MYULLER Dzhordzh V. (US),МЮЛЛЕР Джордж В. (US),MAN Khon-Vakh (US),МАН Хон-Вах (US),KOEN Bendzhamin M. (US),КОЭН Бенджамин М. (US),LI In (US),ЛИ Ин (US),SYUJ Dzhin (US),СЮЙ Джин (US),LEONG Uillyam V. (,MYULLER Dzhordzh V.,МЮЛЛЕР Джордж В.,MAN Khon-Vakh,МАН Хон-Вах,KOEN Bendzhamin M.,КОЭН Бенджамин М.,LI In,ЛИ Ин,SYUJ Dzhin,СЮЙ Джин,LEONG Uillyam V.,ЛЕОНГ Уилльям В.
申请号：
RU2013145518
公开号：
RU0002611007C2
申请日:
2012.03.09
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: pharmaceutics.SUBSTANCE: invention relates to polymorphous solid crystalline forms 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)piperidine-2,6-dione of following structural formula. Solid crystalline forms of compound corresponding to structural formula,represent crystalline form A1 of hydrochloride salt of said compound with indications of powder x-ray peak at approximately 8.6, 13.1, 20.5 and 26.3 degrees 2θ； either crystalline form of A monohydrate of said compound, having powder x-ray, including peaks at approximately 14.6, 15.6, 16.7, 21.9 and 30.0 degrees 2θ； crystalline form B, having powder x-ray, including peaks at approximately 10.6, 14.7, 19.1 and 25.9 degrees 2θ； crystalline form C with powder x-ray, including peaks at approximately 10.8, 15.1, 25.1 and 26.6 degrees 2θ； crystalline form E hydrate with powder x-ray, including peaks at approximately 7.3, 14.6, 22.0, 30.0 and 37.0 degrees 2θ； crystalline form F, having powder x-ray, including peaks at approximately 14.5, 15.7, 22.7 and 29.9 degrees 2θ. Invention covers also data of differential scanning calorimetry, thermogravimetric analysis data, indices of hygroscopicity and stability of obtained solid crystalline forms. Invention also relates to pharmaceutical composition containing therapeutically effective amount of solid shape and pharmaceutically acceptable carrier, thinner or excipient.EFFECT: compound possesses properties of TNF-α and can be used for treating various forms of cancer, angiogenesis, macular degeneration and associated syndrome, pain and other disorders and diseases associated with TNF-α.42 cl, 23 dwg, 10 tbl, 4 exИзобретение относится к полиморфным твердым кристаллическим формам 3-(5-амино-2-метил-4-оксо-4Н-хиназолин-3-ил)пиперидин-2,6-дион указанной ниже структурной формулы. Соединение обладает свойствами ингибитора TNF-α и может использоваться для лечения различных форм рака, ангиогенеза, дегенерации желтого пятна и сопутствующего синдрома, боли и др. расстройств и заболева
