公开(公告)号：US11834432B2

公开(公告)日：2023-12-05

申请号：US15998927

申请日：2017-02-17

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

Inventor： Ao Zhang ,  Meiyu Geng ,  Li Xing ,  Jing Ai ,  Zilan Song ,  Xia Peng ,  Wangting Gu ,  Jian Ding

IPC: C07D213/75 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61P35/00 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4433 ,  A61K31/4409 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/44

CPC classification number: C07D401/12 ,  A61P35/00 ,  C07D213/75 ,  C07D403/12 ,  C07D405/12 ,  C07D413/14 ,  C07D417/14

Abstract: Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.

公开(公告)号：US10829491B2

公开(公告)日：2020-11-10

申请号：US16463868

申请日：2017-11-24

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

Inventor： Ao Zhang ,  Jian Ding ,  Hua Xie ,  Zilan Song ,  Yu Xue ,  Linjiang Tong ,  Meiyu Geng

IPC: C07D471/14 ,  A61P35/00 ,  C07D487/14 ,  A61K31/519 ,  A61P37/02 ,  A61P35/02 ,  A61P29/00

Abstract: The present disclosure relates to a Pyrimido[5,4-b]indolizine or pyrimido[5,4-b]pyrrolizine compound, preparation method thereof and use thereof. The compounds of the present invention have good inhibitory activities against BTK at the molecular and cellular levels. Importantly, the compounds of the present invention have low activity against Ramos cells of normal human B lymphoma cells, and have high activity against BTK-sensitive human diffuse large B lymphoma TMD8 cells, indicating that these type of compounds with novel structural are highly selective, off-target phenomenon and corresponding side effects are low. Thus it is a selective inhibitor of BTK with development potential.

公开(公告)号：US11191761B2

公开(公告)日：2021-12-07

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 ,  A61K47/10 ,  A61K9/10 ,  A61K9/20 ,  A61K9/08 ,  A61K9/14

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：US20190292183A1

公开(公告)日：2019-09-26

申请号：US16463868

申请日：2017-11-24

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

Inventor： Ao Zhang ,  Jian Ding ,  Hua Xie ,  Zilan Song ,  Yu Xue ,  Linjiang Tong ,  Meiyu Geng

IPC: C07D471/14 ,  C07D487/14 ,  A61P35/00

Abstract: The present disclosure relates to a Pyrimido[5,4-b]indolizine or pyrimido[5,4-b]pyrrolizine compound, preparation method thereof and use thereof. The compounds of the present invention have good inhibitory activities against BTK at the molecular and cellular levels. Importantly, the compounds of the present invention have low activity against Ramos cells of normal human B lymphoma cells, and have high activity against BTK-sensitive human diffuse large B lymphoma TMD8 cells, indicating that these type of compounds with novel structural are highly selective, off-target phenomenon and corresponding side effects are low. Thus it is a selective inhibitor of BTK with development potential.

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。