azetidinyldiamine as nociceptin launched last february 1 - receptor ligands

摘要

Disclosed are nociceptin ORL-1 receptor agonists of the formula wherein: (a) Rsubscript1 /highlightis optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl; Rsubscript2 /highlightis H; and Rsubscript3 /highlightis -C(H)(R)-NRsubscript7/highlightRsubscript8/highlight; R is H, optionally substituted aryl or arylalkyl, or heteroaryl; Rsubscript7 /highlightis -(CHsubscript2/highlight)subscriptx/highlightRsubscript9/highlight, optionally substituted tetrahydronaphthyl, or cycloalkyl; and Rsuperscript8 is H; or Rsubscript7 /highlightand Rsubscript8 /highlighttogether form a substituted piperidinyl or piperazinyl ring; x is 0-10; and Rsubscript9 /highlightis H, alkoxy, optionally substituted phenyl, naphthyl, heteroaryl, pyrrolidinyl, pyrrolidonyl, optionally substituted piperidinyl or diphenylmethyl; or (b) Rsubscript2/highlightis -NHRsubscript7/highlightor and Rsubscript3 /highlightis H; pharmaceutical compositions; and methods of using the compounds to treat cough and pain.