Heteroaromatic compounds useful for the treatment of prolferative diseases

a technology of heteroaromatic compounds and prolferative diseases, applied in the direction of drug compositions, organic chemistry, organic active ingredients, etc., can solve the problems of hampered discovery of selective inhibitors of cdk7 and anti-proliferative activity
US20160264551A1Inactive Publication Date: 2016-09-15SYROS PHARMACEUTICALIS INC +1
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Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
SYROS PHARMACEUTICALIS INC
Publication Date
2016-09-15
Estimated Expiration
Not applicable · inactive patent

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Abstract

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, in duce cellular apoptosis and / or inhibit transcription in the subject.
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Description

BACKGROUND OF THE INVENTION

[0001] The members of the cyclin-dependent kinase (CDK) family play critical regulatory roles in proliferation. Unique among the mammalian CDKs, CDK7 has consolidated kinase activities, regulating both the cell cycle and transcription. In the cytosol, CDK7 exists as a heterotrimeric complex and is believed to function as a CDK1 / 2-activating kinase (CAK), whereby phosphorylation of conserved residues in CDK1 / 2 by CDK7 is required for full catalytic CDK activity and cell cycle progression. In the nucleus, CDK7 forms the kinase core of the RNA polymerase (RNAP) II general transcription factor complex and is charged with phosphorylating the C-terminal domain (CTD) of RNAP II, a requisite step in gene transcriptional initiation Together, the two functions of CDK7, i.e., CAK and CTD phosphorylation, support critical facets of cellular proliferation, cell cycling, and transcription.

[0002] Disruption of RNAP II CTD phosphorylation has been shown to preferentially af...

Claims

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