公开(公告)号：US10590159B2

公开(公告)日：2020-03-17

申请号：US15575630

申请日：2015-11-06

申请人： SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES ,  HUZHOU CENTER OF BIO-SYNTHETIC INNOVATION, SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES

发明人： Wen Liu ,  Min Wang ,  Dongxiao Xu ,  Qunfei Zhao ,  Qinglin Zhang

IPC分类号： C07H17/02 ,  C07H15/14 ,  C07H1/00 ,  C07H5/10 ,  C07H13/10 ,  C07H15/207

摘要： Provided in the present invention are a class of Lincomycin biosynthetic intermediates and a preparation method and use thereof. Specifically provided are Lincomycin biosynthetic intermediates obtained from the genetic modification of a Lincomycin producing bacterium, and a method for the production thereof through fermentation and purification through separation.

公开(公告)号：US20230114794A1

公开(公告)日：2023-04-13

申请号：US17284549

申请日：2019-10-10

申请人： SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES

发明人： Wenjun TANG ,  Siyao XU

IPC分类号： C07F15/00

摘要： Provided is a metal complex as represented by formula I. The metal complex may be used as a catalyst for asymmetric catalytic hydrogenation, is capable of efficiently catalyzing and synthesizing a series of chiral p-aryl amides having high optical purity, and is especially capable of asymmetrically catalyzing and hydrogenating a tetra-substituted enamide compound, chiral amides having high optical purity are synthesized, and the carrying amount of ligand may reach 100,000.

公开(公告)号：US20220110936A1

公开(公告)日：2022-04-14

申请号：US17427404

申请日：2019-02-02

申请人： Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences

发明人： Yanshan FANG ,  Yongjia DUAN

IPC分类号： A61K31/502 ,  A61P25/28

摘要： Disclosed are a pharmaceutical composition for treatment of neurodegenerative diseases or diseases caused by abnormality of RNA binding protein and applications thereof, in particular the application in the treatment of ALS. The pharmaceutical composition can significantly enhance the dynamic performance of stress particles containing RNA binding proteins such as hnRNP A1 and TDP-43 proteins; influences the interaction between the RNA binding proteins and other poly ADP ribosylation modified proteins or other PAR binding proteins; influences the subcellular localization and stress response of RNA binding proteins; influences the liquid-liquid phase separation and aggregation tendency of RNA binding proteins; influences the co-phase separation between RNA binding proteins; influences the interaction of RNA binding proteins in cells; and has a significant inhibitory effect on neurotoxicity caused by RNA binding proteins.

公开(公告)号：US20180251486A1

公开(公告)日：2018-09-06

申请号：US15575630

申请日：2015-11-06

申请人： SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES ,  HUZHOU CENTER OF BIO-SYNTHETIC INNOVATION, SHANGH- AI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEM

发明人： Wen LIU ,  Min WANG ,  Dongxiao XU ,  Qunfei ZHAO ,  Qinglin ZHANG

IPC分类号： C07H17/02 ,  C07H15/14 ,  C07H15/207 ,  C07H13/10 ,  C07H5/10

CPC分类号： C07H17/02 ,  C07H1/00 ,  C07H5/10 ,  C07H13/10 ,  C07H15/14 ,  C07H15/207

摘要： Provided in the present invention are a class of Lincomycin biosynthetic intermediates and a preparation method and use thereof. Specifically provided are Lincomycin biosynthetic intermediates obtained from the genetic modification of a Lincomycin producing bacterium, and a method for the production thereof through fermentation and purification through separation.

公开(公告)号：US20180207628A1

公开(公告)日：2018-07-26

申请号：US15746646

申请日：2016-04-15

申请人： Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences

发明人： Dawei Ma ,  Wei Zhou ,  Mengyang Fan ,  Haibo Wu ,  Junli Yin ,  Shanghua Xia

