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：US09914707B2

公开(公告)日：2018-03-13

申请号：US15120771

申请日：2015-02-15

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

Inventor： Wenhu Duan ,  Jian Ding ,  Yongcong Lv ,  Hua Xie

IPC: C07D231/56 ,  C07D261/20 ,  C07D413/12 ,  C07D401/12 ,  C07D491/048 ,  C07D495/04

CPC classification number: C07D231/56 ,  C07D261/20 ,  C07D401/12 ,  C07D413/12 ,  C07D491/048 ,  C07D495/04

Abstract: The present invention relates to a naphthylamide compound of the structure as represented by formula (I), medicinal salts, prodrugs and hydrates or solvates thereof, and also relates to a method of preparing the compounds, pharmaceutical compositions comprising the compounds and the uses thereof as protein tyrosine kinase inhibitors, particularly as VEGFR-2 inhibitors, in preparing drugs for preventing and treating diseases related to abnormal angiogenesis.

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：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：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.