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КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 3-(2,6-ДИХЛОР-3,5-ДИМЕТОКСИФЕНИЛ)-1-{ 6-[4-(4-ЭТИЛПИПЕРАЗИН-1-ИЛ)-ФЕНИЛАМИНО]-ПИРИМИДИН-4-ИЛ} -1-МЕТИЛМОЧЕВИНЫ И ЕЕ ДОЛЕЙ
专利权人:
NOVARTIS AG
发明人:
JERG BERGKHAUZEN,PRASAD KOTESVARA KAPA,DZHOZEF MAKKENNA,DZHOEHL SLEJD,REJANN VU,CHZHEHNMIN DU,FRANK SHTOVASSER,Йёрг БЕРГХАУЗЕН,Прасад Котесвара КАПА,Джозеф МАККЕННА,Джоэл Слейд,Рейанн ВУ,Чжэнмин ДУ,Фр
申请号:
RU2012128351
公开号:
RU2572848C2
申请日:
2010.12.06
申请国别(地区):
RU
年份:
2016
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to novel hydrated and anhydrous crystalline forms, as well as to amorphous form of 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{6-[4-(4-ethylpiperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methylurea of formula (I) and its monophosphoric and hydrochloride salt. Compounds possess properties of inhibitors of activity of kinase, selected from the group, including FGFR1, FGFR2, FGFR3, FGFR4, KDR, HER1, HER2, Bcr-Abl, Tie2 and Ret, and can be used in treatment of diseases, mediated by activity of said kinases. Diseases are selected from the group, including carcinoma of kidneys, liver, adrenal glands, urinary bladder, mammary gland, stomach, ovaries, large intestine, rectum, prostate, pancreas, lungs, vagina or thyroid gland; sarcoma, glioblastoma, leukaemia; tumours of head or neck; psoriasis; prostate gland hyperplasia or neoplasia In particular invention relates to anhydrous crystalline form of formula (I) compound and its monohydrate; to salt of phosphoric acid of formula (I) compound, its anhydrous crystalline forms A and B and its amorphous form; crystalline hydrochloride dehydrate. Crystalline form s are characterised by respective data of powder radiograph, indices of thermogram of differential scanning calorimetry, characteristic peaks of Raman scattering Invention also relates to method for obtaining anhydrous crystalline form A of monophosphoric acid salt.EFFECT: amorphous form of monophosphoric acid salt does not contain characteristic peaks on powder radiogram, does not demonstrate vitrification in DSC determination and has decomposition temperature 115°C, determined by TGA.34 cl, 9 dwg, 10 tbl, 21 exИзобретение относится к новым гидратированным и безводным кристаллическим формам, а также к аморфной форме 3-(2,6-дихлор-3,5-диметоксифенил)-1-{6-[4-(4-этилпиперазин-1-ил)-фениламино]-пиримидин-4-ил}-1-метилмочевины формулы (I) и ее монофосфорной и гидрохлоридной соли. Соединения обладают свойствами ингибиторов активности
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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