C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 17/08 (2006.01) A61K 31/7048 (2006.01) A61P 31/00 (2006.01)
Patent
CA 2472603
Crystal form F of [2S, 4R, 5R, 8R, 9S, 10S, 11R, 12R]-9-[(2,6-dideoxy-3-C- methyl-3-O-methyl-.alpha.-L-ribo-hexopyranosyl)oxy]-5-ethyl-4-methoxy- 2,4,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(isopropylmethylamino)-.beta.- 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 2.theta. = 6.6~ and 8.5~ , Crystal form D anhydrate of said compound showing strong X-ray diffraction peaks at diffraction angles 2.theta. = 7.1~ , 13.5~ and 14.2~ , Crystal form D X-hydrate of said compound showing strong X-ray diffraction peaks at diffraction angles 2.theta.= 7.1~ and 14.2~ but not showing a strong X-ray diffraction peak at a diffraction angle 2.theta. = 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.
L'invention concerne une forme cristalline F d'un sel d'acide [2S, 4R, 5R, 8R, 9S, 10S, 11R, 12R]-9-[(2,6-did~oxy-3-C-m~thyl-3-O-m~thyl-.alpha.-L-ribo-hexopyranosyl)oxy]-5-~thyl-4-m~thoxy-2,4,8,10,12,14-hexam~thyl-11-[[3,4,6-trid~oxy-3-(isopropylm~thylamino)-.beta.-D-xylo-hexopyranosyl]oxy]-6,15-dioxabicyclo[10.2.1]pentadec-14(1)-ne-3,7-dione(E)-2-but~nedio~que (2:1) pr~sentant de forts pics de diffraction des rayons X ~ des angles de diffraction 2.theta. = 6,6~et 8,5~, un anhydrate de forme crystaline D de ce compos~ pr~sentant de forts pics de diffraction des rayons X ~ des anges de diffraction 2.theta. = 7,1~, 13,5~ et 14,2~, un X-hydrate de forme cristalline D de ce compos~ pr~sentant de forts pics de diffraction ~ des angles de diffraction 2.theta. = 7,1~ et 14,2~ mais ne pr~sentant pas de fort pic de diffraction ~ un angle de diffraction 2.theta. = 13,5~, des formes cristallines de solvate G1, G2 et G3 de ce compos~ caract~ris~es par des positions d'angle 2-th~ta dans le motif de diffraction de rayons X de poudre de 5,4~, 10,4~, 10,7~ et 12,1~. Le X-hydrate de forme cristalline D de ce compos~ possde des propri~t~s pr~f~r~es permettant qu'il soit utilis~ en tant que mat~riau pharmaceutique, telles qu'une plus grande stabilit~ par rapport ~ l'anhydrate de forme crystalline D de ce compos~.
Cheruvallath Vandana K.
Hiraide Akira
Kamada Kenji
Koyama Kaichiro
Parent Stephan
Chugai Seiyaku Kabushiki Kaisha
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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