Bin Hu

6933410, Aug 23, 2005

Feb 14, 2003

10/367402

Mahavir Prashad - Montville NJ, US
Bin Hu - North Plainfield NJ, US
Olivier Lohse - Belfort, FR

Novartis AG - Basel

C07C209/44

564414, 564428

A process for preparing 5,6-diethyl-2,3-dihydro-1H-inden-2-amine and acid addition salts thereof from 2-aminoindan. The process comprises protecting the amino group of 2-aminoindan, acetylating the ring in the protected compound, reducing the acetyl group to ethyl to form a monoethyl derivative, acetylating the monoethyl derivative, reducing the acetyl group to form a diethyl derivative, deprotecting the latter by hydrolysis and recovering the product in free or salt form. The process does not use deleterious Grignard reagents or nitrites such as isoamyl nitrite, and provides high regioselectivity and high yield of 5,6-diethyl-2,3-dihydro-1H-inden-2-amine. In addition, the process uses acetyl halide as both a reactant and a solvent.

7452999, Nov 18, 2008

Feb 20, 2004

10/544919

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

Novartis AG - Basel

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

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

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.

20080300410, Dec 4, 2008

Nov 16, 2006

12/093825

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

C07D 211/32

546234

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.

20090131707, May 21, 2009

Nov 17, 2008

12/272552

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

NOVARTIS AG - Basel

C07C 227/16

560 45

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.

20090156585, Jun 18, 2009

Nov 8, 2006

11/722360

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

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

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

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

20090247581, Oct 1, 2009

Nov 16, 2006

12/085056

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

C07D 211/26
A61K 31/445

514317, 546229

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:

20110112121, May 12, 2011

Jun 30, 2010

12/827218

Joerg BERGHAUSEN - Basel, CH
Claire HAUG - Basel, CH
Michael HERBIG - Basel, CH
Bin HU - East Hanover NJ, US
Stéphane JONAT - Basel, CH
Rajender LELETI - East Hanover NJ, US
Josef Gottfried MEINGASSNER - Vienna, AT
Stéphanie MONNIER - Cedex Compiegne, FR
Matthias NAPP - Basel, CH
Mahavir PRASHAD - East Hanover NJ, US
Anton STÜTZ - Wien, AT
Ranjit THAKUR - Basel, CH

A61K 31/505
A61P 17/00
A61P 17/06
C07D 239/02

514269, 544319

The present invention relates to pharmaceutical compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide, to the use of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide and compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide in therapeutic applications, especially indications with a dysregulation/overexpression of VEFG, (neo)-vascularisation and VEGF driven angiogenesis and to methods for manufacturing such compositions, the invention further relates to specific forms of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide and to the manufacturing and use of such forms. The present invention also relates to a new process to produce 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide.

61629197, Dec 19, 2000

Dec 3, 1998

9/204460

Mahavir Prashad - Montville NJ
Bin Hu - North Plainfield NJ

Novartis AG - Basel

C07D21132

546233

A process for preparing the d-threo isomer of methylphenidate hydrochloride comprising converting d,l-threo methylphenidate hydrochloride to the free base form in a first step, resolving the free base prepared in the first step with (R)-(-)-1,1'-binaphthyl-2,2'-diyl hydrogen phosphate to obtain the phosphate salt enriched with the d-threo isomer of methylphenidate in a second step, basifying the phosphate salt to obtain the free base form of the d-threo isomer of methylphenidate in a third step, converting the free base to the hydrochloride salt form of the d-threo isomer of methylphenidate in high optical purity in a fourth step, and recrystallizing the hydrochloride salt form to obtain the desired d-threo isomer in a higher optical purity. An alternative embodiment relates to the preparation of the d-threo isomer of methylphenidate hydrochloride utilizing the hydrochloride salt form of the racemic mixture of threo-methylphenidate directly.