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NOVEL FORMS OF AN INDAZOLO [5,4-A] PYRROLO [3,4-C] CARBAZOLE COMPOUND
专利权人:
CEPHALON; INC.
发明人:
BIERLMAIER, STEPHEN,COURVOISIER, LAURENT,FIELD, RAYMOND SCOTT,HALTIWANGER, R
申请号:
NZ59286809
公开号:
NZ592868A
申请日:
2009.11.19
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are crystalline forms of Compound I and salts of Compound I para-toluenesulfonic acid salts in a 1:1 or 1:2 ratio. Compound 1 is 11-isobutyl-2-methyI-8-(2-pyrimidinylamino)-2,5,6,11,12,13-hexahydro-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one - an orally active, TIE-2/VEGF-R inhibitor having antitumour and anti-angiogenic activity. The crystalline forms disclosed are: pTSA-A1 having an X-ray powder diffraction pattern comprising a peak at 5.37, 6.79, 13.64, and 22.58 +/- 0.2 degrees 2-theta, pTSA-A2, having an X-ray power diffraction pattern comprising peaks at 5.63, 8.48, 12.46, 18.21, and 23.95 +/- 0.2 degrees 2-theta, and A0 having an X-ray power diffraction pattern comprising peaks at 6.70, 7.00, 8.19, 13.69, and 24.27 +/- 0.2 degrees 2-theta. Also disclosed is the use of crystalline compound I for treating an angiogenic disorder and solid tumours.
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