Smithkline Beckman Corporation

Adolor Corporation

Smithkline Beecham Corporation

Sanshin Kogyo Kabushiki Kaisha

Smith Kline & French Laboratories Limited

Symphar S.a.

Sanofi Pharmaceuticals, Inc.

Smithklein Beckman Corporation

Lawrence I Kruse

Carl Kaiser

Virendra Kumar

Alan L Maycock

John J Farrar

An-Chih Chang

Stephen T Ross

Diane L DeHaven-Hudkins

Wei Yuan Zhang

Michael Anthony Marella

Forrest Gaul

Joseph A Finkelstein

Thomas B Leonard

James S Frazee

Eliot H Ohlstein

William J Coates

Rodney C Young

Thomas D Gordon

Teruna J Siahaan

Mark A Ator

Alberto J Kaumann

Virendra P Shah

Pamela A Chambers

James Arthur Gainor

Barry Arnold Morgan

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

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 ;

Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compound of formulae IV having the structure: ##STR1## wherein X.sub.9 ;

Peptides or peptides having an amino acid-like moiety in place of an amino acid moiety thereof immobilized on glass beads, especially controlled-pore glass beads, by a C-terminal .alpha.-carboxyl-.omega.-amino linker and .alpha.-silyl-.omega.-amino anchor, especially wherein the anchor has the structural formula

N-terminal-marked peptides immobilized on glass beads 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 formular I, II, III and IV have the structure: ##STR1## wherein X, X.sub.4, X.sub.5, X.sub.7, X.sub.9 ;

Kappa agonist compounds pharmaceutical formulations and method of

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

Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae I, II, III and IV have the structure: ##STR1## wherein X, X.sub.4, X.sub.5, X.sub.7, X.sub.9 ;

Compounds, compositions and method of treating hyperalgesia comprising a compound of formula I, II, III and IV as defined in the specification.

Tryptamine analogues, their synthesis and their use as 5-HT.sub.1 -like

Substituted gem-diphosphonate compounds having use as cholesterol lowering agents are disclosed. A compound of the invention is tetraethyl-2-[3-t-butyl-4-hydroxynaphthyl]ethenylidene-1,1-diphosphonate.

Naphthyl-,tetrahydronaphthyl-, and indanyl-substituted

This invention relates to quinazolinone derivatives which have bronchodilator activity. A compound of the invention is 2-(2-propoxyphenyl)quinazolin-4(3H)-one.

2-(substituted phenyl)-4-oxo-quinazolines

Potent DBH inhibitors having the formula ##STR1## can be used to inhibit DBH activity in mammals.

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Haddonfield, NJ, United States of America

Lawrence I Kruse