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公开(公告)号：EP3124486B1
公开(公告)日：2020-12-09
申请号：EP15769858.0
申请日：2015-03-21
发明人： DONG, Xiaowu , YANG, Bo , LI, Jia , ZHAN, Wenhu , WENG, Qinjie , ZHOU, Yubo , HU, Yongzhou , XU, Lei , LIU, Tao , HE, Qiaojun
IPC分类号： C07D405/14 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D401/12 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/506 , A61K31/497 , A61K31/4155 , A61K31/5377 , A61P35/00 , A61P35/02
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公开(公告)号：EP3904343A1
公开(公告)日：2021-11-03
申请号：EP19904796.0
申请日：2019-12-04
发明人： SHENG, Rong , LI, Jia , GU, Dongyan , ZHOU, Yubo , WEI, Jun , ZHANG, Mengmeng , HU, Yongzhou , ZHANG, Kaixiang , LIU, Jieyu , KAN, Weijuan
IPC分类号： C07D239/95 , C07D401/12 , C07D403/12 , C07D417/12 , C07D413/14 , C07D473/00 , C07D491/056 , A61K31/517 , A61K31/5377 , A61K31/519 , A61K31/506 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/08 , A61P11/06 , A61P19/02 , A61P19/08 , A61P11/00 , A61P17/06 , A61P13/12
摘要： Provided by the present invention are an amino quinazolinone and amino isoquinolone derivatives. It is verified by numerous experiments that the compounds provided by the present invention have good inhibiting effects on PI3Kα and PI3Kγ, most of the compounds have prominent inhibiting effect on PI3Kα, and show strong growth inhibiting effect on PIK3CA mutant tumor cells such as human breast cancer cell strain (MCF7). Therefore, the amino quinazolinone and amino isoquinolone derivatives according to the present invention can be applied in the preparation of anti-tumor and anti-inflammatory medicines, and can be used as PI3Kα inhibitors in the preparation of medicines for treatment of human or animal cell proliferation related tumors, the medicines comprising the derivatives any one or more of pharmaceutically acceptable salts and solvates thereof as well as pharmaceutically acceptable carriers. Formulas a and b for the compounds of the present invention are shown as below:
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3.发明公开
公开(公告)号：EP3530656A1
公开(公告)日：2019-08-28
申请号：EP17869906.2
申请日：2017-11-08
发明人： LIU, Tao , LI, Jia , HU, Yongzhou , ZHOU, Yubo , DONG, Xiaowu , GAO, Anhui , SONG, Pinrao , WANG, Peipei , TONG, Lexian , HU, Xiaobei , SU, Mingbo
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
摘要： A 2-substituted aromatic ring-pyrimidine derivative as shown in a general fomula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chkl inhibitors by using N -substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chkl kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chkl kinase inhibitory activity and are promising Chkl inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.
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4.发明公开SUBSTITUTED NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND APPLICATIONS OF ANTITUMOR THEREOF 审中-公开取代的含氮杂环衍生物，药物组合物ORDER及抗肿瘤它们的应用
公开(公告)号：EP3124486A1
公开(公告)日：2017-02-01
申请号：EP15769858.0
申请日：2015-03-21
发明人： DONG, Xiaowu , YANG, Bo , LI, Jia , ZHAN, Wenhu , WENG, Qinjie , ZHOU, Yubo , HU, Yongzhou , XU, Lei , LIU, Tao , HE, Qiaojun
IPC分类号： C07D405/14 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D401/12 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/506 , A61K31/497 , A61K31/4155 , A61K31/5377 , A61P35/00 , A61P35/02
CPC分类号： C07D417/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.
摘要翻译： 本发明公开了新的取代的由式（I）表示的杂环衍生物作为AKT抑制剂，光学异构体，药学上可接受的盐或溶剂化物，含氮其中R1，R2，R3，R4，R5，R6，环A，环C的定义 ，B，Q，Y，Z和m表示在对细节的描述。 此外，药物，其包含衍生物作为活性成分因此游离缺失盘，其可用于治疗增殖性疾病，：如癌症和炎症，特别是爱疾病有关AKT激酶是有用的。
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公开(公告)号：EP3530657A1
公开(公告)日：2019-08-28
申请号：EP17870509.1
申请日：2017-11-08
发明人： LIU, Tao , LI, Jia , HU, Yongzhou , ZHOU, Yubo , DONG, Xiaowu , GAO, Anhui , SONG, Pinrao , WANG, Peipei , TONG, Lexian , HU, Xiaobei , SU, Mingbo
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D409/14 , C07D405/14 , A61K31/506 , A61P35/00
摘要： The present invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof, the compound, and an optical isomer thereof or a pharmaceutically thereof acceptable salts or solvates can be used in the preparation of anti-tumor drugs. The invention designs and synthesizes a series of novel small molecule Chkl inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained by structure-based virtual screening as a lead compound, and carries out Chkl kinase inhibitory activity test. The experiment confirmed that said compounds possess potent anticancer activity, Chkl kinase inhibitory activity, and are promising Chkl inhibitors, and can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal. The 2-polysubstituted aromatic ring-pyrimidine derivatives provided by the present invention has the structure of the formula I:
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6.发明公开TRIPEPTIDE EPOXYKETONE COMPOUND CONSTRUCTED BY HETEROCYCLE AND PREPARATION METHOD AND USE THEREOF 审中-公开与杂环流构建三肽EPOXYKETONVERBINDUNGEN和方法及用途
公开(公告)号：EP3127912A1
公开(公告)日：2017-02-08
申请号：EP15773896.4
申请日：2015-03-11
发明人： HU, Yongzhou , LI, Jia , LIU, Tao , ZHANG, Jiankang , ZHOU, Yubo , YANG, Bo , HE, Qiaojun , XU, Lei , HU, Xiaobei
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/06043 , C07K5/06121 , C07K5/0808 , Y02P20/55
摘要： Disclosed are a tripeptide epoxyketone compound, a preparation method thereof, and a use thereof in the preparation of anti-tumor drugs.
