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Friday, 30 October 2015

John Y. L. Chung



John Y. L. Chung

†Department of Process Chemistry, §Department of Chemical Process Development & Commercialization,Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, United States
Merck, Whitehouse Station · Department of Process Chemistry
  • Merck
    Department of Process Chemistry
    Whitehouse Station, United States
 
LINKS
https://www.researchgate.net/profile/John_Chung2
†Department of Process Chemistry, §Department of Chemical Process Development & Commercialization,Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, United States
 

CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND

Application number: 20150197490
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.
Type: Application
Filed: March 26, 2015
Issued: July 16, 2015
Assignee: Merck Sharp & Dohme Corp.
Inventors: John Y. L. Chung, Yanfeng Zhang, Aaron S. Cote, Jeremy Scott, Yekaterina Vaynshteyn

Crystalline polymorphic forms of an antidiabetic compound

Patent number: 9012488
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.
Type: Grant
Filed: February 21, 2014
Issued: April 21, 2015
Assignee: Merck Sharp & Dohme Corp.
Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn

PROCESS FOR MAKING BETA 3 AGONISTS AND INTERMEDIATES

Application number: 20150087832
Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
Type: Application
Filed: October 22, 2012
Issued: March 26, 2015
Assignee: MERCK SHARP & DOHME, CORP.
Inventors: John Y.L. Chung, Kevin Campos, Edward Cleator, Robert F. Dunn, Andrew Gibson, R. Scott Hoerrner, Stephen Keen, Dave Liebermann, Zhuqing Liu, Joseph Lynch, Kevine M. Maloney, Feng Xu, Nobuyoshi Yasuda, Naoki Yoshikawa, Yong-Li Zhong

PROCESS FOR MAKING BETA 3 AGONISTS AND INTERMEDIATES

Application number: 20140242645
Abstract: The present invention is directed to a process for preparing a compound of formula I-11 through multiple-step reactions.
Type: Application
Filed: October 22, 2012
Issued: August 28, 2014
Inventors: John Y.L. Chung, Kevin Campos, Edward Cleator, Robert F. Dunn, Andrew Gibson, R Scott Hoerrner, Stephen Keen, Dave Lieberman, Zhuqing Liu, Joseph Lynch, Kevin M. Maloney, Feng Xu, Nobuyoshi Yasuda, Naoki Yoshikawa, Yong-Li Zhong

CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND

Application number: 20140171480
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.
Type: Application
Filed: February 21, 2014
Issued: June 19, 2014
Assignee: Merck Sharp & Dohme Corp.
Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn

Crystalline polymorphic forms of an antidiabetic compound

Patent number: 8697740
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.
Type: Grant
Filed: January 8, 2010
Issued: April 15, 2014
Assignee: Merck Sharp & Dohme Corp.
Inventors: John Y. L. Chung, Yanfeng Zhang, Laura Artino, Jennifer Baxter, Aaron S. Cote, Yekaterina Vaynshteyn, Donal Desmond, Jeremy Scott

PREPARATION OF ALKYL ESTERS OF N-PROTECTED OXO-AZACYCLOALKYLCARBOXYLIC ACIDS

Application number: 20120053350
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 PG1 is an amine protective group; k is 0, 1, or 2; and RU, R1, R2, and R3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (RU)3S(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 ?-lactamase inhibitors.
Type: Application
Filed: April 26, 2010
Issued: March 1, 2012
Inventors: Ian Mangion, Mark A. Huffman, Rebecca T. Ruck, Joseph Lynch, John Y.L. Chung, Benjamin Marcune

CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND

Application number: 20120010262
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.
Type: Application
Filed: January 8, 2010
Issued: January 12, 2012
Inventors: John Y.L. Chung, Yanfeng Zhang, Laura Artino, Jennifer Baxter, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn

Process for the synthesis of gonadotropin releasing hormone antagonists

Patent number: 6620824
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.
Type: Grant
Filed: April 5, 2002
Issued: September 16, 2003
Assignee: Merck & Co., Inc.
Inventors: John Y. L. Chung, Roger N. Farr, Guy R. Humphrey

Process for the synthesis of gonadotropin releasing hormone antagonists

Application number: 20030013876
Abstract: The present invention relates to a process for preparing a compound of gonadotropin releasing hormone antagonists having a Formula I, 1
Type: Application
Filed: April 5, 2002
Issued: January 16, 2003
Inventors: John Y. L. Chung, Roger N. Farr, Guy R. Humphrey

N-(R)-(2-hydroxy-2-pyridine-3-yl-ethyl)-2-(4-nitro-phenyl)-acetamide

Patent number: 5846791
Abstract: Asymmetric bioreduction of a ketone substrate with yeast produces the corresponding (R)-alcohol of structure: ##STR1## a key intermediate in the synthesis of a .beta..sub.
Type: Grant
Filed: June 26, 1997
Issued: December 8, 1998
Assignee: Merck & Co., Inc.
Inventors: Michel M. Chartrain, John Y. L. Chung, Christopher Roberge

