公开(公告)号：US20220002278A9

公开(公告)日：2022-01-06

申请号：US17075206

申请日：2020-10-20

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

发明人： Bing Zhou ,  Cheng Luo ,  Hualiang Jiang ,  Yaxi Yang ,  Lianghe Mei ,  Wenchao Lu ,  Senhao Xiao ,  Shijie Chen ,  Shili Wan ,  Gang Qiao ,  Rukang Zhang

IPC分类号： C07D413/06 ,  C07D417/06 ,  C07D413/14 ,  C07D491/107 ,  C07D513/04 ,  C07D471/04 ,  C07D495/04 ,  C07D495/10

摘要： Disclosed is a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by the general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereoisomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising same and use thereof in the treatment of various HAT-related diseases or conditions.

公开(公告)号：US20240150300A1

公开(公告)日：2024-05-09

申请号：US18278063

申请日：2022-02-18

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

发明人： Youhong HU ,  Meiyu GENG ,  Daqiang LI ,  Aijun SHEN ,  Zhuo ZHANG ,  Yalei LI ,  Huajie YANG ,  Hongchun LIU ,  Hanyue ZHONG ,  Jian DING

IPC分类号： C07D237/14 ,  A61P35/00 ,  A61P35/02 ,  C07C67/00 ,  C07C67/10 ,  C07D401/04 ,  C07D403/04

CPC分类号： C07D237/14 ,  A61P35/00 ,  A61P35/02 ,  C07C67/00 ,  C07C67/10 ,  C07D401/04 ,  C07D403/04

摘要： The present invention relates to an S-configuration-containing amino benzamide pyridazinone compound, a preparation method therefor, and a pharmaceutical composition and application thereof. Specifically, the present invention relates to a compound represented by the following general formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition and application thereof. The S-configuration compound of the present application has very strong binding activity on class I histone deacetylase (HDAC1), and shows inhibitory activity on in-vitro proliferation of various tumor cells.

公开(公告)号：US20240059676A1

公开(公告)日：2024-02-22

申请号：US18267298

申请日：2021-12-10

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

发明人： Bing Zhou ,  Ying Leng ,  Yaxi Yang ,  Mengmeng Ning ,  Liuyu Hu ,  Lei Feng ,  Ju Liang

IPC分类号： C07D403/10 ,  C07D413/10 ,  C07D471/04 ,  A61P3/06

CPC分类号： C07D403/10 ,  C07D413/10 ,  C07D471/04 ,  A61P3/06

摘要： The present invention relates to a thyroid hormone receptor β selective agonist compound represented by formula I, a pharmaceutical composition and use thereof. The compound improves the selectivity to THR-α and the druggability of the compound while maintaining good THR-β agonistic activity, and shows a certain activity in in vivo pharmacological experiments.

公开(公告)号：US11873292B2

公开(公告)日：2024-01-16

申请号：US16306751

申请日：2017-06-02

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

发明人： Hong Liu ,  Jia Li ,  Wei Zhu ,  Yubo Zhou ,  Jiang Wang ,  Mingbo Su ,  Shuni Wang ,  Wei Xu ,  Chunpu Li ,  Weijuan Kan ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07D403/12 ,  C07D215/58 ,  C07D209/04 ,  C07D215/00 ,  C07D487/04 ,  C07D209/08 ,  C07D401/12 ,  C07D405/12 ,  A61P35/00

CPC分类号： C07D403/12 ,  A61P35/00 ,  C07D209/04 ,  C07D209/08 ,  C07D215/00 ,  C07D215/58 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04 ,  Y02P20/55

摘要： The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.

公开(公告)号：US20230219993A1

公开(公告)日：2023-07-13

申请号：US17996430

申请日：2021-04-16

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  WUHAN INSTITUTE OF VIROLOGY, CHINESE ACADEMY OF SCIENCE ,  XINJIANG TECHNICAL INSTITUTE OF PHYSICS AND CHEMISTRY, CHINESE ACADEMIY OF SCIENCES ,  VIGONVITA LIFE SCIENCES CO., LTD.

发明人： Yuanchao XIE ,  Gengfu XIAO ,  Yang HE ,  Leike ZHANG ,  Heji Akber AISA ,  Hualiang JIANG ,  Jingshan SHEN

IPC分类号： C07H7/06 ,  A61P31/14 ,  A61P31/16

CPC分类号： C07H7/06 ,  A61P31/14 ,  A61P31/16 ,  C07B2200/05

摘要： The present invention relates to an antiviral application of nucleoside analogs. Specifically, the present invention relates to uses of nucleoside analogs and a pharmaceutical composition thereof as: (a) inhibitors for inhibiting the replication of coronaviruses, influenza viruses, respiratory syncytial viruses, flaviviridae viruses, filoviridae viruses and/or porcine epidemic diarrhea virus (PEDV); and/or (b) medicines for treating and/or preventing and mitigating diseases caused by coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and/or porcine epidemic diarrhea virus (PEDV) infections. The nucleoside analogs according to the invention may treat and/or prevent and mitigate respiratory infection, pneumonia
(COVID-19) and other related diseases caused by 2019 novel coronavirus infection.

公开(公告)号：US11555009B2

公开(公告)日：2023-01-17

申请号：US16490186

申请日：2018-03-01

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

发明人： Caiguang Yang ,  Yue Huang ,  Ze Dong ,  Tao Zhang ,  Hongjiao Xu

IPC分类号： 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

摘要： 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

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

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

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

摘要： 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

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

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

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

摘要： 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

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

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

IPC分类号： A61K31/702 ,  A61P25/28

摘要： 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

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

发明人： 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分类号： C07D409/12

摘要： 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.