- Discovery of pyrrolo-benzo-1,4-diazines as potent Nav1.7 sodium channel blockers
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A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described. Compound 41 displayed anti-nociceptive efficacy in the rat CFA pain model at 100 mpk oral dosing.
- Ho, Ginny D.,Tulshian, Deen,Bercovici, Ana,Tan, Zheng,Hanisak, Jennifer,Brumfield, Stephanie,Matasi, Julius,Heap, Charles R.,Earley, William G.,Courneya, Brandy,Jason Herr,Zhou, Xiaoping,Bridal, Terry,Rindgen, Diane,Sorota, Steve,Yang, Shu-Wei
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p. 4110 - 4113
(2014/11/07)
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- PYRROLO-BENZO-1,4-DIAZINES USEFUL AS SODIUM CHANNEL BLOCKERS
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Pyrrolo-benzo-1,4-diazine compounds represented by Formula I or II, or pharmaceutically acceptable salts thereof, are blockers of voltage-gated sodium channels. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, voltage-gated sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy or epilepsy conditions, irritable bowel syndrome, depression, anxiety, bipolar disorder, neurodegenerative disorders, psychiatric disorders, myotonia, arrhythmia, movement disorders, neuroendocrine disorders, ataxia, multiple sclerosis, irritable bowel syndrome, incontinence, neuropathy and tinnitus, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
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Page/Page column 62
(2011/01/12)
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