Treatment of diseases by epigenetic regulation
AssigneeRVX Therapeutics Inc.
InventorsKevin G. McLure, Peter Ronald Young
Life of this patent
Estimating the term…
Abstract
The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.
Claims22
A method for inhibiting BET proteins comprising administering to a mammal, such as a human, a therapeutically effective amount of a compound of Formula I:
- wherein:
- X is selected from CR11 and N;
- Y is selected from CO and SO2;
- R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11, are each independently selected from alkoxy, aryloxy, alkyl, amide, amino, aryl, arylalkyl, carbamate, carboxy, cycloalkyl, halogen, haloalkyl, heteroaryl, heterocyclyl, hydrogen, hydroxyl, ketone, phosphate, sulfide, sulfinyl, sulfonyl, sulfonic acid, sulfonamide and thioketone;
- and
- each W is independently selected from C and N, wherein if W is N, then p is 0 and if W is C, then p is 1;
- or tautomer, stereoisomer, pharmaceutically acceptable salt, or hydrate thereof.
A method of inhibiting BET proteins in a mammal, such as a human, comprising administering a therapeutically effective amount of a compound of Formula II:
- wherein:
- X is selected from CH and N;
- R1 and R3 are each independently selected from alkoxy, alkyl, and halogen;
- R4 is H;
- R6 and R8 are each independently selected from alkoxy, alkyl, halogen, and hydrogen;
- R7 is selected from alkoxy, alkyl, amino, ether, hydrogen, and hydroxyl;
- and
- W is selected from C and N, wherein if W is N, then p is 0 or 1, and if W is C, then p is 1;
- or tautomer, stereoisomer, pharmaceutically acceptable salt, or hydrate thereof.
Dependencies are inferred from the claim text.