Richard Storer - Folkestone, GB Adel Moussa - Burlington MA, US Jingyang Wang - Acton MA, US Narayan Chaudhuri - Acton MA, US Steven Mathieu - Salem NH, US Alistair Stewart - Somerville MA, US
An improved process for the preparation of 2′-modified nucleosides and 2′-deoxy-nucleosides, such as, β-L-2′-deoxy-thymidine (LdT), is provided. In particular, the improved process is directed to the synthesis of a 2′-deoxynucleoside that may utilize different starting materials but that proceeds via a chloro-sugar intermediate or via a 2,2′-anhydro-1-furanosyl-nucleobase intermediate. Where an 2,2′-anhydro--furanosyl base intermediate is utilized, a reducing agent, such as Red-Al, and a sequestering agent, such as 15-crown-5 ether, that cause an intramolecular displacement reaction and formation of the desired nucleoside product in good yields are employed. An alternative process of the present invention utilizes a 2,2′-anhydro-1-furanosyl base intermediate without a sequestering agent to afford 2′-deoxynucleosides in good yields. The compounds made according to the present invention may be used as intermediates in the preparation of other nucleoside analogues, or may be used directly as antiviral and/or antineoplastic agents.
Process For The Production Of 3'-Nucleoside Prodrugs
Richard Storer - Folkestone, GB Adel Moussa - Burlington MA, US Steven Mathieu - Salem NH, US
International Classification:
C07H019/067 C07H019/073
US Classification:
536/027100, 536/028500, 536/028400
Abstract:
Provided is a single-step process for the selective 3′-acylation of a ribofuranosyl 2′ or 3′-branched nucleoside. These compounds are useful as antiviral agents, and in particular, can be used to treat Flaviviridae infections in a host in need thereof.
- Cambridge MA, US - Boston MA, US Steven L. MATHIEU - Somerville MA, US Yukari Y. PERRELLA - Cambridge MA, US Vincent DARMENCY - Bougy Villars, CH Hrvoje LUSIC - Boston MA, US Kevin J. HODGETTS - Framingham MA, US
The present invention relates to 2-amino-4-arylpyrimidine and 2-amino-4-aryltriazine compounds as inhibitors of heat shock protein 90 family of chaperone proteins. The invention also features pharmaceutical compositions and kits that include the compounds and compositions of the invention. The invention further relates to the medical use of these compounds and compositions for the treatment of a disorder hi a subject. For example, the disorder is a neurodegenerative disease.
Salt Form Of A Human Histone Methyltransferase Ezh2 Inhibitor
- Cambridge MA, US - Tokyo, JP Hyeong Wook CHOI - Andover MA, US Kristen SANDERS - Gilmanton NH, US Steven MATHIEU - Andover MA, US Arani CHANDA - Malden MA, US Francis FANG - Andover MA, US
International Classification:
A61K 31/5377 C07D 405/12
Abstract:
Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.
- Cambridge MA, US - Tokyo, JP Steven MATHIEU - Andover MA, US Kristen SANDERS - Gilmanton NH, US Arani CHANDA - Malden MA, US
International Classification:
C07D 405/12 A61K 31/5377 C07D 413/12
Abstract:
Provided herein are novel solid forms of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrochloride, and related compositions and methods.
- Cambridge MA, US - Boston MA, US Kevin J. HODGETTS - Framingham MA, US Steven L. MATHIEU - Somerville MA, US Yukari Y. PERRELLA - Cambridge MA, US Vincent DARMENCY - Bougy Villars, CH Hrvoje LUSIC - Boston MA, US
The present invention relates to 2-amino-4-arylpyrimidine and 2-amino-4-aryltriazine compounds as inhibitors of heat shock protein 90 family of chaperone proteins. The invention also features pharmaceutical compositions and kits that include the compounds and compositions of the invention. The invention further relates to the medical use of these compounds and compositions for the treatment of a disorder in a subject. For example, the disorder is a neurodegenerative disease.
Salt Form Of A Human Histone Methyltransferase Ezh2 Inhibitor
- Cambridge MA, US - Tokyo, JP Hyeong Wook CHOI - Andover MA, US Kristen SANDERS - Gilmanton NH, US Steven MATHIEU - Andover MA, US Arani CHANDA - Malden MA, US Francis FANG - Andover MA, US
International Classification:
A61K 31/5377 C07D 405/12
Abstract:
Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.
- Cambridge MA, US - Tokyo, JP Steven MATHIEU - Andover MA, US Kristen SANDERS - Gilmanton NH, US Arani CHANDA - Malden MA, US
Assignee:
Epizyme, Inc. - Cambridge MA Eisai R&D Management Co., Ltd. - Tokyo
International Classification:
C07D 405/12 A61K 31/5377 C07D 413/12
Abstract:
Provided herein are novel solid forms of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrochloride, and related compositions and methods.
Wave Life Sciences Jun 2014 - Feb 2020
Associate Scientist
Yuma Therapeutics Dec 2012 - May 2014
Scientist I
Ensemble Therapeutics Corporation Jul 2007 - Sep 2012
Senior Associate Scientist
Northeastern University Jul 2006 - Jul 2008
Research Assistant
Northeastern University Sep 2004 - Apr 2005
Undergraduate Laboratory Assistant
Education:
Northeastern University 2014 - 2014
Bachelors, Bachelor of Science
Northeastern University 2004 - 2008
Bachelors, Bachelor of Science, Chemistry
Skills:
Drug Discovery Chemistry Purification Hplc Organic Synthesis Lc Ms Dna Conjugation Biochemistry Dna Purification Biotechnology Uv/Vis Assay Development Dna Conjugation Inventory Management Drug Design Nmr Mass Spectrometry Chromatography Sds Page Medicinal Chemistry Laboratory
Biogen
Scientist Ii - Chemical Process Development
Biogen Aug 2018 - May 2019
Contract Scientist I - Chemical Process Development
Eisai Dec 1, 2013 - Aug 2018
Senior Principal Researcher - Integrated Chemistry Group
Eisai May 2011 - Dec 2013
Senior Principal Researcher- Process Research
Eisai Jul 2007 - May 2011
Principal Researcher - Process Research
Education:
University of New Hampshire 1996 - 2003
Master of Science, Masters, Chemistry
Saint Anselm College 1992 - 1996
Bachelors, Bachelor of Arts, Chemistry
Skills:
Chemistry Organic Synthesis Process Research Organic Chemistry Lc Ms Chromatography Nmr Mass Spectrometry Drug Discovery Hplc Medicinal Chemistry Uv/Vis Analytical Chemistry Pharmaceutical Industry Drug Design Lead Change Purification Gmp Good Laboratory Practice Standard Operating Procedure Research and Development Research Liquid Chromatography Mass Spectrometry Microsoft Office Microsoft Excel Microsoft Word Microsoft Powerpoint Electronic Lab Notebooks Scifinder Large Scale Optimization Chemdraw Isis Draw Xrd Ir Spectroscopy D360 Reaxys Recrystallization Karl Fischer Titration Nuclear Magnetic Resonance Pilot Plant Drug Development Technical Transfers Laboratory Safety
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