Patent References 3320262 Selective opioid receptor alkylating agents Non-addictive narcotic antitussive preparation Opiate agonists and antagonists Patent #: 4608376 InventorAssigneeApplicationNo. 06/809051 filed on 12/12/1985US Classes:546/45, Nitrogen or divalent chalcogen double bonded directly to carbocyclic ring of the pentacyclo ring system (e.g., morphinones, etc.)546/44, One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)546/46, A single chalcogen is bonded directly to ring carbon of the pentacyclo ring system (e.g., desoxy morphine, etc.)562/560, Ureido, hydrazino, or nitrogen double bonded directly to carbon562/565PolycarboxylicExaminersPrimary: Daus, Donald G.Assistant: Rivers, Diana G. Attorney, Agent or FirmInternational ClassesC07D 489/06 (20060101)C07D 489/00 (20060101) AbstractGut-selective agonist or antagonist opiates of the formula: ##STR1## 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 CO2 H, OH or phenyl and C is CO2 H, SO3 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.Other References
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