公开(公告)号：US20180134677A1

公开(公告)日：2018-05-17

申请号：US15870276

申请日：2018-01-12

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

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

CPC classification number: C07D307/24 ,  A61K31/167 ,  A61K31/17 ,  A61K31/27 ,  A61K31/277 ,  A61K31/341 ,  C07C231/02 ,  C07C233/62 ,  C07C235/16 ,  C07C235/74 ,  C07C237/04 ,  C07C237/22 ,  C07C237/48 ,  C07C269/04 ,  C07C269/06 ,  C07C271/28 ,  C07C273/18 ,  C07C275/64 ,  C07C333/08 ,  C07C2601/02 ,  C07C2601/14

Abstract: 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.

公开(公告)号：US20180133215A1

公开(公告)日：2018-05-17

申请号：US15574557

申请日：2016-05-13

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  Shanghai Acebright Pharmaceuticals Co., Ltd.

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

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

CPC classification number: A61K31/502 ,  A61K9/08 ,  A61K9/10 ,  A61K9/146 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/28 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/10 ,  A61K47/32 ,  A61K47/34 ,  A61K47/38 ,  A61K47/40 ,  A61P35/00

Abstract: 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.

公开(公告)号：US20180036293A1

公开(公告)日：2018-02-08

申请号：US15523315

申请日：2015-11-01

Applicant: Shanghai Fochon Pharmaceutical Co., Ltd. ,  Shanghai Institute of Materia Medica Chinese Academy of Sciences ,  ChongQing Fochon Pharmaceutical Co., Ltd.

Inventor： 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: A61K31/437 ,  C07D519/00 ,  A61K45/06 ,  A61K31/4375 ,  A61K31/52

CPC classification number: A61K31/437 ,  A61K31/4375 ,  A61K31/505 ,  A61K31/52 ,  A61K45/06 ,  C07D519/00 ,  A61K2300/00

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

公开(公告)号：US20170283398A1

公开(公告)日：2017-10-05

申请号：US15529333

申请日：2015-11-18

Applicant: Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences ,  GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES

Inventor： Ke Ding ,  Jian Ding ,  Shingpan Chan ,  Meiyu Geng ,  Xiaomei Ren ,  Hua Xie ,  Zhengchao Tu ,  Yi Chen

IPC: C07D403/12 ,  C07D401/12 ,  C07D239/48

CPC classification number: C07D403/12 ,  A61K31/4523 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/551 ,  C07D239/47 ,  C07D239/48 ,  C07D401/02 ,  C07D401/12

Abstract: Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R1, R2, R3, R4, R5, X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.

公开(公告)号：US20170275291A1

公开(公告)日：2017-09-28

申请号：US15504854

申请日：2015-08-19

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

Inventor： Meiyu GENG ,  Lei LIU ,  Lei JIANG ,  Min HUANG ,  Chuantao ZHA ,  Jing AI ,  Lei WANG ,  Jianhua CAO ,  Jian DING

IPC: C07D487/04 ,  C07D231/56 ,  C07D519/00 ,  C07D401/12 ,  C07D471/04 ,  C07D403/12 ,  C07D498/04

Abstract: The present invention provides an indazole compound as a FGFR kinase inhibitor, preparation and use thereof. Specifically, the present invention provides a compound represented by formula (I), wherein the definitions of each group are described in the specification. The compound of the present invention has good FGFR kinase-inhibiting activity, and can be used in preparing a series of medicines for treating FGFR kinase activity related diseases.

公开(公告)号：US09643941B2

公开(公告)日：2017-05-09

申请号：US15301763

申请日：2015-03-27

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun Nan ,  Jia Li ,  Xin Xie ,  Chaojun Gong ,  Yubo Zhou ,  Hui Chai ,  Yangming Zhang ,  Mingbo Su

IPC: C07D277/56 ,  C07D417/04 ,  C07D417/14 ,  C07D277/66 ,  C07D277/60

CPC classification number: C07D277/56 ,  C07D277/60 ,  C07D277/66 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention relates to a thiazole-based compound, a preparation method therefor, and a use thereof. More specifically, the present invention relates to a 2,2′-bis-thiazole-based compound, a preparation method therefor, and a use of 2,2′-bis-thiazole-based compound a histone deacetylase inhibitor in the preparation of an antitumor medicament, a medicament for treating autoimmune diseases, a medicament for treating type II diabetes mellitus and complication thereof, or a medicament for treating neurodegenerative diseases.

