公开(公告)号：EP2813495B1

公开(公告)日：2016-09-28

申请号：EP13746724.7

申请日：2013-01-14

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

发明人： YANG, Chunhao ,  MIAO, Zehong ,  DING, Jian ,  WANG, Meng ,  HE, Jinxue ,  TAN, Cun ,  CHEN, Yi

IPC分类号： C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D307/81 ,  C07C67/08 ,  C07C67/307 ,  C07D405/04 ,  C07D405/12 ,  C07D407/12

公开(公告)号：EP2813495A1

公开(公告)日：2014-12-17

申请号：EP13746724.7

申请日：2013-01-14

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

发明人： YANG, Chunhao ,  MIAO, Zehong ,  DING, Jian ,  WANG, Meng ,  HE, Jinxue ,  TAN, Cun ,  CHEN, Yi

IPC分类号： C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  A61P35/00 ,  A61P29/00

CPC分类号： C07D307/81 ,  C07C67/08 ,  C07C67/307 ,  C07D405/04 ,  C07D405/12 ,  C07D407/12

摘要： Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, wherein R 1 and R 2 are each independently hydrogen, straight or branched chained C 1 -C 4 alkyl, C 3 -C 4 cycloalkyl or saturated 5- or 6-membered heterocyclyl containing oxygen or nitrogen; or R 1 and R 2 together with N form an unsubstituted or substituted saturated 5- or 6-membered heterocyclyl containing at least one heteroatom, wherein the heteroatom is O, N and S, the substituent is a methyl on N; R 3 is a hydrogen atom or a chlorine atom; R 4 is a hydrogen atom or a fluorine atom; X is CH, CF or N; and Y is CH, CF or N.

摘要翻译： 本发明提供了通式Ⅰ所示的2-芳基苯并呋喃-7-甲酰胺化合物或其药理学或生理学上可接受的盐，其制备方法和其制备抗肿瘤药物的用途，其中R 1和R 2 各自独立地为氢，直链或支链C 1 -C 4烷基，C 3 -C 4环烷基或含有氧或氮的饱和5-或6-元杂环基; 或R 1和R 2与N一起形成含有至少一个杂原子的未取代或取代的饱和的5-或6-元杂环基，其中杂原子是O，N和S，取代基是N上的甲基; R 3为氢原子或氯原子; R 4为氢原子或氟原子; X是CH，CF或N; Y为CH，CF或N.

公开(公告)号：EP3299014B1

公开(公告)日：2019-11-20

申请号：EP16795854.5

申请日：2016-05-13

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Shanghai Acebright Pharmaceuticals Co. Ltd.

发明人： GUO, Shiyan ,  GAN, Yong ,  ZHANG, Ao ,  MIAO, Zehong ,  GAO, Li ,  DING, Jian

IPC分类号： A61K9/28 ,  A61K9/48 ,  A61K31/502 ,  A61K47/32 ,  A61K47/38 ,  A61K47/40 ,  A61K47/34 ,  A61P35/00 ,  A61K47/10 ,  A61K9/08 ,  A61K9/10 ,  A61K9/14 ,  A61K9/20

公开(公告)号：EP2881395A1

公开(公告)日：2015-06-10

申请号：EP13825341.4

申请日：2013-07-24

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

发明人： ZHANG, Ao ,  MIAO, Zehong ,  YE, Na ,  HUAN, Xiajuan ,  SONG, Zilan ,  CHEN, Chuanhuizi ,  CHEN, Yi ,  DING, Jian

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/502 ,  A61P9/10 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/502

摘要： Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.

摘要翻译： 本发明提供一种由通式表示的异构体，药学上可接受的盐，酯，前药或水合物的I或其化合物piperazinotriazole。 这样提供了用于制备所述化合物，药物组合物含有该化合物，并且作为高选择性的聚（ADP-核糖）在制备药物用于预防聚合酶-1（PARP 1）抑制剂及其使用的方法和/ 或治疗的PARP有关的疾病。

公开(公告)号：EP3381919A1

公开(公告)日：2018-10-03

申请号：EP16867946.2

申请日：2016-11-22

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

发明人： ZHANG, Ao ,  MIAO, Zehong ,  WANG, Pingyuan ,  SONG, Shanshan ,  SONG, Zilan ,  HUAN, Xiajuan ,  FAN, Zhoulong ,  DING, Jian

IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/502 ,  A61K31/437 ,  A61K31/444 ,  A61P25/28 ,  A61P25/16 ,  A61P9/10 ,  A61P27/02 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/502 ,  A61P35/00 ,  C07D471/04

摘要： The present invention relates to a class of substituted triazolopiperazine compounds represented by formula ( I ), tautomers, enantiomers, diastereomers, racemates, metabolites, metabolic precursors, and pharmaceutically acceptable salts, esters, prodrugs or hydrate thereof, a preparation methods therefor, intermediates and a use thereof in the preparation of drugs for prevention and treatment of diseases associated with PARP including various ischemic diseases, neurodegenerative diseases and cancers.

