Title:
PYRIMIDO[5,4-B]INDOLIZINE OR PYRIMIDO[5,4-B]PYRROLIZINE COMPOUND, PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/095398
Kind Code:
A1
Abstract:
The present invention relates to a pyrimido[5,4-b]indolizine or pyrimido[5,4-b]pyrrolizine compound, a preparation method and a use thereof. The compound of the present invention has good inhibitory activity on BTK both at the molecular level and the cellular level. Importantly, the compound of the present invention has relatively low activity on the common human B lymphoma cell Ramos cell, and has high activity on the BTK-sensitive human diffuse large B lymphoma TMD8 cell, which suggests that this structural type of compound has a very relative selectivity, and has a relatively low off-target and corresponding side effect, and is a BTK-selective inhibitor having a development potential.
Inventors:
ZHANG AO (CN)
DING JIAN (CN)
XIE HUA (CN)
SONG ZILAN (CN)
XUE YU (CN)
TONG LINJIANG (CN)
GENG MEIYU (CN)
DING JIAN (CN)
XIE HUA (CN)
SONG ZILAN (CN)
XUE YU (CN)
TONG LINJIANG (CN)
GENG MEIYU (CN)
Application Number:
PCT/CN2017/112729
Publication Date:
May 31, 2018
Filing Date:
November 24, 2017
Export Citation:
Assignee:
SHANGHAI INST MATERIA MEDICA CAS (CN)
International Classes:
C07D471/14; A61K31/519; A61P29/00; A61P35/00; A61P35/02; A61P37/02; C07D487/14
Foreign References:
| CN105073752A | 2015-11-18 | |||
| CN104136438A | 2014-11-05 |
Other References:
RIXSON, JAMES E. ET AL.: "The Development of Domino Reactions Incorporating the Heck Reaction: The Formation of N-Heterocycles", EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, vol. 2012, no. 3, 30 November 2011 (2011-11-30), pages 544 - 558, XP055272224
HUANG, QINHUA ET AL.: "Synthesis of Cyclopropanes by Pd-catalyzed Activation of Alkyl C-H Bonds", TETRAHEDRON LETTERS, vol. 50, no. 52, 8 October 2009 (2009-10-08), pages 7235 - 7238, XP026753910
HUANG, QINHUA ET AL.: "Synthesis of Cyclopropanes by Pd-catalyzed Activation of Alkyl C-H Bonds", TETRAHEDRON LETTERS, vol. 50, no. 52, 8 October 2009 (2009-10-08), pages 7235 - 7238, XP026753910
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (CN)
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