公开(公告)号：US10710996B2

公开(公告)日：2020-07-14

申请号：US15575903

申请日：2016-05-23

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

Inventor： Yaqiu Long ,  Meiyu Geng ,  Zhongliang Xu ,  Jing Ai

IPC: C07D471/04 ,  A61K31/501 ,  A61K31/4985 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/5377 ,  A61P35/00

Abstract: The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.

公开(公告)号：US20200163983A1

公开(公告)日：2020-05-28

申请号：US16630309

申请日：2018-07-12

Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY ,  YUNNAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Honglin LI ,  Weilie XIAO ,  Lili ZHU ,  Lina QUAN ,  Qiao LI ,  Yanyan DIAO ,  Zhenjiang ZHAO ,  Hualiang JIANG

IPC: A61K31/704 ,  A61P35/00 ,  A61K31/56

Abstract: Provided are use of a saponin compound of formula (I) or (II), or a pharmaceutically acceptable salt, prodrug or solvate thereof, in the manufacture of a medicament targeting PD-1. The medicament targeting PD-1 is one which treats a disease by inhibiting PD-1 from binding to a ligand thereof. The disease may be a tumor, an infection caused by a bacterium, a virus or a fungus, or an inflammatory disease.

公开(公告)号：US20200079727A1

公开(公告)日：2020-03-12

申请号：US16490186

申请日：2018-03-01

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

Inventor： Caiguang YANG ,  Yue HUANG ,  Ze DONG ,  Tao ZHANG ,  Hongjiao XU

IPC: C07C229/58 ,  A61P35/00 ,  C07D261/08 ,  A61K31/42 ,  A61K31/196 ,  C07C227/16 ,  C07D231/12 ,  A61K31/415 ,  C07D213/38 ,  A61K31/4418 ,  C07D333/20 ,  A61K31/381 ,  C07D239/26 ,  A61K31/505 ,  C07D333/40 ,  C07D239/42 ,  C07D211/70 ,  C07D209/14 ,  A61K31/404 ,  C07D233/64 ,  A61K31/4164 ,  C07D257/04 ,  A61K31/41 ,  C07D407/12 ,  A61K31/422 ,  A61K31/4245 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/5355

Abstract: The invention provides 2-(substituted phenylhetero) aromatic formate FTO inhibitors, a preparation method thereof, and applications thereof. Specifically, disclosed in the present invention are a 2-(substituted phenylhetero) aromatic formate compound represented by the following formula (I), and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, which can be used as an FTO targeting inhibitor for treating diseases associated with FTO targets, including obesity, metabolic syndrome (MS), type 2 diabetes (T2D), Alzheimer's diseases, and cancers such as breast cancers, small-cell lung cancers, human bone marrow rhabdomyosarcoma, pancreatic cancer, malignant glioblastoma and the like.

公开(公告)号：US20190315703A1

公开(公告)日：2019-10-17

申请号：US16461234

申请日：2017-11-17

Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Jian LI ,  Lefu LAN ,  Baoli LI ,  Feifei CHEN ,  Shuaishuai NI ,  Yifu LIU ,  Hanwen WEI ,  Fei MAO ,  Jin ZHU

IPC: C07D307/81 ,  C07D333/58 ,  C07D409/12 ,  A61P31/04 ,  A61P31/10 ,  C07D307/82

Abstract: Disclosed are benzoheterocyclic alkylamine compounds, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and a preparation method thereof, and use of the same in the manufacture of an antibacterial drug as an inhibitor of staphyloxanthin synthesis in Staphylococcus aureus.

