40224-22-4Relevant academic research and scientific papers
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit
Nakano, Hirofumi,Hasegawa, Tsukasa,Imamura, Riyo,Saito, Nae,Kojima, Hirotatsu,Okabe, Takayoshi,Nagano, Tetsuo
supporting information, p. 2370 - 2374 (2016/04/20)
A non-selective inhibitor (1) of FMS-like tyrosine kinase-3 (FLT3) was identified by fragment screening and systematically modified to afford a potent and selective inhibitor 26. We confirmed that 26 inhibited the growth of FLT-3-activated human acute myeloid leukemia cell line MV4-11. Our design strategy enabled rapid development of a novel type of FLT3 inhibitor from the hit fragment in the absence of target-structural information.
ARYLALKYLPIPERAZINES FOR USE AS NEUROPROTECTIVE AGENTS
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Page/Page column 29-30, (2016/07/05)
A compound of the general formula A or a or a pharmaceutically acceptable salt or solvate thereof, wherein: R1 is selected from the group consisting of: C1-C12-alkyl, C3-C12-cycloalkyl, C6-
Click chemistry on solid support: Synthesis of a new REM resin and application for the preparation of tertiary amines
L?ber, Stefan,Gmeiner, Peter
, p. 8699 - 8702 (2007/10/03)
1,3-Dipolar cycloaddition was employed for the synthesis of a highly practical REM resin. Exploiting this concept, the resulting triazolylmethyl acrylate (TMA) resin was used for an efficient parallel synthesis of tertiary amines by Michael addition, subs
Substituted indolines which inhibit receptor tyrosine kinases
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Page column 43, (2008/06/13)
Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
Solid phase supports
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, (2008/06/13)
Embodiments of the present invention generally relate to carrying out organic chemistry on solid supports comprising derivatised functionalities, methods for synthesizing said supports, methods for synthesizing compounds comprising amine groups or N-containing heterocycles using said solid supports, intermediate compounds linked to said supports and uses thereof.
Investigation of mixed D2/5-HT1A activity of N-heteroarylmethyl-N-phenylpiperazines, N-heteroarylethyl-N-phenylpiperazines and N-heteroarylpropyl-N-phenylpiperazines.
Roglic,Dukic-Stefanovic,Andric,Kostic-Rajacic,Soskic
, p. 803 - 807 (2007/10/03)
Eight novel N-heteroarylalkyl-N-phenylpiperazines have been synthesized, chemically characterized and evaluated for in vitro binding affinity at the dopamine and serotonin receptors. Synaptosomal membranes of fresh bovine caudate nuclei (D1 and D2), the m
Substituted indolinones with kinase inhibitory activity
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, (2008/06/13)
Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-a
Soluble polymer bound cleavage reagents: A multipolymer strategy for the cleavage of tertiary amines from REM resin
Toy, Patrick H.,Reger, Thomas S.,Janda, Kim D.
, p. 2205 - 2207 (2007/10/03)
(equation presented) Soluble polymer bound reagent 1 has been prepared to cleave tertiary amines from REM resin. Normally, amines cleaved from REM resin require extraction or chromatography to remove excess cleavage reagent and its byproducts. The solubility profile of non-crosslinked polystyrene (NCPS) based reagent 1 eliminates the need for such purification and allows for the direct isolation of a library of pure tertiary amines through simple filtration and concentration operations.
Synthesis of tertiary amines using a polystyrene (REM) resin
Brown, Angus R.,Rees, David C.,Rankovic, Zoran,Morphy, J. Richard
, p. 3288 - 3295 (2007/10/03)
A range of tertiary amines was constructed using a 'traceless' linker on a polystyrene resin (REM resin), starting from seconday amines, primary amines, and resin-bound 'ammonia'. The methodology is characterized by three essential steps conducted under ambient conditions: (1) coupling of the starting amine (Michael addition) to the resin, (2) activation (quaternization), and (3) cleavage of the product amine (Hofmann elimination). The linker is compatible with both acid and base sensitive protecting group strategies. The nature of the chemistry ensures that the tertiary amine products are obtained in consistently high purity (95% or greater). After cleavage of the product, REM resin is regenerated and can be reused for repeat syntheses. The yield and purity of repeat batches is maintained over 5 cycles, allowing the automated synthesis of >0.5 g quantities of pure tertiary amine.
Piperazino methyl phenyl aminoquinolines
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, (2008/06/13)
Antihypertensive compounds of the formula III STR1 wherein X is chloro or trifluoromethyl; wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; wherein R1 is phenyl or phenyl substituted with one or two alkyl, alkoxy, trifluorometh
