PYRIMIDO[5,4-B]INDOLIZINE OR PYRIMIDO[5,4-B]PYRROLIZINE COMPOUND, PREPARATION METHOD AND USE THEREOF

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...

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Main Authors ZHANG, AO, XIE, HUA, SONG, ZILAN, TONG, LINJIANG, XUE, YU, DING, JIAN, GENG, MEIYU
Format Patent
LanguageEnglish
French
Published 31.05.2018
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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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.
AbstractList 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.
Author ZHANG, AO
SONG, ZILAN
GENG, MEIYU
XIE, HUA
DING, JIAN
XUE, YU
TONG, LINJIANG
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– fullname: GENG, MEIYU
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Snippet 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...
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SubjectTerms CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
Title PYRIMIDO[5,4-B]INDOLIZINE OR PYRIMIDO[5,4-B]PYRROLIZINE COMPOUND, PREPARATION METHOD AND USE THEREOF
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