Crystalline free bases of C-Met inhibitor or crystalline acid salts thereof, and preparation methods and uses thereof
AssigneeJiangsu Hansoh Pharmaceutical Group Co., Ltd.
InventorsXiang Li, Aifeng Lv
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AssigneeJiangsu Hansoh Pharmaceutical Group Co., Ltd.
InventorsXiang Li, Aifeng Lv
Estimating the term…
Crystalline free bases and crystalline acid salts of 9-((8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridine-3-yl)thio)-4-methyl-2H-[1,4]oxaazido[3,2-c]quinoline-3(4H)-one are disclosed as C-Met inhibitors. Their preparation methods and uses are also described. In particular, crystal forms I, II, III and IV of the free base; crystal form I of the hydrochloride salt; crystal forms I and II of the sulfate salt; crystal forms I, II, III and IV of the phosphate salt; crystal forms I, II, III, IV and V of the mesylate salt; crystal forms I, II and III of the p-toluenesulfonate salt; and crystal forms I, II and III of the 1,5-naphthalenedisulfonate salt are disclosed. Also disclosed are methods for preparing the above-mentioned crystal forms, pharmaceutical compositions thereof, methods for regulating the catalytic activity of a protein kinase, and methods of treating protein kinase-related diseases.
A crystalline acid salt of 9-((8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridine-3-yl)thio)-4-methyl-2H-[1,4]oxaazido[3,2-c]quinoline-3 (4H)-one, wherein the crystalline acid salt is an inorganic acid salt or an organic acid salt;
A crystalline acid salt of 9-((8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridine-3-yl)thio)-4-methyl-2H-[1,4]oxaazido[3,2-c]quinoline-3 (4H)-one, wherein the crystalline acid salt is crystal form III of a mesylate salt having an X-ray powder diffraction (XRPD) spectrum comprising peaks at diffraction angles (2θ) of 16.7±0.2°, 19.3±0.2°, 23.2±0.2°, 26.5±0.2°, 8.7±0.20, 19.5±0.2°, 21.8±0.2°, 23.6±0.2° and 24.3±0.2°.
Dependencies are inferred from the claim text.