Tertiary amino compounds having opioid receptor affinity
AssigneeEuro-Celtique S.A.
InventorsDonald Kyle, R. Richard Goehring, Sam Victory
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Abstract
Disclosed are compounds of the formula (I) 1 wherein R1, R2 R3 R4 R5, R6 and N are as disclosed herein. The compounds are useful for the treatment of chronic and acute pain.
Claims10
Compounds of the formula (I):
- 4
- R1 is selected from the group consisting of a bond and C1-10 alkyl, alkenyl or alkenylene;
- R2 and R3 are independently selected from the group consisting of hydrogen and C1-10 alkyl, alkenyl or alkenylene
- R4 is selected from the group consisting of a bond and C1-10 alkyl, alkenyl or alkenylene, said C1-10 alkyl, alkenyl or alkenylene optionally substituted with 1-3 halogen or oxo groups;
- R5 is selected from the group consisting of hydrogen, a 5 or 6 membered aromatic or heteroaromatic group, and a C3-12 cycloalkyl;
- R6 is selected from the group consisting of C1-10 alkyl, C3-12 cycloalkyl and halogen;
- and
- N is an integer from 0-3;
- and pharmaceutically acceptable salts thereof.
A method of reducing side effects associated with the administration of opioid analgesics in a human patient comprising administering to said human patient an analgesically effective amount of a non-opioid compound which exhibits a binding affinity specificity for the μ receptor as compared to the ° 2 receptor (Kl (nM) at the δ2 receptor/Ki (nM) at the μ receptor) of greater than about 250.
Dependencies are inferred from the claim text.