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：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。

公开(公告)号：US20190276453A1

公开(公告)日：2019-09-12

申请号：US16420140

申请日：2019-05-22

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 ,  C07D403/04

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

公开(公告)号：US20190100507A1

公开(公告)日：2019-04-04

申请号：US16085311

申请日：2017-03-16

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

Inventor： Hong LIU ,  Jia LI ,  Jiang WANG ,  Mingbo SU ,  Shuni WANG ,  Yubo ZHOU ,  Wei ZHU ,  Wei XU ,  Chunpu LI ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07D401/12 ,  C07D401/06 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D409/06 ,  C07D417/12 ,  C07D471/04 ,  C07D205/04 ,  C07D265/30 ,  C07D211/38 ,  C07D211/96 ,  A61P35/00

Abstract: Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers.

公开(公告)号：US20190211005A1

公开(公告)日：2019-07-11

申请号：US16329336

申请日：2017-08-24

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

Inventor： Fajun NAN ,  Jia LI ,  Jian DING ,  Meiyu GENG ,  Yangming ZHANG ,  Yi CHEN ,  Yubo ZHOU ,  Chaojun GONG ,  Mingbo SU ,  Anhui GAO

IPC: C07D417/04 ,  A61P35/02

Abstract: The invention describes an aryl-2,2′-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2′-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.

公开(公告)号：US20180222904A1

公开(公告)日：2018-08-09

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 ,  A61K45/06 ,  A61K31/437 ,  A61K31/56 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/519 ,  A61K31/42

CPC classification number: C07D471/04 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/437 ,  A61K31/4545 ,  A61K31/501 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/56 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  C07D235/22 ,  C07D473/34 ,  C07D487/04

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

公开(公告)号：US20240270753A1

公开(公告)日：2024-08-15

申请号：US18560605

申请日：2022-03-30

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

Inventor： Bing ZHOU ,  Jia LI ,  Yubo ZHOU ,  Xiangbo YANG ,  Bo FENG ,  Yaxi YANG ,  Xiaobei HU

IPC: C07D491/107 ,  A61K31/497 ,  A61K31/5025 ,  C07D519/00

CPC classification number: C07D491/107 ,  A61K31/497 ,  A61K31/5025 ,  C07D519/00

Abstract: The present invention relates to a heterocyclic compound for inhibiting SHP2 activity that is represented by formula I, a preparation method therefor and use thereof. The compound of the present invention is effective in treating a disease or disorder or condition mediated by SHP2.

公开(公告)号：US20170107213A1

公开(公告)日：2017-04-20

申请号：US15128298

申请日：2015-03-21

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

Inventor： Xiaowu DONG ,  Jia LI ,  Bo YANG ,  Yongzhou HU ,  Yubo ZHOU ,  Qinjie WENG ,  Wenhu ZHAN ,  Lei XU ,  Tao LIU ,  Qiaojun HE

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

CPC classification number: C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.