477312-85-9Relevant academic research and scientific papers
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: Synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis
Dyckman, Alaric J.,Langevine, Charles M.,Quesnelle, Claude,Kempson, James,Guo, Junqing,Gill, Patrice,Spergel, Steven H.,Watterson, Scott H.,Li, Tianle,Nirschl, David S.,Gillooly, Kathleen M.,Pattoli, Mark A.,McIntyre, Kim W.,Chen, Laishun,McKinnon, Murray,Dodd, John H.,Barrish, Joel C.,Burke, James R.,Pitts, William J.
experimental part, p. 383 - 386 (2011/02/27)
The synthesis, structure-activity relationships (SAR) and biological evaluation of thiazole based tricyclic inhibitors of IKK2 are described. Compound 9 was determined to be orally efficacious in a murine model of rheumatoid arthritis.
PYRIDAZINE DERIVATIVES FOR INHIBITING BETA AMYLOID PEPTIDE PRODUCTION
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Page/Page column 59, (2009/05/28)
The present invention relates to novel compounds that inhibit the production of β- amyloid peptide (1-42), processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
3-Heterocyclic benzylamide derivatives as potassium channel openers
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Page 8, (2010/02/07)
The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specifi
Synthesis and structure-activity relationship of acrylamides as KCNQ2 potassium channel openers
Wu, Yong-Jin,He, Huan,Sun, Li-Qiang,L'Heureux, Alexandre,Chen, Jie,Dextraze, Pierre,Starrett Jr., John E.,Boissard, Christopher G.,Gribkoff, Valentin K.,Natale, Joanne,Dworetzky, Steven I.
, p. 2887 - 2896 (2007/10/03)
A new class of acrylamides was synthesized, and the effects of these analogues on outward potassium current were evaluated by using two electrode voltage clamp recordings from Xenopus laevis oocytes expressing cloned mKCNQ2 channels. SAR studies indicated that the pharmacophore of the acrylamide series includes the (S) absolute configuration at the (1-phenyl)ethyl moiety and the α,β-unsaturated acrylamide functionality with a free NH. This study identified (S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide ((S)-1) and (S)-N-[1-(4-fluoro-3-morpholin-4-yl-phenyl)-ethyl]-3- (4-fluoro-phenyl)-acrylamide ((S)-2) as KCNQ2 openers for further electrophysiological evaluations. These two acrylamides demonstrated significant activity in the cortical spreading depression model of migraine as we reported previously.
3-(Pyridinyl-piperazin-1-yl)-phenylethyl amides as potassium channel openers
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Page/Page column 7, (2008/06/13)
The present invention provides piperazinyl phenylethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and B are as defined in the specificatio
Arylcyclopropylcarboxylic amides as potassium channel openers
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Page 12-13, (2010/02/07)
The present invention provides novel arylcyclopropylcarboxylic amides and related derivatives having the general Formula I wherein R, R1, R2, R3, R4, R5, R6 and R7 are as defined
