The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Nov. 10, 2020

Filed:

Nov. 24, 2017
Applicant:

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, CN;

Inventors:

Ao Zhang, Shanghai, CN;

Jian Ding, Shanghai, CN;

Hua Xie, Shanghai, CN;

Zilan Song, Shanghai, CN;

Yu Xue, Shanghai, CN;

Linjiang Tong, Shanghai, CN;

Meiyu Geng, Shanghai, CN;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 471/14 (2006.01); A61P 35/00 (2006.01); C07D 487/14 (2006.01); A61K 31/519 (2006.01); A61P 37/02 (2006.01); A61P 35/02 (2006.01); A61P 29/00 (2006.01);
U.S. Cl.
CPC ...
C07D 471/14 (2013.01); A61K 31/519 (2013.01); A61P 29/00 (2018.01); A61P 35/00 (2018.01); A61P 35/02 (2018.01); A61P 37/02 (2018.01); C07D 487/14 (2013.01);
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.


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