首页> 外国专利> DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USED AS CHINESE INHIBITORS FOR TREATING PROLIFERATIVE DISEASES

DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USED AS CHINESE INHIBITORS FOR TREATING PROLIFERATIVE DISEASES

机译:二氢萘乙二酮和相关化合物用作中国抑制类药物治疗增生性疾病

摘要

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.
机译:本发明涉及二氢萘啶及相关化合物。包含有效量的二氢萘啶或相关化合物的组合物;和用于治疗或预防增生性疾病的方法,包括给予有效量的二氢萘啶或相关化合物。本发明公开了在广泛的c-KIT突变中抑制cKIT激酶的化合物的出乎意料的用途,所述c-KIT突变包括初级突变(KIT外显子9或11)和次级KIT突变(外显子13、14、17、18)的复杂出现。在个别难治性GIST患者中可能会出现这种情况。还出乎意料的是,本发明的化合物用于抑制有问题的外显子17 D816V c-KIT突变的用途,目前尚无有效的疗法。

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