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:

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:

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:

7947850, May 24, 2011

Filed:

Jul 30, 2008

Appl. No.:

12/182918

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:

C07C 323/58

US Classification:

562426, 548201

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:

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:

8158796, Apr 17, 2012

Filed:

May 21, 2009

Appl. No.:

12/470377

Inventors:

Jin She - Shanghai, CN
Jonathan Bryan deCamp - Raleigh NC, US
Paul S. Watson - Carrboro NC, US
David J. Slade - Claremont CA, US

Assignee:

Inspire Pharmaceuticals, Inc. - Whitehouse Station NJ

International Classification:

C07D 217/22

US Classification:

546145

Abstract:

The present invention is directed to practical high-yielding synthetic processes to prepare compounds of general Formula III, IV, V, VII, VIII, IX, X, XII, XIV, and XV. Such compounds are useful as final products or can be used as intermediates and be further modified to prepare other desired products such as rho-kinase inhibitors. The present invention is also directed to certain novel compounds and/or novel solid forms of certain compounds.

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.