PREPARATION METHOD FOR MORPHOLINQUINAZOLINE COMPOUND AND MIDBODY THEREOF

    公开(公告)号:EP3912978A1

    公开(公告)日:2021-11-24

    申请号:EP19910900.0

    申请日:2019-12-24

    摘要: The present disclosure relates to a preparation method morpholinquinazoline compound and a midbody thereof. The preparation method for morpholinquinazoline compound comprises the following steps: S1, performing a Suzuki reaction of compound S and compound IV as represented by the following formula, so as to obtain compound V; step S2, performing a reaction of methylsufonyl chloride and compound V in an organic solvent as represented by the following formula, so as to obtain compound VI; and S3, performing a coupled reaction of compound VII and compound VI in a solvent as represented by the following formula, so as to obtain compound YY-20394. The preparation method has the advantages of higher yield, better selectivity, simple operation and mild reaction condition, and is applicable to industrial production.

    FUSED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USES THEREOF
    4.
    发明公开
    FUSED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USES THEREOF 审中-公开
    稠合杂环化合物,用于生产该药物组合物及其用途

    公开(公告)号:EP3059238A4

    公开(公告)日:2017-04-12

    申请号:EP14853907

    申请日:2014-09-19

    摘要: Disclosed are a fused heterocyclic compound, a preparation method therefor, a pharmaceutical composition, and uses thereof. The fused heterocyclic compound is shown in formula I, formula II, or formula III. The preparation method of the fused heterocyclic compound and/or the pharmaceutically acceptable salt thereof in the present invention comprises three synthesizing routes. The present invention also provides a pharmaceutical composition of the fused heterocyclic compound, the pharmaceutical composition containing one or more of the fused heterocyclic compound shown in formula I, formula II, or formula III, the pharmaceutically acceptable salt thereof, hydrates, solvent compounds, polymorphs and prodrugs thereof, and a pharmaceutically acceptable carrier. The present invention also relates to an application of the fused heterocyclic compound and/or the pharmaceutical composition in preparing kinase inhibitors and in preparing drugs for preventing and treating diseases related to kinase. The fused heterocyclic compound of the present invention has selective inhibition function on PI3K ´ , and can be used for preparing drugs for preventing and treating cell proliferation diseases such as cancers, infections, inflammations, or autoimmune diseases.

    摘要翻译: 本发明公开了稠合的杂环化合物,其制备方法为此,药物组合物,及其用途。 所述稠合杂环化合物示于式I,式II或式III。 所述稠合杂环化合物和/或在本发明的药学上可接受的盐的制备方法包括三个合成路线。 本发明因此提供了稠合杂环化合物的药物组合物,在式I,式II或式III中,药学上可接受的盐,水合物,溶剂化合物,多晶型示出为包含稠合杂环化合物的一种或多种药物组合物 和前药,以及药学上可接受的载体。 因此,本发明涉及对稠合杂环化合物和/或在制备激酶抑制剂的药物组合物的应用和在制备药物用于预防和治疗有关疾病的激酶。 本发明的稠合杂环化合物对PI3K”选择性抑制功能,并且可以被用于制备药物用于预防和治疗细胞增殖性疾病:如癌症,感染,炎症或自身免疫疾病。