Merrell Pharmaceuticals, Inc.

Merrell Dow Pharmaceuticals

Aventis Pharma Limited

David M Stemerick

Michael L Edwards

Boyd Lynn Harrison

Sai P Sunkara

Alan J Bitonti

George Ku

Nellikunja J Prakash

Ian A McDonald

Philippe Bey

Bruce M Baron

Christopher R Dalton

Albert Sjoerdsma

Terry L Bowlin

Esa T Jarvi

Keith A Diekema

Robert J Dinerstein

Peter P McCann

Scott B Meikrantz

Peter P Mccann

James R Mccarthy

Ian A Mcdonald

Bruce Michael Baron

This invention relates to certain polyamine derivatives, to the methods and intermediates useful for their preparation, and to their use in treating diseases caused by infestation with a variety of parasitic protozoa.

Polyamine derivatives

Benzenesulfonylimine derivatives as inhibitors of IL-1 action

Heterocyclic benzenesulfonylimine derivatives as inhibitors of IL-1

The present invention relates to certain inhibitors of farnesyl:protein transferase which are useful as antineoplastic agents.

Farnesyl:protein transferase inhibitors as anticancer agents

The present invention relates to a method for the treatment of patients suffering from certain neoplastic disease states which comprises administering a therapeutically effective amount of a compound of the formula: ##STR1## wherein m is an integer 6 to 9, Z is a saturated (C.sub.2 -C.sub.6) alkylene moiety, each R group independently is hydrogen, methyl, ethyl, or n-propyl except that both R groups cannot be hydrogen when Z is a straight chain; or a pharmaceutically acceptable acid addition salt thereof. Said treatment can optionally comprise conjunctive therapy with a polyamine oxidase inhibitor. The invention also relates to certain novel polyamine derivatives.

Polyamine derivatives as antineoplastic agents

The present invention is directed to a new class of 4-sulfanimide-quinoline derivatives and to their use as NMDA antagonists.

NMDA antagonists

This invention relates to 1-aryl-3-pyridinyl-2-propene-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.

Calcium uptake inhibitors

Farnesyl: protein transferase inhibitors as anticancer agents

The present invention relates to certain novel polyamine compounds of the formula: ##STR1## wherein Z is a saturated (C.sub.2 -C.sub.6) alkylene moiety, each R group independently is hydrogen, methyl, ethyl, or n-propyl with the provisos that both R groups cannot be hydrogen and that R is hydrogen or methyl when Z is a branched chain alkylene; or a pharmaceutically acceptable acid addition salt thereof.

The importance of polyamines in biological systems is discussed as well as the implications of polyamines in the treatment of various diseases. Novel N-substituted-2,3-butadienyl tri- and tetra-aminoalkanes are disclosed as well as their use inthe treatment of diseases and the pharmaceutical compositions.

N-2,3-butadienyl tri- and tetraaminoalkane derivatives

Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used to control the growth of tumor tissue and can be used as antigout agents.

Controlling the growth of certain tumor tissue with chalcone derivatives

Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used as antigout agents. The chalcone derivatives are also reported to inhibit the destruction of the myelin sheath in the central nervous system of multiple sclerosis patients and are thus useful in controlling the progressive nature of the disease.

Methods of treating gout with chalcone derivatives

Method of treating multiple sclerosis with chalcone derivatives

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Fairfield, OH, United States of America

David M Stemerick