公开(公告)号：EP4353706A1

公开(公告)日：2024-04-17

申请号：EP22806814.4

申请日：2022-05-11

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： NAN, Fajun ,  LI, Jingya ,  ZHANG, Zheng ,  DUAN, Yanan ,  ZHANG, Yangming ,  CHEN, Dandan ,  DAI, Chengqiu

IPC分类号： C07C39/08 ,  C07C39/19 ,  C07C39/24 ,  A61K31/05 ,  A61P3/00

CPC分类号： A61K31/05 ,  A61K31/055 ,  A61K31/085 ,  A61K31/09 ,  A61K31/136 ,  A61K31/18 ,  A61K31/341 ,  A61K31/381 ,  A61K31/404 ,  A61K31/426 ,  A61K31/44 ,  A61K31/513 ,  A61K31/664 ,  A61P1/16 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07C39/08 ,  C07C39/10 ,  C07C39/15 ,  C07C39/17 ,  C07C39/19 ,  C07C39/24 ,  C07C39/367 ,  C07C43/20 ,  C07C43/23 ,  C07C215/76 ,  C07C233/25 ,  C07C233/27 ,  C07C233/29 ,  C07C233/75 ,  C07C255/30 ,  C07C261/04 ,  C07C307/10 ,  C07C311/08 ,  C07C311/11 ,  C07C311/14 ,  C07C311/21 ,  C07D209/08 ,  C07D213/69 ,  C07D213/74 ,  C07D239/54 ,  C07D239/56 ,  C07D277/36 ,  C07D307/42 ,  C07D333/16 ,  C07D333/34 ,  C07F9/24

摘要： Provided in the present invention are a class of alkylphenol compounds and a preparation method therefor. Specifically provided in the present invention are a new alkyl polyphenol compound as represented by chemical formula I, and a preparation method therefor and the use thereof in the treatment of metabolic syndrome.

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

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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.

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

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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。

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 。

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

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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.

公开(公告)号：EP3214079B1

公开(公告)日：2020-06-24

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

公开(公告)号：EP3421447A1

公开(公告)日：2019-01-02

申请号：EP17755775.8

申请日：2017-02-20

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： NAN, Fajun ,  LI, Jia ,  LI, Jingya ,  ZHANG, Mei ,  XIE, Zhifu ,  WANG, Jingtao ,  GUO, Dongdong

IPC分类号： C07C57/13 ,  C07C61/35 ,  C07C57/42 ,  C07C55/28 ,  C07C51/09 ,  A61K31/194 ,  A61P3/04 ,  A61P3/10

摘要： The present invention relates to a class of fatty acid compounds, a preparation method thereof and use thereof. The fatty acid compounds have the structure of the formula I, which has the ability to activate APMK and inhibit the glucose output in mouse primary hepatocytes. The fatty acid compounds can be used in preparing a medicament for the treatment of obesity or diabetes.

公开(公告)号：EP2133342A1

公开(公告)日：2009-12-16

申请号：EP08706537.1

申请日：2008-02-26

申请人： Shanghai Institute Of Materia Medica Chinese Academy of Sciences

发明人： NAN, Fajun ,  LI, Jia ,  WEI, Yi ,  ZHANG, Wei ,  LI, Jingya ,  SHI, Lei

IPC分类号： C07D277/22 ,  C07D263/32 ,  C07D213/55 ,  C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  A61K31/421 ,  A61K31/44 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D277/30 ,  C07D417/12

摘要： PTP1B inhibitors with the following structure (formula I). Experiments indicate that these inhibitors can effectively inhibit the activity of protein tyrosine phosphatase 1B (PTP1B). They can be used as insulin sensitisers. They can be used to prevent, delay or treat diseases which are related to insulin antagonism mediated by PTP1B, especially diabetes type II and obesity. The invention also provides methods for preparing these inhibitors.

摘要翻译： 具有以下结构的PTP1B抑制剂（式I）。 实验表明，这些抑制剂可有效抑制蛋白酪氨酸磷酸酶1B（PTP1B）的活性。 它们可以用作胰岛素敏化剂。 它们可用于预防，延迟或治疗与PTP1B介导的胰岛素拮抗相关的疾病，特别是II型糖尿病和肥胖症。 本发明还提供了制备这些抑制剂的方法。

公开(公告)号：EP4406935A1

公开(公告)日：2024-07-31

申请号：EP22872031.4

申请日：2022-09-21

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： NAN, Fajun ,  LI, Jingya ,  CHEN, Yi ,  SONG, Gaolei ,  XIE, Zhifu ,  FANG, Yanfen ,  ZHANG, Mei ,  SUN, Xinyu ,  CAO, Lei ,  MA, Hui ,  YANG, Yurou

IPC分类号： C07C57/13 ,  C07C57/42 ,  C07C61/35 ,  C07C55/28 ,  A61P3/10 ,  A61P3/04 ,  A61P35/00 ,  A61K31/194

CPC分类号： A61K31/201 ,  A61K31/225 ,  A61K31/194 ,  A61K31/496 ,  A61K38/05 ,  A61P1/16 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  A61P35/00 ,  A61P35/02 ,  C07C55/28 ,  C07C57/13 ,  C07C57/42 ,  C07C61/35 ,  C07C69/74 ,  C07D401/14 ,  C07K5/06017

摘要： A long-chain compound, a preparation method therefor and the use thereof are disclosed. The structure of said compound is represented by formula (I). The definition of each substituent in the formula is as set out in the description and claims. The compound of the present invention can directly inhibit ACLY, inhibit lipid synthesis in primary hepatocytes, inhibit lipid de novo synthesis and histone acetylation in various cancer cells such as H358, and inhibit cancer cell proliferation. The compound may be used to prepare drugs that treat metabolic diseases such as hyperlipidemia and atherosclerosis or various cancers such as lung cancer, pancreatic cancer, breast cancer, ovarian cancer, liver cancer, intestinal cancer, brain cancer, and acute myeloid leukemia.

公开(公告)号：EP3257856A1

公开(公告)日：2017-12-20

申请号：EP16748699.2

申请日：2016-02-03

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： LIU, Hong ,  WANG, Jian ,  LI, Jian ,  LI, Jia ,  LI, Jingya ,  ZHOU, Shengbin ,  SU, Mingbo ,  JIANG, Hualiang ,  LUO, Xiaomin ,  CHEN, Kaixian

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P3/10

摘要： The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.

摘要翻译： 本发明涉及化合物的晶型A. 本发明还公开了晶型A的制备方法和药物组合物。晶型A在体内具有强烈的降血糖活性，并且预期为用于治疗或预防II型糖尿病和/或并发症的新型药物活性成分 II型糖尿病。