Theresa R Fletcher

US Patent:

6956052, Oct 18, 2005

Filed:

Sep 19, 2002

Appl. No.:

10/247096

Inventors:

Arija A. Bergmanis - Des Plaines IL, US
Michael Clare - Skokie IL, US
Joyce Z. Crich - Glenview IL, US
Lifeng Geng - Skokie IL, US
Timothy J. Hagen - Gurnee IL, US
Gunnar J. Hanson - Skokie IL, US
Stephen C. Houdek - Des Plaines IL, US
He Huang - Northbrook IL, US
Donna M. Iula - Palatine IL, US
Francis J. Koszyk - Prospect Heights IL, US
Shuyuan Liao - Northbrook IL, US
Scott B. Mohler - Chicago IL, US
Maria Nguyen - Morton Grove IL, US
Richard A. Partis - Evanston IL, US
Michael A. Stealey - Libertyville IL, US
Michael B. Tollefson - Hainesville IL, US
Richard M. Weier - Lake Bluff IL, US
Xiangdong Xu - Gumee IL, US
Dominique Bonafoux - Saint Louis MO, US
Theresa R. Fletcher - Kirkwood MO, US
Bruce C. Hamper - Kirkwood MO, US
Patrick J. Lennon - Webster Groves MO, US
Subo Liao - Ballwin MO, US
Suzanne Metz - Chesterfield MO, US
David S. Oburn - Ferguson MO, US
Thomas J. Owen - Chesterfield MO, US
Angela M. Scates - Des Peres MO, US
Michael L. Vazquez - Ballwin MO, US
Serge G. Wolfson - Chesterfield MO, US

Assignee:

Pharmacia Corporation - St. Louis MO

International Classification:

A61K031/416
C07D231/54

US Classification:

514406, 5483591, 5462681, 5462757

Abstract:

The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

US Patent:

7186743, Mar 6, 2007

Filed:

Apr 25, 2005

Appl. No.:

11/113926

Inventors:

Arija A. Bergmanis - Des Plaines IL, US
Michael Clare - Skokie IL, US
Joyce Z. Crich - Glenview IL, US
Lifeng Geng - Skokie IL, US
Timothy J. Hagen - Gurnee IL, US
Gunnar J. Hanson - Skokie IL, US
Stephen C. Houdek - Des Plaines IL, US
He Huang - Northbrook IL, US
Donna M. Iula - Palatine IL, US
Francis J. Koszyk - Prospect Heights IL, US
Shuyuan Liao - Northbrook IL, US
Scott B. Mohler - Chicago IL, US
Maria Nguyen - Morton Grove IL, US
Richard A. Partis - Evanston IL, US
Michael A. Stealey - Libertyville IL, US
Michael B. Tollefson - Hainesville IL, US
Richard M. Weier - Lake Bluff IL, US
Xiangdong Xu - Gurnee IL, US
Dominique Bonafoux - Saint Louis MO, US
Theresa R. Fletcher - Kirkwood MO, US
Bruce C Hamper - Kirkwood MO, US
Patrick J. Lennon - Webster Groves MO, US
Subo Liao - Ballwin MO, US
Suzanne Metz - Chesterfield MO, US
David S. Oburn - Ferguson MO, US
Thomas J. Owen - Chesterfield MO, US
Angela M. Scates - Des Peres MO, US
Michael L. Vazquez - Ballwin MO, US
Serge G. Wolfson - Chesterfield MO, US

Assignee:

Pharmacia Corporation - St. Louis MO

International Classification:

A61K 31/416
A61K 31/454
A61K 31/5395
A61K 31/429
A61K 31/433
A61K 31/506
A61K 31/496

US Classification:

514406, 514338, 514364, 514370, 514362, 514274, 51425309, 5142328

Abstract:

The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

US Patent:

20040048852, Mar 11, 2004

Filed:

Jan 7, 2003

Appl. No.:

10/337942

Inventors:

Thomas Barta - Evanston IL, US
Daniel Becker - Glenview IL, US
Terri Boehm - Ballwin MO, US
Gary DeCrezcenzo - St. Charles MO, US
John Freskos - Clayton MO, US
Daniel Getman - Chesterfield MO, US
Joseph McDonald - Wildwood MO, US
Clara Villamil - Glenview IL, US
Louis Bedell - Mt. Prospect IL, US
Jeffery Carroll - Columbia IL, US
Theresa Fletcher - Kirkwood MO, US
Susan Hockerman - Lincolnwood IL, US
Stephen Kolodziej - Ballwin MO, US
Madeleine Li - Vernon Hills IL, US
Deborah Mischke - Defiance MO, US
Patrick Mullins - St. Louis MO, US
Carol Howard - Fenton MO, US
Joseph Rico - Ballwin MO, US
Nathan Stehle - Grafton WI, US

International Classification:

A61K031/55
A61K031/54
A61K031/537
A61K031/445
A61K031/497
A61K031/495
A61K031/44
A61K031/19
A61K031/421
A61K031/426
A61K031/4172

US Classification:

514/217120, 514/227500, 514/237800, 514/252120, 514/317000, 514/357000, 514/365000, 514/374000, 514/400000, 514/408000, 514/575000

