# US 10,765,678 B2 · Polymorphs of ARRY-380, a selective HER2 inhibitor and pharmaceutical compositions containing them > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,765,678 B2 - Document ID: US10765678B2 - Status: Granted - Kind: B2 - Application number: 16/169,937 - Filed: 2018-10-24 - Published: 2019-05-02 - Granted: 2020-09-08 - Earliest claimed: 2011-10-14 - Assignees: Array BioPharma Inc. - Applicants: Array BioPharma Inc. - Inventors: Donald T. Corson; Christopher M. Lindemann; Daniel J. Watson - Web page: https://patentgrep.com/patent/US10765678B2 ## CPC - A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine - A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61P 35/00: Antineoplastic agents - C07D 471/04: Ortho-condensed systems - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) ## 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. ## Claims ### Claim 1 A method of treating cancer in a mammal in need thereof comprising administering a therapeutically 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 to the mammal, wherein the polymorph is selected from the group consisting of Form A, Form B, Form C, Form D, Form E, Form F, Form G, Form H, Form I, Form J, Form K, Form L, Form M, Form N, Form O and Form P, and wherein the cancer is ErbB2 positive colorectal, gastric or esophageal cancer. ### Claim 2 (depends on 1) The method of claim 1, wherein one or more additional compounds having anti-cancer properties are administered in combination. ### Claim 3 (depends on 1) The method of claim 1, wherein the mammal is a human. ### Claim 4 (depends on 1) The method of claim 1, wherein said polymorph is Form A and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 20.3. ### Claim 5 (depends on 1) The method of claim 1, wherein said polymorph is Form B and is characterized by XRPD diffraction peaks (2θ degrees±0.2) at about 9.9 and 25.5. ### Claim 6 (depends on 1) The method of claim 1, wherein said polymorph is Form C and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 5.0. ### Claim 7 (depends on 1) The method of claim 1, wherein said polymorph is Form D and is characterized by XRPD diffraction peaks (2θ degrees±0.2) at about 8.0 and 12.7. ### Claim 8 (depends on 1) The method of claim 1, wherein said polymorph is Form E and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 16.1. ### Claim 9 (depends on 1) The method of claim 1, wherein said polymorph is Form F and is characterized by at least one XRPD diffraction peak (2θ degrees±0.2) at about 16.6. ### Claim 10 (depends on 1) The method of claim 1, wherein said polymorph is Form G and is characterized by XRPD diffraction peaks (2θ degrees±0.2) at about 7.8 and 23.1. ### Claim 11 (depends on 1) The method of claim 1, wherein said polymorph is Form H and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 11.2. ### Claim 12 (depends on 1) The method of claim 1, wherein said polymorph is Form I and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 7.2. ### Claim 13 (depends on 1) The method of claim 1, wherein said polymorph is Form J and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 17.0. ### Claim 14 (depends on 1) The method of claim 1, wherein said polymorph is Form K and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 22.8. ### Claim 15 (depends on 1) The method of claim 1, wherein said polymorph is Form L and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 17.0. ### Claim 16 (depends on 1) The method of claim 1, wherein said polymorph is Form M and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 9.0. ### Claim 17 (depends on 1) The method of claim 1, wherein said polymorph is Form N and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 22.9. ### Claim 18 (depends on 1) The method of claim 1, wherein said polymorph is Form O and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 11.2. ### Claim 19 (depends on 1) The method of claim 1, wherein said polymorph is Form P and is characterized by at least one specific XRPD diffraction peak (2θ degrees±0.2) at about 23.5.