Patent ID: 7199129

Claim:
A compound of formula I in which YN is a morphine-like opioid radical of Formula II wherein: R a is H, C 1-4 alkyl, C 1-4 alkanoyl, C 1-4 carboxyalkyl, or an O— protecting group; R b is H, OH, protected hydroxy, C 1-4 alkanoyloxy or C 1-4 alkoxy; or, when C6 does not have a double bond to C7, and does not have an endoetheno or endoethano bridge to C14, R b may be ═O or ═CH 2 ; R c is absent, or, when C6 does not have a double bond to C7, and does not have an endoetheno or endoethano bridge to C14, R c is H, OH or protected hydroxy; R d is H or C 1-4 alkyl; R c is H, CN, C 1-4 alkanoyl, C 1-4 alkoxycarbonyl, C 2-8 alkenyl, in which R f is H, alkyl, aryl, or alkaryl, and R g is C 1-8 alkyl, C 2-6 alkenyl, C 2-6 alkenyl, each of these three groups being optionally substituted by aryl, or R g is substituted aryl (the substituent(s) on the aryl group being chosen from halo, alkyl, C 1-4 alkoxy, haloalkyl), tetrahydrofuranyl, C 1-4 alkoxy; and wherein the oxygen between C4 and C5 may or may not be present, as represented by the broken lines; wherein the brackets around the group between C6 and C14 represents that the group may or may not be present, and when present the group may be an endoetheno or an endoethano bridge, as represented by the broken line; and wherein the dashed line between C6, C7, C8 and C14 represents that there is or are either zero, one or two double bonds, with the one double bond being either between C6 and C7, or C7 and C8, and the two double bonds being between C6 and C7, and C8 and C14; X is—a direct bond, an optionally substituted, branched, straight-chained or cyclic alkylene having from 1 to 6 carbon atoms, optionally containing one or two heteroatoms in the alkyl chain, or an optionally substituted, branched or straight-chained alkenylene having from 4 to 10 carbon atoms; and R, R′ and K″ are independently hydrogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, substituted alkyne, aryl, substituted aryl, heterocycle, substituted heterocycle or cyano provided that at least one of R and R′ is aryl, substituted aryl, heterocycle or substituted heterocycle which is directly attached to the nitrogen atom of the guanidine group through an atom of the aryl or heterocycle group; or a pharmaceutically acceptable salt, hydrate, solvate, tautomer and/or isomer thereof.