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Claims for Patent: 8,877,776

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Claims for Patent: 8,877,776

Title:(L)-malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxami- de
Abstract: Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cy- clopropane -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)-cy- clopropane-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)cyc- lopropane-1,1-dicarboxamide.
Inventor(s): Brown; Adrian St. Clair (Ely, GB), Lamb; Peter (Oakland, CA), Gallagher; William P. (Princeton, NJ)
Assignee: Exelixis, Inc. (South San Francisco, CA)
Application Number:13/145,054
Patent Claims: 1. N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)- cyclopropane-1,1-dicarboxamide (L)-malate salt, wherein said salt is in crystalline Form N-2 and said Form N-2 is characterized by at least one of the following: (i) a solid state .sup.13C NMR spectrum with four or more peaks selected from 23.0, 25.9, 38.0, 41.7, 69.7, 102.0, 122.5, 177.3, 179.3, 180.0, and 180.3, .+-.0.2 ppm; (ii) a powder x-ray diffraction pattern (CuK.alpha. .lamda.=1.5418 .ANG.) comprising 2.theta. values at 20.9.+-.0.2 .degree.2.theta. and 21.9.+-.0.2 .degree.2.theta., and two or more 2.theta. values selected from: 6.4.+-.0.2 .degree.2.theta., 9.1.+-.0.2 .degree.2.theta., 12.0.+-.0.2 .degree.2.theta., 12.8.+-.0.2, 13.7.+-.0.2, 17.1.+-.0.2, 22.6.+-.0.2, 23.7.+-.0.2, wherein measurement of the crystalline form is at room temperature; and/or (iii) an x-ray powder diffraction (XRPD) pattern substantially in accordance with the pattern shown in FIG. 8.

2. A pharmaceutical composition comprising the N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}-phenyl)-N-(4-fluorophenyl)cyc- lopropane-1,1-dicarboxamide (L)-malate salt according to claim 1; and a pharmaceutically acceptable excipient.

3. A method for treating thyroid cancer in a subject comprising administering the crystalline form N-2 of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-flurophenyl)cycl- opropane-1,1-dicarboxamide (L)-malate salt according to claim 1.

4. A method for treating glioblastoma in a subject comprising administering the crystalline form N-2 of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-flurophenyl)cycl- opropane-1,1-dicarboxamide (L)-malate salt according to claim 1.

5. The method of claim 3, wherein the thyroid cancer is medullary thyroid cancer.
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