首页> 外国专利> novel forms in 3- (1,2,4-triazol 4,3-a pyridin-3-ylethynyl) -4-methyl-n- (4 - ((4-methylpiperazin-1-yl) methyl) crystalline salt ) -3-trifluoromethylphenyl) benzamide for medical application

novel forms in 3- (1,2,4-triazol 4,3-a pyridin-3-ylethynyl) -4-methyl-n- (4 - ((4-methylpiperazin-1-yl) methyl) crystalline salt ) -3-trifluoromethylphenyl) benzamide for medical application

机译:3-(1,2,4-三唑[4,3-a]吡啶-3-基乙炔基)-4-甲基-n-(4-((4-甲基哌嗪-1-基)甲基)结晶盐)-3-三氟甲基苯基)苯甲酰胺

摘要

The invention relates to organic chemistry, pharmacology and medicine and is concerned 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, leukemia. chronic myeloid, acute lymphocytic leukemia, breast cancer, non-small cell lung cancer, gastrointestinal stromal tumors, ovarian cancer, lymphoma, using a new salt form of 3- (1,2,4-triazole [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, in particular of 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.
机译:本发明涉及有机化学,药理学和医学,并且涉及与各种激酶,特别是abl激酶的活性破坏有关的人类和动物疾病的预防和治疗,例如诸如白血病,急性髓细胞性白血病,白血病的疾病。慢性髓样,急性淋巴细胞性白血病,乳腺癌,非小细胞肺癌,胃肠道间质瘤,卵巢癌,淋巴瘤,使用新的盐形式的3-(1,2,4-三唑[4,3 -a]吡啶-3-基乙炔基)-4-甲基-正-(4-(((4-甲基哌嗪-1-基)甲基)-3-三氟甲基苯基)苯甲酰胺。该化合物与甲磺酸的式(I)的盐或其水合物,溶剂化物以及多晶型修饰物具有抑制激酶特别是ab1激酶活性的能力。本发明还涉及包含治疗有效量的本发明的盐的药物组合物,制备本发明的结晶盐的方法以及治疗患者的肿瘤疾病的方法。

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