公开(公告)号：US09637454B2

公开(公告)日：2017-05-02

申请号：US14438457

申请日：2013-10-17

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Hong Liu ,  Haiyan Zhang ,  Yu Zhou ,  Yan Fu ,  Hualiang Jiang ,  Xican Tang ,  Kaixian Chen

IPC: C07D211/32 ,  C07D405/06 ,  C07D451/04 ,  C07D211/38 ,  A61K45/06 ,  C07D211/34 ,  C07D471/08 ,  C07D491/107

CPC classification number: C07D211/32 ,  A61K45/06 ,  C07D211/34 ,  C07D211/38 ,  C07D405/06 ,  C07D451/04 ,  C07D471/08 ,  C07D491/107

Abstract: The present invention relates to the field of pharmaceutical chemistry and pharmacotherapeutics, and in particular to compounds of general formula I, racemates, R-isomers, S-isomers, and pharmaceutically acceptable salts thereof and their mixtures, and the preparation methods thereof and a pharmaceutical composition containing the compounds and uses thereof as an acetylcholine esterase inhibitor.

公开(公告)号：US20170107213A1

公开(公告)日：2017-04-20

申请号：US15128298

申请日：2015-03-21

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

Inventor： Xiaowu DONG ,  Jia LI ,  Bo YANG ,  Yongzhou HU ,  Yubo ZHOU ,  Qinjie WENG ,  Wenhu ZHAN ,  Lei XU ,  Tao LIU ,  Qiaojun HE

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

CPC classification number: C07D417/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

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.

公开(公告)号：US09567342B2

公开(公告)日：2017-02-14

申请号：US14926729

申请日：2015-10-29

Applicant: SHANGHAI FOCHON PHARMACEUTICAL CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES

Inventor： Weibo Wang ,  Meiyu Geng ,  Jian Ding ,  Xingdong Zhao ,  Jing Ai ,  Qiang Tian ,  Xia Peng ,  Weipeng Zhang ,  Hongbin Liu ,  Haohan Tan ,  Ling Chen

IPC: A61K31/506 ,  C07D487/04 ,  C07D405/12 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D405/14

CPC classification number: C07D487/04 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D405/12 ,  C07D405/14 ,  A61K2300/00

Abstract: Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.

Abstract translation: 本文公开了蛋白激酶抑制剂，更具体地是新颖的嘧啶衍生物及其药物组合物及其使用方法。

公开(公告)号：US09359372B2

公开(公告)日：2016-06-07

申请号：US14683726

申请日：2015-04-10

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Hong Liu ,  Xin Xie ,  Xuechu Zhen ,  Haifeng Sun ,  Jing Li ,  Liyuan Zhu ,  Zeng Li ,  Ying Chen ,  Hualiang Jiang ,  Kaixian Chen

IPC: A61K31/4741 ,  C07D491/12 ,  C07D491/153 ,  C07D455/03 ,  C07D491/147 ,  C07D491/22 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D491/056

CPC classification number: C07D491/153 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D455/03 ,  C07D491/056 ,  C07D491/147 ,  C07D491/22

Abstract: The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.

Abstract translation: 本发明涉及由通式（I）表示的新型六氢二苯并[a，g]喹啉化合物及其衍生物，对映体，非对映异构体，外消旋及其混合物，以及其药学上可接受的盐。 本发明还涉及一种制备该化合物的方法，该化合物对神经系统疾病，特别是与多巴胺受体和5-羟色胺受体相关的疾病具有良好的预防和治疗作用。 生物活性实验表明，该化合物预计将发展成为一种新颖有力的化学实体，用于治疗与多巴胺受体和5-羟色胺受体，特别是精神分裂症，帕金森病，药物成瘾，偏头痛等有关的疾病。