用衍生自脂族α,α-二取代的酯和腈的阴离子对2-或4-氰基嗪进行亲核芳族取代会导致氰化物官能团的置换。使氰化物能够在S N Ar反应中用作高活性离去基团,为合成原料提供了额外的灵活性。我们表明,在许多情况下,氰化物离去基团在卤素存在下优先被取代。所得的杂芳基碘化物,溴化物和氯化物随后可用作进一步化学多样化的处理方法。
Compounds of formula (I):
wherein variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are described.
[EN] AMIDO COMPOUNDS AND THEIR USE AS PHARMACEUTICALS<br/>[FR] COMPOSÉS AMIDO ET LEUR UTILISATION COMME PRODUITS PHARMACEUTIQUES
申请人:INCYTE CORP
公开号:WO2005110992A1
公开(公告)日:2005-11-24
The present invention relates to inhibitors of 11-ß hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-ß hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
[EN] ARYL SULFONAMIDE COMPOUNDS AND USES RELATED THERETO<br/>[FR] COMPOSES DE SULFONAMIDE D'ARYLE ET PROCEDES D'UTILISATION CORRESPONDANTS
申请人:AMGEN SF LLC
公开号:WO2005063247A1
公开(公告)日:2005-07-14
The present invention provides Aryl Sulfonamide Compounds having the formula: (I); and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, and other diseases and disorders.
Aryl sulfonamide compounds and uses related thereto
申请人:DeGraffenreid R. Michael
公开号:US20050277649A1
公开(公告)日:2005-12-15
The present invention provides Aryl Sulfonamide Compounds having the formula:
and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, and other diseases and disorders.
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.