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US 9,751,859 B2Granted
Process for preparing an anti-cancer agent, 1-((4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine, its crystalline form and its salts
AssigneeAdvenchen Pharmaceuticals, LLC
InventorsGuoqing Paul Chen, Changren Yan
Life of this patent
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Abstract
The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of Al3818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.
Claims9
A crystalline form of 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquino-lin-7-yloxy)methyl)cyclopropanamine of AL3818 exhibiting at least one of following characters:
- a melting point at 208° C.-210° C.;
- a DSC Melting Range (Endo):
- 207-220° C. with Peak Temp=216° C., pattern shown in FIG. 1;
- a TGA thermogram that doesn't exhibit significant weight loss until at 205-215° C., pattern shown in FIG. 2.
1 more element
Dependencies are inferred from the claim text.