Ronald Keith Webber - St. Charles MO Richard C. Durley - Chesterfield MO Alok K. Awasthi - Skokie IL Arija A. Bergmanis - Des Plaines IL Kam F. Fok - St. Louis MO Scott S. Ganser - Chicago IL Timothy J. Hagen - Gurne IL E. Ann Hallinan - Evanston IL Brian S. Hickory - Wildwood MO Pamela T. Manning - Labadie MO Michael Mao - Chesterfield MO Alan E. Moormann - Weldon Spring MO Barnett S. Pitzele - Skokie IL Michelle A. Promo - Chesterfield MO Richard R. Schartman - Evanston IL Jeffrey A. Scholten - Chesterfield MO Jeffrey S. Snyder - Manchester MO Mihaly V. Toth - St. Louis MO Mahima Trivedi - Glenview IL Sofya Tsymbalov - Skokie IL Foe Siong Tjoeng - Ballwin MO
Assignee:
Pharmacia Corporation - St. Louis MO
International Classification:
A61K 31195
US Classification:
514562, 560153, 562557
Abstract:
The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
Amidino Compounds Useful As Nitric Oxide Synthase Inhibitors
Ronald Keith Webber - Charles MO, US Richard C. Durley - Chesterfield MO, US Alok K. Awasthi - Skokie IL, US Arija A. Bergmanis - Des Plaines IL, US Kam F. Fok - St. Louis MO, US Scott S. Ganser - Chicago IL, US Timothy J. Hagen - Gurne IL, US E. Ann Hallinan - Evanston IL, US Brian S. Hickory - Wildwood MO, US Pamela T. Manning - Labadie MO, US Michael Mao - Chesterfield MO, US Alan E. Moormann - Weldon Springs MO, US Barnett S. Pitzele - Skokie IL, US Michelle A. Promo - Chesterfield MO, US Richard R. Schartman - Evanston IL, US Jeffrey A. Scholten - Chesterfield MO, US Jeffrey S. Snyder - Manchester MO, US Mihaly V. Toth - St. Louis MO, US Mahima Trivedi - Glenview IL, US Sofya Tsymbalov - Skokie IL, US Foe Siong Tjoeng - Ballwin MO, US
Assignee:
Pharmacia Corporation - St. Louis MO
International Classification:
C07C323/00
US Classification:
562557
Abstract:
The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
Methods Of Making Amidino Compounds Useful As Nitric Oxide Synthase Inhibitors
Ronald Keith Webber - St. Charles MO, US Richard C. Durley - Chesterfield MO, US Alok K. Awasthi - Skokie IL, US Arija A. Bergmanis - Des Plaines IL, US Kam F. Fok - St. Louis MO, US Scott S. Ganser - Chicago IL, US Timothy J. Hagen - Gurne IL, US E. Ann Hallinan - Evanston IL, US Brian S. Hickory - Wildwood MO, US Pamela T. Manning - Labadie MO, US Michael Mao - Chesterfield MO, US Alan E. Moormann - Weldon Springs MO, US Barnett S. Pitzele - Skokie IL, US Michelle A. Promo - Chesterfield MO, US Richard R. Schartman - Evanston IL, US Jeffrey A. Scholten - Chesterfield MO, US Jeffrey S. Snyder - Manchester MO, US Mihaly V. Toth - St. Louis MO, US Mahima Trivedi - Glenview IL, US Sofya Tsymbalov - Skokie IL, US Foe Siong Tjoeng - Ballwin MO, US
Assignee:
Pharmacia Corporation - St. Louis MO
International Classification:
C07D 233/40 C07C 271/00 C07C 323/00
US Classification:
5483195, 5483171, 560148, 562557
Abstract:
Method of making an alpha-amino acid compound having the structure of Formula 32: comprising treating under hydrolyzing conditions a hydantoin compound having the structure of Formula 33: where the substituents are described herein.
