Paul J Collins

US Patent:

6413960, Jul 2, 2002

Filed:

May 30, 2000

Appl. No.:

09/609011

Inventors:

John J Talley - St. Louis MO
Thomas D Penning - Elmhurst IL
Paul W Collins - Deerfield IL
James W Malecha - Libertyville IL
Julie M Miyashiro - Chicago IL
Stephen R Bertenshaw - Brentwood MO
Ish K Khanna - Vernon Hills IL
Matthew J Graneto - St. Louis MO
Roland S Rogers - Richmond Heights MO
Jeffery S Carter - Chesterfield MO
Stephen H. Docter - Mt. Prospect IL
Stella S Yu - Morton Grove IL

Assignee:

G.D. Searle Co. - Chicago IL

International Classification:

A61P 1106

US Classification:

5142365, 514406

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

6423713, Jul 23, 2002

Filed:

Jul 31, 2001

Appl. No.:

09/918481

Inventors:

Ashok Anantanarayan - Hainesville IL
Michael Clare - Skokie IL
Paul W. Collins - Deerfield IL
Joyce Zuowu Crich - Glenview IL
Rajesh Devraj - Ballwin MO
Daniel L. Flynn - Clarkson Valley MO
Lifeng Geng - Skokie IL
Matthew J. Graneto - Chesterfield MO
Cathleen E. Hanau - Chesterfield MO
Gunnar J. Hanson - Skokie IL
Susan J. Hartmann - Kirkwood MO
Michael Hepperle - St. Charles MO
He Huang - Chicago IL
Francis J. Koszyk - Prospect Heights IL
Shuyuan Liao - Glen Ellyn IL
Suzanne Metz - Chesterfield MO
Richard A. Partis - Evanston IL
Thao D. Perry - Chesterfield MO
Shashidhar N. Rao - St. Louis MO
Shaun Raj Selness - Chesterfield MO
Michael S. South - St. Louis MO
Michael A. Stealey - Libertyville IL
John Jeffrey Talley - St. Louis MO
Michael L. Vazquez - Ballwin MO
Richard M. Weier - Lake Bluff IL
Xiangdong Xi - Evanston IL
Ish K. Khanna - Libertyville IL
Yi Yu - Skokie IL

Assignee:

G. D. Searle Company - Skokie IL

International Classification:

A61K 31496

US Classification:

5142358, 51425301, 51425405, 514319, 514341, 544124, 544364, 546206, 546256, 5462754

Abstract:

A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R , R , R and R are as described in the specification.

US Patent:

6426360, Jul 30, 2002

Filed:

May 15, 2000

Appl. No.:

09/571033

Inventors:

Richard M Weier - Lake Bluff IL
Paul W Collins - Deerfield IL
Michael A Stealey - Libertyville IL
Thomas E Barta - Evanston IL
Renee M Huff - Park Ridge IL

Assignee:

G D Searle Co. - Chicago IL

International Classification:

A01N 4350

US Classification:

514396, 514398, 548254, 5483117, 5483421, 5483335, 5483345, 5483371, 5483381, 5483411, 5483425, 5483255, 5483251, 5483451, 5483435, 5483431

Abstract:

A class of compounds is described for treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula wherein R is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower alkenyloxyalkyl, mercapto, lower alkylcarbonyl, lower haloalkylcarbonyl, phenylcarbonyl, lower aralkylcarbonyl, lower aralkenyl, lower aryloxyalkyl, lower aralkyloxyalkyl, lower arylsulfonyl, lower aralkylsulfonyl, lower arylthioalkyl, lower heteroarylalkylthioalkyl, and heteroaryl selected from 2-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 4-pyridyl and 2-benzofuryl; wherein R and R are independently selected from heteroaryl, cycloalkyl and aryl, wherein the heteroaryl, cycloalkyl and aryl radicals are substituted at a substitutable position with one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminosulfonyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkoxy, amino, lower alkylamino, phenylamino and nitro; and wherein R is selected from hydrido, lower alkyl and acyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

6492411, Dec 10, 2002

Filed:

Apr 17, 2002

Appl. No.:

10/125325

Inventors:

John J Talley - St. Louis MO
Thomas D Penning - Elmhurst IL
Paul W Collins - Deerfield IL
James W Malecha - Libertyville IL
Julie M Miyashiro - Chicago IL
Stephen R Bertenshaw - Brentwood MO
Ish K Khanna - Vernon Hills IL
Matthew J Graneto - St. Louis MO
Roland S Rogers - Richmond Heights MO
Jeffery S Carter - Chesterfield MO
Stephen H. Docter - Mt. Prospect IL
Stella S Yu - Morton Grove IL

Assignee:

G. D. Searle Co. - Chicago IL

International Classification:

A61P 2900

US Classification:

514406, 5142365

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

6509361, Jan 21, 2003

Filed:

