Sushil K Srivastava

Author:

Sushil Srivastava

ISBN #:

8170362121

Author:

Sushil Srivastava

ISBN #:

8185199531

US Patent:

6515170, Feb 4, 2003

Filed:

Apr 26, 2001

Appl. No.:

09/843226

Inventors:

Ramesh N. Patel - Bridgewater NJ
Amit Banerjee - St. Louis MO
Venkata B. Nanduri - East Brunswick NJ
Steven L. Goldberg - Basking Ridge NJ
Robert M. Johnston - Whitehouse Station NJ
Thomas P. Tully - Middlesex NJ
Laszlo J. Szarka - East Brunswick NJ
Shankar Swaminathan - North Brunswick NJ
John J. Venit - North Brunswick NJ
Jerome L. Moniot - Chester NJ
William J. Winter - New Brunswick NJ
Neal G. Anderson - Stockton NJ
David A. Lust - Roosevelt NJ
Gerard Crispino - Princeton NJ
Sushil K. Srivastava - Dayton NJ

Assignee:

Bristol-Myers Squibb Co. - Princeton NJ

International Classification:

C07C 3200

US Classification:

562432, 562433, 562426, 562485, 562400

Abstract:

The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.

US Patent:

7829720, Nov 9, 2010

Filed:

May 2, 2005

Appl. No.:

11/119558

Inventors:

Soojin Kim - West Orange NJ, US
Bruce T. Lotz - Yardville NJ, US
Mary F. Malley - Lawrenceville NJ, US
Jack Z. Gougoutas - Princeton NJ, US
Martha Davidovich - East Brunswick NJ, US
Sushil K. Srivastava - Dayton NJ, US

Assignee:

Bristol-Myers Squibb Company - Princeton NJ

International Classification:

C07D 213/56

US Classification:

546332

Abstract:

A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

US Patent:

7838678, Nov 23, 2010

Filed:

Jan 27, 2009

Appl. No.:

12/360468

Inventors:

Soojin Kim - Demarest NJ, US
Bruce T. Lotz - Yardville NJ, US
Mary F. Malley - Lawrenceville NJ, US
Jack Z. Gougoutas - Princeton NJ, US
Martha Davidovich - East Brunswick NJ, US
Sushil K. Srivastava - Dayton NJ, US

Assignee:

Bristol-Myers Squibb Company - Princeton NJ

International Classification:

C07D 213/56

US Classification:

546332

Abstract:

A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

US Patent:

8513428, Aug 20, 2013

Filed:

Oct 8, 2010

Appl. No.:

12/900588

Inventors:

Soojin Kim - Demarest NJ, US
Bruce T. Lotz - Yardville NJ, US
Mary F. Malley - Lawrenceville NJ, US
Jack Z. Gougoutas - Princeton NJ, US
Martha Davidovich - East Brunswick NJ, US
Sushil K. Srivastava - Dayton NJ, US

Assignee:

Bristol-Meyers Squibb Company - Princeton NJ

International Classification:

C07D 213/56
A61K 31/44

US Classification:

546332, 514357

Abstract:

A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

US Patent:

62488821, Jun 19, 2001

Filed:

Oct 12, 2000

Appl. No.:

9/689209

Inventors:

Jollie D. Godfrey - Trenton NJ
David R. Kronenthal - Yardley PA
Mark D. Schwinden - Holland PA
Sushil K. Srivastava - Dayton NJ
Keith Ramig - Orange NJ
John J. Venit - North Brunswick NJ
Paul A. Jass - Charles City IA
Saibaba Racha - East Syracuse NY
John L. Dillon - East Syracuse NY
Nachimuthu Soundararajan - Kendall Park NJ
Gerald L. Powers - North Brunswick NJ
Atul S. Kotnis - Kendall Park NJ

Assignee:

Bristol-Myers Squibb Co. - Princeton NJ

International Classification:

C07D26702

US Classification:

540490

Abstract:

The glycinamide of the formula ##STR1## is reacted with the dioxolane of the formula ##STR2## wherein L is a leaving group such as iodo, bromo, alkylsulfonyloxy, or arylsulfonyloxy to give the dioxolane of the formula ##STR3## Treating the dioxolane of formula III under aqueous refluxing conditions followed by exchanging the dioxolane acetal with a dimethoxy acetal and introduction of the methyl ester gives (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester which is an intermediate in the preparation of the dual inhibitor [4S-[4. alpha. (R*),7. alpha. , 10a. beta. ]]-)octahydro-4-[(2-mercapto-1-oxo-3-phenylpropy)-amino]-5-oxo-7H -pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid. Also disclosed are storage stable salts of (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester.

