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For Excellence in Organic Chemistry

Howard P. Sard

Vice President of Organix, Inc.

Education

Institution

Degree

Year Conferred

Field of Study

Tufts University, Medford MA

BS

1978

Chemistry, Russian

Massachusetts Institute of Technology

PhD

1982

Organic Chemistry

Sisa Institute for Research

Post-doctoral

1982-83

Organic Chemistry

Research and Professional Experience

1986-Co-founder, Vice-President and member of the Board of Directors of Organix Inc., a Massachusetts Research and Development Company,

1983-1986  SISA Inc., Cambridge, MA. Group Leader in Chemistry.

1982-1983  Research Associate, The SISA Institute for Research, Cambridge, MA.

1979-1982  Graduate Research, Massachusetts Institute of Technology, Cambridge MA.

1978-1979  Teaching Assistant, Massachusetts Institute of Technology, Cambridge MA.

1977-1978  Undergraduate Research, Tufts University, Medford MA.

Professional Activities

1978-  Member, American Chemical Society.

Publications

1. "(Trimethylsilyl)vinylketene, a stable vinylketene and reactive enophile in 4+2 cycloadditions," R. Danheiser and H. Sard, J. Org. Chem., 45, 4810, 1980.

2. "Cyclohexenol annulation via the alkoxy-accelerated rearrangement of vinylcyclobutanes," R. Danheiser, C. Martinez-Davila and H. Sard, Tetrahedron, 37, 3943, 1981.

3. "A 4+4 annulation approach to eight-membered carbocyclic compounds," R. Danheiser, S. Gee and H. Sard, J. Am. Chem. Soc., 104, 7670, 1982.

4. "The regiochemical course of 2+2 cycloadditions of dichloroketene with vinyl- and alkynylsilanes," R. Danheiser and H. Sard, Tet. Letters, 23, 1983.

5. "A novel route to 1-(N,N-dimethylamino)-2-butanol," H. Sard, R. Duffley and R. Razdan, Syn. Comm.,13, 813, 1983.

6. "Improved procedure for the preparation of chiral 1,2-epoxybutanes: Total Synthesis of (S)-3'-hydroxy-delta-9-tetrahydrocannabinol (THC), a highly active metabolite of delta-9-THC", H. Sard, R. Duffley, L. Robertson, and R. Razdan, Synthesis, 506, 1984.

7. "The reaction between an azomethine and malonyl dichloride," H. Sard, P. Meltzer and R. Razdan, J. Het. Chem. 22, 257, 1985.

8. "Ring closure of thiosemicarbazides with sulfuric acid-A structure correction," H. Sard, P. Meltzer and R. Razdan, J. Het. Chem., 22, 361, 1985.

9. "Synthesis and Pharmacological Evaluation of Mercapto and Thioacetyl Analogs of Cannabidiol and delta-8-Tetrahydrocannabinol," D. Compton, P. Little, B. Martin, J. Saha, J. Gilman, H. Sard, and R. Razdan, Eur. J. Med. Chem., 24, 293, 1989.

10. "Synthesis and Pharmacological Evaluation of Amino, Azido, and Nitrogen Mustard Analogues of 10-Substituted Cannabidiol and 11- or 12-Substituted delta-8- Tetrahydrocannabinol," D. Compton, P. Little, B. Martin, J. Saha, J. Gilman, V. Jorapur, H. Sard, and R. Razdan, J. Med. Chem., 33, 1437, 1990.

11. "An Unexpected Product During Synthesis of 3-Phenylisoquinoline: Improved Preparation of 4-Hydroxy-3-phenylisoquinoline" H. Sard, J. Het. Chem. 31, 1085, 1994.

12. "Synthesis and Antiviral Activity of the Cyclopropano Homolog of 2,3-Didehydro- 2,3-dideoxythymidine" H. Sard, Nucleosides and Nucleotides 13, 2321, 1994.

13. "The Synthesis and Pharmacological Evaluation of the Cannabinoid Antagonist SR 141716" A. Dutta, H. Sard, W. Ryan, R. Razdan, D. Compton, and B. Martin, Med. Chem. Res. 5, 54, 1994.

14. "Cyclization of 3-Fluorophenol and 3,3-Dimethylacrylic acid: A Structure Correction" F. Shawcross and H. Sard J. Het. Chem., 32, 1393, 1995.

15. "Preparation of 4,5-Disubstituted Pyrimidines: Ring Substitution of 5-Mesyloxymethylpyrimidines" H. Sard, M. Gonzalez, A. Mahdevan, and J. McKew J. Org. Chem. 65, 9261, 2000.

16. "A General Method for C3 Reductive Alkylation of Indoles" A. Mahadevan, H. Sard, M. Gonzalez, and J. McKew Tetrahedron Letters 44, 4589, 2003.

17. "SAR of Psilocybin Analogs: Discovery of a Selective 5-HT2C Agonist" H. Sard, G. Kumaran, C. Morency, B. Roth, B. Toth, P. He, and L. Shuster Bioorg. Med. Chem. Lett. 15, 4555, 2005.

