Inspire Pharmaceuticals, Inc.

University of North Carolina at Chapel Hill

Nicox Ophthalmics, Inc.

José L Boyer

James G Douglass, Iii

Sammy Ray Shaver

Benjamin R Yerxa

Robert Plourde, Jr

Melwyn A Abreo

Chi Tu

Daniel F Harvey

Yangbo Feng

Lorenzo Josue Alfaro-Lopez

Tatyana V Khasonova

Paul Steven Watson

Edward G Brown

Gillian M Olins

Ward M Peterson

Christopher S Crean

Catherine C Redick

Tomas Navratil

Ramesh Krishnamoorthy

Romulus Kimbro Brazzell

Krzysztof Bednarski

Brigitte Duquesroix-Chakroun

John C Ice, Jr

Robert J Dempsey

Akshay Nadkarni

Donald J Kellerman

Jean-Michel Bukowski

Amy E Schaberg

Kurt E Brubaker

Reza M Haque

Tatyana V Khasanova

Joseph B Boyd

Reza Haque

Melwyn Anthony Abreo

A process of manufacturing sterile topical ophthalmic aqueous nanosuspensions of nanocrystals of fluticasone propionate Form A. The sterile topical ophthalmic nanosuspensions may be used in the treatment of eye inflammation conditions such as blepharitis, posterior blepharitis, Meibomian gland dysfunction and dry eye through topical administration of said nanosuspensions to eyelids, eyelashes and eyelid margin.

Process for the preparation of sterile ophthalmic aqueous fluticasone propionate form a nanocrystals suspensions

The present invention relates to a method for treating non-infectious, inflammatory chronic posterior blepharitis in a subject. The present invention also relates to a method for treating chronic posterior blepharitis in a subject for over two weeks. The method comprises identifying a subject in need thereof, and topically administering to the eye of the subject a pharmaceutical formulation consisting essentially of an effective amount azithromycin. The present invention further relates to a method for treating dry eye secondary to blepharitis in a subject. The method comprises the steps of: identifying a subject suffering from dry eye secondary to posterior blepharitis, and topically administering to the eye of the subject a pharmaceutical formulation comprising an effective amount of azithromycin. The present invention further relates to method for reducing contact lens intolerance of a subject due to blepharitis or dry eye secondary to blepharitis.

Method of treating blepharitis

The present invention is directed to a method for treating cystic fibrosis. The method comprises the steps of: identifying a patient suffering from cystic fibrosis, and administering to the patient an effective amount of denufosol or a pharmaceutically acceptable salt thereof and an effective amount of a macrolide. In one method, denufosol and the macrolide are administered by inhalation, preferably in a single formulation. In another method, denufosol is administered by inhalation and the macrolide is administered orally. The present invention is also directed to a pharmaceutical formulation comprising denufosol or a pharmaceutically acceptable salt thereof, a macrolide, and a pharmaceutically acceptable carrier. Preferred denufosol is denufosol tetrasodium and preferred macrolide is azithromycin. The pharmaceutical formulation preferably is in a form of an inhalable dry powder or in a liquid form.

Method for treating cystic fibrosis

This invention is directed to a method of enhancing or facilitating the clearance or the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Yreceptor agonist compound, wherein said amount is effective to activate the P2Yreceptors on the luminal surface of lung epithelia. The P2Yreceptor agonist compounds useful for this invention include mononucleoside 5'-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof. This invention is also directed to novel P2Yreceptor agonist compounds.

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This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Yreceptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formulae I and III-XII, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and III-XII.

Non-nucleotide composition for inhibiting platelet aggregation

This invention is directed to a method of enhancing or facilitating the clearance of the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Yreceptor agonist compound, wherein said amount is effective to activate the P2Yreceptors on the luminal surface of lung epithelia. The P2Yreceptor agonist compounds useful for this invention include mononucleoside 5'-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof.

P2Y6 receptor agonists for treating lung diseases

The present invention provides a drug-eluting stent, wherein the stent is coated with one or more non-nucleotide P2Yreceptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Yreceptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Yreceptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.

The present invention provides a P2Yreceptor antagonist compound-eluting stent, wherein the stent is coated with one or more P2Yreceptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Yreceptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Yreceptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.

The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.

Degradation-resistant mononucleoside phosphate compounds

This invention is directed to compounds of Formulae III and V, useful for treating diseases or conditions associated with platelet aggregation. 

Non-nucleotide composition and method for inhibiting platelet aggregation

This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a non-nucleotide compound, preferably a P2Yreceptor antagonist compound, wherein said amount is effective to inhibit platelet aggregation. The compounds useful for this invention include compounds of general Formula I and III-XI, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds according to Formula I and III-XI.

Non-nucleotide compositions and method for inhibiting platelet aggregation

This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis or related disorders. The method comprises administering to a compounds useful for this invention include compounds of general Formulae I and III-XII, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and III-XII.

This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Yreceptor antagonist compound, wherein said amount is effective to bind the P2Yreceptors on platelets and inhibit ADP-induced platelet aggregation. The P2Yreceptor antagonist compounds useful for this invention include mononucleoside 5'-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5&#x2032;-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates. The present invention further provides pharmaceutical formulations comprising mononucleoside 5&#x2032;-monophosphates, mononucleoside polyphosphates, or dinucleoside polyphosphates.

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Chapel Hill, NC, United States of America

José L Boyer