公开(公告)号：US11174237B2

公开(公告)日：2021-11-16

申请号：US16623297

申请日：2018-05-31

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  FUKANG (SHANGHAI) HEALTH TECHNOLOGY CO., LTD.

Inventor： Chunhao Yang ,  Zehong Miao ,  Cun Tan ,  Xiajuan Huan ,  Jian Ding ,  Yi Chen

IPC: C07D307/84

Abstract: Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs.

公开(公告)号：US20170000800A1

公开(公告)日：2017-01-05

申请号：US15269069

申请日：2016-09-19

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

Inventor： CHUNHAO YANG ,  Linghua Meng ,  Yanhong Chen ,  Xiang Wang ,  Cun Tan ,  Jiapeng Li ,  Jian Ding ,  Yi Chen

IPC: A61K31/5377 ,  A61K31/5386

CPC classification number: A61K31/5377 ,  A61K31/53 ,  A61K31/5386 ,  C07D419/04 ,  C07D419/14

Abstract: 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.

Abstract translation: 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：US20160367591A1

公开(公告)日：2016-12-22

申请号：US14901297

申请日：2014-07-02

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES

Inventor： Jian Ding ,  Jing Ai ,  Yi Chen ,  Xun Huang

IPC: A61K31/737 ,  C08B37/00

CPC classification number: A61K31/737 ,  C08B37/0084 ,  C08L5/00

Abstract: A polygulonic acid sulfate or pharmaceutically acceptable salt thereof, preparation method therefor and use thereof in the preparation of tumor growth and/or metastasis inhibitors are disclosed. The polygulonic acid sulfate or pharmaceutically acceptable salt thereof of the present invention can be used in the preparation of any one or more of tumor growth inhibitors, tumor metastasis inhibitors, angiogenesis inhibitors, heparanase inhibitors, C-Met enzyme inhibitors, microtubule polymerization inhibitors, actin-depolymerising factor activity inhibitors and actin-aggregation inhibitors.

Abstract translation: 公开了多糖酸硫酸盐或其药学上可接受的盐，其制备方法及其在制备肿瘤生长和/或转移抑制剂中的用途。 本发明的多糖酸硫酸盐或其药学上可接受的盐可用于制备肿瘤生长抑制剂，肿瘤转移抑制剂，血管生成抑制剂，乙酰肝素酶抑制剂，C-Met酶抑制剂，微管聚合抑制剂，肌动蛋白 聚合因子活性抑制剂和肌动蛋白聚集抑制剂。

公开(公告)号：US11465984B2

公开(公告)日：2022-10-11

申请号：US16652148

申请日：2018-09-29

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

Inventor： Lei Li ,  Meiyu Geng ,  Ying Huang ,  Jian Ding ,  Qiong Zhang ,  Min Huang ,  Shuai Tang ,  Ning Shen ,  Yi Chen

IPC: C07D401/14 ,  C07D403/14 ,  C07D405/14

Abstract: The invention relates to a compound of formula (I): wherein variables are as defined in the specification. The compound is an inhibitor of an ERK kinase, e.g. ERK1 and/or ERK2 kinase. The invention also relates to the use of the compound and a method for preparing the compound, and a pharmaceutical composition containing the compound.

公开(公告)号：US10766889B2

公开(公告)日：2020-09-08

申请号：US16329336

申请日：2017-08-24

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

Inventor： Fajun Nan ,  Jia Li ,  Jian Ding ,  Meiyu Geng ,  Yangming Zhang ,  Yi Chen ,  Yubo Zhou ,  Chaojun Gong ,  Mingbo Su ,  Anhui Gao

IPC: C07D277/56 ,  C07D277/60 ,  C07D417/04 ,  A61P35/02 ,  A61K31/427 ,  A61P35/00

Abstract: The invention describes an aryl-2,2′-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2′-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.

公开(公告)号：US09533965B2

公开(公告)日：2017-01-03

申请号：US14375742

申请日：2013-01-14

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

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

IPC: 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 classification number: C07D307/81 ,  C07C67/08 ,  C07C67/307 ,  C07D405/04 ,  C07D405/12 ,  C07D407/12

Abstract: 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.

Abstract translation: 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：US09447101B2

公开(公告)日：2016-09-20

申请号：US14403014

申请日：2013-04-23

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

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

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

CPC classification number: C07D487/04 ,  A61K31/5377 ,  A61K31/5386 ,  C07D498/08 ,  C07D519/00

Abstract: 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.

Abstract translation: 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：US09255106B2

公开(公告)日：2016-02-09

申请号：US14418705

申请日：2013-07-24

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

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

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

CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/502

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US10059694B2

公开(公告)日：2018-08-28

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: C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/4523 ,  A61P35/00 ,  A61K31/551

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：US10058566B2

公开(公告)日：2018-08-28

申请号：US14901297

申请日：2014-07-02

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES

Inventor： Jian Ding ,  Jing Ai ,  Yi Chen ,  Xun Huang

IPC: A61K31/737 ,  C08B37/00 ,  C08L5/00

CPC classification number: A61K31/737 ,  C08B37/0084 ,  C08L5/00

Abstract: A polygulonic acid sulfate or pharmaceutically acceptable salt thereof, preparation method therefor and use thereof in the preparation of tumor growth and/or metastasis inhibitors are disclosed. The polygulonic acid sulfate or pharmaceutically acceptable salt thereof of the present invention can be used in the preparation of any one or more of tumor growth inhibitors, tumor metastasis inhibitors, angiogenesis inhibitors, heparanase inhibitors, C-Met enzyme inhibitors, microtubule polymerization inhibitors, actin-depolymerizing factor activity inhibitors and actin-aggregation inhibitors.