Gilead Sciences, Inc.

Chiron Corporation

Amgen (europe) Gmbh

Pro-onics Pharmaceuticals LLC

William Baker

David MacLeod

Gary Bruce Phillips

Alan Bruce Montgomery

Musong Kim

Joshua A Kaplan

Marcin Stasiak

Lafe J Purvis, Ii

Shaopei Cai

Josh Van Veldhuizen

Kirk L Stevens

Kevin Stapleton

Thomas Hofmann

Stephane Perreault

Jennifer Alissa Loyer-Drew

Kirk K Stevens

Provided herein are azo prodrugs of small-molecule isoindoline-1,3-diones and isoindoles anti-inflammatory inhibitors according to formula IA, in particular PDE4 inhibitors, which prodrugs can be administered orally to a subject in need thereof, whereby the prodrugs are cleaved in the colon and the PDE4 inhibitor released. 

Methods and compositions of isoindoline-1,3-dione and isoindole prodrugs useful for treating cancer, ulcerative colitis and related inflammatory diseases

A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having mass median aerodynamic diameter predominantly between 1 to 5&#x3bc;, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.

Aerosolized fosfomycin/aminoglycoside combination for the treatment of bacterial respiratory infections

This invention provides compounds of the formula:  wherein Rand Rtogether with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring and all other variables are as defined herein, their use in pulmonary inflammation or bronchoconstriction therapy and compositions comprising and processes for preparing the same are provided.

Bi-functional pyrazolopyridine compounds

A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having mass medium average diameter predominantly between 1 to 5 &#x3bc;, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.

Provided are compounds of Formula I:  Rand Rtogether with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.

Bi-functional quinoline analogs

A method for improvement of tolerance for therapeutically effective agents delivered by inhalation comprising a pretreatment of a patient with a nebulized lidocaine or a lidocaine-like compound administered immediately or up to about thirty minutes before administration of the primary therapeutically effective agent. The pretreatment of the patient with the nebulized lidocaine or a lidocaine-like compound improves airway tolerance and deposition of the agent in the lungs and makes such deposition more safe, efficacious, controllable and predictable. The method of the invention is especially useful for enhancement of deposition of immunosuppressive agents in the lung(s) of transplant patients, improved tolerance of the drugs by reducing cough, and improving pulmonary drug deposition.

Method for improvement of tolerance for therapeutically effective agents delivered by inhalation

A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having a mass median aerodynamic diameter predominantly between 1 to 5&#x3bc;, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.

The present invention is directed to a method for the treatment of severe chronic bronchitis, i.e., bronchiectasis, using a concentrated aminoglycoside antibiotic formulation delivering the antibiotic to the lung endobronchial space, including alveoli, in an aerosol or dry powder having a mass medium diameter predominately between 1 to 5 microns.

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Bellevue, WA, United States of America

William Baker