BASTIAN, Jolie Anne,CHEN, Jiehao,COHEN, Jeffrey Daniel,HENRY, James Robert,MCMILLEN, William Thomas,REAMAN, Bradley Earl,RUBIO, Almudena,SALL, Daniel Jon,ZHAO, Gaiying
申请号:
PE2018003199
公开号:
PE20190378A1
申请日:
2017.05.31
申请国别(地区):
PE
年份:
2019
代理人:
摘要:
It refers to 2,3-dihydro-1h-indol derivatives, wherein: R1a is hydrogen, methyl, etene, cyanogen, fluorination, chlorine, fluoroacetylene or difluoromethane; r1b is hydrogen, fluorine or chlorine; r1c is hydrogen, hydrogen Xi, fluorine, benzene, etc.; R2 is hydrogen or methyl; R2A is hydrogen or methyl; R3a is tetrahydropyridine. The most popular compounds are: 4-fluoro-n - (1R) - 1 - [1 - (tetrahydro-2h-piran-4-ilcarbonil) - 2,3-dihydro-1h-indol-5-il] ethyl} benzene zamida crystal,It is characterized by X-ray powder diffraction, with at least one peak at 17.38 degrees. These compounds inhibit the conversion from triarylamide to cyanide and are used in the treatment of some melanoma, acute myeloid leukemia, chronic lymphocytic leukemia and rectal cancer.Mother's cancerLung cancer, ovarian cancer, fallopian tube cancer, major peritoneal cancer, etc.Se refiere a derivados de 2,3-dihidro-1H-indol, en donde: R1a es hidrogeno, metilo, etenilo, ciano, fluoro, cloro, fluorometilo, o difluorometilo; R1b es hidrogeno, fluoro, o cloro; R1c es hidrogeno, hidroxi, fluoro, benciloxi, entre otros; R2 es hidrogeno o metilo; R2a es hidrogeno o metilo; y R3a es tetrahidropiranilo. Entre los compuestos preferidos se tiene el siguiente: 4-fluoro-N-{(1R)}-1-[1-(tetrahidro-2H-piran-4-ilcarbonil)-2,3-dihidro-1H-indol-5-il]etil}benzamida cristalino, el cual se encuentra caracterizado por un patron de difraccion en polvo de rayos X que comprende al menos un pico a 17.38°. Estos compuestos inhiben la conversion de triptofano a cinureina y se emplean en el tratamiento de un cancer seleccionado de melanoma, leucemia mieloide aguda, leucemia linfocitica cronica, cancer colorrectal , cancer de mama , cancer de pulmon, cancer de ovario, carcinoma de trompas de Falopio, carcinoma peritoneal primario, entre otros.