公开(公告)号：EP1245561B1

公开(公告)日：2005-12-28

申请号：EP00941870.8

申请日：2000-07-03

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

发明人： BAI, Donglu ,  CHEN, Weizhou ,  BU, Yunxin ,  WANG, Yiping ,  DONG, Yueli ,  KANG, Aili

IPC分类号： C07C311/21 ,  C07C311/18 ,  C07C311/29 ,  C07C311/41 ,  C07C311/44 ,  C07D295/135 ,  A61K31/18 ,  A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/445 ,  C07D403/08 ,  C07D401/08

CPC分类号： C07D295/135 ,  A61K31/4025 ,  A61K31/4545

摘要： N-(3,5-bis-(di-substituted aminomethyl-4-hydroxy)benzyl aromatic sulfamides and N-(3,5-bis-(di-substituted aminomethyl-4-hydroxy)phenyl aromatic sulfamides compounds, in accordance with the animal tests, are active in the prevention and the treatment of cardiac arrhythmias. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-di-subsituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.

公开(公告)号：EP1418177A1

公开(公告)日：2004-05-12

申请号：EP02758042.2

申请日：2002-08-14

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

发明人： YUE, J., c/o Shangai Institute of Materia Medica, ,  YANG, S., c/o Shangai Institute of Materia Medica, ,  DING,J., c/o Shangai Institute of Materia Medica, ,  XIAO, D., c/o Shangai Institute of Materia Medica, ,  YUAN, S., c/o Shangai Institute of Materia Medica ,  WU, Yan., c/o Shangai Institute of Materia Medica ,  TONG, Y., c/o Shangai Institute of Materia Medica ,  DONG, Lei, c/o Shangai Institute of Materia Medica

IPC分类号： C07D521/00 ,  A61K31/558 ,  A61P31/10 ,  A61P35/00

CPC分类号： A61K31/365 ,  C07D311/94

摘要： The invention relates to pseudolaric acid-B derivatives of general formula (I), wherein (a) R 1 is cyano, heterocyclyl, COXR' or CON(R") 2 , wherein X is O or NH, R' is H, cycloalkyl, alkyl, heterocyclic alkyl or arylalkyl, each R" is independently alkyl, cycloalkyl or heterocyclicalkyl; (b) R 2 is H, alkylacyl, arylalkylacyl, arylacyl or heterocyclylacyl; (c) R 3 is COXY, amino or halogen, wherein X is O or NH, Y is H, NH 2 , hydroxy, alkyl, cycloalkyl, heterocyclicalkyl, hetroatom-substituted alkyl, tertiary amino-substituted ammonioalkyl, aryl, arylalkyl or polyhydroxyalkyl. The invention also relates to processes for preparing such derivatives and antitumor or antifungal pharmaceutical compositions containing the same.

摘要翻译： 本发明涉及通式（I）的假极酸-B衍生物，其中（a）R 1是氰基，杂环基，COXR'或CON（R“）2，其中X是O或NH，R'是H，环烷基， 烷基，杂环烷基或芳烷基，每个R“独立地为烷基，环烷基或杂环烷基; （b）R2是H，烷基酰基，芳基烷基酰基，芳基酰基或杂环基酰基; （c）R3是COXY，氨基或卤素，其中X是O或NH，Y是H，NH2，羟基，烷基，环烷基，杂环烷基，杂原子取代的烷基，叔氨基取代的氨基烷基，芳基，芳烷基或多羟基烷基。 本发明还涉及制备此类衍生物的方法和含有该衍生物的抗肿瘤或抗真菌药物组合物。

公开(公告)号：EP0806416B1

公开(公告)日：2003-05-07

申请号：EP95941572.0

申请日：1995-12-26

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

发明人： ZHU, Dayuan ,  TANG, Xican ,  LIN, Jinlai ,  ZHU, Cheng ,  SHEN, Jingkang ,  WU, Guansong ,  JIANG, Shanhao ,  YAMAGUCHI, Takuji c/o Tsumura & Co. ,  TANAKA, Kazuhiro ,  WAKANATSU, Takeshi c/o Tsumura & Co. ,  NISHIMURA, Hiroaki c/o Tsumura & Co.

IPC分类号： C07D221/22 ,  C07D401/06 ,  C07D401/12 ,  A61K31/44

CPC分类号： C07D401/06 ,  C07D221/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

摘要： The present invention relates to novel huperzine A derivatives of formula (II), wherein Y is (a), or R' and Y together form =CH; R is (C1-C5)alkyl, (b), (c), (d), wherein n is 0 or 1, X is H, (C1-C5)alkyl; (C1-C5)alkyloxy; nitro, halogen, carboxy, alkyloxycarbonyl, hydroxymethyl, hydroxy, amino substituted by bis -(C1-C5)alkyl; -(CH2mCOOZ, wherein m=0∩5, Z is H or (C1-C5)alkyl; -CH=CH-G, wherein G is phenyl, furanyl, carboxy, alkyloxycarbonyl; and dihydro- or tetrahydro-pyridyl1 substituted by (C1-C5)alkyl at the nitrogen atom; R' is H, (C1-C5)alkyl, pyridoyl, benzoyl substituted by (C1-C5)alkyloxy; R' is H or (C1-C5)alkyl; processes for their manufacture and their use as acetyl cholinesterase inhibitor.

