Mark G Pietz

US Patent:

20020045746, Apr 18, 2002

Filed:

Dec 7, 2000

Appl. No.:

09/732209

Inventors:

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.

US Patent:

20030083493, May 1, 2003

Filed:

Jul 9, 2002

Appl. No.:

10/191626

Inventors:

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.

US Patent:

20050159594, Jul 21, 2005

Filed:

Jul 16, 2004

Appl. No.:

10/892406

Inventors:

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.

US Patent:

20050261261, Nov 24, 2005

Filed:

Feb 7, 2005

Appl. No.:

11/051460

Inventors:

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

Assignee:

Pharmacia Corporation - Peapack NJ

International Classification:

C07J071/00
A61K031/58

US Classification:

514173000, 540025000

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.

US Patent:

20050267302, Dec 1, 2005

Filed:

Dec 4, 2003

Appl. No.:

10/727681

Inventors:

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

Assignee:

G.D. Searle & Co. - Chicago IL

International Classification:

C07J021/00

US Classification:

540041000

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.

US Patent:

20090149431, Jun 11, 2009

Filed:

Feb 18, 2009

Appl. No.:

12/388228

Inventors:

Kathleen P. Barton - Lake Forest IL, US
Thomas B. Borchardt - Pleasant Prairie WI, US
Marlow V. Carlos - Des Plaines IL, US
Subhash Desai - Wilmette IL, US
Leonard J. Ferro - Highland Park IL, US
Henry T. Gaud - Evanston IL, US
Scott S. Ganser - Park City IL, US
Clay R. Little - Lindenhurst IL, US
Partha S. Mudipalli - Skokie IL, US
Mark A. Pietz - Grayslake IL, US
Daniel R. Pilipauskas - Glenview IL, US
Yuen-Lung L. Sing - St. Louis MO, US
Glenn L. Stahl - Buffalo Grove IL, US
Joseph J. Wieczorek - Cary IL, US
Chris Y. Yan - Plainsbore NJ, US

International Classification:

C07J 71/00
A61K 31/58
A61P 5/00

US Classification:

514173, 540 23

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.

US Patent:

20020038021, Mar 28, 2002

Filed:

Dec 7, 2000

Appl. No.:

09/732208

Inventors:

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.