40224-23-5Relevant 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
, 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 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-
NOVEL POTASSIUM CHANNEL BLOCKER
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Page/Page column 48, (2010/04/06)
The present invention provides a compound of formula (I):or its salts or pharmaceutically acceptable derivatives wherein; R1 is selected from the group consisting of optionally substituted arylalkyl, optionally substituted aryl, optionally substituted heteroarylalkyl and optionally substituted heteroaryl; R2 is selected from the group consisting of optionally substituted acyl, optionally substituted sulfonyl and optionally substituted sulfamoyl; R3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino carbonyl, optionally substituted amino sulfonyl or nitrile; X1 is selected from a group consisting of a chemical bond, CR7R8, C(=O), C(=NH), NR9, NHC(O), and SO2 wherein; R7 and R8 are independently selected from hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl and optionally substituted heteroaryl or; R7 and R8 together form an optionally substituted C4-6 cycloalkyl ring; R9 is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted aryl and optionally substituted heteroaryl; A represents an optionally substituted saturated or partially saturated 4-7 membered ring with the general formula (A): or is selected from formula (B): For each occurrence; X2 is CH or N; X3 is CH2, CH(R5a), C(R5a)(R5b), NH, N(R5c), O or S; X4 is independently selected from C(=O), CH2, CH(R4a) or C(R4a)(R4b); R4a and R4b for each occurrence is independently halogen, optionally substituted amino, hydroxyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R5a and R5b for each occurrence is independently, halogen, optionally substituted amino, hydroxyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted alkyl, optionally substituted alkanoyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; R5c is optionally substituted acyl, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; n = 1 or 2. The compounds are useful as potassium ion channel inhibitors.
Substituted indolines which inhibit receptor tyrosine kinases
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Page column 48, (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.
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
N-phenyl-imidazolidine-1-ones
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, (2008/06/13)
Compounds of the formula SPC1 Wherein R is hydrogen, halogen, lower alkyl or lower alkoxy, R' is --CHR1 --Q--A, --CHR2 --A or --O--CHR2 --CHR1 --Q--A, each in m- or p-position, Where A is SPC2 Q is straight or branched alkylene of 1 to 4 carbon atoms, R1 is hydrogen, hydroxyl, lower alkoxy or --O--CO--R5, R2 is hydrogen or methyl, R3 and R4, which may be identical to or different from each other, are each hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl or, together with each other and neighboring carbon atoms of the phenyl ring to which they are attached, form a saturated or unsaturated carbocyclic 5- to 6-membered ring, R5 is lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino, (mono-lower alkyl)-amino or (di-lower alkyl)-amino, Z is an aromatic heterocyclic ring with one to two heteroatoms, which may optionally be condensed with a benzene ring, and R" is hydrogen, straight or branched lower alkyl, lower alkenyl, lower alkynyl, hydroxy-lower alkyl, (di-lower alkyl)-amino-lower alkyl or aralkyl, And their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as their salts are useful as CNS-depressants, neuroleptics, analgesics, antiphlogistics, spasmolytics, broncholytics, hypotensives and anti-cholesteremics.
