Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving leading biopharmaceutical companies globally:

Fish and Richardson
Argus Health
Harvard Business School
Chinese Patent Office
Queensland Health
US Army

Generated: February 20, 2018

DrugPatentWatch Database Preview

Claims for Patent: 8,877,776

« Back to Dashboard

Summary 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.

For more information try a trial or see the plans and pricing

Serving hundreds of leading biopharmaceutical companies globally:

US Army
Cantor Fitzgerald
Boehringer Ingelheim

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.