- Peptidyl calcium channel blockers
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The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
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- Substituted diarylalkyl amides as calcium channel antagonists
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The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia
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- Reduced dipeptide analogues as calcium channel antagonists
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The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The nov
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- Aniline derivatives as calcium channel blockers
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The present invention provides compounds that block calcium channels having formula (I). The present invention also provides methods of using the compounds of formula (I) to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of formula (I).
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- Synthesis of a series of 4-benzyloxyaniline analogues as neuronal N-type calcium channel blockers with improved anticonvulsant and analgesic properties
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In this article, the rationale for the design, synthesis, and biological evaluation of a series of N-type voltage-sensitive calcium channel (VSCC) blockers is described. N-Type VSCC blockers, such as ziconotide, have shown utility in several models of str
- Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Feng, M. Rose,Lotarski, Susan M.,Rock, David M.,Sinz, Michael,Stoehr, Sally J.,Taylor, Charles P.,Weber, Mark L.,Bowersox, S. Scott,Miljanich, George P.,Millerman, Elizabeth,Wang, Yong-Xiang,Szoke, Balazs G.
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p. 4239 - 4249
(2007/10/03)
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- Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile
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The pseudotetrapeptide FR-139317 is a potent and highly selective antagonist of the endothelin-A (ET(A)) receptor; however, its peptidic nature leads to poor oral absorption characteristics which make it an unlikely drug candidate. In an attempt to improv
- Von Geldern, Thomas W.,Hutchins, Charles,Kester, Jeffrey A.,Wu-Wong, Jinshyun R.,Chiou, William,Dixon, Douglas B.,Opgenorth, Terry J.
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p. 957 - 967
(2007/10/03)
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- Peptide compound and its preparation
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Novel peptides of the formula (I") STR1 in which R1 is hydrogen or acyl, R2c is lower alkyl, R3c is optionally N-substituted indolylmethyl, R4 is hydrogen, lower alkyl, C6-10 ar(lower)alkyl, amino(lower)alkyl, protected amino (lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or optionally substituted heterocyclic (lower)alkyl, R5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl, R7 is hydrogen or lower alkyl, and A is --O--, --NH--, lower alkylamino or lower alkylene, or a pharmaceutically acceptable salt thereof are disclosed. Additionally, the preparation of such peptides is described. The peptides are used to treat endothelin mediated diseases such as hypertension.
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