81479-48-3Relevant articles and documents
NEW THERAPEUTIC AGENTS FOR THE TREATMENT OF HAEMATOLOGICAL PATHOLOGIES
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Page/Page column 53, (2021/03/05)
The present invention relates to compounds having a tetracyclic system and the use thereof as new therapeutic agents in the treatment of acute myeloid leukemia (AML), preferably in FLT3/ITD hemizygote patients resistant to conventional therapies. The invention also relates to 5,7-dihydro-4H-[1,3]thiazolo[4,5-e]isoindol-2-amine compounds useful as intermediates for the synthesis of tetracyclic imidazo[2',1':2,3][1,3]thiazolo[4,5-e]isoindole compounds.
5-6 -dihydrobenzo [h] quinazoline compound and application thereof
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Paragraph 0087-0089, (2021/09/08)
The invention discloses 5-6 -dihydrobenzo [h] quinazoline compound and application thereof, and belongs to the field of medicines. I, 5-dihydrobenzo [6 -] quinazoline compounds represented by the formula h of the invention have excellent inhibition FLT3 i
Synthesis and biological evaluation of novel 5,6-dihydrobenzo[h]quinazoline derivatives as FLT3 inhibitors
Ding, Lei,Fan, Weizheng,Jiao, Xiaoyu,Tang, Chunlei,Zhang, Qing,Zhao, Kuantao,Zhou, Ying
, (2021/12/22)
Fms-like tyrosine kinase 3 (FLT3) is widely expressed and often mutated in acute myeloid leukemia (AML), which makes it an important target for the treatment of AML. The structure-based synthesis and biological evaluation of 5,6-dihydrobenzo[h]quinazoline
Inhibitors of NEK7 kinase
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Page/Page column 116; 117-118, (2021/11/03)
Compounds having activity as inhibitors of NEK7 are provided. The compounds have Structure (I):or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein, A, X, Y, R1, R2, R3, R4 and R5 are as defined herein. Methods associated with p
Benzo imidazo [2, 1-b] thiazole compound and application thereof (by machine translation)
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Paragraph 0087-0089, (2020/07/15)
The invention discloses a benzoimidazo [2, 1-b] thiazole compound and application thereof, and belongs to the technical field of medicines. The inhibitory activity of the synthesized benzimidazo [2, 1-b] thiazole analogues on FLTT3 is more than 90%, wherein the compounds (compounds 2 , 4, 6, 8 and 10) are IC of FLTT3-ITD kinase. 50 Lower value, in particular compound 2, IC IC50 The value is only 5.60 nm, and therefore the compound of the present invention may be used as an inhibitor FLTT3, or for preparing a drug capable of modulating or suppressing diseases associated with abnormal cell proliferation by affecting the enzymatic activity of one or more tyrosine kinases and interfering with aberrant cell proliferation, having a wide application prospect. (by machine translation)
Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors
Jiao, Xiaoyu,Tang, Chunlei,Zhang, Lixun,Zhang, Qing,Zhang, Yongjie,Zhao, Kuantao
supporting information, (2020/10/02)
As a class III receptor tyrosine kinase (RTK), FMS-like tyrosine kinase 3 (FLT3) is always overexpressed in many cases of acute leukemia. This paper studies the structure-based synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 15b, 16b, 24a, and 24c showed excellent biological activities in a low nanomolar range. In particular, compound 16b demonstrated significant inhibitory potency against FLT3-ITD (IC50 = 5.60 nM) and better antiproliferative activity than quizartinib against MV4-11 cell line (IC50 = 0.176 nM). It is indicated that compound 16b for the treatment of acute myeloid leukemia could be very promising.
SUBSTITUTED N-HETEROCYCLYL- AND N-HETEROARYL-TETRAHYDROPYRIMIDINONES AND THE SALTS THEREOF, AND THE USE OF SAME AS HERBICIDAL ACTIVE SUBSTANCES
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Paragraph 0198-0199; 0218-0221; 0226-0227, (2020/12/25)
The present invention relates to substituted N-heterocyclyl- and N-heteroaryltetrahydropyrimidinones of the general formula (I) or salts thereof, where the radicals in the general formula (I) correspond to the definitions given in the description, and to
Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion
Burslem, George M.,Song, Jayoung,Chen, Xin,Hines, John,Crews, Craig M.
supporting information, p. 16428 - 16432 (2018/12/11)
The receptor tyrosine kinase FLT-3 is frequently mutated in acute myeloid leukemia; however, current small molecule inhibitors suffer from limited efficacy in the clinic. Conversion of a FLT-3 inhibitor (quizartinib) into a proteolysis targeting chimera (
KINASE INHIBITORS
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Paragraph 0659; 0660; 0661, (2017/10/27)
There are provided compounds of formula I, wherein T, A, Q, Z, G, R4, R5a, R5b and n have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members
HERBICIDAL MIXTURES
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Page/Page column 47; 48, (2016/10/31)
The present invention provides a composition comprising (A) a compound of formula (I): wherein R1 is methyl or methoxy, R2 is hydrogen, methyl or ethoxy and A is a substituted heteroaryl group, or an N-oxide or salt form thereof, and