Inspire Pharmaceuticals, Inc.

The University of North Carolina at Chapel Hill

Burroughs Wellcome Co.

Phasebio Pharmaceuticals, Inc.

Other

Nqp 1598, Ltd.

Selenity Therapeutics (bermuda), Ltd.

Ji Xing Pharmaceuticals Hong Kong Limited

Viamet Pharmaceuticals (bermuda), Ltd.

Sammy Ray Shaver

James G Douglass, Iii

Benjamin R Yerxa

José L Boyer

Janet L Rideout

William Pendergast

Christopher M Yates

Melwyn A Abreo

Robert Plourde, Jr

Yangbo Feng

Steven Sparks

Lorenzo Josue Alfaro-Lopez

Paul Steven Watson

Ward M Peterson

Chi Tu

Daniel F Harvey

Christopher S Crean

Tatyana V Khasonova

William Joel Hoekstra

Richard C Boucher

Edward G Brown

Robert P Dougherty

Dallas Croom

David J Drutz

George A Freeman

Catherine C Redick

Krzysztof Bednarski

Mark W Holladay

Gillian M Olins

Matthew S Cowlen

Zhen Zhang

Tatyana V Khasanova

Melwyn Anthony Abreo

Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Metalloenzyme inhibitor compounds

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

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 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 pyrimidine-based 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 Ia-Ic, or tautomers, salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae I and Ia-Ic.

Pyrimidine-based non-nucleotide composition and method 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 is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and/or pain associated with diseases. The P2X receptor antagonists useful for this invention are non-nucleotide compounds of general Formula I. Compounds of Formula I can be used alone to treat pain. Compounds of Formula I can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the therapeutic effect of pain reduction.

Non-nucleotide compositions and method for treating pain

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

Growing community of inventors

Chapel Hill, NC, United States of America

Sammy Ray Shaver