公开(公告)号：US20170313715A1

公开(公告)日：2017-11-02

申请号：US15523058

申请日：2015-10-30

申请人： EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Honglin LI ,  Hualiang JIANG ,  Yufang XU ,  Jia LI ,  Zhenjiang ZHAO ,  Jingya LI ,  Hongling XU ,  Shiliang LI

IPC分类号： C07D493/04 ,  C07D311/92 ,  C07D311/60

摘要： The present invention relates to six-membered ring benzo derivatives as a DPP-4 inhibitor and a use thereof. In particular, the present invention relates to a compound as shown in formula I, a pharmaceutical composition containing the compound as shown in formula I and a use of the compound in the preparation of drugs for treating DPP-4 related diseases or inhibiting DPP-4.

公开(公告)号：US09796732B2

公开(公告)日：2017-10-24

申请号：US14842682

申请日：2015-09-01

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

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

IPC分类号： A61K31/519 ,  C07D519/00 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D519/00 ,  C07D471/04 ,  C07D487/04

摘要： 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.

公开(公告)号：US20170298080A1

公开(公告)日：2017-10-19

申请号：US15509796

申请日：2015-09-11

申请人： SUZHOU VIGONVITA LIFE SCIENCES CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  TOPHARMAN SHANGHAI CO., LTD.

发明人： Jingshan SHEN ,  Zheng LIU ,  Zhen WANG ,  Guanghui TIAN ,  Jianfeng LI ,  Xiaojun YANG

IPC分类号： C07D495/04 ,  C07D275/04 ,  C07D261/20 ,  C07D333/20 ,  C07D231/56

CPC分类号： C07D495/04 ,  A61K31/33 ,  A61K31/381 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  C07D209/14 ,  C07D231/56 ,  C07D261/20 ,  C07D275/04 ,  C07D307/77 ,  C07D333/20 ,  C07D333/46

摘要： Disclosed are aminosulfonyl-based compounds represented by the general formula I or tautomers, enantiomers, racemates or pharmaceutically acceptable salts thereof, a method for preparing the same, pharmaceutical compositions and uses thereof. The compounds can be used to treat epilepsy, convulsions, obesity and the like.

公开(公告)号：US20170247371A1

公开(公告)日：2017-08-31

申请号：US15326310

申请日：2015-07-14

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

发明人： Fajun NAN ,  Jia LI ,  Jingya LI ,  Mei ZHANG ,  Dakai CHEN ,  Lina ZHANG ,  Runtao ZHANG ,  Zhifu XIE

IPC分类号： C07D471/04 ,  C12N9/12 ,  C07D211/78

CPC分类号： C07D471/04 ,  A61K31/437 ,  C07D211/78 ,  C12N9/12 ,  C12Y207/11031

摘要： Provided are a class of pyrazolone compounds and a use thereof. In particular, a compound represented by formula I is provided, wherein the definition of each variable group is as described in the description. The compounds of formula (I) have a direct AMPK-activating activity and can significantly promote the phosphorylation of AMPK and ACC of L6 myocytes and HepG2 cells in a dose-dependent manner.

公开(公告)号：US20170143717A1

公开(公告)日：2017-05-25

申请号：US14916463

申请日：2014-05-16

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

发明人： Qiang YU ,  Jing HE ,  Qing ZHANG

IPC分类号： A61K31/5025 ,  C12N5/09

CPC分类号： A61K31/5025 ,  C12N5/0693 ,  C12N2501/06

摘要： The present invention provides an anti-tumor use of Anagrelide and derivatives thereof and, more specifically, the present invention provides the use of Anagrelide and derivatives thereof in the preparation of pharmaceuticals or pharmaceutical compositions for the treatment or inhibition of tumors.

公开(公告)号：US09533965B2

公开(公告)日：2017-01-03

申请号：US14375742

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： Chunhao Yang ,  Zehong Miao ,  Jian Ding ,  Meng Wang ,  Jinxue He ,  Cun Tan ,  Yi Chen

IPC分类号： A61K31/343 ,  A61K31/4025 ,  A61K31/443 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5355 ,  A61K31/541 ,  A61K31/551 ,  C07D307/79 ,  C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D307/81 ,  C07D405/12 ,  C07C67/08 ,  C07C67/307 ,  C07D407/12

