公开(公告)号：EP2860181A4

公开(公告)日：2015-11-18

申请号：EP13775600

申请日：2013-04-09

申请人： SHANGHAI YINGLI PHARMACEUTICAL CO LTD

发明人： XU ZUSHENG

IPC分类号： C07D495/04 ,  A61K31/5377 ,  A61K31/5386 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  C07D491/048 ,  C07D519/00

CPC分类号： C07D495/04 ,  C07D491/048 ,  C07D519/00

摘要： Disclosed are a fused pyrimidine compound as represented by formula I, pharmaceutically acceptable salt, hydrate or solvate thereof, an optical isomer or a prodrug thereof, as well as a preparation method, an intermediate, a composition and uses thereof. The fused pyrimidine compound according to the present invention can inhibit activity of PI3 kinase, and can be used to treat diseases such as cancer caused by abnormal activity of the PI3 kinase, or can be used to prepare medicine for treating these diseases.

摘要翻译： 本发明公开了由式I，药学上可接受的盐，水合物或溶剂化物，光学异构体或其前药，以及其制备方法，中间体，组合物和其用途的稠合嘧啶化合物。 的稠合嘧啶化合物gemäß到本发明能够抑制PI3激酶的活性，并且可用于治疗疾病：如癌症由PI3激酶的异常活性引起的，或可用于用于治疗疾病的论文制备药物。

公开(公告)号：EP3059238A4

公开(公告)日：2017-04-12

申请号：EP14853907

申请日：2014-09-19

申请人： SHANGHAI YINGLI PHARMACEUTICAL CO LTD

发明人： XU ZUSHENG ,  LOU YANGTONG

IPC分类号： C07D413/14 ,  A61K31/5377 ,  A61P3/00 ,  A61P5/00 ,  A61P9/00 ,  A61P11/06 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  C07D413/04 ,  C07D473/34 ,  C07D487/04 ,  C07D495/04

CPC分类号： C07D401/14 ,  C07D239/84 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D473/34 ,  C07D487/04 ,  C07D495/04

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。

公开(公告)号：EP3275867A4

公开(公告)日：2018-01-31

申请号：EP16767632

申请日：2016-02-01

申请人： SHANGHAI YINGLI PHARMACEUTICAL CO LTD

发明人： XU ZUSHENG ,  ZHANG NONG ,  SUN QINGRUI ,  WU TIANZHI

IPC分类号： C07D217/00 ,  A61K31/472 ,  A61K31/517 ,  A61P3/00 ,  C07D231/56 ,  C07D237/30 ,  C07D239/78 ,  C07D333/60 ,  C07D405/04 ,  C07D471/04 ,  C07D495/04

CPC分类号： A61K31/472 ,  A61K31/517 ,  C07D217/00 ,  C07D231/56 ,  C07D237/30 ,  C07D239/78 ,  C07D333/60 ,  C07D405/04 ,  C07D471/04 ,  C07D495/04

摘要： Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.

公开(公告)号：EP3053926A4

公开(公告)日：2017-05-03

申请号：EP14847916

申请日：2014-09-17

申请人： SHANGHAI YINGLI PHARMACEUTICAL CO LTD

发明人： XU ZUSHENG

IPC分类号： C07D495/04 ,  A61K31/5377 ,  A61K31/5386 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  C07D491/048 ,  C07D519/00

CPC分类号： C07D495/04 ,  C07D491/048 ,  C07D493/04 ,  C07D519/00

摘要： Disclosed are a fused pyrimidine compound, an intermediate, a preparation method therefor, and a composition and an application thereof. The present invention provides a fused pyrimidine compound shown in formula I, pharmaceutically acceptable salt, hydrate, solvate, and an optical isomer or prodrug of the compound. The present invention further provides applictions of the fused pyrimidine compound shown in formula I, the pharmaceutically acceptable salt, the hydrate, solvate, and the optical isomer or the prodrug of the compound in the preparing drugs for curing and/or preventing a kinase-related disease. The fused pyrimidine compound I of the present invention is an efficient PI3 kinase depressor, and can be used to prepare drugs for preventing and/or curing cell-proliferation diseases such as cancer, infection, inflammation, and an autoimmune disease.

摘要翻译： 本发明公开了稠合的嘧啶化合物，中间体，用于其的制备方法，和一种组合物并涉及其应用。 本发明提供了式I中，药学上可接受的盐，水合物，溶剂化物表示的稠合嘧啶化合物，以及旋光异构体或该化合物的前药。 本发明进一步提供了式I中，药学上可接受的盐，水合物，溶剂化物，以及光学异构体或该化合物的在制备药物的前体药物用于治疗和/或预防激酶相关所示的稠合嘧啶化合物的applictions 疾病。 本发明的稠合嘧啶化合物I是一种有效的PI3激酶抑制剂，并且可用于预防和/或固化的细胞增殖性疾病的药物制备：如癌症，感染，炎症和自身免疫性疾病。