C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 215/227 (2006.01) A61K 31/47 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2758030
Disclosed are malate salts of N-(4-{ [6,7-bis(methyloxy)-quinolin-4- yl]oxy}phenyl)- N'-(4-fluorophenyl)cyclo- propane-1,1-dicarboxamide, including a (L)-malate salt, a (D)- malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{ [6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)- cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{ [6,7- bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4- ffuorophenyl)cyclopropane-1, 1-dicarboxamide.
La présente invention concerne les sels de malate de N-(4-{[6,7-bis(méthyloxy)-quinolin-4-yl]oxy}phényl)-N'-(4-fluorophényl)cyclopropane-1,1-dicarboxamide qui incluent le sel de (L)-malate, le sel de (D)-malate, le sel de (DL)-malate et les mélanges de ceux-ci, ainsi que les formes cristallines et amorphes desdits sels de malate. L'invention concerne également des compositions pharmaceutiques comprenant au moins un sel de malate de N-(4-{[6,7-bis(méthyloxy)quinolin-4-yl]oxy}phényl)-N'-(4-fluorophényl)-cyclopropane-1,1-dicarboxamide, et des procédés de traitement du cancer qui consistent à administrer au moins un sel de malate de N-(4-{[6,7-bis(méthyloxy)quinolin-4-yl]oxy}phényl)-N'-(4-fluorophényl)cyclopropane-1,1-dicarboxamide.
Brown Adrian St. Clair
Gallagher William P.
Lamb Peter
Bennett Jones Llp
Exelixis Inc.
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