Compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals.
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Page/Page column 401
(2016/05/09)
Modulators of S1P and Methods of Making And Using
The invention is directed to Compounds of Formula I: as well as methods of making and using the compounds.
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Page/Page column 61-62
(2010/10/19)
Discovery of an N-(2-aminopyridin-4-ylmethyl)nicotinamide derivative: A potent and orally bioavailable NCX inhibitor
Ca2+ overload in myocardial cells is responsible for arrhythmia. Sodium-calcium exchanger (NCX) inhibitors are more effective than sodium-hydrogen exchanger (NHE) inhibitors with regard to modulation of Ca 2+ overload, because NCX inhibitors can directly inhibit the influx of Ca2+ into cells. NCX is an attractive target for the treatment of heart failure and ischemia-reperfusion. We have designed and synthesized a series of N-(2-aminopyridin-4-ylmethyl)nicotinamide derivatives, based on compound 5. We have discovered a novel NCX inhibitor (23h) with an IC 50 value of 0.12 μM against reverse NCX. The inhibitory activities of our NCX inhibitors against cytochrome P450 were also evaluated. The effects on heart failure and the pharmacokinetic profile of compound 23h are discussed.
A Study of the Photochemically Induced Electron-Transfer Reactions Between Pyridinedicarbonitriles and Primary and Secondary Aliphatic Amines
A study on the photochemically induced electron-transfer from primary and secondary aliphatic amines as donors to pyridinecarbonitriles as the acceptor is reported.A comparison between the substitution positions and the spin density distributions, obtained via teoretical calculations using the 6-31+G basis set, shows some discrepancies, and forms the basis of a hypothesis on the mechanism of the reaction.
Bernardi, Rosanna,Caronna, Tullio,Poggi, Gabriella,Vittimberga, Bruno M.
p. 903 - 908
(2007/10/02)
A Study of the Photochemically Induced Reaction of Pyridine-2,4-dicarbonitrile with Primary and Secondary Amines. A Direct Synthesis of Aminocyanopyridines
A novel synthesis of alkylaminopyridinecarbonitriles by a photoinitiated substitution reaction between pyridine-2,4-dicarbonitrile and certain amines is described.The mechanism is discussed.
Bernardi, Rosanna,Caronna, Tullio,Morrocchi, Sergio,Ursini, Maurizio,Vittimberga, Bruno M.
p. 97 - 100
(2007/10/02)
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