公开(公告)号：EP3299014A1

公开(公告)日：2018-03-28

申请号：EP16795854.5

申请日：2016-05-13

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Shanghai Acebright Pharmaceuticals Co. Ltd.

发明人： GUO, Shiyan ,  GAN, Yong ,  ZHANG, Ao ,  MIAO, Zehong ,  GAO, Li ,  DING, Jian

IPC分类号： A61K9/28 ,  A61K9/48 ,  A61K31/502 ,  A61K47/32 ,  A61K47/38 ,  A61K47/40 ,  A61K47/34 ,  A61P35/00

摘要： Disclosed is an SOMCL-9112 solid dispersion. The SOMCL-9112 solid dispersion is characterized by being prepared from the following raw materials in percentage by weight: 5 percent to 60 percent of SOMCL-9112, 5 percent to 90 percent of pharmaceutically acceptable matrix polymer, 0 percent to 20 percent of surfactant, 0 percent to 20 percent of flow aid and 0 percent to 20 percent of plasticizer. Also disclosed are a preparation method of the SOMCL-9112 solid dispersion, a solid medicinal preparation containing the solid dispersion and application of the solid dispersion for preparing a medicine for treating cancer.

摘要翻译： 公开了一种SOMCL-9112固体分散体。 SOMCL-9112固体分散体的特征是由以下重量百分比的原料制备而成：SOMCL-9112 5％-60％，药用基质聚合物5％-90％，表面活性剂0％-20％ 0％至20％的助流剂和0％至20％的增塑剂。 本发明还公开了SOMCL-9112固体分散体的制备方法，包含该固体分散体的固体药物制剂和该固体分散体在制备用于治疗癌症的药物中的应用。

公开(公告)号：EP2881395B1

公开(公告)日：2018-09-05

申请号：EP13825341.4

申请日：2013-07-24

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Shanghai Acebright Pharmaceuticals Co., Ltd.

发明人： ZHANG, Ao ,  MIAO, Zehong ,  YE, Na ,  HUAN, Xiajuan ,  SONG, Zilan ,  CHEN, Chuanhuizi ,  CHEN, Yi ,  DING, Jian

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/502 ,  A61P9/10 ,  A61P25/28 ,  A61P35/00

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/502

摘要： Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.

公开(公告)号：EP2233467B1

公开(公告)日：2012-09-19

申请号：EP08858616.9

申请日：2008-12-11

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

发明人： NAN, Fajun ,  LI, Jia ,  DING, Jian ,  LIU, Gang ,  XIE, Chuanming ,  MIAO, Zehong ,  TAI, Wanyi

IPC分类号： C07C237/16 ,  C07C233/05 ,  C07C233/09 ,  C07C233/18 ,  C07C233/20 ,  A61K31/16 ,  A61P35/00

CPC分类号： C07C237/22 ,  C07C247/12 ,  C07C271/22 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/20 ,  C07D233/54 ,  C07D307/24 ,  C07D307/94

公开(公告)号：EP1626050A1

公开(公告)日：2006-02-15

申请号：EP04730460.5

申请日：2004-04-30

申请人： East China University of Science and Technology ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Dalian University of Technology

发明人： QIAN, Xuhong ,  LI, Yonggang ,  XU, Yufang ,  DING, Jian ,  LIN, Liping ,  MIAO, Zehong ,  ZHU, Hong ,  QU, Baoyuan

IPC分类号： C07D495/06 ,  C07D513/06 ,  C07D221/06 ,  A61K31/473 ,  A61K31/4743 ,  A61K31/4745 ,  A61P35/00

CPC分类号： C07D495/06 ,  C07D221/14 ,  C07D405/12 ,  C07D513/06 ,  C09B57/08 ,  C09B69/102 ,  C09B69/109

摘要： The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by incorporating 5-or 6-membered heteroaromatic ring and/or introducing S heteroatom, thus increasing the anti-tumor activity of naphthalimide. The compounds of the invention displays significant inhibiting activities to the proliferation of various tumor cells such as human lung cancer, gastric cancer, liver cancer, leucocythemia and the like. The inhibition of cell proliferation is dose-dependent.

摘要翻译： 本发明公开了新型含硫萘二甲酰亚胺衍生物及其制备和用途。 本发明的萘二甲酰亚胺衍生物的共轭平面通过引入5-或6-元杂芳环和/或引入S杂原子而扩大，因此增加了萘二甲酰亚胺的抗肿瘤活性。 本发明的化合物对各种肿瘤细胞如人肺癌，胃癌，肝癌，白血病等的增殖显示出显着的抑制活性。 细胞增殖的抑制是剂量依赖性的。

公开(公告)号：EP3985007A1

公开(公告)日：2022-04-20

申请号：EP20823330.4

申请日：2020-06-12

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

发明人： ZHANG, Ao ,  MIAO, Zehong ,  XIONG, Chaodong ,  SONG, Shanshan ,  HE, Jinxue

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P35/02

摘要： The present disclosure relates to triazolopyrimidine compounds and salts, compositions and uses thereof, and the triazolopyrimidine compounds have the structures represented by the formula (I):

the above-mentioned triazolopyrimidine compounds have good activity and high selectivity for NAE.