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：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。