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公开(公告)号：US10280146B2
公开(公告)日：2019-05-07
申请号：US15540025
申请日：2015-12-28
Inventor： Jianhua Shen , Yiping Wang , Xinde Chen , Wenwei Xu , Kai Wang
IPC: 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
Abstract: 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.
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公开(公告)号：US20190100529A1
公开(公告)日：2019-04-04
申请号：US16087317
申请日：2017-03-20
Inventor： Hong LIU , Jiang WANG , Jian LI , Jia LI , Jingya LI , Hualiang JIANG , Xiaomin LUO , Kaixian CHEN
IPC: C07D495/04 , A61P3/10
Abstract: 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.
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公开(公告)号：US10233180B2
公开(公告)日：2019-03-19
申请号：US15128298
申请日：2015-03-21
Inventor： Xiaowu Dong , Jia Li , Bo Yang , Yongzhou Hu , Yubo Zhou , Qinjie Weng , Wenhu Zhan , Lei Xu , Tao Liu , Qiaojun He
IPC: C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
Abstract: 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.
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公开(公告)号：US10093679B2
公开(公告)日：2018-10-09
申请号：US15509796
申请日：2015-09-11
Applicant: SUZHOU VIGONVITA LIFE SCIENCES CO., LTD. , SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES , TOPHARMAN SHANGHAI CO., LTD.
Inventor： Jingshan Shen , Zheng Liu , Zhen Wang , Guanghui Tian , Jianfeng Li , Xiaojun Yang
IPC: C07D261/20 , C07D495/04 , A61K31/33 , A61K31/381 , C07D209/14 , C07D307/77 , C07D231/56 , C07D275/04 , C07D333/20 , A61K31/415 , A61K31/42 , A61K31/425 , C07D333/46
Abstract: 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.
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75.发明申请公开(公告)号：US20180194767A1
公开(公告)日：2018-07-12
申请号：US15566418
申请日：2016-04-15
Inventor： Hong LIU , Yu ZHOU , Dong ZHANG , Jian LI , Hualiang JIANG , Kaixian CHEN
IPC: C07D487/04 , C07D213/56 , C07D491/10 , C07D277/30 , C07D231/56 , C07D417/10 , C07D417/12 , C07D417/14 , C07D401/06 , C07D417/06 , C07D401/14 , C07D401/12 , C07D239/26 , C07D413/12 , C07D263/32 , C07D413/10 , C07D261/08
CPC classification number: C07D487/04 , C07D213/56 , C07D213/75 , C07D213/82 , C07D231/56 , C07D239/26 , C07D261/08 , C07D263/32 , C07D277/30 , C07D277/32 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14 , C07D491/10
Abstract: Compounds of formula I are provided. Also provided are methods of preparing the compounds of formula (I), and methods of using the compounds of formula (I) as a negative allosteric modulator of a metabotropic glutamate receptor (mGluR) subtype 5.
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Patent Agency Ranking
公开(公告)号：US20170313715A1
公开(公告)日：2017-11-02
申请号：US15523058
申请日：2015-10-30
Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY , SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventor： Honglin LI , Hualiang JIANG , Yufang XU , Jia LI , Zhenjiang ZHAO , Jingya LI , Hongling XU , Shiliang LI
IPC: C07D493/04 , C07D311/92 , C07D311/60
Abstract: 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.
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公开(公告)号：US09796732B2
公开(公告)日：2017-10-24
申请号：US14842682
申请日：2015-09-01
Inventor： Jingkang Shen , Ke Yu , Tao Meng , Lanping Ma , Arie Zask , Lanfang Meng , Xin Wang , Yiyi Chen
IPC: A61K31/519 , C07D519/00 , C07D471/04 , C07D487/04
CPC classification number: C07D519/00 , C07D471/04 , C07D487/04
Abstract: 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.
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公开(公告)号：US20170298080A1
公开(公告)日：2017-10-19
申请号：US15509796
申请日：2015-09-11
Applicant: SUZHOU VIGONVITA LIFE SCIENCES CO., LTD. , SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES , TOPHARMAN SHANGHAI CO., LTD.
Inventor： Jingshan SHEN , Zheng LIU , Zhen WANG , Guanghui TIAN , Jianfeng LI , Xiaojun YANG
IPC: C07D495/04 , C07D275/04 , C07D261/20 , C07D333/20 , C07D231/56
CPC classification number: 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
Abstract: 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.
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公开(公告)号：US20170247371A1
公开(公告)日：2017-08-31
申请号：US15326310
申请日：2015-07-14
Inventor： Fajun NAN , Jia LI , Jingya LI , Mei ZHANG , Dakai CHEN , Lina ZHANG , Runtao ZHANG , Zhifu XIE
IPC: C07D471/04 , C12N9/12 , C07D211/78
CPC classification number: C07D471/04 , A61K31/437 , C07D211/78 , C12N9/12 , C12Y207/11031
Abstract: 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.
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公开(公告)号：US20170143717A1
公开(公告)日：2017-05-25
申请号：US14916463
申请日：2014-05-16
Inventor： Qiang YU , Jing HE , Qing ZHANG
IPC: A61K31/5025 , C12N5/09
CPC classification number: A61K31/5025 , C12N5/0693 , C12N2501/06
Abstract: 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.
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