John G Chung

US Patent:

6346617, Feb 12, 2002

Filed:

Jun 16, 1999

Appl. No.:

09/334397

Inventors:

John Y. Chung - Edison NJ
Nobuyoshi Yasuda - Mountainside NJ
Mark S. Jensen - Holmdel NJ
Kenneth M. Wells - Neshanic Station NJ
Chunhua Yang - Edison NJ

Assignee:

Merck Co., Inc. - Rahway NJ

International Classification:

C07D47714

US Classification:

540302

Abstract:

A process for preparation of a compound of formula I: wherein: R represents CH or H; and P represents a protecting group; comprising reacting a compound of formula IV: âwherein R and P and are defined above and R represents triflate or SO F; in the presence of a catalyst and (R ) SnCH OPâ, wherein each R represents C lower alkyl, and Pâ represents H or a protecting group, to yield the compound of formula I.

US Patent:

20030013876, Jan 16, 2003

Filed:

Apr 5, 2002

Appl. No.:

10/117657

Inventors:

John Chung - Edison NJ, US
Roger Farr - Whitehouse Station NJ, US
Guy Humphrey - Hillsborough NJ, US

International Classification:

C07D413/14
C 07D 4 1/02

US Classification:

544/124000, 546/277400

Abstract:

The present invention relates to a process for preparing a compound of gonadotropin releasing hormone antagonists having a Formula I, in an efficient way, which involves preparation of key intermediates: 2-arylindole core; a chiral aziridine, in particular chiral nosyl aziridine; and an amine salt. The key process involves the coupling reaction of 2-arylindole and nosyl aziridine under boron trifluoride catalysis, which provides the final compound with unprecedented regioselectivity and enantioselectivity.

US Patent:

20060199958, Sep 7, 2006

Filed:

Apr 9, 2004

Appl. No.:

10/550640

Inventors:

Raymond Cvetovich - Scotch Plains NJ, US
John Chung - Edison NJ, US
Joseph Amato - Millerton NY, US
Lisa Dimichele - Berkeley Heights NJ, US

International Classification:

C07D 417/02
C07D 413/02
C07D 403/02

US Classification:

544238000, 544333000, 544405000, 546279100, 548200000, 548215000, 548311100, 546148000, 546176000, 548517000, 548518000, 548465000, 548530000, 548305400

Abstract:

A novel process is provided for the preparation of pyrrolidine carboxylic acids, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, sexual dysfunction, male sexual dysfunction, and female sexual dysfunction.

US Patent:

20110165632, Jul 7, 2011

Filed:

May 18, 2009

Appl. No.:

12/993341

Inventors:

Louis-Charles Campeau - VAudreuil-Dorian, CA
John Y. Chung - Edison NJ, US
Danny Gauvreau - Saint-Lazare, CA
Melina Girardin-Rondeau - Jonquiere, CA
Gregory Hughes - Scotch Plains NJ, US
Kevin M. Maloney - Piscataway NJ, US
Christophe Mellon - Saint-Redempteur, CA
Jeffrey C. Moore - Westfield NJ, US
Paul O'Shea - Westmount, CA
Stephane Quellet - Saint Lazare, CA

International Classification:

C12P 17/16
C07D 401/14

US Classification:

435118, 544333

Abstract:

The present invention is directed to processes for preparing a pyridyl piperidine compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.

US Patent:

20120010262, Jan 12, 2012

Filed:

Jan 8, 2010

Appl. No.:

13/144031

Inventors:

John Y.L. Chung - Edison NJ, US
Yanfeng Zhang - Zhejiang, CN
Laura Artino - Oakhurst NJ, US
Jennifer Baxter - Morris Plains NJ, US
Aaron S. Cote - West Windsor NJ, US
Donal Desmond - Waterford City, IE
Jeremy Scott - Hertford, GB
Yekaterina Vaynshteyn - Woodbridge NJ, US

International Classification:

A61K 31/404
A61P 3/10
C07D 209/20

US Classification:

514415, 548511

Abstract:

The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.

US Patent:

20120053350, Mar 1, 2012

Filed:

Apr 26, 2010

Appl. No.:

13/266871

Inventors:

Ian Mangion - Cranford NJ, US
Mark A. Huffman - Warren NJ, US
Rebecca T. Ruck - Jersey City NJ, US
Joseph Lynch - Plainfield NJ, US
John Y.L. Chung - Edison NJ, US
Benjamin Marcune - Raritan NJ, US

International Classification:

C07D 471/08
C07D 401/12
C07D 211/60

US Classification:

546121, 546242, 546208, 546188

Abstract:

A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein Pis an amine protective group; k is 0, 1, or 2; and R, R, R, and Rare defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (R)S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.

US Patent:

60808543, Jun 27, 2000

Filed:

Jul 27, 1998

Appl. No.:

9/129206

Inventors:

John Y. Chung - Edison NJ
Nobuyoshi Yasuda - Mountainside NJ
Johnnie L. Leazer - Metuchen NJ

Assignee:

Merck & Co., Inc. - Rahway NJ

International Classification:

C07D20508

US Classification:

540200

Abstract:

A process of synthesizing a compound of formula I is described: ##STR1## wherein P and P' independently represent H or a protecting group, R. sub. 1 represents H or C. sub. 1-4 alkyl, and Hal represents a halogen characterized by reacting a compound of formula 2: ##STR2## with R. sub. 2 OH, wherein R. sub. 2 is C. sub. 1-4 alkyl, C. sub. 6-10 aryl or C. sub. 5-10 heteroaryl in the presence of an acid catalyst or carbodiimide reagent to produce a compound of formula 3: ##STR3## and reacting a compound of formula 3 in the presence of a base and a haloalkylating agent to produce a compound of formula 1.

US Patent:

20210122717, Apr 29, 2021

Filed:

Apr 18, 2019

Appl. No.:

17/048833

Inventors:

- Rahway NJ, US
- Werthenstein, CH
John Y.L. Chung - Edison NJ, US
Richard Desmond - Lebanon NJ, US
Michael James Di Maso - Hamilton NJ, US
Guy R. Humphrey - Hillsborough NJ, US
Alfred Y. Lee - Robbinsville NJ, US
Dan Lehnherr - Garwood NJ, US
Feng Peng - Dayton NJ, US
Hong Ren - Green Brook NJ, US
Mark Weisel - Stewartsville NJ, US
Siwei Zhang - Westfield NJ, US
Patrick Larpent - Luzern, CH

Assignee:

Merck Sharp & Dohme Corp. - Rahway NJ
Werthenstein BioPharma GmbH - Werthenstein

International Classification:

C07D 239/48
C07D 487/18
C07C 41/09
C07C 41/30
C07C 253/30

Abstract:

Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.