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：US20160272624A1

公开(公告)日：2016-09-22

申请号：US15030331

申请日：2014-10-20

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

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

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

CPC classification number: C07D409/12 ,  C07D333/54 ,  C07D333/70

Abstract: 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.

Abstract translation: 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

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：US20160137640A1

公开(公告)日：2016-05-19

申请号：US14895832

申请日：2014-06-18

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

Inventor： 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: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D519/00

Abstract: 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.

Abstract translation: 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

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：US20150252365A1

公开(公告)日：2015-09-10

申请号：US14416559

申请日：2013-07-26

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

Inventor： Jin Ren ,  Yizheng Wang ,  Lingling Miao ,  Likun Gong ,  Xinming Qi ,  Chenggang Li ,  Guozhen Xing

IPC: C12N15/113

CPC classification number: C12N15/113 ,  C12N15/111 ,  C12N2310/141 ,  C12N2320/11

Abstract: Provided is a method for screening microRNAs with gene silencing function at both transcriptional and post-transcriptional levels. The microRNA obtained via the screening method can down-regulate the expression of mRNA of a target gene by binding to a specific site of 5′-flanking region of the target gene, and also down-regulate the expression of the protein of the target gene by binding to a specific site of the 3′-untranslated region of the target gene. Also provided are microRNAs obtained via the screening method, the use of the same in gene silencing, and a method of gene silencing by using the same.

Abstract translation: 提供了在转录和转录后水平上筛选具有基因沉默功能的microRNA的方法。 通过筛选方法获得的microRNA可以通过与目标基因的5'侧翼区域的特异位点结合而下调靶基因的mRNA表达，并且下调靶基因的蛋白质的表达 通过结合靶基因的3'非翻译区的特定位点。 还提供了通过筛选方法获得的微小RNA，其在基因沉默中的用途以及使用该基因沉默的方法。

公开(公告)号：US20140323466A1

公开(公告)日：2014-10-30

申请号：US14361920

申请日：2012-10-23

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

Inventor： Hong Liu ,  Jia Li ,  Jian Li ,  Jingya Li ,  Jiang Wang ,  Mingbo Su ,  Jie Lian ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.

Abstract translation: 公开了通式（I）所示的新的噻吩并[3,2-d]嘧啶-4-酮化合物，其制备方法，药物组合物及其药理用途。 该化合物是强DPPIV（二肽肽酶IV）抑制剂，可以通过良好地抑制DPPIV来间接增加体内GLP-1的含量并在体内诱导一系列生理作用来治疗II型糖尿病。 因此，这些化合物可被开发为用于治疗糖尿病的新的有希望的药物。

公开(公告)号：US20140046074A1

公开(公告)日：2014-02-13

申请号：US13982733

申请日：2012-01-31

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

Inventor： Qiang Zhang ,  Rongxia Zhang ,  Guanghui Tian ,  Jianfeng Li ,  Fuqiang Zhu ,  Xiangrui Jiang ,  Jingshan Shen

IPC: C07C213/02 ,  C07C59/64 ,  C07C235/34 ,  C07C309/75 ,  C07C309/66 ,  C07C43/225 ,  C07C215/54 ,  C07D263/26 ,  C07C43/23

CPC classification number: C07C235/34 ,  C07C17/16 ,  C07C41/26 ,  C07C43/225 ,  C07C43/23 ,  C07C59/64 ,  C07C59/68 ,  C07C213/02 ,  C07C215/54 ,  C07C217/62 ,  C07C309/66 ,  C07C309/73 ,  C07C309/75 ,  C07D263/26 ,  C07D263/52 ,  Y02P20/582 ,  C07C22/04

Abstract: The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.

Abstract translation: 本发明涉及式I所示的（2R，3R）-3-（3-取代苯基）-2-甲基正戊酰胺化合物及其制备方法，其中取代基如本说明书中所定义 ，本发明还涉及上述化合物在制备他喷他多II或其药学上可接受的盐中的用途，以及参与制备方法的中间体。

公开(公告)号：US12290505B2

公开(公告)日：2025-05-06

申请号：US18050240

申请日：2022-10-27

Applicant: FUDAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SHANGHAI MIRACOGEN INC.

Inventor： Ke Yu ,  Jingkang Shen ,  Tao Meng ,  Lanping Ma ,  Xuesai Zhang ,  Qingrou Li ,  Qing Lin

IPC: A61K39/395 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/5365 ,  A61K31/537 ,  A61K47/54 ,  A61K47/68 ,  A61P35/00 ,  C07K16/36

Abstract: A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC. The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity.

公开(公告)号：US20240279177A1

公开(公告)日：2024-08-22

申请号：US18392472

申请日：2023-12-21

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

Inventor： Hong LIU ,  Ben NIU ,  Chunpu LI ,  Jianping CHEN ,  Kun HUANG ,  Jiang WANG

IPC: C07D211/60 ,  C07D401/12 ,  C07D409/12

CPC classification number: C07D211/60 ,  C07D401/12 ,  C07D409/12

Abstract: The present invention relates to the fields of medicinal chemistry and pharmaco therapeutics, and specifically to a method for preparing a compound of formula I and a chemically acceptable salt thereof.