Alexza Pharmaceuticals, Inc.

Affymax Technologies, N.v.

Smithkline Beecham Corporation

Alza Corporation

Amy Tsai Lu

Ron L Hale

Joshua D Rabinowitz

Martin J Wensley

Peter Lloyd

Daniel J Myers

Alejandro C Zaffaroni

Craig C Hodges

Jeffrey Alan McKinney

Dennis Solas

Curtis Peter Tom

Reynaldo J Quintana

Michel J Cormier

Nathan Every

Philip Stewart Turnbull

Harold E Selick

Soonho Song

Millard Hurst Lambert, Iii

Paul Kenneth Spearing

Kevin R Oldenburg

Brad Richard Henke

Ronnie Lee Hale

The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1-3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 &#x3bc;m, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided. The device contained in the kit typically, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Also disclosed, are methods for using these aerosols and kits.

Drug condensation aerosols and kits

The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1-3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 &#x3bc;m, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided, wherein the device, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Methods for use are also disclosed.

Described herein are respiratory drug condensation aerosols and methods of making and using them. Kits for delivering condensation aerosols are also described. The respiratory drug aerosols typically comprise respiratory drug condensation aerosol particles. In some variations the respiratory drug compound is selected from the group consisting of &#x3b2;-adrenergics, methylxanthines, anticholinergics, corticosteroids, mediator-release inhibitors, anti-leukotriene drugs, asthma inhibitors, asthma antagonists, anti-endothelin drugs, prostacyclin drugs, ion channel or pump inhibitors, enhancers, or modulators and pharmaceutically acceptable analogs, derivatives, and mixtures thereof. Methods of treating a respiratory ailment using the described aerosols are also described. In general, the methods typically comprise the step of administering a therapeutically effective amount of respiratory drug condensation aerosol to a person with a respiratory ailment. Methods of forming a respiratory drug condensation aerosol are also described. The methods comprise the steps of vaporizing and condensing a respiratory drug composition.

Respiratory drug condensation aerosols and methods of making and using them

Described herein are diuretic condensation aerosols and methods of making and using them. Kits for delivering a condensation aerosol are also described. The diuretic aerosols typically comprise diuretic condensation aerosol particles that comprise a diuretic compound. In some variations the diuretic compound is selected from the group consisting of bumetanide, ethacrynic acid, furosemide, muzolimine, spironolactone, torsemide, triamterene, tripamide, BG 9928, and BG 9719. Methods of treating edema using the described aerosols are also provided. In general, the methods typically comprise the step of administering a therapeutically effective amount of diuretic condensation aerosol to a person with edema. The diuretic condensation aerosol may be administered in a single inhalation, or may be administered in more than one inhalation. Methods of forming a diuretic condensation aerosol are also described. The methods typically comprise the steps of providing a diuretic composition, vaporizing the composition to form a vapor, and then condensing the diuretic composition vapor.

Diuretic aerosols and methods of making and using them

A device, method, and system for producing a condensation aerosol are disclosed. The device includes a chamber having an upstream opening and a downstream opening which allow gas to flow through the chamber, and a heat-conductive substrate located at a position between the upstream and downstream openings. Formed on the substrate is a drug composition film containing a therapeutically effective dose of a drug when the drug is administered in aerosol form. A heat source in the device is operable to supply heat to the substrate to produce a substrate temperature greater than 300&#xb0; C., and to substantially volatilize the drug composition film from the substrate in a period of 2 seconds or less. The device produces an aerosol containing less than about 10% by weight drug composition degradation products and at least 50% of the drug composition of said film.

Rapid-heating drug delivery article and method of use

An article for use in an aerosol device, for producing an aerosol of a drug composition is disclosed. The article includes a heat-conductive substrate having a surface with a selected surface area, and a drug composition film on the substrate surface having a selected film thickness of between 0.05 and 20 &#x3bc;m. The film thickness is such that an aerosol formed by vaporizing the drug composition by heating the substrate and condensing the vaporized compound contains 10% or less drug-degradation product and at least 50% of the total amount of drug composition contained in the film. The selected substrate surface area is such as to yield an effective human therapeutic dose of the drug aerosol. Also disclosed are methods of making and using the article.

Thin-film drug delivery article and method of use

The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1&#x2013;3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 &#x3bc;m, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided. The device contained in the kit typically, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Also disclosed, are methods for using these aerosols and kits.

Triazine derivatives of formula (I), which exhibit pharmacological activity at estrogen receptors alpha (ER alpha) and beta (ER beta) are described herein. The described invention also includes compositions and medicaments containing the triazine derivatives as well as processes for the preparation and use of such compounds, compositions and medicaments.

Piperazinyltriazines as estrogen receptor modulators

Compositions and methods are provided for enhanced transdermal electrotransport of 17-hydroxy sterol compounds, including testosterone. The parent sterols are modified at the 17-hydroxy position by covalent attachment of a charged chemical modifier. The chemical modifier provides the parent sterol with enhanced transport properties and is hydrolyzed under physiological conditions to release the active parent compound. The composition comprises a 17-hydroxy sterol/chemical modifier complex, more generally represented by the formula (sterol--O--)C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+. The portion of the complex derived from the chemical modifier is indicated by 'C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ ', where N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ represents a quaternary ammonium group and R.sup.1, R.sup.2, and R.sup.3 are independently selected from the group consisting of lower alkyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroalkyl, and heteroarylalkyl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached form a substituted heterocycle and R.sup.3 is lower alkyl, and R is a linking moiety, linking the (sterol--O)--C(O)-- to the nitrogen atom.

Testosterone prodrugs for improved drug delivery

The present invention relates to methods of delivering pharmaceutical agents across membranes, including the skin layer or mucosal membranes of a patient. A pharmaceutical agent is covalently bonded to a chemical modifier, via a physiologically cleavable bond, such that the membrane transport and delivery of the agent is enhanced.

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Los Altos, CA, United States of America

Amy Tsai Lu