79173-62-9

Usage

InChI:InChI=1/C8H9N3/c1-5-7-3-2-6(9)4-8(7)11-10-5/h2-4H,9H2,1H3,(H,10,11)

Upstream product

• 6494-19-5 3-methyl-6-nitro-1H-indazole 
• 1313372-75-6 3?methyl?6?nitro?1H?indazole 
• 315203-37-3 6-nitro-1H-indazole-3-carboxaldehyde 

Downstream Products

• 201286-99-9 3-methyl-1H-indazol-6-ol 
• 1122709-91-4 2-chloro-N-(3-methyl-1H-indazol-6-yl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine 
• 1089671-52-2 C₂₁H₁₇FN₄O 

Relevant academic research and scientific papers

PROCESS FOR THE PREPARATION OF PAZOPANIP HCL AND CRYSTALLINE FORMS OF PAZOPANIB HCL

Various crystalline forms of Pazopanib HCl were prepared. In preferred embodiments the obtained Pazopanib HCl is essentially free from CPMI.

2-AMINOQUINAZOLINE DERIVATIVE

An object of the present invention is to provide compounds which are useful as protein kinase inhibitors. Disclosed is a 2-aminoquinazoline derivative represented by the following formula (I): wherein R1 represents a lower alkyl group which may be substituted with a halogen atom, or a halogen atom; R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted acylamino group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, or a substituted or unsubstituted lower alkylureido group; and X, Y and Z each independently represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a halogen atom, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a carbamoyl group, a substituted or unsubstituted lower alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted lower alkoxycarbonylamino group, a substituted or unsubstituted lower alkylaminocarbonyl group, a lower alkylsulfonylamino group, a substituted or unsubstituted lower alkylureido group, or a substituted or unsubstituted acylamino group, or X and Y may be combined to form a 5- to 6-membered ring forming a bicyclic fused ring, wherein the 5- to 6-membered ring may optionally have a substituent, provided that when X and Y are not combined to form a fused ring, R2 represents a hydrogen atom and, when X and Y are combined to form a fused ring, a saturated or unsaturated, bicyclic alicyclic or heterocyclic fused ring can be formed.

PROTEIN KINASE INHIBITORS

Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure: or a pharmaceutically acceptable salt thereof, wherein R1 is structure (a), (b), (c) or (d): and Ra, Rb, Rc, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed, as well as uses of the same to treat a condition or disorder mediated by a Syk and/or JAK kinase.

Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2- pyrimidinyl]amino]-2-methyl-benzenesulfonamide (pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor

Inhibition of the vascular endothelial growth factor (VEGF) signaling pathway has emerged as one of the most promising new approaches for cancer therapy. We describe herein the key steps starting from an initial screening hit leading to the discovery of pazopanib, N4-(2,3-dimethyl-2H-indazol- 6-yl)-N4-methyl-N2-(4-methyl-3-sulfonamidophenyl)-2,4- pyrimidinediamine, a potent pan-VEGF receptor (VEGFR) inhibitor under clinical development for renal-cell cancer and other solid tumors.

BENZAZOLE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE AS AURORA KINASE INHIBITORS

The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.