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 R1 and R2 are each independently hydrogen, straight or branched chained C1-C4 alkyl, C3-C4 cycloalkyl or saturated 5- or 6-membered heterocyclyl containing oxygen or nitrogen; or R1 and R2 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; R3 is a hydrogen atom or a chlorine atom; R4 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，其制备方法及其在制备抗肿瘤药物中的用途，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：US20160272624A1

公开(公告)日：2016-09-22

申请号：US15030331

申请日：2014-10-20

申请人： SUZHOU VIGONVITA LIFE SCIENCES CO., LTD. ,  TOPHARMAN SHANGHAI CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Zheng LIU ,  Chunhui WU ,  Yongjian LIU ,  Rongxia ZHANG ,  Yang HE ,  Guanghui TIAN ,  Jingshan SHEN

IPC分类号： C07D409/12 ,  C07D333/70 ,  C07D333/54

CPC分类号： C07D409/12 ,  C07D333/54 ,  C07D333/70

摘要： The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.

摘要翻译： 本发明涉及制备布立乐拉唑类似物，关键中间体及其盐的方法，具体地说，本发明涉及一种制备布立乐拉唑的新方法，其类似物，关键中间体及其盐，以及关键中间体， 及其盐在制备过程中提供。 制备方法反应条件温和，中间体稳定，操作方便，使用便宜，易于使用的试剂，节省了合成成本，缩短了生产周期，提高了产量和产品质量，适用于质量 生产。

公开(公告)号：US09447101B2

公开(公告)日：2016-09-20

申请号：US14403014

申请日：2013-04-23

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

发明人： Chunhao Yang ,  Linghua Meng ,  Yanhong Chen ,  Xiang Wang ,  Cun Tan ,  Jiapeng Li ,  Jian Ding ,  Yi Chen

IPC分类号： C07D419/04 ,  C07D419/14 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/53 ,  A61P35/00 ,  C07D487/04 ,  C07D519/00 ,  C07D498/08

CPC分类号： C07D487/04 ,  A61K31/5377 ,  A61K31/5386 ,  C07D498/08 ,  C07D519/00

摘要： 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.

摘要翻译： 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：US20160137640A1

公开(公告)日：2016-05-19

申请号：US14895832

申请日：2014-06-18

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SHANGHAI GREEN VALLEY PHARMACEUTICAL CO., LTD.

发明人： Jingkang Shen ,  Meiyu Geng ,  Jian Ding ,  Bing Xiong ,  Jing Al ,  Yuchi Ma ,  Xin Wang ,  Xia Peng ,  Yuelei Chen ,  Danqi Chen ,  Tao Meng ,  Lanping Ma ,  Yinchun Ji

IPC分类号： C07D471/04 ,  C07D519/00

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D519/00

摘要： This invention provides a class of five-member-heterocycle fused pyridine compounds as shown below in Formula (X), pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, a method of producing the same, pharmaceutical compositions containing the compound, and use of the compounds in preparing medicament for preventing and/or treating diseases and tumours associated with abnormal protein tyrosine kinase.

摘要翻译： 本发明提供一类如下式（X）所示的五元杂环稠合吡啶化合物，其药学上可接受的盐或药学上可接受的溶剂合物，其制备方法，含该化合物的药物组合物，以及该化合物的用途 在制备用于预防和/或治疗与异常蛋白酪氨酸激酶相关的疾病和肿瘤的药物中。

公开(公告)号：US09255106B2

公开(公告)日：2016-02-09

申请号：US14418705

申请日：2013-07-24

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

发明人： Ao Zhang ,  Zehong Miao ,  Na Ye ,  Xiajuan Huan ,  Zilan Song ,  Chuanhuizi Chen ,  Yi Chen ,  Jian Ding

IPC分类号： A61K31/4985 ,  C07D241/38 ,  C07D487/04 ,  A61K31/501 ,  A61K31/502

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 a pharmaceutically acceptable salt, stereoisomer, tautomer or hydrate thereof. Also provided are a pharmaceutical composition comprising the compound, a method for preparing the compound and a method of use thereof as a high-selectivity poly(adenosine diphosphate-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： 提供由通式I表示的哌嗪三唑化合物或其药学上可接受的盐，立体异构体，互变异构体或其水合物。 还提供了包含该化合物的药物组合物，该化合物的制备方法及其作为高选择性聚（腺苷二磷酸 - 核糖）聚合酶-1（PARP-1）抑制剂的用途）的制备方法 预防和/或治疗PARP相关疾病。