公开(公告)号：US20170000800A1

公开(公告)日：2017-01-05

申请号：US15269069

申请日：2016-09-19

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

Inventor： CHUNHAO YANG ,  Linghua Meng ,  Yanhong Chen ,  Xiang Wang ,  Cun Tan ,  Jiapeng Li ,  Jian Ding ,  Yi Chen

IPC: A61K31/5377 ,  A61K31/5386

CPC classification number: A61K31/5377 ,  A61K31/53 ,  A61K31/5386 ,  C07D419/04 ,  C07D419/14

Abstract: The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.

Abstract translation: 本发明涉及吡咯并[2,1-f] [1,2,4]三嗪化合物，其异构体或其药学上可接受的盐，酯或水合物及其制备方法和应用。 吡咯并[2,1-f] [1,2,4]三嗪化合物具有通式（I）表示的结构。 由通式（I）表示的吡咯并[2,1-f] [1,2,4]三嗪化合物可抑制磷脂酰肌醇-3激酶（PI3K）信号通路，从而用于制备治疗磷脂酰肌醇-3激酶 相关疾病如癌症。

公开(公告)号：US20160367591A1

公开(公告)日：2016-12-22

申请号：US14901297

申请日：2014-07-02

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES

Inventor： Jian Ding ,  Jing Ai ,  Yi Chen ,  Xun Huang

IPC: A61K31/737 ,  C08B37/00

CPC classification number: A61K31/737 ,  C08B37/0084 ,  C08L5/00

Abstract: A polygulonic acid sulfate or pharmaceutically acceptable salt thereof, preparation method therefor and use thereof in the preparation of tumor growth and/or metastasis inhibitors are disclosed. The polygulonic acid sulfate or pharmaceutically acceptable salt thereof of the present invention can be used in the preparation of any one or more of tumor growth inhibitors, tumor metastasis inhibitors, angiogenesis inhibitors, heparanase inhibitors, C-Met enzyme inhibitors, microtubule polymerization inhibitors, actin-depolymerising factor activity inhibitors and actin-aggregation inhibitors.

Abstract translation: 公开了多糖酸硫酸盐或其药学上可接受的盐，其制备方法及其在制备肿瘤生长和/或转移抑制剂中的用途。 本发明的多糖酸硫酸盐或其药学上可接受的盐可用于制备肿瘤生长抑制剂，肿瘤转移抑制剂，血管生成抑制剂，乙酰肝素酶抑制剂，C-Met酶抑制剂，微管聚合抑制剂，肌动蛋白 聚合因子活性抑制剂和肌动蛋白聚集抑制剂。

公开(公告)号：US20150368274A1

公开(公告)日：2015-12-24

申请号：US14842682

申请日：2015-09-01

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

Inventor： Jingkang Shen ,  Ke Yu ,  Tao Meng ,  Lanping Ma ,  Lanfang Meng ,  Xin Wang ,  Yiyi Chen ,  Arie Zask

IPC: C07D519/00

CPC classification number: C07D519/00 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention belongs to the field of pharmaceutical Chemistry. In particular, the present invention relates to a pyridopyrimidine or pyrimidopyrimidine compound as represented by general formula (I), or an isomer thereof or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof, a preparation method, a pharmaceutical composition and uses thereof in preparing a mTOR inhibitor. As a mTOR inhibitor, the compound or the pharmaceutical composition thereof can be used for treating a disease or condition due to PI3K-AKT-mTOR signalling pathway malfunction.

Abstract translation: 本发明属于药物化学领域。 特别地，本发明涉及由通式（I）表示的吡啶并嘧啶或嘧啶并嘧啶化合物或其异构体或其药学上可接受的盐，酯，前药或溶剂合物，其制备方法，药物组合物及其用途 制备mTOR抑制剂。 作为mTOR抑制剂，化合物或其药物组合物可用于治疗由于PI3K-AKT-mTOR信号传导途径故障引起的疾病或病症。

公开(公告)号：US20150210711A1

公开(公告)日：2015-07-30

申请号：US14683726

申请日：2015-04-10

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

Inventor： Hong LIU ,  Xin XIE ,  Xuechu ZHEN ,  Haifeng SUN ,  Jing LI ,  Liyuan ZHU ,  Zeng LI ,  Ying CHEN ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07D491/153 ,  C07D491/056 ,  C07D217/20 ,  C07D311/20 ,  C07C231/14 ,  C07D455/03 ,  C07C69/736

CPC classification number: C07D491/153 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D455/03 ,  C07D491/056 ,  C07D491/147 ,  C07D491/22

Abstract: The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.

