Back to results
US 5,159,081 AGranted
Intermediates of peripherally selective N-carbonyl-3,4,4-trisubstituted piperidine opioid antagonists
AssigneeEli Lilly and Company
InventorsBuddy E. Cantrell, Dennis M. Zimmerman
Life of this patent
Estimating the term…
Abstract
Intermediates of N-carbonyl-3,4,4-substituted piperidines are provided which are useful in the preparation of peripheral opioid antagonists.
Claims18
An intermediate which is a trans-3,4-stereoisomer of the compound of the formula ##STR14## wherein R.sup.1 is hydrogen or (C.sub.1 -C.sub.5)alkyl;
- R.sup.2 is hydrogen, (C.sub.1 -C.sub.5)alkyl, or (C.sub.2 -C.sub.6)alkenyl;
- R.sup.3 is hydrogen, (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.10)alkenyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.3 -C.sub.8) cycloalkyl-(C.sub.1 -C.sub.3) alkyl, phenyl, (C.sub.5 -C.sub.8) cycloalkenyl, (C.sub.5 -C.sub.8)cycloalkenyl-(C.sub.1 -C.sub.3)alkyl, or phenyl-(C.sub.1 -C.sub.3) alkyl;
- R.sup.4 is hydrogen, (C.sub.3 -C.sub.8) cycloalkyl, (C.sub.1 -C.sub.10) alkyl, (C.sub.3 -C.sub.10)alkenyl, (C.sub.3 -C.sub.8)cycloalkyl-(C.sub.1 -C.sub.3)alkyl, phenyl or phenyl-(C.sub.1 -C.sub.3) alkyl;
- Z is an amino blocking group when R.sup.4 is not phenyl or Z is hydrogen when R.sup.4 is phenyl;
- and
- n is 1-3.
3 more elements
Dependencies are inferred from the claim text.