16148-06-4Relevant articles and documents
Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J- 113397)
Kawamoto, Hiroshi,Ozaki, Satoshi,Itoh, Yoshiki,Miyaji, Mitsuru,Arai, Sachie,Nakashima, Hiroshi,Kato, Tetsuya,Ohta, Hisashi,Iwasawa, Yoshikazu
, p. 5061 - 5063 (1999)
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Inhibition of activated STAT5 in Bcr/Abl expressing leukemia cells with new pimozide derivatives
Rondanin, Riccardo,Simoni, Daniele,Romagnoli, Romeo,Baruchello, Riccardo,Marchetti, Paolo,Costantini, Cristiana,Fochi, Sara,Padroni, Giacomo,Grimaudo, Stefania,Pipitone, Rosaria Maria,Meli, Maria,Tolomeo, Manlio
supporting information, p. 4568 - 4574 (2015/02/19)
STATs are transcription factors acting as intracellular signaling after stimulation with cytokines, growth factors and hormones. STAT5 is also constitutively active in many forms of cancers, including chronic myelogenous leukemia, acute lymphoblastic leukemia and Hodgkin's lymphoma. Recently, literature reported that the neuroleptic drug pimozide inhibits STAT5 phosphorylation inducing apoptosis in CML cells. We undertook an investigation from pimozide structure, obtaining simple derivatives with cytotoxic and STAT5-inhibitory activity, two of them markedly more potent than pimozide.
2-oxoimidazole derivatives
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, (2008/06/13)
The present invention relates to a compound represented by Formula [I] wherein represents an aromatic carbo- or heterocyclic ring which may have a substituent; Cy represents a mono-, bi- or tricyclic aliphatic carbocyclic group having 3 to 20 carbon atoms, which may have a substituent; represents a mono- or bicyclic aliphatic nitrogen-containing heterocyclic group having 3 to 14 carbon atoms, which may have a substituent; R1represents a hydrogen atom, a lower alkenyl group, a lower alkynyl group, a cyclo(lower alkyl) group, an amino group, a lower alkylamino group, a di(lower alkyl)-amino group, a hydroxyl group, a lower alkoxy group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group or a di(lower alkyl)carbamoyl group, or a lower alkyl group which may have a substituent; and R2represents a hydrogen atom or a lower alkyl group, a salt or ester thereof, a production process for the same, and an analgesic, a reliever against tolerance to a narcotic analgesic represented by morphine, a reliever against dependence on a narcotic analgesic represented by morphine, an analgesic enhancer, an antiobestic, a drug for ameliorating brain function, a remedy for schizophrenia, a remedy for Parkinsonism, a remedy for chorea, an antidepressant, a remedy for diabetes insipidus, a remedy for polyuria, or a remedy for hypotension, comprising an effective ingredient of the same.