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US 10,376,511 B2Granted
Pyrazole pyrimidine derivative and uses thereof
AssigneeYissum Research Development Company of the Hebrew University of Jerusalem
InventorsYinon Ben Neriah, Guy Brachya, Ido Burstain, Waleed Minzel, Irit Snir-Alkalay, Joseph Vacca, Dansu Li
Life of this patent
Estimating the term…
Abstract
The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or Interleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.
Claims39
A compound having formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof:
- wherein:
- R1 and R2 are each independently selected from H;
- and straight or branched C1-C8 alkyl, straight or branched C1-C5 alkoxy, straight or branched C1-C5 acyl, C5-C15 aryl, and C3-C7 heteroaryl, each of which is optionally substituted by at least one of halide, hydroxyl, an ester, an ether, C5-C15 aryl, C3-C7 heteroaryl, and an amide;
- or
- R1 and R2 together with the nitrogen atom they are connected to form a 4-7 membered saturated, unsaturated, or aromatic ring that optionally includes at least one of N, O, NH, C═N, C═O, and SO2, and is optionally substituted with at least one of straight or branched C1-C5 alkyl, C5-C15 aryl, C3-C7 heteroaryl, hydroxyl, halide, and cyano;
- R3 and R4 are each independently selected from H, and straight or branched C1-C8 alkyl optionally substituted by at least one of halide, hydroxyl, C1-C5 alkoxy, C5-C15 aryl, C3-C7 heteroaryl, an ester, and an amide;
- or
- R1 or R2 together with R3 and the carbon and nitrogen atoms they are each connected to form a 4-7 membered saturated , unsaturated, or aromatic ring that optionally includes at least one of N, NH, O, C═N, C═O, and SO2, and is optionally substituted with at least one of straight or branched C1-C5 alkyl, C5-C15 aryl, C3-C7 heteroaryl, hydroxyl, and halide;
- R5 and R8 are each independently selected from H and halide;
- and straight or branched C1-C8 alkyl, straight or branched C2-C8 alkenyl, and straight or branched C2-C8 alkynyl, each optionally substituted by at least one halide;
- R6 is selected from straight or branched C1-C8 alkyl, straight or branched C2-C8 alkenyl, straight or branched C2-C8 alkynyl, C5-C10 cycloalkyl, and saturated or unsaturated 4-6 membered heterocyclyl, each of which is optionally substituted by at least one of straight or branched C1-C8 alkyl, C3-C7 cycloalkyl, 4-6 membered heterocyclyl, C5-C15 aryl, C3-C7 heteroaryl, halide, and hydroxyl;
- and
- R7 is selected from straight or branched C1-C8 alkyl, straight or branched C2-C8 alkenyl, and straight or branched C2-C8 alkynyl, each of which is substituted by at least one of C3-C7 cycloalkyl, 4-6 membered heterocyclyl, C5-C15 aryl, C3-C7 heteroaryl, halide, and hydroxyl.
10 more elements
Dependencies are inferred from the claim text.