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AssigneeAdvenchen Pharmaceuticals, LLC
InventorsGuoqing Paul Chen, Zhe Li, Yingyin Li, Lisha Qi, Tingting Yu
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Disclosed herein relates to the biological activities and preparation of 5-(2-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)ethyl)-5-azaspiro[2.4]-heptan-7-ol (Compound A) stable crystalline form (Compound A-Xln); its tablet (Compound A-Xln tablet); its phosphoric acid salt (Compound A-P) and phosphoric acid salt stable crystalline form (Compound A-P-Xln); as well as its enantiomers (Compound R-A, Compound S-A). Furthermore, their anti-cancer activities, stabilities, chirality, dissolutions and treatment indications have also been investigated.
A stable crystalline form (Compound A-Xln) of 5-(2-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)ethyl)-5-azaspiro[2.4]-heptan-7-ol (Compound A) is made by a method comprising subjecting an amorphous form of 5-(2-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)ethyl)-5-azaspiro[2.4]-heptan-7-ol to recrystallization, selected but not limited to using a high boiling point solvent or a mixture of solvents that together have a high boiling point, and using a low boiling point solvent or a mixture of solvents that together have a low boiling point, wherein the high boiling point solvent is DMF and the low boiling point solvent is EtOH.
A method of treating a neoplastic disease, comprising administering a stable crystalline form (Compound A-Xln) of 5-(2-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)ethyl)-5-azaspiro[2.4]-heptan-7-ol (Compound A) or pharmaceutical composition comprising a stable crystalline form (Compound A-Xln) and pharmaceutically acceptable excipients to a subject in need thereof.
Dependencies are inferred from the claim text.