Process for N-Boc-N-(R)-2(3-pyridyl)-2-hydroxy-ethyl)-N-2(4-aminophenyl)ethyl amine and 2-(4-aminophenyl)-N-2-(2(R)-hydroxy-2-phyridin-S-yl-ethyl)acetamide

Patent number: 5792871
Abstract: Compound 9 is prepared by a 9-step ##STR1## process in an overall yield of about 35% from 3-acetylpyridine. Compound 10 is prepared by a seven-step ##STR2## process in an overall yield of about 30% from 3-acetyl pyridine. These compounds are key intermediates in the synthesis of Compound 11, an important .beta.-3 agonist useful in the treatment of obesity and diabetes.
Type: Grant
Filed: June 26, 1997
Issued: August 11, 1998
Assignee: Merck & Co., Inc.
Inventors: Michel M. Chartrain, Christopher Roberge, John Y. L. Chung, Dalian Zhao

Pyridyl ethylation of lactam derivatives

Patent number: 5686607
Abstract: The invention is a highly efficient synthesis for making compounds of formula (iv) wherein R is C.sub.1-4 alkyl or benzyl; and R.sup.1, when present, is C.sub.1-4 alkyl, OH, O--C.sub.1-4 alkyl, or S--C.sub.1-4 alkyl; which are useful intermediates for making compounds such as those represented in formula (I).
Type: Grant
Filed: August 29, 1996
Issued: November 11, 1997
Assignee: Merck & Co., Inc.
Inventors: John Y. L. Chung, Dalian Zhao, David J. Mathre

Pyridyl ethylation of lactams

Patent number: 5665882
Abstract: The invention is a highly efficient synthesis for making compounds of formula: ##STR1## wherein n=0, 1, R is C.sub.1-4 alkyl or benzyl; andR.sup.1, when present, is C.sub.1-4 alkyl, OH, O--C.sub.1-4 alkyl or S--C.sub.1-4 alkyl. The process involves silane-mediated conjugation of 4-vinylpyridine to a substituted lactam.
Type: Grant
Filed: August 29, 1996
Issued: September 9, 1997
Assignee: Merck & Co., Inc.
Inventors: John Y. L. Chung, Dalian Zhao, James M. McNamara, David L. Hughes

Peptide analog type-B CCK receptor ligands

Patent number: 5340802
Abstract: Peptide analog type-B CCK receptor ligands or pharmaceutically-acceptable salts thereof, which are useful for treating central nervous system disorders, substance abuse, gastrointestinal disorders, endocrine disorders, eating-related disorders and for the treatment of shock, respiratory and cardiocirculatory insufficiencies.
Type: Grant
Filed: January 29, 1993
Issued: August 23, 1994
Assignee: Abbott Laboratories
Inventors: Kazumi Shiosaki, Alex M. Nadzan, David S. Garvey, Youe-Kong Shue, Mark S. Brodie, Mark W. Holladay, John Y.-L. Chung, Michael D. Tufano, Paul D. May

Aryl thiopyrano[4,3,2-cd]indoles as inhibitors of leukotriene biosynthesis

Patent number: 5314898
Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, psoriasis, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
Type: Grant
Filed: June 29, 1992
Issued: May 24, 1994
Assignees: Merck & Co., Inc., Merck Frosst Canada Inc.
Inventors: John Y. L. Chung, Robert A. Reamer, Yves Girard, Pierre Hamel

Process for preparing fibrinogen receptor antagonists

Patent number: 5312923
Abstract: The invention is a highly efficient synthesis for making compounds of the formula: ##STR1## wherein: R.sup.1 is a six membered saturated or unsaturated heterocyclic ring containing one or two heteroatoms wherein the heteroatoms are N; or NR.sup.6, wherein R.sup.6 is H or C.sub.1-10 alkyl;m is an integer from two to six; andR.sup.4 is aryl, C.sub.1-10 alkyl, or C.sub.4-10 aralkyl.
Type: Grant
Filed: February 16, 1993
Issued: May 17, 1994
Assignee: Merck & Co., Inc.
Inventors: John Y. L. Chung, David L. Hughes, Dalian Zhao

Aza-spirocyclic compounds that enhance cholinergic neurotransmission

Patent number: 5221675
Abstract: Aza-spirocyclic compounds of formula (I) ##STR1## which enhance cortical cholinergic neurotransmission.
Type: Grant
Filed: February 26, 1991
Issued: June 22, 1993
Assignee: Abbott Laboratories
Inventors: John Y. L. Chung, David S. Garvey

Process for preparing fibrinogen receptor antagonists

Patent number: 5206373
Abstract: The invention is a highly efficient synthesis for making compounds of the formula: ##STR1## wherein: R.sup.1 is a six member saturated or unsaturated heterocyclic ring containing one or two heterocyclic atoms wherein the heteroatoms are N; or NR.sup.6, wherein R.sup.6 is H or C.sub.1-10 alkyl;m is an integer from two to six; andR.sup.4 is aryl, C.sub.1-10 alkyl, or C.sub.4-10 aralkyl.
Type: Grant
Filed: February 28, 1992
Issued: April 27, 1993
Assignee: Merck & Co., Inc.
Inventors: John Y. L. Chung, David L. Hughes, Dalian Zhao
//////John Y. L. Chung
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