- Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain
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A series of new voltage-gated sodium channel blockers were prepared based on the screening lead succinic diamide BPBTS. Replacement of the succinimide linker with the more rigid cyclic 1,2-trans-diamide linker was well tolerated. N-Methylation on the biph
- Shao, Pengchang P.,Ok, Dong,Fisher, Michael H.,Garcia, Maria L.,Kaczorowski, Gregory J.,Li, Chunshi,Lyons, Kathryn A.,Martin, William J.,Meinke, Peter T.,Priest, Birgit T.,Smith, McHardy M.,Wyvratt, Matthew J.,Ye, Feng,Parsons, William H.
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p. 1901 - 1907
(2007/10/03)
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- ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR Xa INHIBITORS
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Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders.
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Page/Page column 17
(2010/02/06)
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- 1,2 DIAMIDO CYCLOALKYL SODIUM CHANNEL BLOCKERS
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1,2 Diamido cycloalkyl compounds that are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidin-dione and aryl-link-aryl oxazolodine-dione compounds and a pharmaceutically acceptable carrier; and a method of treatment of acute pain, chronic pain, visceral pain, inflammatory pain, or neuropathic pain, as well as irritable bowel syndrome, Crohns disease, epilepsy, partial and generalized tonic seizures, multiple sclerosis, bipolar disease, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolodine-dione compounds, either alone, or in combination with one or more therapeutically active compounds, are described.
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- ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR XA INHIBITORS
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Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: STR1 where X is O, S or NR 15.
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- Triazolinone Biphenylsulfonamide Derivatives as Orally Active Angiotensin II Antagonists with Potent AT1 Receptor Affinity and Enhanced AT2 Affinity
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Several series of 2,4-dihydro-2,4,5-trisubstituted-3H-1,2,4-triazol-3-ones with acidic sulfonamide replacements of tetrazole at the 2'-position of the biphenyl-4-ylmethyl side chain at N4 were prepared and tested as angiotensin II (AII) antagon
- Ashton, Wallace T.,Chang, Linda L.,Flanagan, Kelly L.,Hutchins, Steven M.,Naylor, Elizabeth M.,et al.
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p. 2808 - 2826
(2007/10/02)
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