US2022033357A1PendingUtilityA1

Malate salt of N-(4-{[6,7-bis(methyloxy) quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer

79
Assignee: EXELIXIS INCPriority: Jan 16, 2009Filed: Oct 19, 2021Published: Feb 3, 2022
Est. expiryJan 16, 2029(~2.5 yrs left)· nominal 20-yr term from priority
Inventors:Adrian St. Clair BrownPeter LambWilliam P. Gallagher
C07D 215/22C07D 215/233C07B 2200/13A61P 43/00A61P 35/00A61P 5/14A61P 25/00A61K 31/47
79
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Claims

Abstract

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-fluorophenyl)cyclopropane-1,1-dicarboxamide.

Claims

exact text as granted — not AI-modified
1 - 15 . (canceled) 
     
     
         16 . A solid dosage form of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, malate salt for oral administration, wherein said salt is admixed with pharmaceutically acceptable excipients comprising a filler, a binder, a disintegrating agent, and a lubricant. 
     
     
         17 . The solid dosage form of  claim 16 , wherein the malate salt is the (DL)-malate salt. 
     
     
         18 . The solid dosage form of  claim 17 , wherein the malate salt is the (L)-malate salt. 
     
     
         19 . The solid dosage form of  claim 18 , wherein the (L)-malate salt is in an amount of from about 5% to about 75% by weight of the solid dosage form. 
     
     
         20 . The solid dosage form of  claim 19 , wherein the filler is lactose. 
     
     
         21 . The solid dosage form of  claim 20 , wherein the binder is a cellulose derivative. 
     
     
         22 . The solid dosage form of  claim 21 , wherein the disintegrant is croscarmellose sodium. 
     
     
         23 . The solid dosage form of  claim 22 , wherein the lubricant is magnesium stearate. 
     
     
         24 . The solid dosage form of  claim 23 , wherein said salt is crystalline. 
     
     
         25 . The solid dosage form of  claim 16 , wherein said salt is amorphous. 
     
     
         26 . The solid dosage form of  claim 24 , which is a tablet. 
     
     
         27 . A solid dosage form of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, malate salt for oral administration, wherein said salt is crystalline, and wherein said salt is admixed with pharmaceutically acceptable excipients comprising a filler, a binder, a disintegrating agent, and a lubricant. 
     
     
         28 . The solid dosage form of  claim 27 , wherein the malate salt is the (DL)-malate salt. 
     
     
         29 . The solid dosage form of  claim 28 , wherein the malate salt is the (L)-malate salt. 
     
     
         30 . The solid dosage form of  claim 29 , wherein the (L)-malate salt is in an amount of from about 5% to about 75% by weight of the solid dosage form. 
     
     
         31 . The solid dosage form of  claim 30 , wherein the filler is lactose. 
     
     
         32 . The solid dosage form of  claim 31 , wherein the binder is a cellulose derivative. 
     
     
         33 . The solid dosage form of  claim 32 , wherein the disintegrant is croscarmellose sodium. 
     
     
         34 . The solid dosage form of  claim 33 , wherein the lubricant is magnesium stearate. 
     
     
         35 . The solid dosage form of  claim 34 , which is a tablet.

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