John C Spurlino

7030110, Apr 18, 2006

Oct 4, 2002

10/263663

Aihua Wang - Jamison PA, US
Bruce Edward Tomczuk - Collegeville PA, US
Tianbao Lu - Kennett Square PA, US
Richard M. Soll - Lawrenceville NJ, US
John Curtis Spurlino - Downingtown PA, US
Roger Francis Bone - Bridgewater NJ, US

Ortho-McNeil Pharmaceuticals, Inc. - Raritan NJ

A61K 31/535
A61K 31/497
A61K 31/4965
A61K 31/553
A61K 31/55

5142288, 5142521, 51425211, 51425212, 51425505, 51421107, 51421101, 51421115, 51421706, 5142365, 5142368, 5142322, 51421208, 514183

Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R, R, R, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

20020052357, May 2, 2002

Jul 17, 2001

09/905883

Aihua Wang - Jamison PA, US
Bruce Tomczuk - Collegeville PA, US
Tianbao Lu - Kennett Square PA, US
Richard Soll - Lawrenceville NJ, US
John Spurlino - Downingtown PA, US
Roger Bone - Bridgewater NJ, US

3-Dimensional Pharmaceuticals, Inc.

A61K031/553
A61K031/535
C07D413/02

514/211080, 514/228800, 540/545000, 544/063000

Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R, R, R, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

20060058291, Mar 16, 2006

Oct 19, 2005

11/253447

Aihua Wang - Jamison PA, US
Bruce Tomczuk - Collegeville PA, US
Tianbao Lu - Kennett Square PA, US
Richard Soll - Lawrenceville NJ, US
John Spurlino - Downingtown PA, US
Roger Bone - Bridgewater NJ, US

Ortho-McNeil Pharmaceutical, Inc. - Raritan NJ

A61K 31/553
A61K 31/535
A61K 31/4965

514228800, 514255060, 514211080, 540545000, 544406000, 544405000, 544063000

Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R, R, R, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

20090111711, Apr 30, 2009

Apr 25, 2008

12/109723

Francis A. Lewandowski - Washington Crossing PA, US
Joseph Daniel Kwasnoski - Newtown PA, US
John C. Spurlino - Downingtown PA, US

C40B 30/10
C40B 60/12

506 12, 506 39

A high-density high-throughput microplate and methods for simultaneously screening a plurality of protein crystallization solutions and for producing diffraction quality protein crystals in a vapor-diffusion environment are disclosed. The microplate has defined side-by-side paired chambers of equal size, wherein the side-by-side paired chambers have a maximum volume of about 8 μl, and wherein the paired chambers have a vapor channel, therein providing vapor exchange between the side-by-side paired chambers. The microplate further includes a membrane to seal the surface of the microplate. The microplate is adapted to receive a crystallization solution in one of the side-by-side paired chambers and a protein solution in the other of the side-by-side paired chambers, wherein the protein solution and the crystallization solution interact via a vapor diffusion process, which enables the formation of protein crystals within the chamber that contains the protein solution.

20130040360, Feb 14, 2013

Jun 26, 2012

13/533108

Kristi A. Leonard - Lansdale PA, US
Richard Scott Alexander - Newark DE, US
Joseph Kent Barbay - Flourtown PA, US
Roger F. Bone - Bridgewater NJ, US
Ingrid Christa Deckman - Berwyn PA, US
Paul F. Jackson - New Hope PA, US
Lawrence C. Kuo - Gwynedd Valley PA, US
Frank A. Lewandowski - Philadelphia PA, US
Diane M. Maguire - Downingtown PA, US
Cynthia M. Milligan - Rutledge PA, US
Kenneth J. Rhodes - Belmont MA, US
Robert H. Scannevin - Hopkinton MA, US
Celine Schalk-Hihi - Phoenixville PA, US
Barry Springer - Wilmington DE, US
John C. Spurlino - Downingtown PA, US
Matthew J. Todd - Ambler PA, US
Brett Andrew Tongue - Blue Bell PA, US
Aihua Wang - Jamison PA, US

C12N 9/96

435188

The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.

20130040994, Feb 14, 2013

Jun 26, 2012

13/533131

Kristi A. Leonard - Lansdale PA, US
Richard Scott Alexander - Newark DE, US
Joseph Kent Barbay - Flourtown PA, US
Roger F. Bone - Bridgewater NJ, US
Carl Crysler - Pottstown PA, US
Ingrid Christa Deckman - Berwyn PA, US
Paul F. Jackson - New Hope PA, US
Lawrence C. Kuo - Gwynedd Valley PA, US
Frank A. Lewandowski - Philadelphia PA, US
Diane M. Maguire - Downingtown PA, US
Carl Manthey - Chester Springs PA, US
Cynthia M. Milligan - Rutledge PA, US
Beverley Moore - North Wales PA, US
Kenneth J. Rhodes - Belmont MA, US
Robert H. Scannevin - Hopkinton MA, US
Celine Schalk-Hihi - Phoenixville PA, US
Barry Springer - Wilmington DE, US
John C. Spurlino - Downingtown PA, US
Matthew J. Todd - Ambler PA, US
Brett Andrew Tongue - Blue Bell PA, US
Aihua Wang - Jamison PA, US

A61K 31/427
A61P 35/00
A61P 19/02
A61P 9/00
A61P 1/04
A61P 9/12
A61P 11/00
A61P 1/02
A61P 17/02
A61P 1/16
A61P 9/10
A61P 25/00
A61P 11/06
A61P 13/12
A61P 25/06
C12N 9/99
A61K 31/4439

514338, 514371, 514370, 435184

The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.

20130166268, Jun 27, 2013

Jun 26, 2012

13/533201

Kristi A. Leonard - Lansdale PA, US
Richard Scott Alexander - Newark DE, US
Joseph Kent Barbay - Flourtown PA, US
Roger F. Bone - Bridgewater NJ, US
Ingrid Christa Deckman - Berwyn PA, US
Paul F. Jackson - New Hope PA, US
Lawrence C. Kuo - Gwynedd Valley PA, US
Frank A. Lewandowski - Philadelphia PA, US
Diane M. Maguire - Downingtown PA, US
Cynthia M. Milligan - Rutledge PA, US
Kenneth J. Rhodes - Belmont MA, US
Robert H. Scannevin - Hopkinton MA, US
Celine Schalk-Hihi - Phoenixville PA, US
Barry Springer - Wilmington DE, US
John C. Spurlino - Downingtown PA, US
Matthew J. Todd - Ambler PA, US
Brett Andrew Tongue - Blue Bell PA, US
Aihua Wang - Jamison PA, US

G06F 19/12

703 11

The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.

63264927, Dec 4, 2001

May 26, 2000

9/578487

Aihua Wang - Downingtown PA
Tianbao Lu - Collegeville PA
Bruce E. Tomczuk - Collegeville PA
Richard M. Soll - Lawrenceville NJ
John Spurlino - Downingtown PA
Roger Bone - Bridgewater NJ

3-Dimensional Pharmaceuticals, Inc. - Exton PA

C07D26502
C07D21372

544 63

Described are compounds of the Formula VII: ##STR1## wherein Het, R. sup. 1, R. sup. 7 and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.