公开(公告)号：EP1086107A1

公开(公告)日：2001-03-28

申请号：EP99923702.7

申请日：1999-06-09

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

发明人： LI, Ying ,  SHAN, Feng ,  WU, Jin, Ming ,  WU, Guangshao ,  DING, Jian ,  HAN, Jianxian ,  ATASSI, Ghanem ,  RENARD, Pierre

IPC分类号： C07D493/18 ,  C07D519/00 ,  A61K31/335

CPC分类号： C07D493/18 ,  C07D493/20

摘要： The invention relates to compounds of the general formula (I): R - O - A, wherein R represents the radical of formula (II) and A is as defined in the description. The invention also relates to the geometric and/or optic isomers thereof and to the pharmaceutically acceptable acid or basic addition salts thereof.

公开(公告)号：EP4434980A1

公开(公告)日：2024-09-25

申请号：EP22895006.9

申请日：2022-11-22

申请人： Hangzhou HealZen Therapeutics Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： ZHOU, Xinglu ,  LI, Jia ,  LIU, Xingguo ,  ZHOU, Yubo ,  HU, Miao ,  LUO, Xiaomin ,  XIE, Jiangfeng ,  KAN, Weijuan ,  WU, Yizhe ,  HU, Xiaobei ,  SU, Mingbo

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/4427 ,  A61P35/00 ,  A61P37/00

CPC分类号： A61K31/4427 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10

摘要： Disclosed in the present invention are a Bruton's tyrosine kinase degrading agent, which has a structure represented by general formula 1, or a stereoisomer, a mixture of stereoisomers, or a pharmaceutically acceptable salt and a prodrug thereof, Further disclosed are the uses of the compound and a pharmaceutical composition containing same in the preparation of a drug for treating Bruton's tyrosine kinase-related diseases such as B cell or plasma cell proliferative diseases, The compound of the present invention has potent cell proliferation inhibitory activity, effectively degrades Bruton's tyrosine kinase, and has a good liver particle metabolism stability and good oral absorption properties. The compound can be used alone in drugs or in combination with other drugs for treating a disease, disorder or condition that benefits from the inhibition of the Bruton's tyrosine kinase activity or degradation of the Bruton's tyrosine kinase.

公开(公告)号：EP4389736A1

公开(公告)日：2024-06-26

申请号：EP22857522.1

申请日：2022-07-26

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

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

IPC分类号： C07D213/75 ,  A61P35/00 ,  A61K31/506

CPC分类号： Y02P20/55 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/44 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P9/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  C07D213/75 ,  C07D213/85 ,  C07D239/42 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D401/04 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04 ,  A61K31/506

摘要： 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：EP3438108B1

公开(公告)日：2022-08-10

申请号：EP17773232.8

申请日：2017-03-29

发明人： LIU, Hong ,  WANG, Yiping ,  ZHAO, Fei ,  ZHAO, Jing ,  WANG, Jiang ,  XI, Cong ,  WU, Chenglin ,  SHEN, Hao ,  HAN, Xu ,  JIANG, Hualiang ,  CHEN, Kaixian

IPC分类号： C07D471/14 ,  C07D491/22 ,  C07D495/22 ,  A61K31/4745 ,  A61P3/06 ,  A61P3/00 ,  A61P1/16 ,  A61P9/10 ,  A61P3/04

公开(公告)号：EP3311810B1

公开(公告)日：2022-07-27

申请号：EP17182709.0

申请日：2010-11-16

发明人： ELLIOT, Gary, T. ,  WANG, Yiping ,  BAI, Donglu

IPC分类号： A61K31/4025 ,  A61K31/402 ,  A61K31/40 ,  A61K9/22 ,  A61K9/20 ,  A61K9/08 ,  A61P9/00 ,  A61P9/06 ,  A61K31/18

公开(公告)号：EP3239135B1

公开(公告)日：2022-05-04

申请号：EP15871995.5

申请日：2015-12-28

发明人： SHEN, Jianhua ,  WANG, Yiping ,  CHEN, Xinde ,  XU, Wenwei ,  WANG, Kai

IPC分类号： C07D239/52 ,  C07D239/48 ,  C07D403/04 ,  C07D401/04 ,  C07D409/04 ,  A61K31/513 ,  A61K31/541 ,  A61P9/10 ,  A61P3/10 ,  A61P27/02

公开(公告)号：EP3530656B1

公开(公告)日：2022-01-05

申请号：EP17869906.2

申请日：2017-11-08

发明人： LIU, Tao ,  LI, Jia ,  HU, Yongzhou ,  ZHOU, Yubo ,  DONG, Xiaowu ,  GAO, Anhui ,  SONG, Pinrao ,  WANG, Peipei ,  TONG, Lexian ,  HU, Xiaobei ,  SU, Mingbo

IPC分类号： C07D401/14 ,  A61K31/506 ,  A61P35/00 ,  C07D413/14 ,  C07D409/14 ,  C07D417/14