darby, Miller, Tom, Marineau, Jason J, Leblanc, Melissa, Gray, Nathanael, Sprott, Kevin, Bradley, Michael, Roy, Stephanie, Ciblat, Stephane, Zhang, Tinghu, Winter, Dana K, Moore, Joel, Kabro, Anzhelika
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creator Siddiqui, M. Arshad
Schmidt, Darby
Miller, Tom
Marineau, Jason J
Leblanc, Melissa
Gray, Nathanael
Sprott, Kevin
Bradley, Michael
Roy, Stephanie
Ciblat, Stephane
Zhang, Tinghu
Winter, Dana K
Moore, Joel
Kabro, Anzhelika
description 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.
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subjects ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
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