摘要翻译： 本发明公开了一种三肽环氧酮化合物，其制备方法，和在抗肿瘤的药物的制备及其用途。
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公开(公告)号：EP3434677A1
公开(公告)日：2019-01-30
申请号：EP17769393.4
申请日：2017-03-20
发明人： LIU, Hong , WANG, Jiang , LI, Jian , LI, Jia , LI, Jingya , JIANG, Hualiang , LUO, Xiaomin , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61P3/10
摘要： A polymorph of (R) methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothioph ene[3,2-d]pyrimidine-6-carboxylic acid maleate and a preparation method therefor. The polymorph is a crystal having high stability and low hygroscopicity, and the crystal form is selected from crystal form A, crystal form B and crystal form C. Furthermore, the crystal form has a strong in-vivo hypoglycemic activity and can be used for the preparation of a novel drug for the treatment or prevention of diabetes mellitus type H and/or complications of diabetes mellitus type H.
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8.发明公开
公开(公告)号：EP3315502A1
公开(公告)日：2018-05-02
申请号：EP16813720.6
申请日：2016-06-23
发明人： LIU, Hong , LI, Jia , WANG, Jiang , LI, Jingya , CHEN, Hui , LI, Dan , LI, Jian , WANG, Yibing , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D493/10 , A61K31/35 , A61K31/381 , A61K31/427 , A61K31/4436 , A61P3/10 , A61P3/04 , A61P9/10
CPC分类号： C07H19/01 , A61K31/35 , A61K31/381 , A61K31/427 , A61K31/4436 , A61P3/08 , C07D493/10
摘要： The present invention provides C, O-spiro aryl glycoside compounds, preparation therefor and use thereof. Specifically provided are the compounds represented by the formula (I), wherein the definitions of each group are described in the specification. The compound can be used as SGLT2 inhibitors in preparing the pharmaceutical compositions for treating diseases such as diabetes, atherosclerosis, adiposity and etc.
摘要翻译： 本发明提供C，O-螺芳基糖苷化合物，其制备方法及其用途。 具体提供了由式（I）表示的化合物，其中每个基团的定义在说明书中描述。 该化合物可以作为SGLT2抑制剂用于制备治疗糖尿病，动脉粥样硬化，肥胖症等疾病的药物组合物。
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9.发明公开SIX-MEMBERED RING BENZO DERIVATIVES AS DPP-4 INHIBITOR AND USE THEREOF 审中-公开作为DPP-4抑制剂的六元环苯并噻吩衍生物及其用途
公开(公告)号：EP3214079A1
公开(公告)日：2017-09-06
申请号：EP15855852.8
申请日：2015-10-30
申请人： East China University Of Science And Technology , Shanghai Institute of Materia Medica, Chinese Academy of Sciences
发明人： LI, Honglin , JIANG, Hualiang , XU, Yufang , LI, Jia , ZHAO, Zhenjiang , LI, Jingya , XU, Hongling , LI, Shiliang
IPC分类号： C07D311/92 , C07D405/04 , C07D417/04 , C07D221/10 , C07D335/04 , A61K31/352 , A61K31/5377 , A61P3/00 , A61P3/10 , A61P7/10 , A61P29/00
摘要： The present invention relates to six-membered ring benzo derivatives as a DPP-4 inhibitor anda use thereof. In particular, the present invention relates to a compound as shown in formula I, a pharmaceutical composition containing the compound as shown in formula I and a use of the compound in the preparation of drugs for treating DPP-4 related diseases or inhibiting DPP-4.
摘要翻译： 本发明涉及作为DPP-4抑制剂的六元环苯并衍生物及其用途。 具体地说，本发明涉及如式I所示的化合物，含有式I所示化合物的药物组合物以及该化合物在制备治疗DPP-4相关疾病或抑制DPP-4的药物中的用途 。
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10.发明授权13,13A-DIHYDROBERBERINE DERIVATIVES, THEIR PHARMACEUTICAL COMPOSITION AND USE 有权13,13a-DIHYDROBERBERINDERIVATE，及其药物组合物使用
公开(公告)号：EP2070926B1
公开(公告)日：2011-09-07
申请号：EP07816496.9
申请日：2007-09-30
发明人： HU, Lihong , YE, Jiming , LI, Jingya , JAMES, David, E , KRAEGEN, Edward, W , ZHANG, Hankun , CHENG, Zhe , LI, Jia
IPC分类号： C07D455/03 , A61K31/4375 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D455/03
摘要： The present invention provides 13,13a-dihydroberberine derivatives as shown below, their physiologically acceptable salts, use and pharmaceutical composition comprising the said derivatives. The said 13,13a-dihydroberberine derivatives are glucose sorbefacient to muscle cells and have medical effects for improving glucose-tolerance and insulin-resistance, facilitating weight loss, relaxing fatty liver, etc, approved by tests to integer animals. The said compounds of the present invention can be used for treating diabetes mellitus, adiposity, fatty liver and their complications caused by insulin resistance.
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