Gut-selective opiates

Details Gut-selective opiates Gut-selective opiates

1985-12-12

1988-03-08

Daus, Donald G.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546 44, 546 46, 562560, 562565, C07D48906, C07D48900, A61K 31485

Patent

active

047300485

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.

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