Adolor Corporation

Sterling Winthrop Inc.

Sterling Drug Inc.

Sanofi

Sanofi Winthrop Inc.

Sanofi-synthelabo

Sanofi Sa

Apolor Corp.

Virendra Kumar

Wei Yuan Zhang

Alan L Maycock

An-Chih Chang

John J Farrar

Michael Anthony Marella

Forrest Gaul

Diane L DeHaven-Hudkins

Chakrapani Subramanyam

Malcolm R Bell

Lawrence I Kruse

John P Mallamo

Deqi Guo

John J Court

Ranjit C Desai

Richard P Dunlap

Dennis J Hlasta

Matthew S Miller

William G Earley

Alan Cowan

Neil Warren Boaz

Albert J Mura, Jr

Lee H Latimer

Susan J Ward

Manohar T Saindane

John Alan Dority, Jr

John A Dority, Jr

Philip M Carabateas

Thomas E D'Ambra

Michael A Eissenstat

Edward R Bacon

Denis M Bailey

Robert P Farrell

Robert G Christiansen

Imre Jim Balogh

Imre (Jim) Balogh

Anthony Michael Marella

Edward Richard Bacon

Imre Balogh

Diane L Dehaven-Hudkins

Solid dispersions of stable, amorphous opioid antagonists, particularly [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid, with improved water solubility and bioavailability are disclosed. Also disclosed are methods of preventing or treating a side effect associated with an opioid. In addition, methods of treating or preventing pain, ileus, and opioid bowel dysfunction are disclosed.

Solid dispersions of opioid antagonists

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

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

Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.

Kappa agonist anti-pruritic 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 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 ;

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Paoli, PA, United States of America

Virendra Kumar