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c-met inhibitor crystalline free bases, or acid inhibitor crystalline salts, and methods of preparation and use thereof
专利权人:
LTD.;JIANGSU HANSOH PHARMACEUTICAL GROUP CO.
发明人:
AIFENG LU,XIANG LI
申请号:
BR112017001517
公开号:
BR112017001517A2
申请日:
2015.07.30
申请国别(地区):
BR
年份:
2017
代理人:
摘要:
The present invention relates to 9 - ((8-fluoro-6- (1-methyl-1h-pyrazol-4-yl) - [1,2,4] triazole [4,3-a] crystalline free bases pyridin-3-yl) thio) -4-methyl-2h- [1,4] oxazazido [3,2-c] quinoline-3 (4h) -one as inhibitor of c-met or crystalline salts thereof with acids , and methods of preparation and use thereof. specifically, crystalline forms i, ii, iii and iv of the free bases are described; the crystalline form i of the hydrochloride; crystalline forms i and ii of sulfate; crystalline forms i, ii, iii and iv of phosphate; crystalline forms i, ii, iii, iv and v of mesylate; crystalline forms i, ii and iii of p-toluenesulfonate; crystalline forms i, ii and iii of 1,5-naphthalenedisulfonate; and the methods for preparing the crystalline forms mentioned above, a pharmaceutical composition comprising them and the pharmaceutical use thereof and a method for regulating the catalytic activity of a protein kinase.a presente invenção refere-se a bases livres cristalinas de 9-((8-fluoro-6-(1-metil-1h-pirazol-4-il)-[1,2,4]triazol[4,3-a]piridina-3-il)tio)-4-metil-2h-[1,4]oxa-azido[3,2-c]quinolina-3(4h)-ona como inibidor de c-met ou sais cristalinos destes com ácidos, e métodos de preparo e uso destes. especificamente, são descritas as formas cristalinas i, ii, iii e iv das bases livres; a forma cristalina i do cloridrato; as formas cristalinas i e ii do sulfato; as formas cristalinas i, ii, iii e iv do fosfato; as formas cristalinas i, ii, iii, iv e v do mesilato; as formas cristalinas i, ii e iii do p-toluenossulfonato; as formas cristalinas i, ii e iii do 1,5-naftalenodissulfonato; e os métodos para preparar as formas cristalinas mencionadas acima, uma composição farmacêutica compreendendo as mesmas e o uso farmacêutico destas e um método para regular a atividade catalítica de uma proteína quinase.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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