Rti International
Director, Materials Chemistry
Discovery Innovations Mar 2012 - Dec 2014
Principal and Co-Founder
Scynexis, Inc. Oct 2003 - Jan 2012
Senior Research Scientist
University of Vermont Jun 2001 - Sep 2003
Post-Doc
Education:
University of Orleans - France 1996 - 2001
Doctorates, Doctor of Philosophy, Chemistry
University Hassan Ii - Morocco 1995 - 1996
Master of Science, Masters, Chemistry, Organic Chemistry
Skills:
Medicinal Chemistry Drug Design Drug Discovery Organic Chemistry Synthetic Chemistry Lead Optimization R&D Pharmacokinetics Organic Synthesis Heterocyclic Chemistry Drug Metabolism Chemistry Cross Functional Team Leadership Natural Products Matrix Management Supervisory Experience Mentoring Adme Pharmaceutical Industry Lead Change Biotechnology Drug Development Purification Synthetic Organic Chemistry Clinical Development Small Molecules
Mar 2012 to 2000 PRINCIPAL & CO-FOUNDERSCYNEXIS, Inc Durham, NC Oct 2003 to Jan 2012 Senior Research Scientist
Education:
University of Vermont Burlington, VT 2001 to 2003 doctoralUniversity of Orlans 1996 to 2001 Ph.D. in ChemistryUniversity Hassan II 1995 to 1996 MSc in Chemistry
Michele L. R. Heffernan - Worcester MA, US Robert J. Foglesong - Durham NC, US Seth C. Hopkins - Clinton MA, US Mustapha Soukri - Raleigh NC, US Steven W. Jones - Milford MA, US Kerry L. Spear - Concord MA, US Mark A. Varney - Laguna Niguel CA, US
This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure:.
Michele L. R. Heffernan - Worcester MA, US Qun Kevin Fang - Wellesley MA, US Robert J. Foglesong - Durham NC, US Seth C. Hopkins - Clinton MA, US Cyprian O. Ogbu - Durham NC, US Mustapha Soukri - Raleigh NC, US Kerry L. Spear - Concord MA, US
Assignee:
Sepracor, Inc. - Marlborough MA
International Classification:
A61K 31/403 C07D 209/02
US Classification:
514423, 548531
Abstract:
The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e. g. , schizophrenia) and for the treatment or prevention of pain and ataxia.
James Dorsey - Durham NC, US Michele Heffernan - Worcester MA, US Qun Fang - Wellesley MA, US Robert Foglesong - Durham NC, US Seth Hopkins - Clinton MA, US Cyprian Ogbu - Durham NC, US Mustapha Soukri - Raleigh NC, US Kerry Spear - Concord MA, US
Assignee:
SEPRACOR INC. - Marlborough MA
International Classification:
A61K 31/407
US Classification:
514412000
Abstract:
This invention provides fused heterocycles having the formula: in which Ris a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H, C-Csubstituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from OH and OX, in which X is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.
Fused Heterocyclic Inhibitors Of D-Amino Acid Oxidase
Michele Heffernan - Worcester MA, US James Dorsey - Durham NC, US Qun Fang - Wellesley MA, US Robert Foglesong - Durham NC, US Seth Hopkins - Clinton MA, US Michael Jones - Chapel Hill NC, US Steven Jones - Milford MA, US Cyprian Ogbu - Durham NC, US Joe Perales - Durham NC, US Mustapha Soukri - Raleigh NC, US Kerry Spear - Concord MA, US Mark Varney - Laguna Niguel CA, US
This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. Also provided are methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein Q is a member selected from O, S, CRand N, X and Y are members independently selected from CR, O, S, N and NR.
Michele L. R. Heffernan - Worcester MA, US Qun Kevin Fang - Wellesley MA, US Robert J. Foglesong - Durham NC, US Seth C. Hopkins - Clinton MA, US Cyprian O. Ogbu - Durham NC, US Mustapha Soukri - Raleigh NC, US Kerry L. Spear - Concord MA, US
The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.
James M. Dorsey - Durham NC, US Michele L. R. Heffernan - Worcester MA, US Qun Kevin Fang - Wellesley MA, US Robert J. Foglesong - Durham NC, US Seth C. Hopkins - Clinton MA, US Cyprian O. Ogbu - Durham NC, US Mustapha Soukri - Raleigh NC, US Kerry L. Spear - Concord MA, US
Assignee:
Sepracor Inc. - Marlborough MA
International Classification:
A61K 31/407 A61P 29/00
US Classification:
514412
Abstract:
This invention provides fused heterocycles having the formula:in which Ris a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H, C-Csubstituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from OH and OX, in which X is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula:in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.
James M. Dorsey - Durham NC, US Michele L. R. Heffernan - Worcester MA, US Qun Kevin Fang - Wellesley MA, US Robert J. Foglesong - Durham NC, US Seth C. Hopkins - Clinton MA, US Cyprian O. Ogbu - Durham NC, US Mustapha Soukri - Raleigh NC, US Kerry L. Spear - Concord MA, US
Assignee:
Sepracor Inc. - Marlborough MA
International Classification:
A61K 31/407 A61P 25/00
US Classification:
514412
Abstract:
This invention provides methods of improving cognitive function by administering to a subject a therapeutically effective amount of a fused heterocycle having the formula:in which Ris a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H, C-Csubstituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from OH and OX, in which X is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula:in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.
Prodrugs Of Fused Heterocyclic Inhibitors Of D-Amino Acid Oxidase
Michele L. R. Heffernan - Worcester MA, US Richard Dennis - Garner NC, US James M. Dorsey - Durham NC, US Robert J. Foglesong - Durham NC, US Michael L. Jones - Chapel Hill NC, US Cyprian O. Ogbu - Durham NC, US Mustapha Soukri - Raleigh NC, US Kerry L. Spear - Concord MA, US H. Scott Wilkinson - Westborough MA, US Michael Anthony Orsini - Leominster MA, US
The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective.
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