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US 11,028,079 B2Granted
Small molecule BET bromodomain inhibitors and uses thereof
AssigneesConverGene LLC, The United States of America, as represented by the Secretary, Department of Health and Human Services
InventorsJeffrey William Strovel, Makoto Yoshioka, David J. Maloney, Shyh Yang, Ajit Jadhav, Daniel Jason Urban
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Abstract
The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.
Claims14
A compound of Formula I, or a-pharmaceutically acceptable salt or isomer thereof:
- wherein:
- X is N;
- Z is N;
- R1 and R2, together with the included nitrogen atom and L1, form
- Y is pyrazolyl and may optionally be substituted with 1 or 2 independently selected R8,
- R3 is 2-oxopyridinyl and is optionally substituted by one or two methyl groups;
- R4 is H;
- each R8 is independently selected from the group consisting of H, C3-6 cycloalkyl, phenyl, and C1-6 alkyl, wherein said phenyl or C1-6 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R14;
- and
- R14 is H, OH, or halogen.
7 more elements
Dependencies are inferred from the claim text.