- Patent Title: 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
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Application No.: US15143630Application Date: 2016-05-02
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Publication No.: US09751859B2Publication Date: 2017-09-05
- Inventor: Guoqing Paul Chen , Changren Yan
- Applicant: Advenchen Pharmaceuticals, LLC
- Applicant Address: US CA Moorpark
- Assignee: Advenchen Pharmaceuticals, LLC
- Current Assignee: Advenchen Pharmaceuticals, LLC
- Current Assignee Address: US CA Moorpark
- Agency: Knobbe, Martens, Olson & Bear, LLP
- Main IPC: C07D401/12
- IPC: C07D401/12 ; C07C57/145 ; C07C55/10 ; A61K31/4709 ; A61K45/06 ; A61K33/24 ; A61K31/337 ; A61K39/395 ; C07K16/22 ; A61K31/555 ; A61K39/00

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.
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