US Patent:

61629138, Dec 19, 2000

Filed:

Jul 8, 1999

Appl. No.:

9/349861

Inventors:

Jerome L. Moniot - Chester NJ
Sushil K. Srivastava - Dayton NJ
William J. Winter - Montgomery NY
John J. Venit - North Brunswick NJ
Shankar Swaminathan - North Brunswick NJ
Keith Ramig - Orange NJ
Paul A. Jass - Charles City IA
Mark D. Schwinden - Holland PA
John L. Dillon - East Syracuse NY
Saibaba Racha - East Syracuse NY
James Simpson - Belle Mead NJ
Chien-Kuang Chen - Marlboro NJ
Shawn K. Pack - Plainsboro NJ

Assignee:

Bristol-Myers Squibb Co. - Princeton NJ

International Classification:

C07D28102
C07C26100
C07C22904
C07C22922

US Classification:

540490

Abstract:

N-protected-L-homocysteine disulfide of the formula ##STR1## or an activated form thereof is reacted with (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester to give the disulfide intermediate of the formula ##STR2## Cleavage of the disulfide bond followed by acid catalyzed cyclization produces the N-protected lactam of formula III which is useful for preparing the pharmaceutically active compound omapatrilat.

US Patent:

60310049, Feb 29, 2000

Filed:

Mar 4, 1999

Appl. No.:

9/262526

Inventors:

Peter Timmins - Merseyside, GB
William J. Winter - Lebanon NJ
Sushil K. Srivastava - Dayton NJ
Alison E. Bretnall - Chester, GB
Chenkou Wei - Princeton Junction NJ
Gerald L. Powers - North Brunswick NJ

Assignee:

Bristol-Myers Squibb Company - Princeton NJ

International Classification:

A61K 31155

US Classification:

514635

Abstract:

Novel salts of the antidiabetic agent metformin acre provided which are metformin salts of dibasic acids (2:1 molar ratio), preferably metformin (2:1) fumarate and metformin (2:1) succinate, which may be employed alone or in combination with another antihyperglycemic agent such as glyburide, for treating diabetes. A method for treating diabetes employing the novel metformin salt by itself or in combination with another antidiabetic agent is also provided.

US Patent:

63295423, Dec 11, 2001

Filed:

Oct 12, 2000

Appl. No.:

9/689215

Inventors:

Jollie D. Godfrey - Trenton NJ
David R. Kronenthal - Yardley PA
Mark D. Schwinden - Holland PA
Sushil K. Srivastava - Dayton NJ
Keith Ramig - Orange NJ
John J. Venit - North Brunswick NJ
Paul A. Jass - Charles City IA
Saibaba Racha - East Syracuse NY
John L. Dillon - East Syracuse NY
Nachimuthu Soundararajan - Kendall Park NJ
Gerald L. Powers - North Brunswick NJ
Atul S. Kotnis - Kendall Park NJ

Assignee:

Bristol-Myers Squibb Co. - Princeton NJ

International Classification:

C07C 6966

US Classification:

560186

Abstract:

The glycinamide of the formula ##STR1## is reacted with the dioxolane of the formula ##STR2## wherein L is a leaving group such as iodo, bromo, alkylsulfonyloxy, or arylsulfonyloxy to give the dioxolane of the formula ##STR3## Treating the dioxolane of formula III under aqueous refluxing conditions followed by exchanging the dioxolane acetal with a dimethoxy acetal and introduction of the methyl ester gives (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester which is an intermediate in the preparation of the dual inhibitor [4S-[4. alpha. (R*),7. alpha. ,10a. beta. ]]-octahydro-4-[(2-mercapto-1-oxo-3-ph enylpropyl)-amino]-5-oxo-7H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid. Also disclosed are storage stable salts of (S)-2-amino-6, 6-dimethoxyhexanoic acid, methyl ester.