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1. 发明申请

US20050176938A1 Anhydrate/hydrate of an erythromycin derivative and processes for preparing said anhydrate/hydrate 审中-公开
标题翻译：红霉素衍生物的无水物/水合物和制备所述无水物/水合物的方法
公开(公告)号：US20050176938A1
公开(公告)日：2005-08-11
申请号：US10501215
申请日：2003-01-14
申请人： Kenji Kamada , Akira Hiraide , Kaichiro Koyama , Hitoshi Shimizu , Gary Ward , Vandana Cheruvallath , Stephan Parent
发明人： Kenji Kamada , Akira Hiraide , Kaichiro Koyama , Hitoshi Shimizu , Gary Ward , Vandana Cheruvallath , Stephan Parent
IPC分类号： A61K31/7048 , A61P1/00 , A61P31/00 , C07H17/08
CPC分类号： C07H17/08
摘要： Crystal form F of [2S, 4R, 5R, 8R, 9S, 10S, 11R, 12R]-9-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-5-ethyl-4-methoxy-2,4,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(isopropylmethylamino)-β-D-xylo-hexopyranosyl]oxy]-6,15-dioxabicyclo[10.2.1]pentadec-14(1)-ene-3,7-dione (E)-2-butenedioic acid salt (2:1) showing strong X-ray diffraction peaks at diffraction angles 2θ=6.6° and 8.5°, Crystal form D anhydrate of said compound showing strong X-ray diffraction peaks at diffraction angles 2θ=7.1°, 13.5° and 14.2°, Crystal form D X-hydrate of said compound showing strong X-ray diffraction peaks at diffraction angles 2θ=7.1° and 14.2° but not showing a strong X-ray diffraction peak at a diffraction angle 2θ=13.5°, Solvate Crystal forms G1, G2 and G3 of said compound characterized by 2-theta angle positions in the powder X-ray diffraction pattern of 5.4°, 10.4°, 10.7° and 12.1°. Crystal form D X-hydrate of said compound has more preferred properties for use as a pharmaceutical material such as higher stability as compared with Crystal form D anhydrate of said compound.
摘要翻译： [2S，4R，5R，8R，9S，10S，11R，12R] -9 - [（2,6-二脱氧-3-C-甲基-3-O-甲基-α-L- 己基吡喃糖基）氧基] -5-乙基-4-甲氧基-2,4,8,10,12,14-六甲基-11 - [[3,4,6-三脱氧-3-（异丙基甲基氨基）-β- - 六吡喃糖基]氧基] -6,15-二氧杂双环[10.2.1]十五烷-15（1） - 烯-3,7-二酮（E）-2-丁烯二酸盐（2:1）在衍射角2θ= 6.6°和8.5°处的峰，所述化合物的晶型D无水物，在衍射角2θ= 7.1°，13.5°和14.2°处显示出强X射线衍射峰，所述化合物的晶型D X-水合物显示在衍射角2θ= 7.1°和14.2°处的强X射线衍射峰，但在衍射角2θ= 13.5°处不显示强X射线衍射峰。溶剂化晶体形成所述化合物的G 1，G 2和G 3，在粉末X射线衍射图中为2θ角位置为5.4°，10.4°，10.7°和12.1°。与所述化合物的D型水合物相比，所述化合物的晶形DX-水合物具有更优选的用作药物材料的性质，例如更高的稳定性。

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