Michael L Girgis

US Patent:

6740776, May 25, 2004

Filed:

Jul 15, 2002

Appl. No.:

10/196600

Inventors:

Ratna Shekhar - Madison NJ
Michael John Girgis - Montville NJ

Assignee:

Novartis AG - Basel

International Classification:

C07C 5123

US Classification:

562418, 562421

Abstract:

A low temperature process for preparing an aromatic acid having formula (I), said process comprising reacting an aromatic aldehyde having formula (II) with a gas having an oxygen content of 1 to 100 weight percent, based on the total weight of the gas, at a temperature of about 20Â C. to less than 100Â C. in the presence of a supported Group VIII metal catalyst, and a solvent having a flash point greater than 95Â C. and/or a melting point less than 55Â C. , provided that the flash point of the solvent is greater than the reaction temperature, wherein R and R are independently selected from the group consisting of hydrogen and a C -C linear, branched or cyclic alkyl group. The process of the invention yields an aromatic acid in excellent yield, and (i) does not involve the use of deleterious oxidizing agents; (ii) is essentially free of by-products; and (iii) is accomplished at a temperature of less than 100Â C.

US Patent:

6835838, Dec 28, 2004

Filed:

Jan 24, 2003

Appl. No.:

10/350615

Inventors:

Guang-Pei Chen - Livingston NJ
Prasad Koteswara Kapa - Parsippany NJ
Eric M. Loeser - Lake Hiawatha NJ
Ulrich Beutler - Oberwil, CH
Werner Zaugg - Riehen, CH
Michael John Girgis - Montville NJ

Assignee:

Novartis AG - Basel

International Classification:

C07D21554

US Classification:

546173

Abstract:

A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.

US Patent:

7452999, Nov 18, 2008

Filed:

Feb 20, 2004

Appl. No.:

10/544919

Inventors:

Mahavir Prashad - Montville NJ, US
Bin Hu - Green Brook NJ, US
Joel Slade - Flanders NJ, US
Prasad Koteswara Kapa - Parsippany NJ, US
Michael John Girgis - Montville NJ, US

Assignee:

Novartis AG - Basel

International Classification:

C07D 417/00
C07D 401/00
C07D 277/00
C07D 207/00
C07D 405/00
C07D 317/44

US Classification:

548200, 548518, 548526, 5462697, 5462784, 5462791, 549439

Abstract:

Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular β-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.

US Patent:

7572917, Aug 11, 2009

Filed:

Jul 14, 2004

Appl. No.:

10/891357

Inventors:

Guang-Pei Chen - Livingston NJ, US
Prasad K Kapa - Parsippany NJ, US
Eric M Loeser - Lake Hiawatha NJ, US
Ulrich Beutler - Oberwil, CH
Werner Zaugg - Riehen, CH
Michael J Girgis - Montville NJ, US

Assignee:

Novartis AG - Basel

International Classification:

C07D 215/12

US Classification:

546173, 546174

Abstract:

A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.

US Patent:

20080300410, Dec 4, 2008

Filed:

Nov 16, 2006

Appl. No.:

12/093825

Inventors:

Mahavir Prashad - Montville NJ, US
Yugang Liu - Bridgewater NJ, US
Bin Hu - Green Brook NJ, US
Michael J. Girgis - Montville NJ, US
Frank Schaefer - Rheinfelden, DE

International Classification:

C07D 211/32

US Classification:

546234

Abstract:

The present invention relates to salts of aryl compounds as discussed below and to methods of manufacture thereof, as well as other subject matter. More particularly, the invention relates to salts useful as intermediates for the synthesis of the cinnamanilide of formula (Y): where Ris selected from H, OH, C, C, Cor Calkyl; and Ris C, C, Cor Calkyl.

US Patent:

20090131707, May 21, 2009

Filed:

Nov 17, 2008

Appl. No.:

12/272552

Inventors:

Mahavir Prashad - Montville NJ, US
Bin Hu - Green Brook NJ, US
Joel Slade - Flanders NJ, US
Prasad Koteswara Kapa - Parsippany NJ, US
Michael John Girgis - Montville NJ, US

Assignee:

NOVARTIS AG - Basel

International Classification:

C07C 227/16

US Classification:

560 45

Abstract:

Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular I3-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxypropionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.

US Patent:

20090156585, Jun 18, 2009

Filed:

Nov 8, 2006

Appl. No.:

11/722360

Inventors:

Lili Feng - Pine Brook NJ, US
Sven Erik Godtfredsen - Chatham NJ, US
Bin Hu - Green Brook NJ, US
Yugang Liu - Bridgewater NJ, US
Piotr Karpinski - Lincoln Park NJ, US
Paul Allen Sutton - Parsippany NJ, US
Mahavir Prashad - Montville NJ, US
Michael J. Girgis - Montville NJ, US
Thomas J. Blacklock - Clark NJ, US

International Classification:

A61K 31/41
C07D 257/04
C07D 403/10
A61K 31/4178
A61P 9/10
A61P 25/00
A61K 31/549
A61K 31/4422
A61P 9/00
A61K 31/216
C07D 409/06
C07C 229/34

US Classification:

5142235, 548253, 5483054, 5483151, 560 39, 514381, 514394, 514397, 514382, 514533, 514356

Abstract:

A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.

US Patent:

20090247581, Oct 1, 2009

Filed:

Nov 16, 2006

Appl. No.:

12/085056

Inventors:

Mahavir Prashad - Montville NJ, US
Yugang Liu - Bridgewater NJ, US
Bin Hu - Green Brook NJ, US
Michael J. Girgis - Montville NJ, US
Frank Schaefer - Rheinfelden, DE

International Classification:

C07D 211/26
A61K 31/445

US Classification:

514317, 546229

Abstract:

The present invention relates to a process for the synthesis of (S)-2′[2-1-(methyl-2-piperidyl) ethyl] cinnamanilide (I) or salts or pharmaceutically acceptable prodrugs thereof: