公开(公告)号：US20240309012A1

公开(公告)日：2024-09-19

申请号：US18009981

申请日：2021-01-11

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Wuhan Institute of Virology, Chinese Academy of Science

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

IPC: C07D491/18 ,  A61K31/4748 ,  A61P31/14 ,  C07D491/22 ,  C07D498/22 ,  C07D519/00

CPC classification number: C07D491/18 ,  A61K31/4748 ,  A61P31/14 ,  C07D491/22 ,  C07D498/22 ,  C07D519/00

Abstract: Provided are an isoquinoline compound represented by formula (I), a pharmaceutically acceptable salt thereof, an enantiomer thereof, a diastereomer, a racemate, a crystalline hydrate, and a solvate, as well as an application of a composition thereof in fighting a virus. R1, R2, R3, and R4 are as defined in the description. Further provided are a preparation method for the compound and uses thereof for preparing an inhibitor that inhibits a virus and/or a drug for prophylaxis and/or treatment of an illness related to a respiratory tract infection, pneumonia, etc. caused by a virus.

公开(公告)号：US20220213083A1

公开(公告)日：2022-07-07

申请号：US17603823

申请日：2020-04-20

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

Inventor： Huaqiang XU ,  Jia LI ,  Jingjing SHI ,  Yi ZANG ,  Dandan SUN ,  Mingliang LIU ,  Rongrong XIE ,  Erli YOU ,  Lixin GAO ,  Qian TAN

IPC: C07D413/14 ,  C07D487/08 ,  A61P1/16

Abstract: An FXR small molecule agonist and a preparation method therefor and a use thereof, having a structure as shown in formula (I). The compound represented by formula (I) has FXR agonistic activity and is capable of preparing drugs for treatment of FXR-related diseases.

公开(公告)号：US20190100529A1

公开(公告)日：2019-04-04

申请号：US16087317

申请日：2017-03-20

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

Inventor： Hong LIU ,  Jiang WANG ,  Jian LI ,  Jia LI ,  Jingya LI ,  Hualiang JIANG ,  Xiaomin LUO ,  Kaixian CHEN

IPC: C07D495/04 ,  A61P3/10

Abstract: The invention describes a polymorph of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid maleate and a preparation method therefor. The polymorph is a crystal having high stability and low hygroscopicity, and the crystal form is selected from crystal form A, crystal form B and crystal form C. Furthermore, the crystal form has a strong in-vivo hypoglycemic activity and can be used for the preparation of a novel drug for the treatment or prevention of diabetes mellitus type H and/or complications of diabetes mellitus type H.

公开(公告)号：US20170313715A1

公开(公告)日：2017-11-02

申请号：US15523058

申请日：2015-10-30

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

Inventor： Honglin LI ,  Hualiang JIANG ,  Yufang XU ,  Jia LI ,  Zhenjiang ZHAO ,  Jingya LI ,  Hongling XU ,  Shiliang LI

IPC: C07D493/04 ,  C07D311/92 ,  C07D311/60

Abstract: The present invention relates to six-membered ring benzo derivatives as a DPP-4 inhibitor and a use thereof. In particular, the present invention relates to a compound as shown in formula I, a pharmaceutical composition containing the compound as shown in formula I and a use of the compound in the preparation of drugs for treating DPP-4 related diseases or inhibiting DPP-4.

公开(公告)号：US20170247371A1

公开(公告)日：2017-08-31

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: C07D471/04 ,  C12N9/12 ,  C07D211/78

CPC classification number: C07D471/04 ,  A61K31/437 ,  C07D211/78 ,  C12N9/12 ,  C12Y207/11031

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：US20250042862A1

公开(公告)日：2025-02-06

申请号：US18709473

申请日：2022-11-10

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

Inventor： Bing XIONG ,  Jia LI ,  Tongchao LIU ,  Yubo ZHOU ,  Cong LI ,  Na LI ,  Weijuan KAN ,  Mingbo SU ,  Li SHENG ,  Xiaobei HU

IPC: C07D239/84 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/519 ,  A61K31/55 ,  A61P35/00 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10

Abstract: Disclosed are an aromatic heterocyclic compound and an application thereof. The aromatic heterocyclic compound is represented by formula I, and the compound has good LSD1 enzyme inhibitory activity, and can be used as an LSD1 inhibitor for treatment of tumors etc.

公开(公告)号：US20220017505A1

公开(公告)日：2022-01-20

申请号：US17358002

申请日：2021-06-25

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

Inventor： Rong SHENG ,  Jia LI ,  Dongyan GU ,  Yubo ZHOU ,  Jun WEI ,  Mengmeng ZHANG ,  Yongzhou HU ,  Kaixiang ZHANG ,  Jieyu LIU ,  Weijuan KAN

IPC: C07D413/14 ,  C07D403/12 ,  C07D471/04 ,  C07D239/95 ,  C07D417/12 ,  C07D473/00 ,  C07D401/14 ,  C07D491/107 ,  C07D491/056

Abstract: Provided by the present disclosure are an amino quinazolinone and amino isoquinolone derivatives. It is verified by numerous experiments that the compounds provided by the present disclosure have good inhibiting effects on PI3Kα and PI3Kγ, most of the compounds have prominent inhibiting effect on PI3Kα, and show strong growth inhibiting effect on PIK3CA mutant tumor cells such as human breast cancer cell strain (MCF7). Therefore, the amino quinazolinone and amino isoquinolone derivatives according to the present disclosure can be applied in the preparation of anti-tumor and anti-inflammatory medicines, and can be used as PI3Kα inhibitors in the preparation of medicines for treatment of human or animal cell proliferation related tumors, the medicines comprising the derivatives any one or more of pharmaceutically acceptable salts and solvates thereof as well as pharmaceutically acceptable carriers. Formulas a and b are shown as below:

公开(公告)号：US20190031678A1

公开(公告)日：2019-01-31

申请号：US16087318

申请日：2017-03-22

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

Inventor： Hong LIU ,  Jiang WANG ,  Jian LI ,  Jia LI ,  Jingya LI ,  Hualiang JIANG ,  Xiaomin LUO ,  Kaixian CHEN

IPC: C07D495/04 ,  A61P3/10

Abstract: The invention relates to a salt form of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[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 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：US20180030066A1

公开(公告)日：2018-02-01

申请号：US15549918

申请日：2016-02-03

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

Inventor： Hong LIU ,  Jian WANG ,  Jian LI ,  Jia LI ,  Jingya LI ,  Shengbin ZHOU ,  Mingbo SU ,  Hualiang JIANG ,  Xiaomin LUO ,  Kaixian CHEN

IPC: C07D495/04

CPC classification number: C07D495/04 ,  A61K31/519 ,  C07B2200/13

Abstract: The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.

公开(公告)号：US20170044119A1

公开(公告)日：2017-02-16

申请号：US15301763

申请日：2015-03-27

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

Inventor： Fajun NAN ,  Jia LI ,  Xin XIE ,  Chaojun GONG ,  Yubo ZHOU ,  Hui CHAI ,  Yangming ZHANG ,  Mingbo SU

IPC: C07D277/56 ,  C07D417/14 ,  C07D277/60

CPC classification number: C07D277/56 ,  C07D277/60 ,  C07D277/66 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention relates to a thiazole-based compound, a preparation method therefor, and a use thereof. More specifically, the present invention relates to a 2,2′-bis-thiazole-based compound, a preparation method therefor, and a use of 2,2′-bis-thiazole-based compound a histone deacetylase inhibitor in the preparation of an antitumor medicament, a medicament for treating autoimmune diseases, a medicament for treating type II diabetes mellitus and complication thereof, or a medicament for treating neurodegenerative diseases.

Abstract translation: 本发明涉及一种噻唑类化合物及其制备方法及其应用。 更具体地说，本发明涉及2,2'-双噻唑类化合物及其制备方法，以及使用组氨酸脱乙酰酶抑制剂的2,2'-双噻唑类化合物制备 抗肿瘤药物，用于治疗自身免疫性疾病的药物，用于治疗II型糖尿病的药物及其并发症，或用于治疗神经变性疾病的药物。