公开(公告)号：US20190292183A1

公开(公告)日：2019-09-26

申请号：US16463868

申请日：2017-11-24

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

Inventor： Ao Zhang ,  Jian Ding ,  Hua Xie ,  Zilan Song ,  Yu Xue ,  Linjiang Tong ,  Meiyu Geng

IPC: C07D471/14 ,  C07D487/14 ,  A61P35/00

Abstract: The present disclosure relates to a Pyrimido[5,4-b]indolizine or pyrimido[5,4-b]pyrrolizine compound, preparation method thereof and use thereof. The compounds of the present invention have good inhibitory activities against BTK at the molecular and cellular levels. Importantly, the compounds of the present invention have low activity against Ramos cells of normal human B lymphoma cells, and have high activity against BTK-sensitive human diffuse large B lymphoma TMD8 cells, indicating that these type of compounds with novel structural are highly selective, off-target phenomenon and corresponding side effects are low. Thus it is a selective inhibitor of BTK with development potential.

公开(公告)号：US20190233456A1

公开(公告)日：2019-08-01

申请号：US16337338

申请日：2017-09-19

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES

Inventor： Hong LIU ,  Jiang WANG ,  Shengbin ZHOU ,  Panfeng PENG ,  Yong NIAN ,  Shuni WANG ,  Shuangjie SHU ,  Hao SHEN ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07F15/04 ,  C07D207/16

CPC classification number: C07F15/045 ,  C07C227/34 ,  C07C229/34 ,  C07D207/16 ,  C07D401/04 ,  C07D409/12 ,  C07F15/04 ,  Y02P20/55

Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-β3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.

公开(公告)号：US10358446B2

公开(公告)日：2019-07-23

申请号：US15763095

申请日：2016-10-03

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 ,  A61K31/437 ,  C07D473/34 ,  A61K31/52 ,  A61P35/00 ,  A61P29/00 ,  A61K31/4184 ,  C07D235/22 ,  C07D487/04 ,  A61K31/42 ,  A61K31/4545 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/56 ,  A61K45/06

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

公开(公告)号：US10328060B2

公开(公告)日：2019-06-25

申请号：US15523315

申请日：2015-11-01

Applicant: Shanghai Fochon Pharmaceutical Co., Ltd. ,  Shanghai Institute of Materia Medica Chinese Academy of Sciences ,  Chongqing Fochon Pharmaceutical Co., Ltd.

Inventor： Xingdong Zhao ,  Jian Ding ,  Linghua Meng ,  Meiyu Geng ,  Tongshuang Li ,  Zuwen Zhou ,  Ling Chen ,  Qihong Liu ,  Xianlong Wang ,  Lijun Yang ,  Yue Rong ,  Rui Tan ,  Chuiliang Yu ,  Lihua Jiang ,  Yanxin Liu ,  Li Linghu ,  Jing Sun ,  Weibo Wang

IPC: C07D519/00 ,  A61K31/437 ,  A61K45/06 ,  A61K31/4375 ,  A61K31/505 ,  A61K31/52

Abstract: Provided are certain PI3K inhibitors, pharmaceutical compositions thereof, and methods of use therefor.

公开(公告)号：US10316033B2

公开(公告)日：2019-06-11

申请号：US15561003

申请日：2016-03-24

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES ,  SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Inventor： Jingkang Shen ,  Tao Meng ,  Ting Yu ,  Lanping Ma ,  Xin Wang ,  Lin Chen

IPC: C07D471/04 ,  C07D519/00

Abstract: Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II′, wherein the definition of each of groups is as described as the description. Compound with other methods, the method in the present invention has features of high yield and a result product being easier to separate.

公开(公告)号：US10316008B2

公开(公告)日：2019-06-11

申请号：US15870276

申请日：2018-01-12

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

Inventor： Fajun Nan ,  Min Li ,  Zhaobing Gao ,  Yangming Zhang ,  Haining Hu ,  Haiyan Xu ,  Huanan Liu ,  Xiaoping Pi

IPC: C07D307/24 ,  A61K31/167 ,  A61K31/17 ,  A61K31/27 ,  A61K31/277 ,  A61K31/341 ,  C07C269/04 ,  C07C269/06 ,  C07C271/28 ,  C07C273/18 ,  C07C275/64 ,  C07C231/02 ,  C07C333/08 ,  C07C233/62 ,  C07C235/16 ,  C07C235/74 ,  C07C237/04 ,  C07C237/22 ,  C07C237/48

Abstract: The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.