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US 2014/0179668 A1Published application
Fused pyrimidine compounds and use thereof
AssigneeMedivation Technologies, Inc.
InventorsSarvajit CHAKRAVARTY, Roopa RAI, Michael John GREEN
Life of this patent
Estimating the term…
Abstract
Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.
Claims144
A compound of the formula (I):
- or a salt thereof, wherein:
- D is hydrogen, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted C3-C8 cycloalkyl, substituted or unsubstituted heterocyclyl, or taken together with RD and the nitrogen to which they are attached to form a substituted or unsubstituted heterocyclyl;
- E is substituted or unsubstituted heteroaryl;
- each j, k, m, and n is independently 0 or 1;
- each RA1, RA2, RA3, RA4, RA5, RA6, RA7, RA8, RA9 and RA10, where present, is independently hydrogen, substituted or unsubstituted C1-C6 alkyl, halo, hydroxy, —OR1, —SH, —S(O)pR2, —NR3R4, —C(O)NR5R6, —C(O)OR7, —OC(O)R8, —C(O)R9, substituted or unsubstituted C3-C8 cycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or taken together with a geminal RA(1-10) group and the carbon to which they are attached to form carbonyl, thiocarbonyl, a C3-C6 cycloalkyl, or a heterocyclyl;
- RD is hydrogen, substituted or unsubstituted C1-C6 alkyl, or taken together with D and the nitrogen to which they are attached to form a substituted or unsubstituted heterocyclyl;
- X is O or S;
- RZ is hydrogen, or substituted or unsubstituted C1-C6 alkyl;
- each RZ1 and RZ2 is independently hydrogen, or substituted or unsubstituted C1-C6 alkyl, or RZ1 and RZ2 are taken together with the carbon to which they are attached to form a carbonyl or a C3-C6 cycloalkyl;
- each RZ3, RZ4, RZ5, RZ6, RZ7 and RZ8, where present, is independently hydrogen, substituted or unsubstituted C1-C6 alkyl, halo, hydroxy, —OR1, —O—C1-C6 alkylene-P(O)(OH)2, —SH, —S(O)pR2, —NR3R4, —C(O)NR5R6, —C(O)OR7, —OC(O)R8, —C(O)R9, substituted or unsubstituted C3-C8 cycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or is taken together with a geminal RZ(3-8) group and the carbon to which they are attached to form carbonyl, thiocarbonyl or a C3-C6 cycloalkyl;
- each p is independently 0, 1 or 2;
- each R1 is independently a substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C3-C8 cycloalkyl, or substituted or unsubstituted aryl;
- each R2 is independently a substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C3-C8 cycloalkyl, substituted or unsubstituted aryl or hydroxyl;
- each R3, R4, R5, R6 and R7 is independently hydrogen, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C3-C8 cycloalkyl;
- and
- each R8 and R9 is independently hydrogen, substituted or unsubstituted C1-C6 alkyl, substituted or unsubstituted C3-C8 cycloalkyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
13 more elements
Dependencies are inferred from the claim text.