79456-34-1Relevant academic research and scientific papers
Fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834
Angelaud, Rémy,Beaudry, Danial,Carrera, Diane E.,Gosselin, Francis,Huestis, Malcolm P.,Liu, Wendy,Siu, Michael,Xu, Jie
, (2020/10/02)
A practical fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834 (1) was developed. The key C[sbnd]C bond was constructed via a Suzuki–Miyaura cross-coupling of iodopyrazole 2 and pyridine boronic ester 3 to afford ketone 12. Su
HETEROCYCLIC COMPOUNDS AND THEIR USE FOR TREATMENT OF HELMINTHIC INFECTIONS AND DISEASES
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Paragraph 00249, (2020/11/03)
Provided herein are Heterocyclic compounds of formula (I): and pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein W, X, Y, R1, R2, and RN are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound, and methods for treating or preventing animal and human filarial worm infections and diseases.
Transition metal-free direct C–H trifluoromethyltion of (hetero)arenes with Togni's reagent
Chen, Xiaoyu,Ding, Licheng,Li, Linlin,Li, Jingya,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
supporting information, (2019/12/30)
A new transition-metal-free direct C–H trifluoromethylation reaction of (hetero)arenes with Togni's reagent was developed. This transformation proceeded smoothly under mild conditions and exhibited good tolerance of many synthetically relevant functional groups. It provided an alternative approach for the synthesis of trifluoromethylated (hetero)arenes.
Synthesis method and applications of polysubstituted 2-aminopyridine derivative
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Paragraph 0060-0062; 0063; 0064, (2020/04/22)
The invention belongs to the field of organic synthetic chemistry, and relates to a synthetic method and applications of a polysubstituted 2-aminopyridine derivative. According to the method, a 1,2,3-triazine compound and a cyanomethyl compound are used as substrates and are subjected to a one-step cycloaddition reaction under an alkaline condition to obtain a polysubstituted 2-aminopyridine derivative, wherein the reaction does not involve in danger and control reagents and medicines, and a simple, safe, efficient and environment-friendly strategy is provided for synthesizing the polysubstituted 2-aminopyridine derivative. According to the present invention, the obtained product is subjected to further derivatization, such that the active molecule or the drug molecule containing the 2-aminopyridine structure can be synthesized, such as active molecule SC-53606, drug molecule apatinib and nevirapine.
SUBSTITUTED THIAZOLO-PYRIDINE COMPOUNDS AS MALT1 INHIBITORS
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Page/Page column 314-315, (2018/02/28)
Disclosed are compounds of the general formula (I), wherein R1-R3 are as defined herein, for use as MALT1 inhibitors in the treatment of autoimmune and inflammatory diseases or disorders. Methods of synthesizing the compounds are also disclosed. Also disc
2-MORPHOLIN-4,6-DISUBSTITUTED PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
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Paragraph 0092; 0109, (2017/11/11)
Disclosed is a 2-morpholin-4,6-disubstituted pyrimidine derivative as shown in formula (I) below, and a pharmaceutically acceptable salt, solvate, stereoisomer or prodrug thereof, and a pharmaceutical composition thereof and a use thereof, wherein the definition of each group is as shown in the description. The compound has a PI3K kinase inhibition activity, and has a relatively high inhibitive ability and a low cytotoxicity against PIK3CA mutant breast cancer cell strains T47D and MCF-7.
As the NS4B inhibitor benzofuran analogs (by machine translation)
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Paragraph 0364; 0366; 0367; 0368; 0369, (2016/10/31)
The present invention discloses a kind of as NS4B benzofuran analogue inhibitors, in particular to the formula (I) below or a pharmaceutically acceptable salt thereof. (by machine translation)
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19
Mallinger, Aurélie,Schiemann, Kai,Rink, Christian,Stieber, Frank,Calderini, Michel,Crumpler, Simon,Stubbs, Mark,Adeniji-Popoola, Olajumoke,Poeschke, Oliver,Busch, Michael,Czodrowski, Paul,Musil, Djordje,Schwarz, Daniel,Ortiz-Ruiz, Maria-Jesus,Schneider, Richard,Thai, Ching,Valenti, Melanie,De Haven Brandon, Alexis,Burke, Rosemary,Workman, Paul,Dale, Trevor,Wienke, Dirk,Clarke, Paul A.,Esdar, Christina,Raynaud, Florence I.,Eccles, Suzanne A.,Rohdich, Felix,Blagg, Julian
, p. 1078 - 1101 (2016/02/23)
The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in human disease, particularly in colorectal cancer where it has been reported as a putative oncogene. Here we report the discovery of 109 (CCT251921), a potent, selective, and orally bioavailable inhibitor of CDK8 with equipotent affinity for CDK19. We describe a structure-based design approach leading to the discovery of a 3,4,5-trisubstituted-2-aminopyridine series and present the application of physicochemical property analyses to successfully reduce in vivo metabolic clearance, minimize transporter-mediated biliary elimination while maintaining acceptable aqueous solubility. Compound 109 affords the optimal compromise of in vitro biochemical, pharmacokinetic, and physicochemical properties and is suitable for progression to animal models of cancer.
multi-links class PI3K inhibitors (by machine translation)
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Paragraph 0454; 0455; 0456, (2016/10/09)
The invention belongs to the field of medical technology, in particular of formula (I) shown in multi-links class of PI3K inhibitors, its stereoisomers or its pharmaceutically acceptable salt thereof, wherein the R 1, R 2, R 3, R 4 or R 5 as defined in the specification; the invention also relates to methods of preparing such compounds, pharmaceutical compositions of these compounds in the preparation and treatment and/or prevention of proliferative diseases of the use of the medicament. (by machine translation)
HETEROARYL SUBSTITUTED HETEROCYCLYL SULFONES
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Page/Page column 87; 88, (2015/11/09)
The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