IPC分类号： B01J31/22 ,  C07B41/02 ,  C07B43/04 ,  C07B45/06 ,  C07C233/56 ,  C07C231/14 ,  C07D317/58 ,  C07D307/52 ,  C07D307/81 ,  C07D333/20 ,  C07D207/335 ,  C07D213/40 ,  C07D317/28 ,  C07D207/14 ,  C07D307/22 ,  C07D295/00 ,  C07D207/06 ,  C07D495/04 ,  C07D239/42 ,  C07D241/20 ,  C07D213/89 ,  C07D215/38 ,  C07D217/22 ,  C07D317/66 ,  C07D335/16 ,  C07D277/64 ,  C07D295/135 ,  C07D277/66 ,  C07D215/40 ,  C07D241/42 ,  C07D471/04 ,  C07D213/73 ,  C07D207/325 ,  C07D263/56 ,  C07D213/65 ,  C07D295/096 ,  C07D317/64 ,  C07D215/20 ,  C07D241/18 ,  C07D209/86 ,  C07D231/12 ,  C07D233/60 ,  C07C209/10 ,  C07C209/08 ,  C07C213/02 ,  C07C221/00 ,  C07C41/26 ,  C07C319/20 ,  C07C45/64 ,  C07C253/30 ,  C07C213/08 ,  C07C319/14 ,  C07C231/12 ,  C07C315/04

CPC分类号： B01J31/2243 ,  B01J31/22 ,  B01J2231/4283 ,  B01J2231/4288 ,  B01J2231/4294 ,  B01J2531/16 ,  C07B41/02 ,  C07B43/04 ,  C07B45/06 ,  C07C41/26 ,  C07C45/64 ,  C07C209/08 ,  C07C209/10 ,  C07C213/02 ,  C07C213/08 ,  C07C221/00 ,  C07C231/02 ,  C07C231/12 ,  C07C231/14 ,  C07C233/56 ,  C07C253/30 ,  C07C315/04 ,  C07C319/14 ,  C07C319/20 ,  C07D207/06 ,  C07D207/14 ,  C07D207/27 ,  C07D207/325 ,  C07D207/335 ,  C07D209/08 ,  C07D209/86 ,  C07D211/72 ,  C07D213/40 ,  C07D213/65 ,  C07D213/73 ,  C07D213/74 ,  C07D213/89 ,  C07D215/20 ,  C07D215/38 ,  C07D215/40 ,  C07D217/22 ,  C07D223/12 ,  C07D223/22 ,  C07D231/12 ,  C07D233/60 ,  C07D239/42 ,  C07D239/545 ,  C07D241/18 ,  C07D241/20 ,  C07D241/42 ,  C07D263/56 ,  C07D277/64 ,  C07D277/66 ,  C07D295/00 ,  C07D295/096 ,  C07D295/135 ,  C07D307/22 ,  C07D307/52 ,  C07D307/81 ,  C07D317/28 ,  C07D317/58 ,  C07D317/64 ,  C07D317/66 ,  C07D333/20 ,  C07D333/36 ,  C07D333/54 ,  C07D333/58 ,  C07D335/16 ,  C07D471/04 ,  C07D495/04

摘要： The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of C—N, C—O and C—S bonds.

公开(公告)号：US09499521B2

公开(公告)日：2016-11-22

申请号：US15194413

申请日：2016-06-27

申请人： President and Fellows of Harvard College ,  Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences

发明人： Junying Yuan ,  Yijun Zhou ,  Shan Qian ,  Dawei Ma

IPC分类号： C07D233/78 ,  C07D403/06

CPC分类号： C07D403/06 ,  A61P9/10 ,  A61P29/00 ,  C07D233/78

摘要： A compound having the following structure (I): or a pharmaceutically acceptable salt, prodrug, stereoisomer or tautomer thereof, is provided. Related compounds, methods for preparation of the same and uses of the compounds for treatment of various indications, including treatment of necrotic cell diseases and/or inflammation, are also provided.

摘要翻译： 或其药学上可接受的盐，前药，立体异构体或互变异构体。 还提供了相关化合物，其制备方法和用于治疗各种适应症的化合物的用途，包括治疗坏死性细胞疾病和/或炎症。

公开(公告)号：US20160024098A1

公开(公告)日：2016-01-28

申请号：US14776852

申请日：2014-03-14

申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES ,  TUFTS UNIVERSITY ,  UNIVERSITY OF HOUSTON

发明人： Junying YUAN ,  Alexei DEGTEREV ,  Gregory D. CUNY

IPC分类号： C07D487/04 ,  C07D401/14 ,  C07D471/04

CPC分类号： C07D487/04 ,  C07D401/14 ,  C07D471/04

摘要： The present invention relates to heterocyclic compounds (e.g., compounds described by Formula (I)) and pharmaceutically acceptable salts thereof. The invention also features pharmaceutical compositions that include these compounds and their use in therapy for treating conditions in which necroptosis is likely to play a substantial role. The heterocyclic compounds described herein can also achieve improved activity and selectivity towards RIP1 and/or RIP3.

