857289-52-2Relevant academic research and scientific papers
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275
Siu, Michael,Johnson, Theodore O.,Wang, Yong,Nair, Sajiv K.,Taylor, Wendy D.,Cripps, Stephan J.,Matthews, Jean J.,Edwards, Martin P.,Pauly, Thomas A.,Ermolieff, Jacques,Castro, Arturo,Hosea, Natilie A.,LaPaglia, Amy,Fanjul, Andrea N.,Vogel, Jennifer E.
, p. 3493 - 3497 (2009)
N-(Pyridin-2-yl) arylsulfonamides are identified as inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1), an enzyme that catalyzes the reduction of the glucocorticoid cortisone to cortisol. Dysregulation of glucocorticoids has been implicated in the pathogenesis of diabetes and the metabolic syndrome. In this Letter, we present the development of an initial lead to an efficient ligand with improved physiochemical properties using a deletion strategy. This strategy allowed for further optimization of potency leading to the discovery of the clinical candidate PF-915275.
INHIBITORS OF 11ΒΕΤΑ-HYDROXY STEROID DEHYDROGENASE TYPE 1 (11BETA-HSD1)
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Page/Page column 32, (2010/11/30)
The invention relates to sulfonamide compounds of formula (I) wherein A, B, R1and X1 to X3 have the meaning as cited in the description and the claims. For example A is biphenyl, B is 2-morpholin-4-yl-2-oxo-ethyl, R1 is H and X1 to X3 are CH. Said compounds are useful as 11β-HSD1 inhibitors. The invention also relates to the preparation of such compounds as well as the production and use as medicament.
Amino heterocyclyl inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
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Page/Page column 20; 37, (2010/02/12)
The present invention relates to compounds with the formula (I), or a pharmaceutically acceptable salt thereof: The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) or formula (II) and methods of treating a condition that is mediated by the modulation of 11-β-hsd-1, the method comprising administering to a mammal an effective amount of a compound of formula (I) or formula (II).