Abstract translation: 本发明涉及由通式（I）表示的新型六氢二苯并[a，g]喹啉化合物及其衍生物，对映体，非对映异构体，外消旋及其混合物，以及其药学上可接受的盐。 本发明还涉及一种制备该化合物的方法，该化合物对神经系统疾病，特别是与多巴胺受体和5-羟色胺受体相关的疾病具有良好的预防和治疗作用。 生物活性实验表明，该化合物预计将发展成为一种新颖有力的化学实体，用于治疗与多巴胺受体和5-羟色胺受体，特别是精神分裂症，帕金森病，药物成瘾，偏头痛等有关的疾病。

公开(公告)号：US20140336252A1

公开(公告)日：2014-11-13

申请号：US14353842

申请日：2012-10-23

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

Inventor： Fajun Nan ,  Min Li ,  Zhaobing Gao ,  Fei Chen ,  Yangming Zhang ,  Pingzheng Zhou ,  Haining Hu ,  Haiyan Xu ,  Sheng Liu

IPC: C07C271/28 ,  C07C233/44 ,  C07C231/00 ,  C07C269/04

CPC classification number: C07C271/28 ,  C07C231/00 ,  C07C233/43 ,  C07C233/44 ,  C07C269/04 ,  C07C2601/16 ,  C07D235/26

Abstract: The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medicine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration.

Abstract translation: 本发明提供具有通式I所示结构的化合物，其药学上可接受的盐，其制备方法及其在制备用于治疗神经系统疾病的药物中的用途。 其化合物或其药物组合物可用作治疗神经系统疾病的KCNQ钾通道激动剂。 与瑞替加滨相比，现有技术中的化合物，本发明的化合物具有相同或更好的治疗效果，更易于合成和储存，并且不易氧化劣化。

公开(公告)号：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

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

Inventor： Youhong HU ,  Yi CHEN ,  Zhicheng XIE ,  Jian DING ,  Xin LI ,  Yanfen FANG ,  Qianqian SHEN

IPC: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

Abstract: The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

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：US20240270745A1

公开(公告)日：2024-08-15

申请号：US18569434

申请日：2022-06-15

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  LANZHOU INSTITUTE OF CHEMICAL PHYSICS, CHINESE ACADEMY OF SCIENCES

Inventor： Zhaobing GAO ,  Junli YANG ,  Xianhua MENG ,  Yueming ZHENG ,  Tian CHAI ,  Yin ZHANG

IPC: C07D471/14 ,  A61K31/519 ,  A61P29/00

CPC classification number: C07D471/14 ,  A61K31/519 ,  A61P29/00

Abstract: Provided in the present invention are an isoquinoline alkaloid compound selected from the group consisting of the compounds represented by the following structural formulas, and a preparation method therefor and the use thereof. The present invention proves for the first time that the isoquinoline alkaloid compound is an inhibitor of the IK potassium current and the background potassium current in the nervous system, the cardiovascular system and the pancreas, especially an inhibitor of the Kv2.1 channel and the TRESK channel, and can be used for treating a disease such as stroke, arrhythmia, atrial fibrillation, diabetes, pain, hypoventilation, and depression.

公开(公告)号：US20240208954A1

公开(公告)日：2024-06-27

申请号：US18013696

申请日：2021-06-29

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

Inventor： Hong LIU ,  Jiang WANG ,  Cen XIE ,  Yameng LIU ,  Shulei HU ,  Cuina LI ,  Feng GAO ,  Kanglong WANG ,  Yong WANG ,  Xianchun ZHONG ,  Yuqiang SHI ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07D413/10 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/675 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D271/06 ,  C07D413/14 ,  C07F9/6558

CPC classification number: C07D413/10 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/675 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D271/06 ,  C07D413/14 ,  C07F9/65583

Abstract: The present invention relates to the fields of pharmaceutical chemistry and pharmacotherapeutics, and in particular to a compound as represented by general formula I, a racemate, an R-isomer, an S-isomer and a pharmaceutically acceptable salt thereof and a mixture of same, a preparation method therefor, a pharmaceutical composition containing the compound and the use thereof as an SIP receptor agonist. The oxadiazole compound involved in the present invention can be used for treating SIP receptor agonist related diseases.

公开(公告)号：US20230133600A1

公开(公告)日：2023-05-04

申请号：US17796076

申请日：2021-01-28

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

Inventor： Hong LIU ,  Jian LI ,  Jingjing PENG ,  Xiong XIE ,  Wenhao DAI ,  Shulei HU ,  Chunpu LI ,  Leike ZHANG ,  Zhenming JIN ,  Yechun XU ,  Gengfu XIAO ,  Haitao YANG ,  Fang BAI ,  Xi CHENG ,  Hualiang JIANG ,  Kaixian CHEN

IPC: A61K31/404 ,  A61K31/4412 ,  A61K31/4025 ,  A61K31/498 ,  A61K31/4709 ,  A61K31/443 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/4535 ,  A61K31/453 ,  A61K31/4525 ,  A61K31/4439 ,  A61K31/437 ,  A61K31/4155

Abstract: A class of ketoamide-based compounds, in particular, a ketoarnide-based compound as represented by general formula A is provided. The ketoamide compound may be used as a 2019 novel coronavirus (2019-nCov) 3 CL protease inhibitor and/or human cathepsin L inhibitor, and/or may be used in the preparation of a medicament for treating and/or preventing and relieving respiratory tract infection, pneumonia and other related diseases caused by 2019 novel coronavirus infection. Pharmaceutical compositions of the class of compounds, pharmaceutical salts, enantiomeric forms, diastereoisomers and racemic compounds thereof in the preparation of a medicament for treating and/or preventing and relieving respiratory tract infections and other related diseases caused by the 2019 novel coronavirus infection are also provided.