Paul A 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:

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:

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.

US Patent:

8039465, Oct 18, 2011

Filed:

Jan 28, 2010

Appl. No.:

12/695348

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. - Whitehouse Station NJ

International Classification:

A61K 31/54

US Classification:

5142272, 544122, 544123

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:

8071779, Dec 6, 2011

Filed:

Dec 17, 2007

Appl. No.:

11/958214

Inventors:

John W. Lampe - Cary NC, US
Paul S. Watson - Carrboro NC, US
David J. Slade - Durham NC, US
Ward M. Peterson - Morrisville NC, US
Christopher S. Crean - Pittsboro NC, US
Jason L. Vittitow - Durham NC, US
Jonathan Bryan DeCamp - Raleigh NC, US
Nicholas F. Pelz - Durham NC, US

Assignee:

Inspire Pharmaceuticals, Inc. - Whitehouse Station NJ

International Classification:

C07D 211/32
C07D 231/56

US Classification:

546199, 5483611

Abstract:

The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. 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 Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.

US Patent:

8476295, Jul 2, 2013

Filed:

Dec 10, 2010

Appl. No.:

12/965615

Inventors:

John W. Lampe - Cary NC, US
Paul S. Watson - Carrboro NC, US
David J. Slade - Claremont CA, US

Assignee:

Inspire - Raleigh NC

International Classification:

A01N 43/42
A61K 31/44
C07D 401/00
C07D 405/00
C07D 409/00
C07D 411/00

US Classification:

514304, 546126

Abstract:

The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. 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 cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.

Address:

424 Shoreline Dr, Fayetteville, NC 28311

VIN:

WBAVB73537P101371

Make:

BMW

Model:

3 SERIES

Year:

2007