Smithkline Beecham Corporation

Smithkline Corporation

Smithkline Beckman Corporation

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William Edward Bondinell

Thomas Wen-Fu Ku

Richard McCulloch Keenan

James Martin Samanen

William Henry Miller

William F Huffman

James Francis Callahan

Robert G Pendleton

Kenneth Allen Newlander

Fadia E Ali

Joseph W Venslavsky

James A Chan

Herbert S Ormsbee, Iii

Tobias Oregon Yellin

Robert M DeMarinis

Brian W Metcalf

John J Lafferty

Charles L Zirkle

Thomas Wen Fu Ku

Daniel F Veber

David T Hill

Dennis Shinji Yamashita

Roderick Alan Porter

Dirk Andries Heerding

David Thomas Davies

Dennis Lee

Irene Nijole Uzinskas

Francis R Pfeiffer

Steven Dabbs

James David Winkler

Anthony Joseph Jurewicz

Michael J Neeb

David C Underwood

Chet Kwon

Thomas The Nguyen

Dinubhai H Shah

Jacob P Hieble

Renee Louise DesJarlais

Barry M Weichman

M Amparo Lago

Raul Rolando Calvo

Dennis T Takata

Gerald R Girard

Valerie A Reader

Frank E Blaney

Charles J Kotzer

Thomas Wen Ku

Vitronectin receptor antagonists

The present invention provides bis-aminomethyl carbonyl protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Protease inhibitors

This invention relates to substituted benzanilides which are ligands, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzanilides which are CCR5 receptor antagonists. Furthermore, since CD8&plus; T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.

Substituted benzanilides as CCR5 receptors ligands, antiinflammatory agents and antiviral agents

This invention relates to substituted benzo&lsqb;1,2-b:5,4-b&prime;&rsqb;dipyran-4-amines which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and a topic disorders (for example, a topic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzo&lsqb;1,2-b:5,4-b&prime;&rsqb;dipyran-4-amines which are CCR5 receptor antagonists. Furthermore, since CD8&plus;T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therpeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.

Compounds and methods

C3A receptor ligands

A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Bicyclic fibrinogen antagonists

This invention relates to substituted heteroanilide compounds which are modulators, agonists or antagonists, of the CCR5 receptior. In addition, this invention relates to the treatment and prevention of disease states mediatd by CCR5.

This invention relates to substituted bis-acridines and related compounds which are ligands, in particular, antagonists of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders, rheumatoid arthritis, atherosclerosis, psoriasis, auto immune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted bis-acridines and related compounds which are CCR5 receptor antagonists. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.

Substituted bis-acridines and related compounds as CCR5 receptor ligands, anti-inflammatory agents and anti-viral agents

This invention relates to methods for treating diseases or disorders mediated by lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which method comprises administration to a mammal in need thereof of an effective Coenzyme A independent transacylase (CoA-IT) inhibiting amount of a triphenylmethylazetidinone. This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a triphenylmethylazetidinone.

Beta-lactam inhibitors of CoA-IT

This invention relates to certain tricyclic compounds that are integrin receptor antagonists.

Compounds of the formula: ##STR1## wherein A.sup.1 to A.sup.5 form a seven-membered ring containing one optionally substituted nitrogen atom and one heteroatom selected from oxygen and nitrogen;

Use of GABA uptake inhibitors as anti-tussive agents

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Wayne, PA, United States of America

William Edward Bondinell