Crystalline forms of a BTK inhibitor
AssigneeNovartis AG
InventorsDaniela Angst, Andreas Kordikowski
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Abstract
This application relates to various anhydrous crystalline forms N-(3-(6-Amino-5-(2-(N-methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide, as well as compositions, method of making and methods of using the same. These crystalline forms are useful in the treatment of diseases and disorders which are typically ameliorated by the inhibition of BTK. Such diseases and disorders may include inflammatory and autoimmune disorders and pulmonary and respiratory tract inflammation.
Claims45
A crystalline form of N-(3-(6-amino-5-(2-(N-methylacrylamido) ethoxy) pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide, having an x-ray powder diffraction pattern comprising peaks at 9.28±0.2 °2θ, 10.17±0.2 °2θ, and 18.73±0.2 °2θ, using CuKα1 (λ=1.54056 Å) radiation at about 296 K.
A crystalline form of N-(3-(6-amino-5-(2-(N-methylacrylamido) ethoxy) pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide, having a differential thermogravimetric profile measured by Differential Scanning calorimetry (DSC) with a heating rate of 10° C./min, with a single endothermic peak starting at about 194° C.
A crystalline form of N-(3-(6-Amino-5-(2-(N-methylacrylamido) ethoxy) pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide, having a decomposition point greater than 240° C. and a weight loss on drying of about 0.3% in a temperature range of 40-200° C., as determined by thermogravimetric analysis (TGA).
Dependencies are inferred from the claim text.