Polymorphs of arry-380, a selective her2 inhibitor and pharmaceutical compositions containing them

Abstract

Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.

1 . A crystalline polymorph of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine freebase. 
     
     
         2 . A method of treating cancer in a mammal in need thereof, comprising administering to the mammal an effective amount of a crystalline polymorph of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine freebase. 
     
     
         3 . The method of  claim 2 , wherein the cancer is a ErbB2 positive cancer. 
     
     
         4 . The method of  claim 3 , wherein the ErbB2 cancer is breast, colorectal, gastric, or esophageal cancer. 
     
     
         5 . The method of  claim 2 , wherein one or more additional compounds having anti-cancer properties are administered in combination. 
     
     
         6 . The method of  claim 2 , wherein the mammal is a human. 
     
     
         7 . The method of  claim 3 , wherein one or more additional compounds having anti-cancer properties are administered in combination. 
     
     
         8 . The method of  claim 3 , wherein the mammal is a human. 
     
     
         9 . The method of  claim 4 , wherein one or more additional compounds having anti-cancer properties are administered in combination. 
     
     
         10 . The method of  claim 4 , wherein the mammal is a human.