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NEW FORMS IN CRYSTALLINE SALT OF 3- (1,2,4-TRIAZOL [4,3-A] PYRIDINE-3-ILETINYL) -4-METHYL-N- (4 - ((4-MEPYPYPERAZIN-1-IL) METHYL ) -3-TRIFLUOROMETILPHENYL) BENZAMIDE FOR MEDICAL APPLICATION
专利权人:
LIMITED LIABILITY COMPANY «FUSION PHARMA»
发明人:
GERMES GRIGORIEVICH CHILOV,ILYA YURIEVICH TITOV
申请号:
BR112018071498
公开号:
BR112018071498A2
申请日:
2017.04.18
申请国别(地区):
BR
年份:
2019
代理人:
摘要:
the invention relates to organic chemistry, pharmacology and medicine and deals with the prevention and treatment of human and animal diseases associated with disruption in the activity of various kinases, in particular abl kinase, for example, diseases such as leukemia, acute myeloid leukemia, chronic myeloid leukemia, acute lymphocytic leukemia, breast cancer, non small cell lung cancer, gastrointestinal stromal tumors, Ovary cancer, lymphoma, using a new salt form of 3- (1,2,4-triazol [4,3-a] pyridin-3-ylethynyl) -4-methyl-n- (4 - ((4-methylpiperazin-1-yl) methyl) -3-trifluoromethylphenyl) benzamide. The salt of this compound with methanesulfonic acid, formula (I), or its hydrate, solvate, as well as polymorphic modifications, has the ability to inhibit the activity of kinases, particularly ab1 kinases. The present invention also relates to pharmaceutical compositions comprising a therapeutically effective amount of a salt of the invention, a method for preparing a crystalline salt of the invention, as well as a method for treating oncological diseases in a patient.a invenção refere-se à química orgânica, farmacologia e medicina e trata da prevenção e tratamento de doenças humanas e animais associadas à interrupção na atividade de várias quinases, em particular abl quinase, por exemplo, doenças tais como leucemia, leucemia mieloide aguda, leucemia mieloide crônica, leucemia linfocítica aguda, câncer de mama, câncer de pulmão de células não pequenas, tumores estromais gastrointestinais, câncer de ovário, linfoma, usando uma nova forma em sal de 3-(1,2,4-triazol[4,3-a]piridina-3-iletinil)-4-metil-n-(4-((4-metilpiperazin-1-il)metil)-3-trifluorometilfenil)benzamida. o sal desse composto com ácido metanossulfônico, fórmula (i), ou seu hidrato, solvato, bem como modificações polimórficas, têm a capacidade de inibir a atividade de quinases, em particular de ab1 quinases. a presente invenção também se refere a composições farmacêuticas que c
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