ANHYDROUS CRYSTALLINE FORM OF DIMETHOXY DOCETAXEL AND METHODS FOR PREPARING SAME

• Main Authors: RORTAIS, Patricia, ZASKE, Lionel, GUILIANI, Alexandre, BILLOT, Pascal, ELMALEH, Hagit, DUFRAIGNE, Marielle, MANGIN, Fabrice
• Format: Patent
• Language: English; Lithuanian
• Published: 25.01.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

Anhydrous forms B-F, ethanolic solvate/heterosolvate forms, preferably ethanolate forms B, D and E, heterosolvate form F, hydrate forms, monohydrate form C and dihydrate form C of 4-acetoxy-2alpha -benzoyloxy-5beta ,20-epoxy-1-hydroxy-7beta ,10beta -dimethoxy-9-oxo-tax-11-ene-13alpha -yl-(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (I) are new. Anhydrous forms B-F, ethanolic solvate/heterosolvate forms, preferably ethanolate forms B, D and E, heterosolvate form F, hydrate forms, monohydrate form C, dihydrate form C of 4-acetoxy-2alpha -benzoyloxy-5beta ,20-epoxy-1-hydroxy-7beta ,10beta -dimethoxy-9-oxo-tax-11-ene-13alpha -yl-(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (I) are new, where: the anhydrous forms B-F are characterized by a X-ray diffraction powder (XRDP) having peaks at 7.3, 8.1, 9.8, 10.4, 11.1, 12.7, 13.1, 14.3, 15.4 and 15.9 +- 0.2[deg] 2theta , 4.3, 6.8, 7.4, 8.7, 10.1, 11.1, 11.9, 12.3, 12.6 and 13.1 +- 0.2[deg] 2theta , 3.9, 7.7, 7.8, 7.9, 8.6, 9.7, 10.6, 10.8, 11.1 and 12.3 +- 0.2[deg] 2theta , 7.1, 8.1, 8.9, 10.2, 10.8, 12.5, 12.7, 13.2, 13.4 and 13.9 +- 0.2[deg] 2theta and 4.4, 7.2, 8.2, 8.8, 9.6, 10.2, 10.9, 11.2, 12.1 and 12.3 +- 0.2[deg] 2theta , respectively; the ethanolate forms B, D and E are characterized by a XRDP having peaks at 7.3, 7.8, 8.8, 10.2, 12.6, 12.9, 13.4, 14.2, 14.7 et 15.1 +- 0.2[deg] 2theta , 3.8, 7.5, 7.7, 8.4, 9.4, 10.3, 10.5, 11.1, 11.5 and 11.9 +- 0.2[deg] 2theta and 7.1, 8.1, 8.8, 10.2, 10.7, 12.5, 13.2, 13.4, 13.9 and 14.2 +- 0.2[deg] 2theta , respectively; the hetero-solvate form F is characterized by XRDP having peaks at 4.4, 7.2, 8.2, 8.3, 8.8, 9.6, 10.3, 10.9, 11.2 and 12.2 +- 0.2[deg] 2theta ; the monohydrate form C is characterized by XRDP having peaks at 4.3, 6.8, 7.4, 8.6, 10.1, 11.1, 11.9, 12.2, 12.6 and 13.3 +- 0.2[deg] 2theta ; and the dihydrate form C is characterized by XRDP having peaks at 4.2, 6.9, 7.5, 8.4, 9.9, 10.9, 11.7, 12.3, 12.6 and 13.2 +- 0.2[deg] 2theta . Independent claims are included for the preparations of anhydrous forms B-F of (I). ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given.