1012879-10-5Relevant articles and documents
Method for preparing repitinib
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Paragraph 0057; 0066-0067; 0068-0069; 0070-0071, (2021/04/10)
The invention relates to a method for synthesizing and preparing a new drug repitinib. By utilizing the synthesis and preparation method disclosed by the invention, the compound, namely the repitinib shown in the formula I, can be rapidly and effectively prepared in six steps of chemical reactions. According to the synthetic reaction, the reaction steps and the post-treatment steps are greatly simplified, the reaction conditions are mild, industrial industrialization is easy to realize, and the production cost is lower and more economical.
DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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Paragraph 0209, (2014/01/08)
The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound. The present invention discloses the unexpected utility of compounds that inhibit cKIT kinase across a broad range of c-KIT mutations, including complex occurrences of primary mutations (KIT exon 9 or 11) and secondary KIT mutations (exons 13, 14, 17 and 18) that may arise in individual, refractory GIST patients. Also unexpected is the utility of compounds of the present invention to inhibit the problematic exon 17 D816V c-KIT mutation, for which there is currently no effective therapy.