Abstract:

A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein Rand Rare both hydrido or Rand Rtogether with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. Rin formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

US Patent:

20050148627, Jul 7, 2005

Filed:

Mar 16, 2004

Appl. No.:

10/801446

Inventors:

Jeffery Carter - Chesterfield MO, US
David Brown - Chesterfield MO, US
Li Xing - Chesterfield MO, US
Karl Aston - Pacific MO, US
John Springer - O'Fallon MO, US
Francis Koszyk - Prospect Heights IL, US
Steven Kramer - Des Plaines IL, US
Sofya Tsymbalov - Brententon FL, US
Renee Huff - Park Ridge IL, US
Yi Yu - Glenview IL, US
Bruce Hamper - Kirkwood MO, US
Subo Laio - Ballwin MO, US
Angela Deprow - Cape Girardeau MO, US
Theresa Fletcher - Kirkwood MO, US
E. Hallinan - Evanston IL, US
James Kiefer - Chesterfield MO, US
David Limburg - Wildwood MO, US
Lijuan Wang - Wildwood MO, US

International Classification:

A61K031/47
A61K031/382
A61K031/353

US Classification:

514311000, 514456000, 514432000, 546169000, 549023000, 549403000

Abstract:

The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R, R, R, and Rare as described in the specification.

US Patent:

20050148777, Jul 7, 2005

Filed:

Mar 16, 2004

Appl. No.:

10/801429

Inventors:

Jeffery Carter - Chesterfield MO, US
David Brown - Chesterfield MO, US
Li Xing - Chesterfield MO, US
Karl Aston - Pacific MO, US
John Springer - O'Fallon MO, US
Francis Koszyk - Prospect Heights IL, US
Steven Kramer - Des Plaines IL, US
Renee Huff - Park Ridge IL, US
Yi Yu - Glenview IL, US
Bruce Hamper - Kirkwood MO, US
Subo Laio - Ballwin MO, US
Angela Deprow - Cape Girardeau MO, US
Theresa Fletcher - Kirkwood MO, US
E. Hallinan - Evanston IL, US
James Kiefer - Chesterfield MO, US
David Limburg - Wildwood MO, US
Lijuan Wang - Wildwood MO, US
Cindy Ludwig - St. Louis MO, US
John McCall - Highland Park IL, US
John Talley - Sommerville MA, US

International Classification:

C07D335/06
C07D215/38

US Classification:

546169000, 549023000, 549398000

Abstract:

The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with cyclooxygenase-2 mediated disorders. Compounds of particular interest are benzopyrans and their analogs defined by formula 1 Wherein Z, X, R, R 2, R, and Rare as described in the specification.

US Patent:

20050197338, Sep 8, 2005

Filed:

Oct 21, 2004

Appl. No.:

10/970769

Inventors:

He Huang - Durham NC, US
Michael Stealey - Libertyville IL, US
Gunnar Hanson - Durham NC, US
Patrick Lennon - Webster Groves MO, US
Bruce Hamper - Kirkwood MO, US
Jin Xie - Ballwin MO, US
David Oburn - Ferguson MO, US
Serge Wolfson - Chestefield MO, US
Theresa Fletcher - Kirkwood MO, US
Richard Heier - Columbia IL, US
Matthew Reding - University City MO, US
Michael Clare - Skokie IL, US

International Classification:

A61K031/53
A61K031/506
A61K031/497
A61K031/4709
A61K031/454
A61K031/427
A61K031/422
A61K031/416

US Classification:

514241000, 514406000, 514252050, 514255050, 514256000, 514326000, 514365000, 514374000, 514397000, 514314000

Abstract:

Compounds of Formula I: wherein X, X, L, A, R, L, R, R, R, R, Rand Rare as defined herein, are disclosed.

US Patent:

20060084688, Apr 20, 2006

Filed:

Jan 28, 2005

Appl. No.:

11/046645

Inventors:

Thomas Barta - Evanston IL, US
Daniel Becker - Glenview IL, US
Louis Bedell - Mt. Prospect IL, US
Terri Boehm - Ballwin MO, US
Jeffery Carroll - Columbia IL, US
Gary DeCrescenzo - St. Charles MO, US
Theresa Fletcher - Kirkwood MO, US
John Freskos - Clayton MO, US
Daniel Getman - Chesterfield MO, US
Gunnar Hanson - Skokie IL, US
Susan Hockerman - Lincolnwood IL, US
Carol Howard - Fenton MO, US
Stephen Kolodziej - Ballwin MO, US
Madeleine Li - Vernon Hills IL, US
Joseph McDonald - Wildwood MO, US
Deborah Mischke - Defiance MO, US
Patrick Mullins - St. Louis MO, US
Joseph Rico - Ballwin MO, US
Nathan Stehle - Grafton WI, US
Clara Villamil - Glenview IL, US

International Classification:

A61K 31/426
A61K 31/421
A61K 31/4166
A61K 31/19

US Classification:

514369000, 514376000, 514400000, 514575000, 514463000

Abstract:

A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein Rand Rare both hydrido or Rand Rtogether with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. Rin formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.