High affinity ligands for nociceptin receptor ORL-1

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S259500, C514S299000, C514S304000, C544S283000, C544S286000, C544S354000, C546S112000, C546S125000, C546S126000, C546S127000, C546S183000

Reexamination Certificate

active

07094784

ABSTRACT:
Novel compounds of the formulaor a pharmaceutically acceptable salt or solvate thereof, wherein:the dotted line represents an optional double bond;X1is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl;X2is —CHO, —CN, optionally substituted amino, alkyl, or aryl;or X1is optionally substituted benzofused heterocyclyl and X2is hydrogen;or X1and X2together form an optionally benzofused spiro heterocyclyl groupR1, R2, R3and R4are independently H and alkyl, or (R1and R4) or (R2and R3) or (R1and R3) or (R2and R4) together can form an alkylene bridge of 1 to 3 carbon atoms;Z1is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2is H or Z1; Z3is H oralkyl; or Z1, Z2and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.

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