Edward Paul Grabowski

US Patent:

20030176501, Sep 18, 2003

Filed:

Nov 13, 2002

Appl. No.:

10/293153

Inventors:

Richard Tillyer - Cranford NJ, US
Paul Reider - Westfield NJ, US
Edward Grabowski - Westfield NJ, US
Feng Xu - Staten Island NY, US
Robert Wenslow - East Windsor NJ, US
Jose Vega - Trappe PA, US
Richard Varsolona - Scotch Plains NJ, US

International Classification:

C07C069/34
A61K031/225

US Classification:

514/548000, 560/146000

Abstract:

The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a crystalline hydrated form of the calcium salt of dihydroxy open acid simvastatin to a patient in need of such treatment. Methods for making the calcium salt of dihydroxy open acid simvastatin are also provided.

US Patent:

20030211151, Nov 13, 2003

Filed:

Apr 29, 2003

Appl. No.:

10/425154

Inventors:

Richard Tillyer - Cranford NJ, US
Paul Reider - Westfield NJ, US
Edward Grabowski - Westfield NJ, US
Feng Xu - Staten Island NY, US
Jose Vega - Trappe PA, US
Mandana Asgharnejad - Ambler PA, US

Assignee:

Merck & Co., Inc.

International Classification:

A61K031/225
A61K009/22
A61K009/16
A61K009/50

US Classification:

424/468000, 514/548000

Abstract:

The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a compound selected from a dihydroxy open acid statin and a pharmaceutically acceptable salt or ester thereof in a delayed-release pharmaceutical dosage form to a patient in need of such treatment wherein substantial release of the compound from the dosage form is delayed until after passage of the dosage form through the stomach.

US Patent:

20050119343, Jun 2, 2005

Filed:

Nov 5, 2004

Appl. No.:

10/981866

Inventors:

Richard Tillyer - Cranford NJ, US
Paul Reider - Westfield NJ, US
Edward Grabowski - Westfield NJ, US
Feng Xu - Staten Island NY, US
Robert Wenslow - East Windsor NJ, US
Jose Vega - Trappe PA, US
Richard Varsolona - Scotch Plains NJ, US

International Classification:

A61K031/225
C07C069/66

US Classification:

514548000, 560180000

Abstract:

The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a crystalline hydrated form of the calcium salt of dihydroxy open acid simvastatin to a patient in need of such treatment. Methods for making the calcium salt of dihydroxy open acid simvastatin are also provided.

US Patent:

51169835, May 26, 1992

Filed:

May 8, 1990

Appl. No.:

7/520991

Inventors:

Apurba Bhattacharya - Rahway NJ
Alan W. Douglas - Monmouth Junction NJ
Edward J. Grabowski - Westfield NJ
Ulf H. Dolling - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07F 704

US Classification:

546 14

Abstract:

A process for dehydrogenating a compound of the formula ##STR1## which comprises reacting the compound with a silylating agent in the presence of a quinone to introduce a. DELTA. sup. 1 double bond.

US Patent:

50845748, Jan 28, 1992

Filed:

Feb 7, 1990

Appl. No.:

7/478064

Inventors:

Apurba Bhattacharya - Rahway NJ
Alan W. Douglas - Monmouth Junction NJ
Edward J. Grabowski - Westfield NJ
Ulf H. Dolling - Westfield NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

A61K 3158
C07J 7300

US Classification:

546 77

Abstract:

A process for dehydrogenating a compound of the formula ##STR1## which comprises reacting the compound with a silylating agent in the presence of a quinone to introduce a. DELTA. sup. 1 double bond.

US Patent:

56334052, May 27, 1997

Filed:

May 25, 1995

Appl. No.:

8/450330

Inventors:

Andrew S. Thompson - Mountainside NJ
Edward G. Corley - Old Bridge NJ
Edward J.J. Grabowski - Westfield NJ
Nobuyoshi Yasuda - Mountainside NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07C21100
C07C 5116

US Classification:

564321

Abstract:

An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.