- Discovery of diphenyl lactam derivatives as N-type calcium channel blockers
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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.
- 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.
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scheme or table
p. 1716 - 1718
(2012/04/04)
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- LACTAM ACETAMIDES AS CALCIUM CHANNEL BLOCKERS
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The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, 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.
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Page/Page column 23-24
(2011/10/10)
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- NOVEL COMPOUNDS AS CALCIUM CHANNEL BLOCKERS
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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.
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Page/Page column 60
(2010/04/27)
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