Amidino Compounds Useful As Nitric Oxide Synthase Inhibitors
Ronald Keith Webber - St. Charles MO, US Richard C. Durley - Chesterfield MO, US Alok K. Awasthi - Skokie IL, US Arija A. Bergmanis - Des Plaines IL, US Kam F. Fok - St. Louis MO, US Scott S. Ganser - Chicago IL, US Timothy J. Hagen - Gurne IL, US E. Ann Hallinan - Evanston IL, US Brian S. Hickory - Wildwood MO, US Pamela T. Manning - Labadie MO, US Michael Mao - Chesterfield MO, US Alan E. Moormann - Weldon Springs MO, US Barnett S. Pitzele - Skokie IL, US Michelle A. Promo - Chesterfield MO, US Richard R. Schartman - Evanston IL, US Jeffrey A. Scholten - Chesterfield MO, US Jeffrey S. Snyder - Manchester MO, US Mihaly V. Toth - St. Louis MO, US Mahima Trivedi - Glenview IL, US Sofya Tsymbalov - Skokie IL, US Foe Siong Tjoeng - Ballwin MO, US
Assignee:
Pharmacia Corporation - St. Louis MO
International Classification:
A61K 31/195
US Classification:
514562
Abstract:
The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
Amidino Compound And Salts Thereof Useful As Nitric Oxide Synthase Inhibitors
Ronald Webber - St. Charles MO, US Richard Durley - Chesterfield MO, US Alok Awasthi - Skokie IL, US Arija Bergmanis - Des Plaines IL, US Scott Ganser - Chicago IL, US Timothy Hagen - Gurne IL, US E. Hallinan - Evanston IL, US Donald Hansen - Skokie IL, US Brian Hickory - Wildwood MO, US Alan Moormann - Weldon Springs MO, US Barnett Pitzele - Skokie IL, US Michelle Promo - Chesterfield MO, US Richard Schartman - Evanston IL, US Jeffrey Snyder - Manchester MO, US Mahima Trivedi - Glenview IL, US Sofya Tsymbalov - Skokie IL, US
International Classification:
C07C323/25
US Classification:
562/477000, 562/556000
Abstract:
The present invention relates to S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine, or a pharmaceutically acceptable salt thereof.
Eplerenone Crystalline Form Exhibiting Enhanced Dissolution Rate
Kathleen Barton - Lake Forest IL, US Thomas Borchardt - Pleasant Prairie WI, US Marlon Carlos - Des Plaines IL, US Subhash Desai - Wilmette IL, US Leonard Ferro - Highland Park IL, US Henry Gaud - Evanston IL, US Scott Ganser - Park City IL, US Clay Little - Lindenhurst IL, US Partha Mudipalli - Skokie IL, US Mark Pietz - Grayslake IL, US Daniel Pilipauskas - Glenview IL, US Yuen-Lung Sing - St. Louis MO, US Glenn Stahl - Buffalo Grove IL, US Joseph Wieczorek - Cary IL, US Chris Yan - Plainsboro NJ, US
International Classification:
C07J017/00 C07J001/00 C07J021/00
US Classification:
540/002000, 540/116000, 540/041000
Abstract:
A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
Kathleen Barton - Lake Forest IL, US Thomas Borchardt - Pleasant Prairie WI, US Marlon Carlos - Des Plaines IL, US Subhash Desai - Wilmette IL, US Leonard Ferro - Highland Park IL, US Henry Gaud - Evanston IL, US Scott Ganser - Park City IL, US Clay Little - Lindenhurst IL, US Partha Mudipalli - Skokie IL, US Mark Pietz - Grayslake IL, US Daniel Pilipauskas - Glenview IL, US Yuen-Lung Sing - St. Louis MO, US Glenn Stahl - Buffalo Grove IL, US Joseph Wieczorek - Cary IL, US Chris Yan - Plainsboro IL, US
International Classification:
C07J001/00 C07J021/00
US Classification:
540/002000, 540/041000
Abstract:
A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
Eplerenone Drug Substance Having High Phase Purity
Kathleen Barton - Lake Forest IL, US Thomas Borchardt - Pleasant Prairie WI, US Marlon Carlos - Des Plaines IL, US Subhash Desai - Wilmette IL, US Leonard Ferro - Highland Park IL, US Henry Gaud - Evanston IL, US Scott Ganser - Park City IL, US Clay Little - Lindenhurst IL, US Partha Mudipalli - Skokie IL, US Mark Pietz - Grayslake IL, US Daniel Pilipauskas - Glenview IL, US Yuen-Lung Sing - St. Louis MO, US Glenn Stahl - Buffalo Grove IL, US Joseph Wieczorek - Cary IL, US Chris Yan - Vernon Hills IL, US
International Classification:
C07J053/00
US Classification:
540/047000
Abstract:
A novel crystalline form (Form L) of the aldosterone receptor antagonist drug eplerenone is provided having relatively high physical stability at normal temperatures of storage and use. Pharmaceutical compositions are also provided comprising Form L eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form L eplerenone and for preparing compositions comprising Form L eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
Pfizer Oct 1, 1999 - Apr 30, 2015
Senior Scientist
Searle Pharmacia Pfizer Oct 1, 1999 - Apr 30, 2015
Senior Scientist
Kingdom of God Oct 1, 1999 - Apr 30, 2015
Senior Pastor
Education:
St. Norbert College
Bachelors, Bachelor of Science, Mathematics, Chemistry
University of Notre Dame
Dartmouth College
Masters, Organic Chemistry
Skills:
Pharmaceutical Industry Analytical Chemistry Microsoft Office Biotechnology Validation Drug Discovery Drug Development Technology Transfer Gmp Protein Chemistry