Substituted pyrroles with opioid receptor activity

Details Substituted pyrroles with opioid receptor activity Substituted pyrroles with opioid receptor activity

1986-05-08

1987-03-10

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548417, 549432, C07D49122

Patent

active

046492003

ABSTRACT:
Substituted pyrroles of the formula: ##STR1## are disclosed wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl) alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, aryl, aralkyl, trans-(C.sub.4 -C.sub.5) alkenyl, allyl or furan-2-ylalkyl; R.sup.2 is H or OH, R.sup.3 is H, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkanoyl and R.sup.4 is H or (C.sub.1 -C.sub.5) alkyl; as well as the pharmaceutically-acceptable salts thereof. These compounds are useful as analgesics and/or as selective kappa-opioid antagonists.

REFERENCES:
The Condensed Chemical Dictionary, G. G. Hawley, ed., Van Nostrand Reinhold Co., N.Y. (10th ed., 1981) at pp. 90 and 525.
W. R. Martin, Pharmacol. Rev., 35, 283 (1984).
M. Erez et al., J. Med. Chem., 25, 847 (1982).
P. S. Portoghese et al., Life Sciences, 36, 801 (1985).
Rapoport et al, J. A. C. S. 89, 1942(1967).
Astill et al, J. A. C. S. 77, 4079(1955).

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