- Heterocyclic substituted aniline calcium channel blockers
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The present invention provides compounds that block calcium channels having the Formula I shown below. STR1The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.
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- Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers
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Selective N-type Voltage Activated Calcium Channel (VACC) blockers have shown utility in several models of stroke and pain. In the process of searching for small molecules as N-type calcium channel blockers, we have identified a series of N,N-dialkylpeptidylamines (e.g., PD 175069) with potent functional activity at N-type VACC. Further modification of the leucine moiety of PD 175069 with a cyclized ring structure provides a series of novel molecules. Syntheses and pharmacological evaluation of the series are presented.
- Hu, Lain-Yen,Ryder, Todd R.,Nikam, Sham S.,Millerman, Elizabeth,Szoke, Balazs G.,Rafferty, Michael F.
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p. 1121 - 1126
(2007/10/03)
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- NEW SYNTHESIS OF PIPECOLIC ACID AND ANALOGS
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Pipecolic acid congeners are synthesised from α-cyanoamides, obtained by substitution of α-methoxyamides with trimethylsilyl cyanide and in an alternative route via oxidation of amidoalkylationproducts of the α-methoxyamides.
- Asher, Vikram,Becu, Christian,Anteunis, Marc J. O.,Callens, Roland
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p. 141 - 144
(2007/10/02)
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