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publicationNumber US-6455527-B2
titleOfInvention High affinity ligands for nociceptin receptor ORL-1
abstract Novel compounds of the formulaor a pharmaceutically acceptable salt or solvate thereof, wherein:the dotted line represents an optional double bond;X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl;X2 is -CHO, -CN, optionally substituted amino, alkyl, or aryl;or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen;or X1 and X2 together form an optionally benzofused spiro heterocyclyl groupR1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms;Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or -CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and 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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Total number of triples: 2105.