公开(公告)号：US20180222904A1

公开(公告)日：2018-08-09

申请号：US15763095

申请日：2016-10-03

申请人： Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Xibin LIAO ,  Jia LI ,  Zhijian LU ,  Yubo ZHOU ,  Anhui GAO

IPC分类号： C07D471/04 ,  A61K45/06 ,  A61K31/437 ,  A61K31/56 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/519 ,  A61K31/42

CPC分类号： 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

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

公开(公告)号：US20190276453A1

公开(公告)日：2019-09-12

申请号：US16420140

申请日：2019-05-22

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

发明人： Xibin LIAO ,  Jia LI ,  Zhijian LU ,  Yubo ZHOU ,  Anhui GAO

IPC分类号： C07D471/04 ,  C07D403/04

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

公开(公告)号：US20210015824A1

公开(公告)日：2021-01-21

申请号：US16978563

申请日：2019-03-08

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong LIU ,  Jia LI ,  Jiang WANG ,  Yi ZANG ,  Jian LI ,  Jingya LI ,  Dandan SUN ,  Hualiang JIANG ,  Kaixian CHEN

IPC分类号： A61K31/5377 ,  A61K31/519 ,  A61P1/16

摘要： Disclosed is use of a thieno[3,2-d]pyrimidin-4-one compound represented by general formula (I). Definition of each substituent is as stated in the description and claims, and the compound is used for preparing medicines for treating and/or preventing liver fibrosis and related diseases or preparing a DPP-4 inhibitor, or is used as a DPP-4 inhibitor.

公开(公告)号：US20190100507A1

公开(公告)日：2019-04-04

申请号：US16085311

申请日：2017-03-16

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

IPC分类号： 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

摘要： 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：US20220017505A1

公开(公告)日：2022-01-20

申请号：US17358002

申请日：2021-06-25

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

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

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

摘要： 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

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

IPC分类号： C07D495/04 ,  A61P3/10

摘要： 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

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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

IPC分类号： C07D495/04

CPC分类号： C07D495/04 ,  A61K31/519 ,  C07B2200/13

摘要： 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

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

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

CPC分类号： C07D277/56 ,  C07D277/60 ,  C07D277/66 ,  C07D417/04 ,  C07D417/14

摘要： 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.

摘要翻译： 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：US20230357244A1

公开(公告)日：2023-11-09

申请号：US18029359

申请日：2021-09-28

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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

IPC分类号： C07D471/08

CPC分类号： C07D471/08

摘要： A strong FXR small-molecule agonist, and a preparation method therefor and use thereof, the structure of the agonist being represented by formula (I), are provided. In the formula, each substituent is as defined in the description and the claims. The compound provided has the advantages of high FXR agonist activity, simple synthesis, easily available raw materials and the like, and can be used for preparing medicines for treating FXR related diseases.

公开(公告)号：US20190211005A1

公开(公告)日：2019-07-11

申请号：US16329336

申请日：2017-08-24

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

IPC分类号： C07D417/04 ,  A61P35/02

摘要： 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.