SOLID FORMS OF IBRUTINIB

The invention relates to a solid form of 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H- pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one of formula I and to preparation methods of crystalline particles with variable morphology. Crystalline form C of ibrutinib free base with the primary parti...

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Bibliographic Details
Main Authors ZVATORA, Pavel, DAMMER, Ondrej, ZVONICEK, Vit, MIKESOVA, Radka, BERANEK, Josef
Format Patent
LanguageEnglish
French
Published 12.10.2017
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention relates to a solid form of 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H- pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one of formula I and to preparation methods of crystalline particles with variable morphology. Crystalline form C of ibrutinib free base with the primary particle size smaller than or equal to 120 μm, the ratio of the primary particle size to the cluster size being at least 1:5 and the clusters having the minimum size of 150 μm. L'invention concerne une forme solide de la 1-[(3R)-3-[4-amino-3-(4-phénoxyphényl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]pipéridin-1-yl]prop-2-en-1-one de formule (I) et des procédés de préparation de particules cristallines à morphologie variable. La forme cristalline (C) de la base libre de l'ibrutinib présente une taille de particules primaires inférieure ou égale à 120 µm, le rapport entre la taille des particules primaires et la taille des agrégats étant d'au moins 1:5 et les agrégats présentant la taille minimale de 150 µm.
Bibliography:Application Number: WO2017CZ00019