公开(公告)号：US10662187B2

公开(公告)日：2020-05-26

申请号：US16070520

申请日：2017-01-17

Applicant: Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Xibin Liao ,  Jia Li ,  Zhijian Lu ,  Yubo Zhou ,  Anhui Gao

IPC: C07D471/04 ,  C07D231/56 ,  A61K45/06 ,  A61K31/437 ,  A61K31/42 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/519 ,  A61P35/00 ,  A61P37/00

Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):

公开(公告)号：US20190375727A1

公开(公告)日：2019-12-12

申请号：US16348502

申请日：2017-11-08

Applicant: ZHEJIANG UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Tao Liu ,  Jia Li ,  Yongzhou Hu ,  Yubo Zhou ,  Xiaowu Dong ,  Anhui Gao ,  Pinrao Song ,  Peipei Wang ,  Lexian Tong ,  Xiaobei Hu ,  Mingbo Su

IPC: C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D413/14 ,  C07D405/14 ,  C07D409/14 ,  A61P35/00

Abstract: A 2-substituted aromatic ring-pyrimidine derivative as shown in a general formula 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 Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chk1 kinase inhibitory activity and are promising Chk1 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.

公开(公告)号：US20190194185A1

公开(公告)日：2019-06-27

申请号：US16089713

申请日：2017-03-29

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Hong Liu ,  Yiping Wang ,  Fei Zhao ,  Jing Zhao ,  Jiang Wang ,  Cong Xi ,  Chenglin Wu ,  Hao Shen ,  Xu Han ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D459/00 ,  C07D495/22 ,  A61P3/06

CPC classification number: C07D459/00 ,  A61K31/4745 ,  A61P3/06 ,  C07D471/14 ,  C07D491/22 ,  C07D495/22

Abstract: The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of drugs for treating diseases related to a proprotein convertase subtilisin Kexin-9 (PCSK9), comprising the applications in the preparation of drugs for treating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty liver deformation, atherosclerosis, obesity and other metabolic diseases.

公开(公告)号：US20190039989A1

公开(公告)日：2019-02-07

申请号：US16075528

申请日：2017-02-20

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

IPC: C07C61/35 ,  C07C57/13 ,  C07C57/26

CPC classification number: C07C61/35 ,  A61K31/194 ,  C07C55/28 ,  C07C57/13 ,  C07C57/26 ,  C07C57/42 ,  C07C61/16 ,  C07C61/20 ,  C07C61/22 ,  C07C2601/08 ,  C07C2601/16 ,  Y02P20/55

Abstract: 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：US10196389B2

公开(公告)日：2019-02-05

申请号：US15326310

申请日：2015-07-14

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun Nan ,  Jia Li ,  Jingya Li ,  Mei Zhang ,  Dakai Chen ,  Lina Zhang ,  Runtao Zhang ,  Zhifu Xie

IPC: A61K31/437 ,  C07D401/14 ,  C07D471/04 ,  C07D211/78 ,  C12N9/12

Abstract: Provided are a class of pyrazolone compounds and a use thereof. In particular, a compound represented by formula I is provided, wherein the definition of each variable group is as described in the description. The compounds of formula (I) 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.

公开(公告)号：US10105362B2

公开(公告)日：2018-10-23

申请号：US14916463

申请日：2014-05-16

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Qiang Yu ,  Jing He ,  Qing Zhang

IPC: A61K31/5025 ,  C12N5/09

Abstract: The present invention provides an anti-tumor use of Anagrelide and derivatives thereof and, more specifically, the present invention provides the use of Anagrelide and derivatives thereof in the preparation of pharmaceuticals or pharmaceutical compositions for the treatment or inhibition of tumors.

公开(公告)号：US10100044B2

公开(公告)日：2018-10-16

申请号：US15030331

申请日：2014-10-20

Applicant: SUZHOU VIGONVITA LIFE SCIENCES CO., LTD. ,  TOPHARMAN SHANGHAI CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Zheng Liu ,  Chunhui Wu ,  Yongjian Liu ,  Rongxia Zhang ,  Yang He ,  Guanghui Tian ,  Jingshan Shen

IPC: C07D333/70 ,  C07D409/12 ,  C07D333/54

Abstract: The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.

公开(公告)号：US20180265496A1

公开(公告)日：2018-09-20

申请号：US15752896

申请日：2016-08-18

Applicant: JINAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES

Inventor： Ke DING ,  Meiyu GENG ,  Li TAN ,  Jian DING ,  Zhang ZHANG ,  Jing AI ,  Xiaomei REN ,  Donglin GAO ,  Zhengchao TU ,  Xiaoyun LU ,  Dongmei ZHANG

IPC: C07D401/12 ,  C07D487/04 ,  C07D471/04 ,  C07D519/00 ,  C07D513/04 ,  C07D471/06 ,  C07D498/06 ,  C07D491/048

Abstract: Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.

公开(公告)号：US10059694B2

公开(公告)日：2018-08-28

申请号：US15529333

申请日：2015-11-18

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES

Inventor： Ke Ding ,  Jian Ding ,  Shingpan Chan ,  Meiyu Geng ,  Xiaomei Ren ,  Hua Xie ,  Zhengchao Tu ,  Yi Chen

IPC: C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/4523 ,  A61P35/00 ,  A61K31/551

CPC classification number: C07D403/12 ,  A61K31/4523 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/551 ,  C07D239/47 ,  C07D239/48 ,  C07D401/02 ,  C07D401/12

Abstract: Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R1, R2, R3, R4, R5, X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.

公开(公告)号：US10058566B2

公开(公告)日：2018-08-28

申请号：US14901297

申请日：2014-07-02

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES

Inventor： Jian Ding ,  Jing Ai ,  Yi Chen ,  Xun Huang

IPC: A61K31/737 ,  C08B37/00 ,  C08L5/00

CPC classification number: A61K31/737 ,  C08B37/0084 ,  C08L5/00

Abstract: A polygulonic acid sulfate or pharmaceutically acceptable salt thereof, preparation method therefor and use thereof in the preparation of tumor growth and/or metastasis inhibitors are disclosed. The polygulonic acid sulfate or pharmaceutically acceptable salt thereof of the present invention can be used in the preparation of any one or more of tumor growth inhibitors, tumor metastasis inhibitors, angiogenesis inhibitors, heparanase inhibitors, C-Met enzyme inhibitors, microtubule polymerization inhibitors, actin-depolymerizing factor activity inhibitors and actin-aggregation inhibitors.