John J Talley - Brentwood MO, US John R Medich - Gurnee IL, US Kathleen T McLaughlin - Arlington Heights IL, US Henry T Gaud - Evanston IL, US Edward E Yonan - Carol Stream IL, US
Assignee:
G. D. Searle & Co. - Skokie IL
International Classification:
A61K 31/42 C07D 261/08
US Classification:
514378, 548247
Abstract:
A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.
Leo J. Letendre - Manchester MO, US William D. McGhee - Fenton MO, US Cynthia Snoddy - St. Louis MO, US George Klemm - Webster Groves MO, US Henry T. Gaud - Evanston IL, US
Assignee:
Pharmacia Corporation - St. Louis MO
International Classification:
C07D 231/12 C07D 231/13
US Classification:
5483771
Abstract:
A process for the qualitative preparation of 3-haloalkyl-1H-pyrazoles suitable for efficient, high payload commercial application.
Leo J. Letendre - Manchester MO, US William D. McGhee - Fenton MO, US Cynthia Snoddy - St. Louis MO, US George Klemm - Webster Groves MO, US Henry T. Gaud - Evanston IL, US
Assignee:
Pfizer Inc. - New York NY
International Classification:
C07D 231/12
US Classification:
5483771
Abstract:
A process for the qualitative preparation of 3-haloalkyl-1H-pyrazoles suitable for efficient, high payload commercial application.
Crystalline Form Of 4- [ 5-Methyl-3-Phenylisoxazol-4-Yl ] Benzenesulfonamide
John Talley - Brentwood MO, US John Medich - Curnee IL, US Kathleen McLaughlin - Arlington Heights IL, US Henry Gaud - Evanston IL, US Edward Yonan - Carol Stream IL, US
Assignee:
G.D. Searle & Co. - Chicago IL
International Classification:
A61K031/42
US Classification:
514/378000, 548/240000
Abstract:
A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.
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.
Eplerenone Crystal 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 L. Stahl - Buffalo Grove IL, US Joseph Wieczorek - Cary IL, US Chris Yan - Plainsboro NJ, US
Assignee:
Pharmacia Corporation - Peapack NJ
International Classification:
A61K031/585 C07J071/00
US Classification:
540016000, 514173000
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.
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