首页> 外国专利> PI3K Novel Quinazolinone derivatives as PI3K inhibitors and pharmaceutical composition comprising the same

PI3K Novel Quinazolinone derivatives as PI3K inhibitors and pharmaceutical composition comprising the same

机译:PI3K新型作为PI3K抑制剂的喹唑啉酮衍生物及其药物组合物

摘要

The present invention relates to novel quinazolinone derivatives inhibiting PI3K, a method of preparing the quinazolinone derivatives, and a pharmaceutical composition for treatment of hematologic tumor or liver disease comprising the quinazolinone derivatives. According to the present invention, a method of preparing a compound represented by chemical formula 1 comprises the steps of: making a compound represented by chemical formula 2 react with a compound represented by chemical formula 3 to prepare a compound represented by chemical formula 4; deprotecting the compound represented by chemical formula 4 to prepare a compound represented by chemical 5; and making the compound represented by chemical formula 5 react with a compound represented by chemical formula 6 to prepare the compound represented by chemical formula 1. According to the present invention, the novel quinazolinone derivatives have useful effects in treatment of hematologic tumor or liver disease. Particularly, the novel quinazolinone derivatives have high selectivities compared to anticancer drugs of existing PI3Kδ inhibitors, remarkably reduce immunotoxicity by inhibiting PI3Kδ, and enable treatment of autoimmune diseases as well as anticancer treatment of hematologic malignancy or the like by inhibiting PI3Kδ and PI3Kγ at the same time. Such a targeted therapeutic agent has an advantage capable of solving side effect problems of existing highly toxic anticancer treatment.
机译:本发明涉及抑制PI3K的新型喹唑啉酮衍生物,喹唑啉酮衍生物的制备方法和包含该喹唑啉酮衍生物的用于治疗血液系统肿瘤或肝病的药物组合物。根据本发明,化学式1表示的化合物的制备方法包括以下步骤:使化学式2表示的化合物与化学式3表示的化合物反应以制备化学式4表示的化合物;将化学式4表示的化合物脱保护以制备化学式5表示的化合物;使化学式5表示的化合物与化学式6表示的化合物反应以制备化学式1表示的化合物。根据本发明,新型喹唑啉酮衍生物在血液肿瘤或肝脏疾病的治疗中具有有用的作用。特别地,与现有PI3Kδ抑制剂的抗癌药相比,新型喹唑啉酮衍生物具有高选择性,通过抑制PI3Kδ可显着降低免疫毒性,并且通过同时抑制PI3Kδ和PI3Kγ可实现自身免疫疾病的治疗以及血液系统恶性肿瘤的抗癌治疗等。时间。这种靶向治疗剂具有能够解决现有的高毒性抗癌治疗的副作用问题的优点。

著录项

  • 公开/公告号KR20180136930A

    专利类型

  • 公开/公告日2018-12-26

    原文格式PDF

  • 申请/专利权人 BIOWAY. INC.;

    申请/专利号KR1020180164132

  • 发明设计人 KIM JONG WOO;LEE CHI WOO;HONG SUJI;

    申请日2018-12-18

  • 分类号A61K31/52;A61K31/517;C07D239/88;C07D473/34;

  • 国家 KR

  • 入库时间 2022-08-21 11:52:12

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