专利检索 ap:"SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES" 第 7 页

61.

发明申请
METHOD FOR SYNTHESIZING NOVEL CHIRAL LIGAND, METAL CHELATE, A VARIETY OF NON-NATURAL AMINO ACIDS, MARAVIROC AND KEY INTERMEDIATE THEREOF 审中-公开

公开(公告)号：US20190233456A1

公开(公告)日：2019-08-01

申请号：US16337338

申请日：2017-09-19

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

发明人： Hong LIU , Jiang WANG , Shengbin ZHOU , Panfeng PENG , Yong NIAN , Shuni WANG , Shuangjie SHU , Hao SHEN , Hualiang JIANG , Kaixian CHEN

IPC分类号： C07F15/04 , C07D207/16

CPC分类号： C07F15/045 , C07C227/34 , C07C229/34 , C07D207/16 , C07D401/04 , C07D409/12 , C07F15/04 , Y02P20/55

摘要： Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-β3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.

62.

发明授权
Bruton's tyrosine kinase inhibitors 有权

公开(公告)号：US10358446B2

公开(公告)日：2019-07-23

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

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

63.

发明授权
Certain protein kinase inhibitors 有权

公开(公告)号：US10328060B2

公开(公告)日：2019-06-25

申请号：US15523315

申请日：2015-11-01

申请人： Shanghai Fochon Pharmaceutical Co., Ltd. , Shanghai Institute of Materia Medica Chinese Academy of Sciences , Chongqing Fochon Pharmaceutical Co., Ltd.

发明人： Xingdong Zhao , Jian Ding , Linghua Meng , Meiyu Geng , Tongshuang Li , Zuwen Zhou , Ling Chen , Qihong Liu , Xianlong Wang , Lijun Yang , Yue Rong , Rui Tan , Chuiliang Yu , Lihua Jiang , Yanxin Liu , Li Linghu , Jing Sun , Weibo Wang

IPC分类号： C07D519/00 , A61K31/437 , A61K45/06 , A61K31/4375 , A61K31/505 , A61K31/52

摘要： Provided are certain PI3K inhibitors, pharmaceutical compositions thereof, and methods of use therefor.

64.

发明授权
Process of synthesizing substituted pyridine and pyrimidine compound 有权

公开(公告)号：US10316033B2

公开(公告)日：2019-06-11

申请号：US15561003

申请日：2016-03-24

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES , SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

发明人： Jingkang Shen , Tao Meng , Ting Yu , Lanping Ma , Xin Wang , Lin Chen

IPC分类号： C07D471/04 , C07D519/00

摘要： Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II′, wherein the definition of each of groups is as described as the description. Compound with other methods, the method in the present invention has features of high yield and a result product being easier to separate.

65.

发明授权
KCNQ potassium channel agonist, and preparation method therefor and use thereof 有权

公开(公告)号：US10316008B2

公开(公告)日：2019-06-11

申请号：US15870276

申请日：2018-01-12

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

发明人： Fajun Nan , Min Li , Zhaobing Gao , Yangming Zhang , Haining Hu , Haiyan Xu , Huanan Liu , Xiaoping Pi

IPC分类号： C07D307/24 , A61K31/167 , A61K31/17 , A61K31/27 , A61K31/277 , A61K31/341 , C07C269/04 , C07C269/06 , C07C271/28 , C07C273/18 , C07C275/64 , C07C231/02 , C07C333/08 , C07C233/62 , C07C235/16 , C07C235/74 , C07C237/04 , C07C237/22 , C07C237/48

摘要： The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.

66.

发明授权
Pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof 有权

公开(公告)号：US10280146B2

公开(公告)日：2019-05-07

申请号：US15540025

申请日：2015-12-28

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

发明人： Jianhua Shen , Yiping Wang , Xinde Chen , Wenwei Xu , Kai Wang

IPC分类号： A61K31/541 , C07D239/54 , A61K31/513 , C07D401/04 , C07D403/04 , C07D239/48 , C07D409/04 , C07D239/52 , C07D239/545 , C07D239/56 , C07D401/12 , C07D403/06 , C07D413/04

摘要： The present invention relates to pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R1, R2, R3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA2 enzyme.

67.

发明申请
POLYMORPH OF DPPIV INHIBITOR MALEATE AND PREPARATION METHOD THEREFOR 审中-公开

公开(公告)号：US20190100529A1

公开(公告)日：2019-04-04

申请号：US16087317

申请日：2017-03-20

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 describes a polymorph of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid maleate and a preparation method therefor. The polymorph is a crystal having high stability and low hygroscopicity, and the crystal form is selected from crystal form A, crystal form B and crystal form C. Furthermore, the crystal form has a strong in-vivo hypoglycemic activity and can be used for the preparation of a novel drug for the treatment or prevention of diabetes mellitus type H and/or complications of diabetes mellitus type H.

68.

发明授权
Substituted nitrogen-containing heterocyclic derivatives, pharmaceutical compositions comprising the same and applications of antitumor thereof 有权

公开(公告)号：US10233180B2

公开(公告)日：2019-03-19

申请号：US15128298

申请日：2015-03-21

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

发明人： Xiaowu Dong , Jia Li , Bo Yang , Yongzhou Hu , Yubo Zhou , Qinjie Weng , Wenhu Zhan , Lei Xu , Tao Liu , Qiaojun He

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

摘要： 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.