摘要 |
Gut-selective agonist or antagonist opiates of the formula: <IMAGE> <IMAGE> wherein R is (C1-C5) alkyl, C3-C6(cycloalkyl)alkyl, aryl, aralkyl or trans-(C2-C5)alkenyl; Z is H or OH, R' is (C=O)-A(B)(C) wherein A is selected from the group consisting of (C1-C5)alkyl, (C2-C5)alkenyl and (C2-C6)alkoxy (alkyl); B is selected from the group consisting of H, amino and a (C1-C5)alkyl group optionally substituted with CO2H, OH or phenyl and C is CO2H, SO3H, 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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