公开(公告)号：US11555009B2

公开(公告)日：2023-01-17

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 ,  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 ,  C07C227/16

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：US20220356202A1

公开(公告)日：2022-11-10

申请号：US17860468

申请日：2022-07-08

Applicant: GREEN VALLEY (SHANGHAI) PHARMACEUTICALS CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Meiyu Geng ,  Jian Ding ,  Zhenqing Zhang ,  Zhongping Xiao ,  Xiaoguang Du ,  Xianliang Xin

IPC: C07H15/04 ,  A61P25/28 ,  A61K31/7032 ,  A61K31/715 ,  C08B37/00

Abstract: The present invention relates to a mannuronic diacid oligosaccharide composition, comprising a mannuronic diacid of Formula (III) or a pharmaceutically acceptable salt thereof, wherein n is an integer from 1 to 9, m is 0, 1 or 2, and m′ is 0 or 1, and wherein the total weight of mannuronic diacids wherein n=1-5 is 80-95% of the total weight of the composition, and the ratio of the total weight of mannuronic diacids wherein n=1-3 to the total weight of mannuronic diacids wherein n=4-7 is between 1.0 and 3.5.

公开(公告)号：US11464794B2

公开(公告)日：2022-10-11

申请号：US17256853

申请日：2019-06-28

Applicant: GREEN VALLEY (SHANGHAI) PHARMACEUTICALS CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Meiyu Geng ,  Zhenqing Zhang ,  Yingshen Jin ,  Zhongping Xiao ,  Jian Ding

IPC: A61K31/702 ,  A61P25/28 ,  A61P29/00

Abstract: The present invention relates to an alginic oligosaccharic diacid composition comprising a mannuronic diacid of Formula (IV) or a pharmaceutically acceptable salt thereof, wherein n is an integer selected from 1 to 9, m is selected from 0, 1 or 2, m′ is selected from 0 or 1, and wherein the total weight of alginic oligosaccharic diacid wherein n=1-5 accounts for more than 60% of the total weight of the composition; the total weight of guluronic acids accounts for less than 50% of the total weight of the composition.

公开(公告)号：US11406651B2

公开(公告)日：2022-08-09

申请号：US17256738

申请日：2019-06-28

Applicant: GREEN VALLEY (SHANGHAI) PHARMACEUTICALS CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Meiyu Geng ,  Xianliang Xin ,  Xiaoguang Du ,  Zhenqing Zhang ,  Jian Ding

IPC: A61K31/702 ,  A61P25/28

Abstract: The present invention relates to the application of mannuronic diacid oligosaccharide composition in the treatment of vascular dementia.

公开(公告)号：US11384073B2

公开(公告)日：2022-07-12

申请号：US17127350

申请日：2020-12-18

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

Inventor： Jingshan Shen ,  Yang He ,  Zhen Wang ,  Jianfeng Li ,  Yongjian Liu ,  Jin Suo ,  Guanghui Tian ,  Weiming Chen ,  Feipu Yang ,  Yu Wang ,  Xiangrui Jiang ,  Rongxia Zhang ,  Hualiang Jiang

IPC: C07D409/12

Abstract: The present disclosure relates to a maleate salt of a benzothiophene compound, a crystalline form thereof, and a use thereof. Specifically, the present disclosure relates to a compound represented by formula (I-A), a crystalline form A thereof, a preparation method of a pharmaceutical composition including the same, and a use of the pharmaceutical composition in the preparation of drugs for preventing or treating diseases of the central nervous system. The compound represented by formula (I-A) and the crystalline form A thereof in the present disclosure have excellent physical and chemical properties, high oral bioavailability, excellent drugability, and are well-suited for pharmaceutical preparation, application, and preservation.

公开(公告)号：US20220177515A1

公开(公告)日：2022-06-09

申请号：US17594199

申请日：2020-03-30

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

Inventor： Bo LI ,  Peng LIU ,  Haiguo SUN ,  Mengyu XI ,  Zhijian XU ,  Yong ZHANG ,  Weiliang ZHU

IPC: C07K1/13 ,  C07D215/38 ,  C07D401/12 ,  C07D217/22 ,  C07K5/078 ,  C07K1/113 ,  C07K7/06

Abstract: The present disclosure relates to a method for modifying or marking an amino group in a molecule, wherein the amino group in the molecule is modified or marked with zolinium(s) shown in the following formula 1, wherein the molecule comprises amino acid ester, aminoamide, or peptide/protein. The method has advantages of economy and site selectivity, and has huge potential application value in the field such as pharmaceutical molecular synthesis, probe molecule and diagnostic marker reagent development.

公开(公告)号：US11192916B2

公开(公告)日：2021-12-07

申请号：US16648123

申请日：2018-09-17

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

Inventor： Fajun Nan ,  Xin Xie ,  Chenlu Zhang ,  Shimeng Guo ,  Yangming Zhang ,  Siwei Wang

IPC: C07J63/00

Abstract: Disclosed are a pentacyclic triterpene compound as shown in general formula (I) and a preparation method therefor. The compound has an effective antagonistic effect on FXR receptors.

公开(公告)号：US11174237B2

公开(公告)日：2021-11-16

申请号：US16623297

申请日：2018-05-31

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  FUKANG (SHANGHAI) HEALTH TECHNOLOGY CO., LTD.

Inventor： Chunhao Yang ,  Zehong Miao ,  Cun Tan ,  Xiajuan Huan ,  Jian Ding ,  Yi Chen

IPC: C07D307/84

Abstract: Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs.

公开(公告)号：US20210322449A1

公开(公告)日：2021-10-21

申请号：US17256889

申请日：2019-06-28

Applicant: SHANGHAI GREEN VALLEY PHARMACEUTICAL CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Meiyu Geng ,  Xianliang Xin ,  Zhenqing Zhang ,  Jian Ding

IPC: A61K31/702 ,  A61K31/7012 ,  A61K31/7016 ,  A61K31/715 ,  A61P3/10

Abstract: The present invention relates to the use of mannuronic diacid oligosaccharide composition in the treatment of diabetes.

公开(公告)号：US20210261539A1

公开(公告)日：2021-08-26

申请号：US16967664

申请日：2019-02-01

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

Inventor： Lin Xia ,  Meiyu Geng ,  Yan Ye ,  Jian Ding ,  Qiong Zhang ,  Aijun Shen ,  Ying Huang ,  Hongchun Liu ,  Haoran Yang ,  Jing Ai ,  Minmin Zhang

IPC: C07D471/04 ,  C07D519/00 ,  C07D403/04 ,  C07D498/04 ,  C07D401/14 ,  C07D487/04 ,  C07D413/14

Abstract: The invention relates to the field of pharmaceutical chemistry. Specifically, the present invention relates to a series of BET (bromodomain and extra-terminal domain) inhibitors having a novel structure, particularly inhibitors targeting BRD4 (Bromodomain-containing protein 4), and a preparation method and use therefor. The structure thereof is shown in the following general formula (I). Said compounds or a stereoisomer, racemate, geometric isomer, tautomer, prodrug, hydrate, solvate, or crystal form thereof, or a pharmaceutically acceptable salt thereof, and the pharmaceutical composition thereof can be used for the treatment and/or prevention of related diseases mediated by bromodomain proteins.