Feb 12, 2001

Appl. No.:

09/674653

Inventors:

Richard M. Weier - Lake Bluff IL
Joyce Z. Crich - Glenview IL
Xiang Dong Xu - Gurnee IL
Paul W. Collins - Deerfield IL

Assignee:

Pharmacia Corporation - Saint Louis MO

International Classification:

A61K 314439

US Classification:

514341, 5462754, 546256, 544360, 514252, 514333

Abstract:

The present invention contemplates 1,5-diaryl-substituted pyrazole compounds that, inter alia, inhibit the activity of p38 MAP kinase. Also contemplated by the invention are processes for the preparation of the contemplated compounds and for the use of a contemplated compound in treating a mammalian host having a p38 kinase- or TNF-mediated disease.

US Patent:

6514977, Feb 4, 2003

Filed:

Nov 20, 1998

Appl. No.:

09/196623

Inventors:

Ashok Anantanarayan - Hainesville IL
Michael Clare - Skokie IL
Paul W. Collins - Deerfield IL
Joyce Zuowu Crich - Glenview IL
Rajesh Devraj - Ballwin MO
Daniel L. Flynn - Clarkson Valley MO
Lifeng Geng - Skokie IL
Matthew J. Graneto - Chesterfield MO
Cathleen E. Hanau - Chesterfield MO
Gunnar J. Hanson - Skokie IL
Susan J. Hartmann - Kirkwood MO
Michael Hepperle - St. Charles MO
He Huang - Chicago IL
Francis J. Koszyk - Prospect Heights IL
Shuyuan Liao - Glen Ellyn IL
Suzanne Metz - Chesterfield MO
Richard A. Partis - Evanston IL
Thao D. Perry - Chesterfield MO
Shashidhar N. Rao - St. Louis MO
Shaun Raj Selness - Chesterfield MO
Michael S. South - St. Louis MO
Michael A. Stealey - Libertyville IL
John Jeffrey Talley - St. Louis MO
Michael L. Vazquez - Ballwin MO
Richard M. Weier - Lake Bluff IL
Xiangdong Xu - Evanston IL
Ish K. Khanna - Libertyville IL
Yi Yu - Skokie IL

Assignee:

G.D. Searle Company - Skokie IL

International Classification:

A61K 31454

US Classification:

51425401, 544370, 544333, 546210, 514326

Abstract:

A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R , R , R and R are as described in the specification.

US Patent:

6525059, Feb 25, 2003

Filed:

Feb 24, 2000

Appl. No.:

09/513351

Inventors:

Ashok Anantanarayan - Hainesville IL
Michael Clare - Skokie IL
Paul W. Collins - Deerfield IL
Joyce Zuowu Crich - Glenview IL
Rajesh Devraj - Chesterfield MO
Daniel L. Flynn - Clarkson Valley MO
Lifeng Geng - Skokie IL
Matthew J. Graneto - Chesterfield MO
Cathleen E. Hanau - Chesterfield MO
Gunnar J. Hanson - Skokie IL
Susan J. Hartmann - Kirkwood MO
Michael Hepperle - St. Charles MO
He Huang - Chicago IL
Francis J. Koszyk - Prospect Heights IL
Shuyuan Liao - Northbrook IL
Suzanne Metz - Chesterfield MO
Richard A. Partis - Evanston IL
Thao D. Perry - Chesterfield MO
Shashidhar N. Rao - Mundelein IL
Shaun Raj Selness - St. Louis MO
Michael S. South - St. Louis MO
Michael A. Stealey - Libertyville IL
John Jeffrey Talley - St. Louis MO
Michael L. Vazquez - Ballwin MO
Richard M. Weier - Lake Bluff IL
Xiangdong Xu - Gurnee IL
Ish K. Khanna - Libertyville IL
Yi Yu - Skokie IL

Assignee:

G. D. Searle Company - Skokie IL

International Classification:

A61K 31506

US Classification:

514256, 544333, 544335

Abstract:

A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R , R , R and R are as described in the specification.

US Patent:

6586603, Jul 1, 2003

Filed:

Oct 21, 2002

Appl. No.:

10/274679

Inventors:

John J Talley - St. Louis MO
Thomas D Penning - Elmhurst IL
Paul W Collins - Deerfield IL
James W Malecha - Libertyville IL
Julie M Miyashiro - Chicago IL
Stephen R. Bertenshaw - Brentwood MO
Ish K Khanna - Vernon Hills IL
Matthew J Graneto - St. Louis MO
Roland S Rogers - Richmond Heights MO
Jeffery S Carter - Chesterfield MO
Stephen H Docter - Mt. Prospect IL
Stella S Yu - Morton Grove IL

Assignee:

G.D. Searle Co. - Chicago IL

International Classification:

C07D23112

US Classification:

5483771

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.