227626-62-2Relevant academic research and scientific papers
Oxadiazolone bioisosteres of pregabalin and gabapentin
Wustrow, David J.,Belliotti, Thomas R.,Capiris, Thomas,Kneen, Clare O.,Bryans, Justin S.,Field, Mark J.,Williams, Dic,El-Kattan, Ayman,Buchholz, Lisa,Kinsora, Jack J.,Lotarski, Susan M.,Vartanian, Mark G.,Taylor, Charles P.,Donevan, Sean D.,Thorpe, Andrew J.,Schwarz, Jacob B.
scheme or table, p. 247 - 250 (2009/05/26)
A series of oxadiazolone bioisosteres of pregabalin 1 and gabapentin 2 were prepared, and several were found to exhibit similar potency for the α2-δ subunit of voltage-gated calcium channels. Oxadiazolone 9 derived from 2 achieved low brain upt
1-substituted-1-aminomethyl-cycloalkane derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders
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, (2008/06/13)
Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A′ is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1to Z4are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, especially irritable bowel syndrome.
