Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1987-12-24
1989-02-21
Daus, Donald G.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
546 45, 546 46, C07D48900, C07D48906, A61K 31485
Patent
active
048065560
ABSTRACT:
Gut-selective agonist or antagonist opiates of the formula: ##STR1## wherein R is (C.sub.1 -C.sub.5) alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, aryl, aralkyl or trans-(C.sub.2 -C.sub.5)alkenyl; Z is H or OH, R' is (C.dbd.O)-A(B)(C) wherein A is selected from the group consisting of (C.sub.1 -C.sub.5)alkyl, (C.sub.2 -C.sub.5)alkenyl and (C.sub.2 -C.sub.6)alkoxy (alkyl); B is selected from the group consisting of H, amino and a (C.sub.1 -C.sub.5)alkyl group optionally substituted with CO.sub.2 H, OH or phenyl and C is CO.sub.2 H, SO.sub.3 H, amino or guanidino; and R" is selected from the group consisting of NH-A(B) (C) or is guanidino; and the pharmaceutically-acceptable salts thereof.
REFERENCES:
patent: 3320262 (1967-05-01), Lewenstein et al.
patent: 4362870 (1982-12-01), Portoghese
patent: 4401672 (1983-08-01), Portoghese
patent: 4608376 (1986-08-01), Pasternak
Bognar, et al., Chemical Abstracts, vol. 71, 13243 (1969).
Jiang, et al., Chemical Abstracts, vol. 87, 62629s (1977).
Portoghese, et al., Chemical Abstracts, vol. 90, 80864f (1979).
Portoghese, et al., Chemical Abstracts, vol. 92, 121619s (1980).
Pasternak, et al., Chemical Abstracts, vol. 93, 19120f (1980).
Hahn, et al., Chemical Abstracts, vol. 104, 102337y (1986).
Remington's Pharmaceutical Sciences, A. Osol, ed., Mack Publishing Co., Easton, Pa. (16th ed. 1980), p. 395.
Sigma Price List 1987, Sigma Chem. Co., St. Louis, Mo., pp. 197-200.
D. R. Brown et al., Neuropharmacology, 24, 181-191 (1985).
L. M. Sayre et al., J. Org. Chem., 45, 3366-3368 (1980).
P. S. Portoghese et al., J. Med. Chem., 23, 233 (1980).
A. E. Takemori et al., Eur. J. Pharmacol., 70, 445 (1981).
Daus Donald G.
Regents of the University of Minnesota
Rivers Diana G.
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