Icotinib hydrochloride, synthesis, crystalline forms, drug...

C - Chemistry – Metallurgy – 07 – D

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C07D 491/056 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2730311

The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3--ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4--[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.

La présente invention concerne le chlorhydrate de 4-[(3-éthynylphényl)amino]-6,7-benzo-12-couronne-4-quinazoline et sa nouvelle forme cristallographique. Linvention a également pour objet le procédé de préparation, la combinaison médicale, le procédé de traitement clinique, les intermédiaires pertinents du composé ci-dessus.

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