Pfizer Corporation

Parion Sciences, Inc.

Glaxo Inc.

Paul L. Feldman

Michael Ross Johnson

Harry Jefferson Leighton

Marcus F. Brackeen

Michael K. James

Lawrence S Melvin, Jr

Jasjit S Bindra

Thomas K Schaaf

Hans-Jurgen E Hess

James F Eggler

Charles A Harbert

Richard C Boucher

Thomas H Althuis

William Robert Thelin

Jianzhong Zhang

Bruce Francis Molino

Bruce Sargent

Andrew J Hirsh

Tomas Navratil

Brian Button

Stephen V Frye

Jacob J Plattner

Ronald A Aungst, Jr

Robert A Volkmann

Gerald F Holland

James B Fink

Anthony James Hickey

David A Clark

Harry J Leighton

Paul L Feldman

George M Milne, Jr

Marcus F Brackeen

Mark Jeffrey Edhouse

Samuel E Hopkins

Michael K James

Philip Jerome Driver

Stuart Robert Abercrombie

Donal Joseph Taylor

Jonathan Hugh Wilkins

Lawrence Sherman

Bruce J Sargent

Paul Boucher

Nicholas O Heijne

William R Thelin

Andrew J Hirch

The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.

3,5-diamino-6-chloro-N-(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide

Provided are mucolytic agents represented by formula (Ia)-(Id): where the structural variables R, R, Rand Rare as defined herein. Also provided are a variety of methods of treatment which take advantage of the mucolytic properties of the compounds represented by formula (Ia)-(Id).

Monothiol mucolytic agents

3,5-diamino-6-chloro-N&#x2014;(N-(4-(4-(2-(hexyl(2,3,4,5,6-pentahydroxyhexyl)amino)ethoxy)phenyl)butyl)carbamimidoyl)pyrazine-2-carboxamide

Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.

Dendrimer like amino amides possessing sodium channel blocker activity for the treatment of dry eye and other mucosal diseases

Provided are mucolytic compounds that are more effective, and/or absorbed less rapidly from mucosal surfaces, and/or are better tolerated as compared to N-acetylcysteine (NAC) and DTT. The compounds are represented by compounds of Formula I which embrace structures (Ia)-(Ib): where the structural variables are as defined herein.

Prodrugs of dithiol mucolytic agents

Embodiments disclosed herein are directed to methods, compositions and apparatus for administering active agents to the lungs of a subject.

Methods of treatment

The present invention relates compounds of the formula: or pharmaceutically acceptable salts thereof, useful as sodium channel blockers, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including cystic fibrosis, chronic obstructive pulmonary disease, asthma, bronchiectasis, acute and chronic bronchitis, emphysema, and pneumonia.

3,5-diamino-6-chloro-N-(N-(4-phenylbutyl)carbamimidoyl) pyrazine-2-carboxamide compounds

Arylalkyl- and aryloxyalkyl-substituted epithelial sodium channel blocking compounds

The present invention relates to compounds of Formula (I) and pharmaceutical compositions thereof. Compounds of Formula (I) are epithelial sodium channel (ENaC) blockers useful in the hydration of mucosal surfaces, enhancement of mucociliary clearance, or restoration of mucosal defense in a subject. The compounds and compositions can therefore be used to treat diseases which rely on the hydration of mucosal surfaces. 

Sodium channel blockers

A very stable, selective and nrenally safe sodium channel blocker represented by the formula:  The invention also includes a variety of compositions, combinations and methods of treatment using this inventive sodium channel blocker.

Chemically and metabolically stable dipeptide possessing potent sodium channel blocker activity

This invention provides compounds of the formula I: and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.

Chloro-pyrazine carboxamide derivatives with epithelial sodium channel blocking activity

The invention described herein is directed to method of treating chronic obstructive pulmonary disease, comprising administering an effective amount of an osmolyte by at least one nasal cannula to a subject in need thereof. Also provided is a nasal cannula system for delivering an osmolyte, comprising a nebulizer and tubing having two ends, where the first end of the tubing is connected to the nebulizer and the second end of the tubing is tapered to fit in the nostril of a subject.

Inhaled hypertonic saline delivered by a heated nasal cannula

Provided are dithiol mucolytic agents. These agents increase the liquefaction of mucus in a patient with excessive mucus or mucus with increased viscoelastic, cohesive, or adhesive properties. Also provided are a variety of methods of treatment using these inventive mucolytic agents.

Dithiol mucolytic agents

Arylalkyl-and aryloxyalkyl-substituted epithelial sodium channel blocking compounds

Growing community of inventors

Chapel Hill, NC, United States of America

Michael Ross Johnson