Paul L Watson

US Patent:

7320974, Jan 22, 2008

Filed:

Mar 23, 2006

Appl. No.:

11/389665

Inventors:

John W. Lampe - Cary NC, US
Robert Plourde, Jr. - Chapel Hill NC, US
Jin She - Chapel Hill NC, US
Jason L. Vittitow - Durham NC, US
Paul S. Watson - Carrboro NC, US
Michael T. Crimmins - Chapel Hill NC, US
David J. Slade - Durham NC, US

Assignee:

Inspire Pharmaceuticals, Inc. - Durham NC

International Classification:

A61K 31/351
A61K 31/357
C07D 309/06
C07D 313/02
C07D 313/16

US Classification:

51421109, 514450, 540451, 540456, 540468, 548182

Abstract:

The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.

US Patent:

7335648, Feb 26, 2008

Filed:

May 5, 2005

Appl. No.:

11/124619

Inventors:

Robert Plourde, Jr. - Chapel Hill NC, US
Sammy R. Shaver - Chapel Hill NC, US
Paul S. Watson - Carrboro NC, US
José L. Boyer - Chapel Hill NC, US
Chi Tu - San Diego CA, US
Melwyn A. Abreo - Jamul CA, US
Lorenzo J. Alfaro-Lopez - San Marcos CA, US
Yangbo Feng - Palm Beach Gardens FL, US
Daniel F. Harvey - San Diego CA, US

Assignee:

Inspire Pharmaceuticals, Inc. - Durham NC

International Classification:

A01N 43/04
A61K 31/70
C07H 19/16

US Classification:

514 46, 536 2723

Abstract:

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.

US Patent:

7414137, Aug 19, 2008

Filed:

Mar 22, 2007

Appl. No.:

11/690048

Inventors:

Jonathan B. DeCamp - Raleigh NC, US
Paul S. Watson - Carrboro NC, US
Jin She - Chapel Hill NC, US

Assignee:

Inspire Pharmaceuticals, Inc. - Durham NC

International Classification:

C07D 277/56

US Classification:

548188

Abstract:

The present invention is directed to practical high-yielding synthetic processes for preparing 3,4-disubstituted-thiazolidin-2-ones, which do not compromise the absolute stereochemical integrity of the compounds. The present invention is also directed to novel compounds of 3,4-disubstituted-thiazolidin-2-ones. The compounds prepared by the present invention are useful in the synthesis and manufacture of compounds (such as latrunculins and/or their analogs) for treating diseases or conditions associated with inhibiting actin polymerization.

US Patent:

7504497, Mar 17, 2009

Filed:

Nov 9, 2006

Appl. No.:

11/595837

Inventors:

Paul S. Watson - Carrboro NC, US
Carl A. Samuelson - Durham NC, US
Christopher S. Crean - Pittsboro NC, US

Assignee:

Inspire Pharmaceuticals, Inc. - Durham NC

International Classification:

C07H 19/16
A01N 43/04
A61K 31/70

US Classification:

536 273, 514 46

Abstract:

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 III, IIIa, and IIIb, or salts, hydrates, and solvates thereof. The present invention also provides novel compounds of Formulae IIIa and IIIb, which are potent and have a good oral bioavailability.

US Patent:

7592445, Sep 22, 2009

Filed:

Jan 4, 2008

Appl. No.:

11/969539

Inventors:

Robert Plourde, Jr. - Chapel Hill NC, US
Sammy R. Shaver - Chapel Hill NC, US
Paul S. Watson - Carrboro NC, US
José L. Boyer - Chapel Hill NC, US
Chi Tu - San Diego CA, US
Melwyn A. Abreo - Jamul CA, US
Lorenzo J. Alfaro-Lopez - San Marcos CA, US
Yangbo Feng - Palm Beach Gardens FL, US
Daniel F. Harvey - San Diego CA, US

Assignee:

Inspire Pharmaceuticals, Inc. - Durham NC

International Classification:

C07H 19/16
A01N 43/04
A61K 31/70

US Classification:

536 273, 514 46

Abstract:

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

US Patent:

7666861, Feb 23, 2010

Filed:

Dec 4, 2007

Appl. No.:

11/950327

Inventors:

John W. Lampe - Cary NC, US
Robert Plourde, Jr. - Chapel Hill NC, US
Jin She - Chapel Hill NC, US
Jason L. Vittitow - Durham NC, US
Paul S. Watson - Carrboro NC, US
Michael T. Crimmins - Chapel Hill NC, US
David J. Slade - Durham NC, US

Assignee:

Inspire Pharmaceuticals, Inc. - Durham NC

International Classification:

A61K 31/351
A61K 31/357
C07D 309/06
C07D 313/02
C07D 313/16

US Classification:

51421109, 514450, 540451, 540456, 540468, 548182

Abstract:

The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.

US Patent:

7741473, Jun 22, 2010

Filed:

Mar 30, 2006

Appl. No.:

11/393374

Inventors:

Paul S. Watson - Carrboro NC, US
Bob Suchozak - Newmarket, CA
Subramanian Pandiaraju - Brampton, CA
Craig E. Dixon - Whitby, CA
Daniel Levin - Toronto, CA

Assignee:

Inspire Pharmaceuticals, Inc. - Durham NC

International Classification:

C07H 19/067
C07H 19/167

US Classification:

536 2711, 536 2762, 536 285

Abstract:

The present invention is directed to a processes for the synthesis of trans isomer of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles (Formula I). The process comprises the steps of: (a) obtaining a compound of Formula II, which is a mixture of cis and trans-diastereomers, and (b) chemically decomposing the compound of Formula II in a solution comprising a solvent and an acid that is a hydrogen donor or an electron pair acceptor, whereby the cis diastereomer is decomposed and the compound of Formula I is obtained. The compounds prepared by the present invention are useful in treating diseases or conditions associated with platelet aggregation and/or platelet activation.

US Patent:

7932376, Apr 26, 2011

Filed:

Apr 28, 2006

Appl. No.:

11/413600

Inventors:

Paul S. Watson - Carrboro NC, US
Sammy R. Shaver - Chapel Hill NC, US
Krzysztof Bednarski - Springville UT, US

Assignee:

Inspire Pharmaceuticals, Inc. - Durham NC

International Classification:

C07H 19/06
C07H 19/067
C07D 239/47
A61K 31/7068
A61K 31/506
A61P 7/02

US Classification:

536 268, 514 49, 514269, 544309, 544317

Abstract:

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.