摘要翻译： 本发明涉及杂环化合物（例如由式（I）表示的化合物）及其药学上可接受的盐。 本发明还包括药物组合物，其包括这些化合物及其在治疗中用于治疗其中人工神经根可能起重要作用的病症的用途。 本文所述的杂环化合物还可以实现对RIP1和/或RIP3的改善的活性和选择性。

公开(公告)号：US20240254095A1

公开(公告)日：2024-08-01

申请号：US18290266

申请日：2022-05-11

申请人： SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES

发明人： Jidong ZHU ,  Yelin CHEN ,  Yang GENG ,  Hengyi CAO ,  Shiyun LI ,  Ziwen LI ,  Qiuyan WANG ,  Tonghui SU ,  Chaoying FU

IPC分类号： C07D265/36 ,  A61K31/538 ,  A61K31/553 ,  A61P23/00 ,  C07D267/14 ,  C07D413/04

CPC分类号： C07D265/36 ,  A61K31/538 ,  A61K31/553 ,  A61P23/00 ,  C07D267/14 ,  C07D413/04

摘要： The present invention relates to a NMDA receptor antagonist and use thereof. The NMDA receptor antagonist of the present invention is a compound of formula I below, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a tautomer, a solvate, an isotopic substituent, a polymorphic substance, a prodrug or a metabolite thereof. In the formula, ring A, ring B, and R2 are as described herein. The present invention also provides a pharmaceutical composition comprising these compounds, and use of these compounds in the preparation of a drug for treating or preventing NMDA receptor-mediated diseases.

公开(公告)号：US20240132492A1

公开(公告)日：2024-04-25

申请号：US18462373

申请日：2023-09-06

申请人： JINAN UNIVERSITY ,  SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES

发明人： Ke DING ,  Xin ZHANG ,  Fang XU ,  Xiaomei REN ,  Xiaoyun LU ,  Dawei MA ,  Weixue HUANG

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07D519/00

CPC分类号： C07D471/04 ,  A61P35/00 ,  C07D519/00

摘要： The present disclosure provides a class of Pyridopyrimidine compounds having a structure shown in Formula (I) or their pharmaceutically acceptable salts, or stereoisomers or prodrug molecules and applications thereof. The compounds in the present disclosure can efficiently and selectively degrade AKT3 protein in cells without affecting AKT1/2, thereby significantly inhibiting tumor cell proliferation mediated by high expression of AKT3 protein. It can be used to prepare therapeutic drugs for cancer and other diseases related to abnormal expression of AKT3 protein.

公开(公告)号：US11325875B2

公开(公告)日：2022-05-10

申请号：US16060424

申请日：2016-12-12

申请人： ZHEJIANG JIUZHOU PHARMACEUTICAL CO., LTD. ,  SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES

发明人： Kuiling Ding ,  Yuxi Cao ,  Zhiyao Zheng ,  Qinglei Chong ,  Zheng Wang

IPC分类号： C07C13/72 ,  B01J31/22 ,  C07C39/17 ,  C07C43/21 ,  C07C43/225 ,  C07F9/6571 ,  C07B53/00 ,  C07C231/12 ,  C07C233/51

摘要： Chiral spirobiindane skeleton compound and preparation method thereof is disclosed in the present invention. The spirobiindane skeleton compound of the present invention having the structure formula of I or I′; the preparation method for synthesizing the spirobiindane skeleton compound of the present invention comprising the following steps: in the presence of solvent and catalysts, the structure formula compound III reacted through intramolecular Friedel-Crafts reaction to obtain the compound of formula I; the catalyst is a Browsteric acidor Lewis acid. The preparation method of chiral fused spirobiindane skeleton compound of the present invention does not need to adopt chiral starting materials or chiral resolving agents, does not require chiral resolving steps, is simple in method, is simple in post-treatment, and is economic and environment friendly. High product yield, high product optical purity and chemical purity. The catalyst for the asymmetric reaction is obtained from the chiral spirobiindane skeleton ligand of the present invention, under the catalytic reagent of transition metal, the catalyzed hydrogenation reaction can arrive at a remarkable catalytic effect with a product yield of >99%, and a product ee value of up to >99%.