- NEW THERAPEUTIC AGENTS FOR THE TREATMENT OF HAEMATOLOGICAL PATHOLOGIES
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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.
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Page/Page column 53
(2021/03/05)
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- 5-6 -dihydrobenzo [h] quinazoline compound and application thereof
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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
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Paragraph 0087-0089
(2021/09/08)
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- Synthesis and biological evaluation of novel 5,6-dihydrobenzo[h]quinazoline derivatives as FLT3 inhibitors
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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
- Ding, Lei,Fan, Weizheng,Jiao, Xiaoyu,Tang, Chunlei,Zhang, Qing,Zhao, Kuantao,Zhou, Ying
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- Inhibitors of NEK7 kinase
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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
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Page/Page column 116; 117-118
(2021/11/03)
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- Benzo imidazo [2, 1-b] thiazole compound and application thereof (by machine translation)
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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)
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Paragraph 0087-0089
(2020/07/15)
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- Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors
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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.
- Jiao, Xiaoyu,Tang, Chunlei,Zhang, Lixun,Zhang, Qing,Zhang, Yongjie,Zhao, Kuantao
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supporting information
(2020/10/02)
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- SUBSTITUTED N-HETEROCYCLYL- AND N-HETEROARYL-TETRAHYDROPYRIMIDINONES AND THE SALTS THEREOF, AND THE USE OF SAME AS HERBICIDAL ACTIVE SUBSTANCES
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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
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Paragraph 0198-0199; 0218-0221; 0226-0227
(2020/12/25)
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- Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion
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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 (
- Burslem, George M.,Song, Jayoung,Chen, Xin,Hines, John,Crews, Craig M.
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supporting information
p. 16428 - 16432
(2018/12/11)
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- KINASE INHIBITORS
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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
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Paragraph 0659; 0660; 0661
(2017/10/27)
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- HERBICIDAL MIXTURES
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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
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Page/Page column 47; 48
(2016/10/31)
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- HERBICIDAL COMPOUNDS
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The invention relates to dihydro-hydantoincompounds of the formula (I) wherein X, Rb, Rc, R2 and R3 are as defined in the specification. Furthermore, the present invention relates to processes and intermediates
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Page/Page column 33
(2016/05/09)
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- PROCESS FOR THE PREPARATION OF IMIDAZO[2,1-B][1,3]BENZOTHIAZOLE DERIVATIVES
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Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)- N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,l-fe][l,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert- Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,l-and][l,3]benzo- thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers. N-(5-ferf-Butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl- ethoxy)imidazo[2,l-and][l,3]benzothiazol-2-yl]phenyl}urea is represented by the structure:
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Page/Page column 84-85
(2011/06/11)
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- Pyridyloxyindoles Inhibitors of VEGF-R2 and Use Thereof for Treatment of Disease
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The invention relates to novel organic compounds of formula (I), and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in the treatment of tumour diseases and ocular neovascular diseases.
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Page/Page column 65
(2010/06/22)
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- COMPOUNDS HAVING TIE2 (TEK) INHIBITORY ACTIVITY
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The invention relates to a compound of the Formula (I) I or salt, prodrug or solvate thereof, wherein R1, R5, R6, D, A, B, L, n, m and p are as defined in the description. The invention also relates to pharmaceutical compo
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Page/Page column 86
(2008/06/13)
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- PYRIMIDINES WITH TIE2 (TEK) ACTIVITY
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The invention relates to a compound of the Formula (I); or salt thereof, wherein R1, R2, R3, R4, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to ph
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Page/Page column 98
(2010/02/12)
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- PYRIMIDINES WITH TIE2 (TEK) ACTIVITY
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The invention relates to a compound of the Formula (I). or salt thereof wherein R1, R2, R3, R4, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.
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Page/Page column 98
(2010/02/12)
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