John Y Chiu

US Patent:

7541471, Jun 2, 2009

Filed:

Jan 12, 2006

Appl. No.:

11/330935

Inventors:

Tao Wang - Springfield NJ, US
Jing Liao - Edison NJ, US
John S Chiu - Parsippany NJ, US
David Jieh-Shyh Tsai - Warren NJ, US
Hong-Chang Lee - Livingston NJ, US
Wenxue Wu - Princeton Junction NJ, US
Xiaoyong Fu - Edison NJ, US

Assignee:

Schering Corporation - Keniworth NJ

International Classification:

C07D 405/06

US Classification:

5462841

Abstract:

The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows:.

US Patent:

7553987, Jun 30, 2009

Filed:

Jun 29, 2007

Appl. No.:

11/824246

Inventors:

Tao Wang - Springfield NJ, US
John S. Chiu - Parsippany NJ, US
Jing Liao - Livingston NJ, US

Assignee:

Schering Corporation - Kenilworth NJ

International Classification:

C07C 205/00
C07C 61/08

US Classification:

560125, 562507

Abstract:

This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising:.

US Patent:

7626045, Dec 1, 2009

Filed:

Apr 23, 2009

Appl. No.:

12/428773

Inventors:

Tao Wang - Sprinfield NJ, US
Jing Liao - Livingston NJ, US
John S. Chiu - Parsippany NJ, US
David J. S. Tsai - Warren NJ, US
Hong-Chang Lee - Livingston NJ, US
Wenxue Wu - Princeton Junction NJ, US
Xiaoyong Fu - Edison NJ, US

Assignee:

Schering Corporation - Kenilworth NJ

International Classification:

C07D 307/92

US Classification:

549299

Abstract:

The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows:.

US Patent:

8383810, Feb 26, 2013

Filed:

Dec 12, 2011

Appl. No.:

13/323366

Inventors:

John S. Chiu - Parsippany NJ, US
Xiaoyong Fu - Edison NJ, US
Timothy L. McAllister - Philadelphia PA, US

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ

International Classification:

C07D 205/08
C07H 7/02

US Classification:

540200, 536 2911

Abstract:

A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

US Patent:

20040176418, Sep 9, 2004

Filed:

Jan 9, 2004

Appl. No.:

10/755066

Inventors:

Wenxue Wu - Princeton Junction NJ, US
Tao Wang - Springfield NJ, US
John Chiu - Parsippany NJ, US
Anastasia Pavlovsky - Morris Plains NJ, US
William Greenlee - Teaneck NJ, US
Michael Graziano - Scotch Plains NJ, US
Teddy Kosoglou - Jamison PA, US
Madhu Chintala - Colts Neck NJ, US
Samuel Chackalamannil - Califon NJ, US

Assignee:

Schering Corporation

International Classification:

C 07D 4 5/02
A61K031/4433

US Classification:

514/337000, 546/284100

Abstract:

A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. , or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. , and is represented by the formula for Compound 2: and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.

US Patent:

20060135755, Jun 22, 2006

Filed:

Dec 19, 2005

Appl. No.:

11/305926

Inventors:

John Chiu - Parsippany NJ, US
Xiaoyong Fu - Edison NJ, US
Timothy McAllister - Westfield NJ, US

International Classification:

C07D 205/02
C07H 17/02

US Classification:

536017400, 540200000

Abstract:

A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

US Patent:

20070203193, Aug 30, 2007

Filed:

May 2, 2007

Appl. No.:

11/743347

Inventors:

Wenxue Wu - Princeton Junction NJ, US
Tao Wang - Springfield NJ, US
John Chiu - Parsippany NJ, US
Anastasia Palovsky - Morris Plains NJ, US
William Greenlee - Teaneck NJ, US
Michael Graziano - Scotch Plains NJ, US
Teddy Kosoglou - Jamison NJ, US
Madhu Chintala - Colts Neck NJ, US
Samuel Chackalamannil - Califon NJ, US

International Classification:

A61K 31/443
C07D 405/06

US Classification:

514337000, 546284100

Abstract:

A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. and is represented by the formula for Compound 2: and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.

US Patent:

20090203936, Aug 13, 2009

Filed:

Nov 19, 2008

Appl. No.:

12/274075

Inventors:

Tao Wang - Springfield NJ, US
John S. Chiu - Parsippany NJ, US
Jing Liao - Livingston NJ, US

International Classification:

C07C 51/16

US Classification:

562507

Abstract:

This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising:Where Rand Rare as defined above.