发明名称 Solid state forms of cabazitaxel and processes for preparation thereof
摘要 The invention relates to solid state forms of Cabazitaxel and processes for preparing the solid state forms. The invention further relates to pharmaceutical compositions and formulations comprising one or more of the solid state forms.
申请公布号 US9394266(B2) 申请公布日期 2016.07.19
申请号 US201314382958 申请日期 2013.03.07
申请人 Ivax International GmBh 发明人 Vraspir Pavel;Jegorov Alexandr;Gabriel Roman;Gavenda Ales
分类号 C07D305/14 主分类号 C07D305/14
代理机构 Baker & Hostetler LLP 代理人 Baker & Hostetler LLP
主权项 1. A crystalline Cabazitaxel alkyl acetate solvate selected from: a) Crystalline Cabazitaxel ethyl acetate solvate, designated as Form VII, characterized by data selected from one or more of the following: a powder X-ray diffraction pattern having peaks at 7.9, 8.6, 10.0, 10.2 and 15.8 degrees two theta±0.1 degrees two theta, and also having no peak in the area from 10.5 to 12.1 degrees two theta; a powder X-ray diffraction pattern as depicted in FIG. 1; or combinations of these data; b) Crystalline isopropyl acetate solvate of cabazitaxel, designated as Form VIII, characterized by data selected from one or more of the following: a powder X-ray diffraction pattern having peaks at 7.9, 8.6, 10.0, 10.2 and 16.6 degrees two theta±0.1 degrees two theta, and also having no peak in the area from 10.5 to 12.1 degrees two theta; a powder X-ray diffraction pattern as depicted in FIG. 4; or a combination of these data; c) Crystalline Cabazitaxel methyl acetate solvate, designated as Form XVII, characterized by data selected from one or more of the following: a powder X-ray diffraction pattern having peaks at 8.0, 8.7, 14.2, 15.1 and 15.9 degrees two theta±0.1 degrees two theta; a powder X-ray diffraction pattern as depicted in FIG. 37; or combination of these data; d) Crystalline Cabazitaxel butyl acetate solvate, designated as Form XVIII, characterized by data selected from: a powder X-ray diffraction pattern having peaks at 8.6, 13.6, 14.0, 19.2 and 19.8 degrees two theta±0.1 degrees two theta; a powder X-ray diffraction pattern as depicted in FIG. 40; or a combination of these data; or e) Crystalline Cabazitaxel isobutyl acetate, designated as Form XXI, characterized by data selected from one or more of the following: a powder X-ray diffraction pattern having peaks at 8.6, 14.0, 15.6, 16.3 and 19.6 degrees two theta±0.1 degrees two theta; a powder X-ray diffraction pattern as depicted in FIG. 49; or a combination of these data.
地址 Rapperswil CH