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Polymorphic forms of (1.1 - - L - [4 - tiomorfolinil) {- 6 - [3 - (4-fluorophenyl) - 5 - methyl - 4 - ilmetoxi isoxazole] pyridin-3-yl) - methanone and their use in the treatment of Neurological Disorders
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
PASCAL DOTT,OLAF GRASSMANN,MICHAEL KAMMERER,JOACHIM MANNS,URS SCHWITTER,ANDREW THOMAS,NICOLE WYTTENBACH
申请号:
ARP120103860
公开号:
AR088359A1
申请日:
2012.10.17
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
The solid state (1) of the formula compound,as well as to solvates, inclusion complexes with other suitable compounds, to obtaining processes, to pharmaceutical compositions containing these solid forms and to their use as medicines. Claim 2: La (1,1-dioxo-1l⁶-thiomorpholin-4-yl) - {6- [3- (4-fluoro-phenyl) -5-methyl-isoxazol-4-ylmethoxy] -pyridin-3-yl } -Crystalline monohydrate monohydrate of the polymorphic form B according to claim 1, characterized by an XRPD diffraction diagram containing XRPD peaks at 2-q diffraction angles of approximately 13.3 °,20.6%22.5º. Claim 6: 1,1-dioxo-1l⁶-thiomorpholin-4-yl) - {6- [3- (4-fluoro-phenyl) -5-methyl-isoxazol-4-ylmethoxy] -pyridin-3-yl} crystalline methanone of the anhydrous polymorphic form C according to claim 1, characterized by an XRPD diffraction diagram containing XRPD peaks at the 2-q diffraction angles of approximately 17.4 °,23.4 degrees 1. Claim 10: according to claim 1 (1, 1-dioxo-1l8310a-tiomofollin-4-il) {6 - [3 - (4-fluoro-fenil) - 5-methyl-isoxazol-4-ilmetroxi] - piridin-3-il} - methane - monosoluble trifluoromethane, and polymetal d-form trifluoromethane, Characterized by the XRPD diffraction pattern, it contains the XRPD peak value of about 6.1 2-Q diffraction angle16.8 degrees22.6º. Claim 13: La (1,1-dioxo-1l⁶-thiomorpholin-4-yl) - {6- [3- (4-fluoro-phenyl) -5-methyl-isoxazol-4-ylmethoxy] -pyridin-3-yl } -Crystalline methanone of the anhydrous polymorphic form E according to claim 1, characterized by an XRPD diffraction diagram containing XRPD peaks at the 2-q diffraction angles of approximately 16.5 °,20.8º. Claim 16: A 1: 1 inclusion complex of (1,1-dioxo-1l⁶-thiomorpholin-4-yl) - {6- [3- (4-fluoro-phenyl) -5-methyl-isoxazol-4- ylmethoxy] -pyridin-3-yl} -methanone with the g-cyclodextrin according to claim 1. Claim 17: The inclusion complex according to claim 16, characterized by an XRPD diffraction pattern containing XRPD peaks at diffraction angles 2 -q of approximately 7.4º,14.9 degrees16.7 degrees21
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