6309-36-0Relevant articles and documents
Discovery of diphenyl lactam derivatives as N-type calcium channel blockers
Doherty, George A.,Bhatia, Pramila,Vortherms, Timothy A.,Marsh, Kennan C.,Wetter, Jill M.,MacK, Helmut,Scott, Victoria E.,Jarvis, Michael F.,Stewart, Andrew O.
, p. 1716 - 1718 (2012/04/04)
A novel series of diphenyl lactam containing calcium channel blockers is described. Extensive SAR studies resulted in compounds with low molar activity and good plasma exposure after oral dosing. Compounds 2, 6 and 7 demonstrated significant efficacy in the capsaicin model of secondary hyperalgesia following oral administration.
NOVEL COMPOUNDS AS CALCIUM CHANNEL BLOCKERS
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Page/Page column 59-60, (2010/04/27)
The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Reactions with Azirridines, 36 Arene Hydrides 2 SN2 and SET Reactions of N-Acylaziridines with Diphenylmethanide and "Naphthalene Hydride" (Anion of Dihydronaphthalene)
Woderer, Anton,Stamm, Helmut
, p. 2050 - 2054 (2007/10/02)
Diphenylmethane is incompletely deprotonated by sodium naphthalenide in THF so that some "naphthalene hydride" 4 (anion of 1,4-dihydronaphthalene) remains present in the deprotonation equilibrium.The generated diphenylmethanide anion 3a reacts with the N-acylaziridines 6a-c to form the expected amidoethyl derivatives 7a-c in yields of less than 50percent.The formation of by-products from 6b and 6c can be rationalized on the basis of classic ionic mechanisms.However, for 6a the by-product N-ethylbenzamide clearly points to a SET mechanism with "naphthalene hydride" 4 as the electron source and with the radical 8 as a hydrogen source.