Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
AssigneeRigel Pharmaceuticals, Inc.
InventorsAnkush Argade, Rajinder Singh, Hui Li
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Abstract
The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.
Claims23
A method of inhibiting proliferation of a cell comprising contacting the cell with an amount of (1R,2R,3S,4S)—N4-(3-aminocarbonylbicyclo[2.2.1]hept-5-ene-2-yl)-5-fluoro-N2-[3-methyl-4-(4-methylpiperazin-1-yl)]phenyl-2,4-pyrimidinediamine effective to inhibit its proliferation.
A method of inhibiting an activity of an Aurora kinase comprising contacting the Aurora kinase with an amount of (1R,2R,3S,4S)—N4-(3-aminocarbonylbicyclo[2.2.1]hept-5-ene-2-yl)-5-fluoro-N2-[3-methyl-4-(4-methylpiperazin-1-yl)]phenyl-2,4-pyrimidinediamine effective to inhibit its activity.
A method of inhibiting an Aurora kinase-mediated process comprising contacting a cell expressing an Aurora kinase with an amount of (1R,2R,3S,4S)—N4-(3-aminocarbonylbicyclo[2.2.1]hept-5-ene-2-yl)-5-fluoro-N2-[3-methyl-4-(4-methylpiperazin-1-yl)]phenyl-2,4-pyrimidinediamine effective to inhibit the Aurora kinase-mediated process.
A method of treating an Aurora kinase-mediated disease, comprising administering to a subject in need thereof an amount of (1R,2R,3S,4S)—N4-(3-aminocarbonylbicyclo[2.2.1]hept-5-ene-2-yl)-5-fluoro-N2-[3-methyl-4-(4-methylpiperazin-1-yl)]phenyl-2,4-pyrimidinediamine effective to treat the disease.
Dependencies are inferred from the claim text.