公开(公告)号：EP3170823A1

公开(公告)日：2017-05-24

申请号：EP15822833.8

申请日：2015-07-14

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

发明人： NAN, Fajun ,  LI, Jia ,  LI, Jingya ,  ZHANG, Mei ,  CHEN, Dakai ,  ZHANG, Lina ,  ZHANG, Runtao ,  XIE, Zhifu

IPC分类号： C07D471/04 ,  C07D211/78 ,  A61K31/437 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00

CPC分类号： C07D471/04 ,  A61K31/437 ,  C07D211/78 ,  C12N9/12 ,  C12Y207/11031

摘要： Provided in the present invention are one class of pyrazolone compounds and a use thereof. In particular, provided in the present invention is a compound as represented by general formula I, wherein the definition of each group is as described in the description. The compounds of the present invention have a direct AMPK-activating activity and can significantly promote the phosphorylation of AMPK and ACC of L6 myocytes and HepG2 cells in a dose-dependent manner.

摘要翻译： 本发明提供了一类吡唑啉酮化合物及其用途。 特别是，本发明提供的是由通式I表示的化合物，其中每个基团的定义如说明书中所述。 本发明化合物具有直接的AMPK激活活性，并且可以剂量依赖性方式显着促进L6肌细胞和HepG2细胞的AMPK和ACC的磷酸化。

公开(公告)号：EP3763716A1

公开(公告)日：2021-01-13

申请号：EP19763907.3

申请日：2019-03-08

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

发明人： LIU, Hong ,  LI, Jia ,  WANG, Jiang ,  ZANG, Yi ,  LI, Jian ,  LI, Jingya ,  SUN, Dandan ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D495/04 ,  A61K31/55 ,  A61P1/16

摘要： Disclosed is use of a thiophene [3,2-d] pyrimidine-4-ketone compound represented by general formula (I). Definition of each substituent is as stated in the description and claims, and the compound is used for preparing medicines for treating and/or preventing liver fibrosis and related diseases or preparing a DPP-4 inhibitor, or is used as a DPP-4 inhibitor.

公开(公告)号：EP2786998A1

公开(公告)日：2014-10-08

申请号：EP12853993.9

申请日：2012-10-23

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

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.

摘要翻译： 公开了通式（I）所示的新的噻吩并[3,2-d]嘧啶-4-酮化合物，其制备方法，药物组合物及其药理用途。 这些化合物是强DPPIV（二肽肽酶IV）抑制剂，可以通过良好地抑制DPPIV来间接增加体内GLP-1的含量并在体内诱发一系列生理作用来治疗II型糖尿病。 因此，这些化合物可以作为治疗糖尿病的新药物开发。

公开(公告)号：EP2070926A1

公开(公告)日：2009-06-17

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 or their physiologically acceptable salts represented by the following formula, pharmaceutical compositions comprising the same, and uses thereof. The 13,13a-dihydroberberine derivatives have an activity of promoting glucose absorption in muscle cells, and the whole animal tests show that the present compounds have effects on improving glucose-tolerance and insulin-resistance, facilitating weight loss, relieving fatty liver and the like. Thus, the present compounds can be used in treating diabetes mellitus, adiposity, fatty liver and complications thereof induced by insulin resistance.

摘要翻译： 本发明提供由下式表示的13,13a-二氢小檗碱衍生物或其生理学上可接受的盐，其包含其的药物组合物及其用途。 13,13a-二氢小檗碱衍生物具有促进肌肉细胞中葡萄糖吸收的活性，整个动物试验表明，本发明化合物具有改善葡萄糖耐量和胰岛素抵抗，促进体重减轻，缓解脂肪肝等作用 。 因此，本发明化合物可用于治疗由胰岛素抵抗引起的糖尿病，肥胖，脂肪肝及其并发症。

公开(公告)号：EP3257856B1

公开(公告)日：2020-04-08

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

公开(公告)号：EP3434678A1

公开(公告)日：2019-01-30

申请号：EP17769445.2

申请日：2017-03-22

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 ,  A61P9/12 ,  A61P9/10 ,  A61P13/12 ,  A61P25/00 ,  A61P9/00 ,  A61P27/02

摘要： The present invention relates to a salt form of (R)-methyl-2-(3-aminopiperidin-1 -yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothioph ene[3,2-d]pyrimidine-6-carboxylic acid and a preparation method for the salt form. Also disclosed is a pharmaceutical composition of the formula I compound salt form. The salt form of the present invention provides powerful in vivo hypoglycemic activity and is expected to be a novel pharmaceutical active ingredient for treating or preventing diabetes mellitus type 2 and/or complications of diabetes mellitus type 2

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.