One Organic Chemist One Day............Honouring Profiles of leading Organic Chemists brought to you by DR ANTHONY MELVIN CRASTO, worlddrugtracker, helping millions, amcrasto@gmail.com, +91 9323115463, India, skype amcrasto64
DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 29Yrs Exp. in the feld of Organic Chemistry,Working for GLENMARK PHARMA at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution
Gary Moore and students win best paper in division at Boston ACS meeting
Gary Moore's lab (GFMooreLab.com)
including students Diana Khusnutdinova, Anna Beiler, Samuel Jacob,
Edward Skibo and Avraham Echeverri were awarded best paper in session at
the recent Boston ACS meeting in the Environmental Chemistry Division.
The presentation was entitled: Running on Sun: Bioinspired Approaches to
Achieving Solar Fuels.
It focused on recent efforts from Moore's
lab to design and synthesize integrated photocathode materials with
applications to solar-to-fuels technologies. The constructs are capable
of using water or carbon dioxide as chemical inputs to yield hydrogen or
reduced forms of carbon as products.
Independent Business Development and Scientific Professional
Dr. Thiruvazhi has several years of scientific and management experience gained during his tenure at Therachem, HepatoChem, Incedis Therapeutics, Abbott Labs, ChemBridge Research Labs (CRL), and GVK BIO.
He has a proven track record of success in managing
collaborations in medicinal chemistry, custom synthesis, and library
synthesis.
t Abbott Labs, his chemistry R&D efforts led to
commercialization of assays for diagnosis of certain nutritional
disorders, and diseases such as CAD, stroke, deep vein thrombosis, dementia, and Alzheimer.
At CRL, he championed a chemistry research department dedicated to support clientsÂ' medicinal chemistry programs.
He also managed and co-chaired a multi-year $100 million ChemBridge-Pfizer file enrichment collaboration.
Starting from HTS results, Dr. Thiruvazhi has delivered high quality leads in internal and external medicinal chemistry collaborations.
Prior to founding Incedis, he was an Associate Director at GVK Biosciences (an Indian Contract Research Organization) where his responsibilities spanned from collaboration management to business development.
Dr. Thiruvazhi received his Ph.D. in synthetic chemistry from SUNY-Albany and was a Postdoctoral fellow at University of Pittsburgh and Research Triangle Institute
Therachem
is an innovative, chemistry-driven global service provider for
pharmaceutical and biopharmaceutical companies. Therachem believes in
quality work and timely deliverance of services.
With high-end standard processes and guidance of technical experts, we
provide comprehensive solutions to support medicinal chemistry research
and chemical process research and development.
Therachem,a world-class research & development facility is located at Jaipur, Rajasthan, India.
Hepatochem is a C-H Activation chemistry technology company helping cleints with
(a) rapid analoging of hits/leads in a single chemical transformation in order to develop SAR or fix potential DMPK liabilities
(b) synthesize metabolites in single step in single digit mg to 100 mg quantities and deliver these in 2-4 weeks.
(c) supplying BMO (Biomimetic Oxidation Kits) for synthesis of
metabolites and Glucuronidation kits that allows to identify reaction
condition that produces glucuronide adduct of a drug compound. The
reaction conditions are derivative of the Koenigs–Knorr reaction
visit our website at www.hepatochem.com
My responsibilities include but is not limited to
- acquisition of new clients, expansion of services to existing clients, helping clients best leverage Hepatochem technology.
- Strategy to expand technology to new service lines and secure funding for the same.
- develop and implement a well-defined sales strategy for increased revenue generation
- acquire new customer and expand services within existing customers
- out reach into North America or specific North American territory(ies)
- market on one or more products or services w/o committing to a full time business development professional
- define and implement marketing strategy
- retain and expand CRO-Client relationships via synthetic chemistry consulting
I
was responsible for a global team of business development professionals
in US, Europe, APAC, and India. Delivered revenues in excess of budget
and beat market growth by delivering 20% growth in drug discovery
services. Built high performing teams in each territory and trained,
motivated, and empowered them to deliver their targets.
