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公开(公告)号：EP2786998B1
公开(公告)日：2018-07-25
申请号：EP12853993.9
申请日：2012-10-23
申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Cisen Pharmaceutical Co., Ltd.
发明人： LIU, Hong , LI, Jia , LI, Jian , LI, Jingya , WANG, Jiang , SU, Mingbo , LIAN, Jie , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61K31/55 , A61P3/10
CPC分类号： C07D495/04
摘要： Disclosed are new thienyl [3, 2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.
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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：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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4.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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5.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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6.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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公开(公告)号：EP4342892A1
公开(公告)日：2024-03-27
申请号：EP22832202.0
申请日：2022-06-30
申请人： Hangzhou Healzen Therapeutics Co., Ltd. , Shanghai Institute of Materia Medica, Chinese Academy of Sciences
发明人： ZHOU, Xinglu , LI, Jia , LIU, Xingguo , ZHOU, Yubo , HU, Miao , LUO, Xiaomin , XIE, Jiangfeng , KAN, Weijuan , SU, Mingbo , WU, Yizhe
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , A61P35/00 , A61K31/4427
摘要： Disclosed are a Bruton's tyrosine kinase and a mutant degrader thereof, or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, and an application thereof in the preparation of a drug for treating diseases, disorders or conditions that would benefit from the degradation of the Bruton's tyrosine kinase and the mutant thereof. The compound of the present invention can degrade BTK protein, can degrade BTKC481S protein, has an anti-proliferation inhibiting effect on tumor cell strains Mino and OCI-LY10, shows good anti-tumor activity in an OCI-LY10 subcutaneous transplantation tumor model, has an inhibiting effect on B cell activation, and can be applied to B cell or plasma cell proliferative diseases and autoimmune diseases. The compound of the present invention has good oral absorption properties, and can be applied to oral treatment of human or animal B cell or plasma cell proliferative diseases and autoimmune diseases.
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8.发明公开
公开(公告)号：EP4328228A1
公开(公告)日：2024-02-28
申请号：EP22806337.6
申请日：2022-03-30
发明人： ZHOU, Bing , LI, Jia , ZHOU, Yubo , YANG, Xiangbo , FENG, Bo , YANG, Yaxi , HU, Xiaobei
IPC分类号： C07D491/107 , A61K31/497 , A61K31/506 , A61P35/00
摘要： The present invention relates to a heterocyclic compound for inhibiting SHP2 activity that is represented by formula I, a preparation method therefor and use thereof. The compound of the present invention is effective in treating a disease or disorder or condition mediated by SHP2.
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公开(公告)号：EP4223757A1
公开(公告)日：2023-08-09
申请号：EP21874475.3
申请日：2021-09-28
发明人： XU, Huaqiang , LI, Jia , SHI, Jingjing , ZANG, Yi , SUN, Dandan , LIU, Mingliang , XIE, Rongrong , YOU, Erli , GAO, Lixin , TAN, Qian
IPC分类号： C07D471/08 , A61K31/46
摘要： A strong FXR small-molecule agonist, and a preparation method therefor and use thereof, the structure of the agonist being represented by formula (I). In the formula, each substituent is as defined in the description and the claims. The compound provided by the present invention has the advantages of high FXR agonist activity, simple synthesis, easily available raw materials and the like, and can be used for preparing medicines for treating FXR related diseases.
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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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