18. "Inhibition of Cytosolic Phospholipase A2a: Hit to Lead Optimization" J. McKew, M. Foley, P. Thakker, M. Behnke, F. Lovering, F.-W. Sum, S. Tam, K. Wu, M. Shen, W. Zhang, M. Gonzalez, S. Liu, A. Mahadevan, H. Sard, S. Khor, J. Clark J. Med. Chem. 49, 135, 2006.

Books

1. Contributor to "Encyclopedia of Reagents for Organic Synthesis", L. Paquette, Editor, John Wiley and Sons, Ltd., Sussex, UK, 1995.

Patents

1. "Use of Spiperone Derivatives as Immunosuppressant Agents," R. Sharpe, K. Arndt, S. Galli, P. Meltzer, R. Razdan, and H. Sard, U. S. Patent No. 5,574,041 (1996).

2. "Buspirone as a Systemic Immunosuppressant," R. Sharpe, K. Arndt, S. Galli, P. Meltzer, R. Razdan, and H. Sard, U. S. Patent No.5,484,788 (1996).

3. "Use of Spiperone or Spiperone Derivatives as Immunosuppressant Agents," R. Sharpe, K. Arndt, S. Galli, P. Meltzer, R. Razdan, and H. Sard, U. S. Patent No. 5,693,645 (1997).

4. "Topical Application of Spiperone or Derivatives Thereof for Treatment of Pathological Conditions Associated with Immune Responses" R. Sharpe, K. Arndt, S. Galli, P. Meltzer, R. Razdan, and H. Sard, U. S. Patent No. 5,703,088 (1997).

5. "Indole Compounds Useful as Serotonin Selective Agents" H. Sard, L. Shuster, B. Roth, C. Morency, G. Kumaran, L. Xu, U.S. Patent Application No. 11/237,318; International Patent Application No. PCT/US05/34413, filed September 27, 2005.

 

6. "Indole Compounds and Methods of Use Thereof" H. Sard, Y. Zhang, J. Li,  L. Shuster, B. Roth, U.S. Patent Application No. 61/027825; filed February 11, 2008.

 

7.  "Irinotecan Immunoassay" S. Salamone, J. Courtney, A. Volkov, H. Zhang, H. Sard,

V. Hegde, U.S. Patent Application No. 2011/0136253; filed June 9, 2011.

 

8.  "Compounds and Methods of Use Thereof" A. Elder, G. Harriman, S. Leit, J. Li, H.

Sard, Y. Zhang, D. Wilson, U.S. Patent Application No. 2011/0144090; filed June 16,

2011.

 

9.  "Risperidone Immunoassay" S. Salamone, J. Courtney, D. Cline, H. Sard, V. Hegde,

U.S. 8,088,594, issued January 3, 2012.

 

10.  "Lenalidomide and Thalidomide Immunoassays" S. Salamone, J. Courtney, A.

Volkov, H. Sard, V. Hegde, U.S. 8,114,621, issued February 14, 2012.

 

11.  "Lenalidomide and Thalidomide Immunoassays" S. Salamone, J. Courtney, A.

Volkov, H. Sard, V. Hegde, U.S. 8,293,492, issued October 23, 2012.

 

12. "Gemcitabine Immunoassay" S. Salamone, J. Courtney, H. Sard, Spedaliere, C. U.S.

Patent Application No. 2012/0301901; filed November 29, 2012.

 

13. "Carriers for Improved Drug Delivery" WO/2013/172967, M. Amere, H. Sard, L.

Hales, T. Soliman; published November 23, 2013.

 

14. "Melatonin Monoclonal Antibody, Detection, Methods and Uses Thereof" J.

Peterson, D. Li, X. Liu, M.-Y. Chou, H. Sard, WO/2014/144725; filed March 14, 2014.

 

15. "Vitamin D-Ghrelin Conjugates" T. Soliman, L. Hales, H. Sard, M. Amere, U.S. 9,173,950, issued November 3, 2015.

 

Grants

 

R43-MH63529, Indole Analogs as Novel Treatments for OCD

SBIR Phase One 3/2002-9/2002

Howard Sard, Principal Investigator.

Synthesis, binding, and in vivo evaluation of novel indole derivatives as potential therapies for Obsessive Compulsive Disorder.

 

R43-DK065322, Indole Analogs as Novel Appetite Suppressants

SBIR Phase One 9/2003-8/2005

Howard Sard, Principal Investigator.

Synthesis, binding, and in vivo evaluation of novel indole derivatives as potential appetite suppressants.

 

R44-MH63529, Indole Analogs as Novel Treatments for OCD

SBIR Phase Two 4/2006-3/2009

Howard Sard, Principal Investigator.

Synthesis, binding, and in vivo evaluation of novel indole derivatives as potential therapies for Obsessive Compulsive Disorder.

 

R44-DK065322, Indole Analogs as Novel Appetite Suppressants

SBIR Phase Two 9/2007-9/2009

Howard Sard, Principal Investigator.

Synthesis, binding, and in vivo evaluation of novel indole derivatives as potential appetite suppressants.

 

R43-MH095315, Benzodiazepine Analogs as Novel Treatments for Catatonia

SBIR Phase One 9/2011-8/2013

Howard Sard, Principal Investigator.

Synthesis, binding, and in vivo evaluation of novel benzodiazepine derivatives as potential treatments for catatonia

 

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