abstract |
The present invention relates to the use of an ORL-1 receptor agonist, optionally in combination with other agents, for the treatment of cough, and pharmaceutical compositions containing such compounds. The ORL-1 receptor agonist may be, for example, a compound of the formula: wherein the aponted line is a double bond; X1 is -R5-alkyl, R6-cycloalkyl, R7-aryl, R8-heteroaryl or R10-heterocycloalkyl, X2 is -CHO, -CN, -NHC (= NR26) NHR26-, -CH (= NOR26), -NHOR26, R7-aryl, R7-arylalkyl, R7-arylalkenyl, R7-arylalkynyl, (CH2) vOR13, - (CH2) vCOOR27, - (CH2) vCONR14R15, - (CH2). vNR21R22 or - (CH2) vNHC (O) R21 or X1 and X2 are hydrogen: either X1 and X2 together are a general spiro group, R1, R2, R3 and R4 are hydrogen, alkyl, or two together are an alkylene bridge bridge; Z1 is R5-alkyl, R7-aryl, R8-heteroaryl, R6-cycloalkyl, R10-heterocycloalkyl, -CO2-alkyl, cyano or -C (O) NR19R20, Z2 is hydrogen or Z1, Z3 is hydrogen or or Z1, Z2 and Z3 together with the carbon atom to which they are attached form a group. HE |