Interacted very strongly with Operational Heads and next level leaders
to ensure projects were delivered on time and under budget. Matrix
interactions with Finance & Legal teams, and reporting
responsibilities into the CEO and the executive leadership team.
Incedis
is a San Diego drug discovery services company specializing in
medicinal chemistry. We provide expertise in medicinal chemistry,
synthetic chemistry, and project management to support our clients’
preclinical discovery chemistry efforts. We have seamlessly integrated
U.S. based medicinal chemistry expertise with synthetic chemistry
operations in India and manage these to U.S. standards. This integration
has enabled us to provide unique, cost-effective, high-quality
medicinal chemistry outsourcing solutions to our clients.
At Incedis, we
― strive to understand the needs, requirements, and objectives of our clients’ projects
― focus our efforts to help our clients achieve their project objectives
― take pride in providing value-added services to our clients
Championed
new Chemistry Research Department, managed daily chemistry operations.
Co-chaired Chemical Working Group of multi-year, multinational Global
Pfizer/ChemBridge Collaboration in support of Pfizer's Discovery
Efforts.
Executed external discovery collaborations and internal discovery efforts in kinase inhibitors.
Since my graduation in 1993 from Professor
Block’s group, I have traversed a diverse professional path starting
with postdoc stints at the University of Pittsburgh and Research
Triangle Institute (RTI), to chemistry in diagnostics, to heading a
chemistry research department and managing global chemistry
collaborations, to heading business development for a CRO in India.
In
Professor Block’s group, I was exposed to very exciting and rewarding
chemistry research leading to more discoveries than I could handle. I
thoroughly enjoyed sharing much of my Ph.D. days with all the other
group members, and to date cherish those moments. The famous ‘What’s
New?’ or its variant ‘Anything New?’ asked by Dr. Block daily or even
multiple times in a day still rings in my ears.
Since January 2001, I
have lived in beautiful San Diego with my wife Sujitha and kids Meghna
(15 years) and Naveen (14 years)[as of January 2013]. Interestingly, my
stay in San Diego has been the longest in a city thus far! As part of my
business development responsibilities, Sujitha
Meghna
Naveen
I travel to the East Coast
quite, often visiting Boston, NY and NJ cities, Philadelphia, and the
Research Triangle Park area of NC.
I enjoy reading non-fiction books, am
deeply interested in philosophy, love playing volleyball, and ardently
follow cricket. I would love to be reconnected with Prof. Block’s past
and present students. I can be reached at mthiruvazhi@gmail.com
Abstract: Provided are
compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate
or prodrug thereof that modulate tyrosine kinase activity, compositions
comprising the compounds and methods of their use.
Type:
Grant
Filed:
March 18, 2009
Issued:
August 26, 2014
Assignee:
Chembridge Corporation
Inventors:
Yahua Liu, Alexey Vyacheslavovich Anikin,
Charles Chamchoumis Mikel, Douglas Eric McGrath, Goverdhan Reddy
Vavilala, Jason Conrad Pickens, Aleksander Kadushkin, Luyong Jiang,
Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong
Zhu, Alexander Chucholowski, Zheng Yan, Alisher Khasanov, Christina
Gregor
Abstract: The present
invention is directed to pyridazinone compounds of formula (I) and furan
compounds of formula (II), pharmaceutical compositions of compounds of
formula (I) and (II), kits containing these compounds, methods of
syntheses, and a method of treatment of a proliferative disease in a
subject by administration of a therapeutically effective amount of a
compound of formulae (I) or (II). Both classes of compounds were
identified through screening of a collection of small molecule
libraries.
Type:
Application
Filed:
December 21, 2007
Issued:
May 23, 2013
Inventors:
Hakim Djaballah, Harold E. Varmus, David
Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
Abstract: Provided are
compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate
or prodrug thereof that modulate tyrosine kinase activity, compositions
comprising the compounds and methods of their use.
