Large substituent, non-phenolic opioids and methods of use thereof

A method of treating a patient suffering from a disease or condition wherein said disease or condition is chosen from the group consisting of pain, pruritis, irritable bowel syndrome, respiratory depression, and drug addiction comprising administering to said patient a compound having the formula:

• wherein
• is an aryl or heteroaryl residue of one to three rings;
• A is (CH2)n, wherein one or more CH2 may be replaced by —O—, cycloalkyl or CR1aR1b;
• R1a and R1b are chosen independently from hydrogen, halogen, lower alkyl, lower alkoxy and lower alkylthio;
• R2 and R2a are both hydrogen or taken together R2 and R2a are ═O;
• R3 is chosen from hydrogen, C1-C8 hydrocarbon, heterocyclyl, heterocyclylalkyl and hydroxyalkyl;
• R4 is chosen from hydrogen, hydroxyl, amino, lower alkoxy, C1-C20 alkyl and C1-C20 alkyl substituted with hydroxyl or carbonyl;
• R5 is lower alkyl;
• R6 is lower alkyl;
• R7 is chosen from hydrogen and hydroxyl;
• or
• together R4, R5, R6 and R7 may form one to three rings, said rings having optional additional substitution;
• R10 is one or two residues chosen independently from hydrogen, hydroxyl, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl and halo(C1-C6)alkoxy and (C1-C6)alkylthio;
• R11 is H or
• is an aryl or heteroaryl residue of one to three rings;
• A′ is (CH2)m wherein one or more CH2 may be replaced by —O—, cycloalkyl, —CR1aR1b, —C(═O)— or —NH—;
• R12 is chosen from hydrogen and lower alkyl;
• R15 is one or two residues chosen independently from hydrogen, hydroxyl, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl and halo(C1-C6)alkoxy and (C1-C6)alkylthio;
• m is zero or an integer from 1 to 6;
• and
• n is an integer from 1 to 6;
• with the proviso that A is other than CH2.