Merck + Co., Inc.

Rhone-poulenc Rorer Pharmaceuticals Inc.

Other

Michael N Chang

Yuan-Ching P Chiang

Shu S Yang

Kathryn L Thompson

Milton L Hammond

James V Heck

Robert A Zambias

John C Chabala

Norman P Jensen

Donald W Graham

Tesfaye Biftu

John R Regan

John McDonald

Kathleen M Rupprecht

Robert A Galemmo, Jr

David A Boulton

Fu-Chih Huang

Jack Newman

San-Bao Hwang

Daniel G McGarry

Michael D Lewis

Charles A Sutherland

Wan K Chan

Schmuel Ben-Sasson

Conrad P Dorn

James B Doherty

Mitree M Ponpipom

Robert L Bugianesi

Jeffrey N Barton

Raymond D Cooper

Dorothy M Morr&eacute;

D James Morr&eacute;

Narindar M Girotra

Francis A Volz

The invention described herein encompasses a methods and compositions of treating cancer or solid tumors comprising the administration of a therapeutically effective amount of catechins, a group of polyphenols found in green tea, to a mammal in need of such therapy. Compositions of catechins include but not limited to, epigallocatechin gallate (EGCg), epicatechin (EC), epicatechin gallate (ECG), epigallocatechin (EGC). The unique compositions of the invention contain various combinations of the catechins, alone or in combination with each other or other therapeutic agents and are used to treat primary and metastatic cancers in humans. The invention also encompasses the varying modes of administration of the therapeutic compounds, including a sustained release formulation which may be used as a therapeutic compound for the treatment of cancer or as a dietary supplement for the prevention of cancer.

Tea catechins in sustained release formulations as cancer specific proliferation inhibitors

A biologically active polymeric compound comprising an alkylaryl or heteroalkylaryl backbone having about 5 to about 50 repeating aromatic ring-containing units and which, according to the computer program marketed as SYBYL.RTM. version 5.2 running on a DEC VAX.RTM. 11/750 computer, is capable of forming a linear backbone having a helical secondary structure, and wherein the maximum diameter of the helical structure, as measured by the alkylaryl or heteroalkylaryl backbone, is less than 3 times greater than the maximum diameter of the aryl group of the alkylaryl or heteroalkylaryl backbone.

Polymers with alkyl- or heteroalkyl -aryl backbone and pharmaceutical

This invention relates to aromatic oligomeric compounds useful in the treatment of cardiovascular, bone metabolic, hypolipidaemic, neuronal, gastrointestinal and elastase-mediated connective tissue degradation disorders and disorders which may be treated by agents effective in binding DNA, to processes for preparation of such oligomeric compounds, to pharmaceutical compositions including such oligomeric compounds, and to their use in the treatment of such disorders.

Aromatic oligomeric compounds useful as mimics of bioactive

Monocyclic aryl compounds having selective LTB.sub.4 antagonists properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, therapeutic compositions and methods of treatment of disorders which result from LTB.sub.4 activity using the monocyclic aryl compounds are disclosed.

Substituted monocyclic aryl compounds exhibiting selective leukotriene

This invention relates to compounds which are steroidyl derivatives of 4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one and the corresponding ring-opened hydroxy acid form thereof which are useful as antihypercholesterolemic agents, to pharmaceutical compositions including such compounds, and to their use in treating hypercholesterolemia.

Compounds having hypocholesterolemic properties

Monocyclic and bicyclic aryl ring compounds having selective LTB.sub.4 properties and comprising two ring substituents, the first substituent comprising a lipophilic group and a terminal carboxylic acid or derivative group, and the second substituent comprising an amido group, therapeutic compositions and methods of treatment of disorders which result from LTB.sub.4 activity using the mono- and bicyclic aryl compounds are disclosed.

Disubstituted aryl compounds exhibiting selective leukotriene B4

Novel 1,3-Diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediated by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.

1,3-diaryl cyclopentanes and derivatives thereof as PAF antagonists

This application relates to compounds of formula (I), which are useful as antihypercholesterolemic agents. ##STR1##

Beta-lactams as antihypercholesterolemics

Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.

This invention relates to triyne cyclic carbonates that are useful in the treatment of fungal diseases and hypercholesterolemic conditions.

Triyne cyclic carbonates

Compounds of formula (I), which are useful as antihypercholesterolemic agents, are disclosed. ##STR1##

Beta-lactams as anticholesterolemic agents

This invention relates to acetylenic cyclic carbonates that are useful in the treatment of fungal diseases and hypercholesterolemic conditions.

Acetylenic cyclic carbonates

The compounds of the following general structural formula (I) ##STR1## are 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatment of disease in which the inhibition of cholesterol biosynthesis would be useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.

Antihypercholesterolemic .beta.-lactones

The compounds of the following structural formula (I) ##STR1## are 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatmet of disease in which the inhibition of cholesterol biosynthesis would be useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.

Antihypercholesterolemic beta-lactones

Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.

Growing community of inventors

Westfield, NJ, United States of America

Michael N Chang