Azetidinyl diamines useful as ligands of the nociceptin...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C514S408000, C546S268100, C548S950000

Reexamination Certificate

active

06903123

ABSTRACT:
Disclosed are nociceptin ORL-1 receptor agonists of the formulawherein:(a) R1is optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl;R2is H; and R3is —C(H)(R)—NR7R8;R is H, optionally substituted aryl or arylalkyl, or heteroaryl;R7is —(CH2)xR9, optionally substituted tetrahydronaphthyl, or cycloalkyl; and R8is H;or R7and R8together form a substituted piperidinyl or piperazinyl ring;x is 0-10; andR9is H, alkoxy, optionally substituted phenyl, naphthyl, heteroaryl, pyrrolidinyl, pyrrolidonyl, optionally substituted piperidinyl or diphenylmethyl; or(b) R2is —NHR7orand R3is H;pharmaceutical compositions; and methods of using the compounds to treat cough and pain.

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Fawzi et al,Eur. J. Pharmacology, 336 (1997), p. 233-242.
Hey, Bolser et al,Brit. J. Pharmacology, 114 (1995), p. 735-738.
West et al,Molecular Pharmacology, 38 (1990), p. 610-613.

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