Adolor Corporation

Merck + Co., Inc.

Other

Alan L Maycock

Virendra Kumar

Wei Yuan Zhang

Michael Anthony Marella

Forrest Gaul

An-Chih Chang

John J Farrar

Lawrence I Kruse

Diane L DeHaven-Hudkins

Deqi Guo

Imre Jim Balogh

Arthur A Patchett

Eugene D Thorsett

William K Hagmann

Elbert E Harris

Tony L Yaksh

Wilson B Knight

Anthony Michael Marella

Imre (Jim) Balogh

Diane L Dehaven-Hudkins

Compounds having kappa opioid agonist activity, compositions containing them and 5 method of using them as analgesics and pruritic agents are provided. The compounds of formulae I, II, III and IV have the structure: wherein

Kappa agonist compounds and pharmaceutical formulations thereof

Methods for prevention or treatment of pruritus are provided. The methods comprise administering to a patient an effective amount of a kappa opioid receptor agonist compound. The involved kappa opioid receptor agonist compounds are of the type represented by the following formula III

Kappa agonist compounds, pharmaceutical formulations and method of prevention and treatment of pruritus therewith

Compositions and methods using the compositions for treatment of peripheral hyperalgesia are provided. The compositions contain an anti-hyperalgesia effective amount of one or more compounds that directly or indirectly interact with peripheral opiate receptors, but that do not, upon topical or local administration, elicit substantial central nervous system effects. The anti-diarrheal compound 4-(p-chlorophenyl)-4-hydroxy-N-N-dimethyl-&agr;,&agr;-diphenyl-1-piperidinebutyramide hydrochloride is preferred for use in the compositions and methods.

Peripherally active anti-hyperalgesic opiates

Method for the prevention or treatment of pruritis by administering to a patient an antipruritic compound, or pharmaceutically acceptable salt thereof, of the class arylacetamide, which is exemplified by compounds of the formulae I, II, IIA, III, IV and IVA having the structures:

Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith

Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compound of formula I, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;

Kappa agonist compounds pharmaceutical formulations and method of

Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compound of formulae IIA, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;

Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compounds of formula III having the structure: ##STR1## wherein Ar and X.sup.7 ;

Kappa agonist compounds, pharmaceutical formulations and method of

Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compounds of formula II having the structure: ##STR1## wherein X.sub.4, X.sub.5 ;

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Malvern, PA, United States of America

Alan L Maycock