公开(公告)号：EP4458820A1

公开(公告)日：2024-11-06

申请号：EP22914967.9

申请日：2022-12-28

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

发明人： LIU, Hong ,  LI, Jia ,  WANG, Jiang ,  ZANG, Yi ,  CHEN, Feiyang ,  GAO, Lixin ,  ZHAO, Jing ,  SUN, Dandan ,  WANG, Ke'an ,  JIANG, Hualiang ,  XIE, Rongrong

IPC分类号： C07D403/12 ,  C07D403/14 ,  C07D401/12 ,  C07D401/14 ,  C07D407/14 ,  C07C409/14 ,  C07D471/00 ,  C07D405/14 ,  C07K14/705 ,  C07K14/72 ,  A61K31/53 ,  A61P1/16 ,  A61P9/10 ,  A61P9/12 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P3/00 ,  A61P9/00

摘要： Provided in the present invention are a class of quinoline compounds and a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided in the present invention are a compound as shown in formula(I), and a stereoisomer, a deuterated compound, a solvate, a metabolite, a pharmaceutically acceptable salt, a eutectic or a prodrug thereof, and a pharmaceutical composition thereof. Further provided in the present invention are a preparation method for the compound and the use thereof in the preparation of a drug for treating diseases mediated by thyroid hormone receptors. Related diseases include, but are not limited to, diseases such as non-alcoholic fatty liver diseases, atherosclerosis, coronary heart disease, hypertension, hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, dyslipidemia, obesity, diabetes, metabolic disorders, lipid metabolism disorders, 1A type glycogen storage diseases, hypothyroidism and thyroid cancer.

公开(公告)号：EP4446326A1

公开(公告)日：2024-10-16

申请号：EP22903630.6

申请日：2022-12-12

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

发明人： SHEN, Jingshan ,  GAO, Zhaobing ,  XIAO, Gengfu ,  LI, Jia ,  YANG, Feipu ,  ZHANG, Leike ,  XIA, Bingqing ,  JIANG, Xiangrui ,  HE, Yang ,  JIANG, Hualiang

IPC分类号： C07D491/18 ,  A61K31/4748 ,  A61P31/12 ,  A61P31/14 ,  A61P19/10 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P25/00 ,  A61P27/00 ,  A61P43/00

摘要： The present invention provides a cyclic bisbenzyl tetrahydroisoquinoline compound as represented by formula (I), and a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, a racemate, a crystalline hydrate, and a solvate thereof, wherein R 1 and R 2 are as defined in the description. The present invention further provides a method for preparing the compound and the use of the compound for the preparation of an inhibitor for inhibiting viruses, inflammation, fibrosis and abnormal differentiation of T cells and/or for the preparation of a drug for preventing and/or treating related diseases caused by viruses, such as respiratory tract infections and pneumonia, inflanmmation-related diseases, fibrosis-related diseases and autoimmune diseases.

公开(公告)号：EP4434980A1

公开(公告)日：2024-09-25

申请号：EP22895006.9

申请日：2022-11-22

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 ,  WU, Yizhe ,  HU, Xiaobei ,  SU, Mingbo

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/4427 ,  A61P35/00 ,  A61P37/00

CPC分类号： A61K31/4427 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

摘要： Disclosed in the present invention are a Bruton's tyrosine kinase degrading agent, which has a structure represented by general formula 1, or a stereoisomer, a mixture of stereoisomers, or a pharmaceutically acceptable salt and a prodrug thereof, Further disclosed are the uses of the compound and a pharmaceutical composition containing same in the preparation of a drug for treating Bruton's tyrosine kinase-related diseases such as B cell or plasma cell proliferative diseases, The compound of the present invention has potent cell proliferation inhibitory activity, effectively degrades Bruton's tyrosine kinase, and has a good liver particle metabolism stability and good oral absorption properties. The compound can be used alone in drugs or in combination with other drugs for treating a disease, disorder or condition that benefits from the inhibition of the Bruton's tyrosine kinase activity or degradation of the Bruton's tyrosine kinase.

公开(公告)号：EP4001267A1

公开(公告)日：2022-05-25

申请号：EP20844824.1

申请日：2020-07-17

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

发明人： XIONG, Bing ,  LI, Jia ,  GENG, Meiyu ,  SHEN, Jingkang ,  ZANG, Yi ,  AI, Jing ,  CHEN, Danqi ,  WANG, Qi ,  DONG, Ying ,  PENG, Xia ,  JI, Yinchun ,  TAN, Qian

IPC分类号： C07D239/84 ,  A61K31/517 ,  A61P35/00

摘要： The present disclosure relates to a fused ring pyrimidine amino compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically disclosed in the present disclosure are the compound shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof. The fused ring pyrimidine amino compound of the present application has good inhibitory activity against DDRs, particularly DDR2, and has a good therapeutic effect on tumors and fibrotic diseases, especially pulmonary inflammation and pulmonary fibrosis. Also disclosed in the present disclosure are a preparation method for the compound shown in formula I, and a use thereof.

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：EP1640367B1

公开(公告)日：2011-02-09

申请号：EP04738186.8

申请日：2004-05-31

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

发明人： NAN, Fajun ,  LI, Jia ,  CHEN, Yihua ,  ZHANG, Yahui ,  GU, Min ,  ZHANG, Huajie

IPC分类号： C07D217/04 ,  A61P25/00 ,  A61P25/28

CPC分类号： C07D417/04 ,  C07D217/24

摘要： The invention relates to all types of substituted isoquinoline -1,3,4-trione, the synthetic method thereof and the use for treatding neurodegenerative diseases , especially as the medicine for Alzhermer's disease, appplexy and brain ischernic injuries, the compound is represented by the structure, Formula (I); Dihydroisoquinoline-1,3,4-trione) wherein substituents R, can be one , two or three groups optionally selected from the group consisting of H; alkyl; hydroxyl; alkyl substituted by the groups including halogen , alkoxyl, hydroxyl; alkyl or alkylamine substituted by the groups including halogen , alkoxyl, hydroxyl; C,-,alkenyl substituted by oxygen or amine; C, 6cycloalkyl; substituted aryl; benzyl; alkanoyl; alkanoyl substituted by the groups including halogen , alkoxyl, hydroxyl; C2-6enc,yl ; C,-,cycloalkanoyl; tert­butoxycarbonyl; benzoyl; benzoyl. substituted by one, two or three groups including alkylarnine; benzylacryl; benzylacryl. substituted by one, two or three groups including alkylamine; thienylfonnyl; admantyliForrnyl; mandeloyl; alkoxyl; alkylamine; cycloalkoxyl; cycloalkoxycarbonyl; alkanoylxy; alkanoylamine; cycloalkyanoylxy; cycloalkanoylarnine; ureido; urenylene; alkanoyl; nitro; carboxyl; R2 is H; alkyl; alkyl. or Cl-C4cycloalkyl which are substituted by the groups including halogen, alkoxyl, hydroxyl; C2-C,alkenyl; acryl; substituted acryl; X is H, CH2, N-H, 0, S; is CH, N.

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。