ТЯВАНАГИМАТТ Шантхакумар Р. (US),СТОУН Мелиалани А.К.Л. (US),УЭЙМЕРС Уилльям К. (US),НЕЛЬСОН Дилан (US),БОЛКЕН Тоув К. (US),ХРУБИ Деннис Э. (US),О'НЕЙЛЛ Майкл Х. (US),СВИТЭППЛ Гари (US),МакКЛУН Келли,ОНЕЙЛЛ Майкл Х. (US),МакКЛУН Келли А
申请号：
RU2012144818/04
公开号：
RU2012144818A
申请日:
2011.03.23
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
1. Polymorph of Form I 4-trifluoromethyl-N- (3,3a, 4,4a, 5,5a, 6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop [f] isoindole-2 (1H) -yl) benzamide (compound ST-246), which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle of 2θ of about 7.63, 10.04, 11.47, 14.73, 15.21, 15.47, 16.06, 16.67, 16.98, 18.93, 19.96, 20.52, 20.79, 22.80, 25.16, 26.53, 27.20, 27.60, 29, 60, 30.23, 30.49, 30.68, 31.14, 33.65, 34.33, 35.29, 35.56, 36.30, 37.36, 38.42, 38.66 degrees .2. The polymorph according to claim 1, which is an isolated polymorph, and which is at least about 70% free from other forms, preferably is at least about 80% free from other forms, more preferably is at least about 90 % free from other forms, even more preferably is at least about 95% free from other forms, in particular is at least about 99% free from other forms. Polymorph of Form II 4-trifluoromethyl-N- (3,3a, 4,4a, 5,5a, 6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop [f] isoindole-2 (1H) -yl ) benzamide (compound ST-246), which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle of 2θ in accordance with FIG. 2.4. The polymorph according to claim 3, which is an isolated polymorph, and which is at least about 70% free from other forms, preferably is at least about 80% free from other forms, more preferably is at least about 90 % free from other forms, even more preferably is at least about 95% free from other forms, in particular is1. Полиморф формы I 4-трифторметил-N-(3,3а,4,4а,5,5а,6,6а-октагидро-1,3-диоксо-4,6-этеноциклопроп[f]изоиндол-2(1Н)-ил)бензамида (соединение ST-246), который демонстрирует картину рентгеновской порошковой дифракции, имеющую характеристические пики при угле отражения 2θ приблизительно 7,63, 10,04, 11,47, 14,73, 15,21, 15,47, 16,06, 16,67, 16,98, 18,93, 19,96, 20,52, 20,79, 22,80, 25,16, 26,53, 27,20, 27,60, 29,60, 30,23, 30,49, 30,68, 31,14, 33,65, 34,33, 35,29, 35,56, 36,30, 37,36, 38,42, 38,66 градусов.2. П