Type:
Application
Filed:
March 18, 2009
Issued:
February 28, 2013
Inventors:
Yahua Liu, Alexey Vyacheslavovich Anikin,
Charles Chamchoumis Mikel, Douglas Eric McGrath, Goverdhan Reddy
Vavilala, Jason Conrad Pickens, Aleksander Kadushkin, Luyong Jiang,
Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong
Zhu, Alexander Chucholowski, Zheng Yan, Alisher Khasanov, Christina
Gregor
Abstract: Provided are
compounds of the formula (I): or a stereoisomer, tautomer, salt,
hydrate or prodrug thereof that modulate tyrosine kinase activity,
compositions comprising the compounds and methods of their use.
Type:
Grant
Filed:
August 10, 2007
Issued:
November 22, 2011
Assignee:
Chembridge Corporation
Inventors:
Vlad E. Gregor, Yahua Liu, Alexey Anikin,
Danny Peter Claude McGee, Charles Mikel, Douglas Eric McGrath, Goverdhan
Reddy Vavilala, Jason C. Pickens, Alexander Kadushkin, Luyong Jiang,
Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong
Zhu, Alexander Chucholowski, Thomas Webb, Vidyasagar Reddy Gantla,
Zheng Yan
Abstract: The present
invention is directed to pyridazinone compounds of formula (I) and furan
compounds of formula (II), pharmaceutical compositions of compounds of
formula (I) and (II), kits containing these compounds, methods of
syntheses, and a method of treatment of a proliferative disease in a
subject by administration of a therapeutically effective amount of a
compound of formulae (I) or (II). Both classes of compounds were
identified through screening of a collection of small molecule
libraries.
Type:
Application
Filed:
December 21, 2007
Issued:
August 19, 2010
Assignee:
Sloan-Kettering Institute for Cancer Research
Inventors:
Hakim Djaballah, Harold E. Varmus, David
Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
Abstract: Provided are
compounds of the formula (I): or a stereoisomer, tautomer, salt,
hydrate or prodrug thereof that modulate tyrosine kinase activity,
compositions comprising the compounds and methods of their use.
Type:
Application
Filed:
August 10, 2007
Issued:
July 17, 2008
Inventors:
Vlad E. Gregor, Yahua Liu, Alexey Anikin,
Danny Peter Claude McGee, Charles Mikel, Douglas Eric McGrath, Goverdhan
Reddy Vavilala, Jason C. Pickens, Alexander Kadushkin, Luyong Jiang,
Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong
Zhu, Alexander Chucholowski, Thomas Webb, Vidyasagar Reddy Gantla,
Zheng Yan
Spectroscopic, Theoretical, and Electrochemical Studies of 1,2-Dithiins,Richard
S. Glass, John R. Pollard, T. Benjamin Schroeder, Dennis L.
Lichtenberger, Eric Block, Russell Deorazio, Chuangxing Guo, Mohan
Thiruvazhi.Phosphorus, Sulfur Silicon Relat. Elem., 1997, 120 (1), pp 439–440.DOI: 10.1080/10426509708545587
Significant Intramolecular Sulfur-Sulfur Interactions incis- andtrans-2,3-Dimethyl-5,6-dithiabicyclo[2.1.1]hexane,Eric
Block, Richard. Glass, Russell DeOrazio, Dennis L. Lichtenberger, John
R. Pollard, Erin E. Russell, T. Benjamin Schroeder, Mohan Thiruvazhi,
Paul J. Toscano. Synlett, 1997, (SI), pp525-528.DOI: 10.1055/s-1997-6136
Don Bosco Matriculation School- Egmore,Chennai,School was founded in 1959 as ... of Madras,On 1st July 1978 it was upgraded as a Higher Secondary School.
13, Casa Major Road, Egmore, Chennai, Tamil Nadu 600008 044 2819 1274
†Department of Process Chemistry, §Department of Chemical Process Development & Commercialization,Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, United States
†Department of Process Chemistry, §Department of Chemical Process Development & Commercialization,Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, United States
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
Got Young scientist Award in First National Conference on "Recent Advances in Pharmaceutical Biotechnology with emphasis on Biodiversity Conservation"-2012
Sujitha
Meghna
Naveen
.
.
.
