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Diazo derivatives as JAK inhibitors
专利权人:
INCYTE CORPORATION
发明人:
YUN-LONG, Li,ZHUO, Jincong,QIAN, Ding-Quan,MEI, Song,PAN, Yongchun,CAO, Ganfeng,LI, Qun,JIA, Zhongjiang
申请号:
PE2020000001
公开号:
PE20200527A1
申请日:
2014.05.16
申请国别(地区):
PE
年份:
2020
代理人:
摘要:
The invention refers to the formula (I) of 4 - [3 - (cyanomethyl) - 3 - (3 ', 5' - dimethyl-1h, 1'h-4, 4 '- diphosphate-1-il) azetidin-1-il] - 2, 5-difluoro-n - [(1 (s) - 2,2,2-trifluoro-1-methyl) benzene zamida (1 phosphoric acid) formula (I),The solid form of salt salt salt is crystalline, and there are at least 10 thin temperature 2-theta heat X-wave de peak value, from 6.8 + / - 0.2, 7.3 + / - 0.2, 8.2 + / - 0.2, 11.1 + / - 0.2, 11.7 + / / -0.2, 11.7 + / / -0.2, 11.7 + / -0.2, 11.7 + / -0.2, 12.8 + / -0.2, 13.5 + / -0.2, 13.5 + / -0.2, 14.7 + / -0.2, 15.9 + / -0.2, 15.9 + / -0.2, 16 + / -0.0.0.2, 2 + / -0.2, 17 + + 2.2.2.2.2.2, 17 + + + + 2.2, 17 + / -0.2.2 + + 2, 17.3 + / -0.2, 18.0 + / -0.2, 18.4 + / -0.2, among others. The activity of the compound is in Yanu Quinza (JAK)It is very useful in the treatment of inflammation, autoimmune disorders, cancer and so on.La presente invencion se refiere a una sal fosfato de 4-[3-(cianometil)-3-(3',5'-dimetil-1H,1'H-4,4'-bipirazol-1-il)azetidin-1-il]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-metiletil]benzamida (compuesto 1 fosfato) de formula (i), donde la forma solida de la sal es cristalina y tiene al menos diez picos XPRD en terminos 2-theta, seleccionados de: 6.8 +/- 0.2, 7.3 +/- 0.2, 8.2 +/- 0.2, 11.1 +/- 0.2, 11.7 +/- 0.2, 12.8 +/- 0.2, 13.5 +/- 0.2, 14.7 +/- 0.2, 15.9 +/- 0.2, 16.5 +/- 0.2, 17.0 +/- 0.2, 17.3 +/- 0.2, 18.0 +/- 0.2, 18.4 +/- 0.2, entre otros. Dicho compuesto modula la actividad de la Janus quinasa (JAK), siendo util en el tratamiento de trastornos inflamatorios, trastornos autoinmunitarios, cancer, entre otros.
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