RECENT PATENTS & PUBLICATIONS: Selected from >280 Since 1961

Fabio KM, Guillon CD, Lu S-F, Heindel ND, Brownstein MJ, Lacey CJ, Garippa C, Simon NG. Pharmacokinetics and metabolism of SRX246:A potent and selective vaspressin 1a antagonist. J Pharm Sci. 2013, 102: 2033-2043.

Laskin JD, Heck DE, Lacey CJ, Aponte E, Huang M-T, Heindel ND, Pharmacologically-active vanilloid carbamates, U.S.Patent 8,343,971, issued 31 December 2012

Haddad GL, Young SC, Heindel ND, Bornhop DJ, Flowers RA 2nd,  Back-scattering interferometry:an ultrasensitive method for the unperturbed delection of acetylcholinesterase-inhibitor interactions, Angew Chem Int Ed Engl. 2012 Oct 29;51(44):11126-30

Heindel ND and Rapp RD, The Nineteenth-Century Horse Doctor: A Pennsylvania Dutchman’s Practical Guide to Treating Horses,  Coffeetown Press, Seattle, WA, 2012, ISBN 978-1-60381-121-7

Fabio K, Guillon C, Lacey CJ, Lu S-F, Heindel ND, Ferris C F, Placzek M, Jones G, Brownstein MJ, Simon NG. Synthesis and evaluation of potent and selective human V1a receptor antagonists as potential ligands for PET or SPECT imaging. Bioorg & Med Chem, 2012, 20: 1337-1345.  Doi:10.1016/j.bmc/2011.12.013.

Laskin JD, Fabio K,  Lacey CJ, Young S, Mohanta P, Guillon CD, Heindel ND, Huang M-T, Heck DE, Unique Dual-Action Therapeutics, U. S. Patent Pending, PCT/US2009/005961, Pub. No. US2012/0010168 A1, published January 12, 2012.

Young, SC, Fabio KM, Huang M-T, Saxena J, Harman M P, Guillon CD, Vetrano AM, Heck DE. Flowers RA II, Heindel ND and Laskin JD (2012), Investigation of anticholinergic and non-steroidal anti-inflammatory prodrugs which reduce chemically induced skin inflammation. Journal of Applied Toxicology, 2012, 32: 135-141. doi: 10.1002/jat.1645

Laskin JD, Heck DE, Heindel ND, Dimethyl amino ethyl ether psoralens and methods for their production and use. Issued 6 December 2011, U.S. Patent 8,071,642 (2011)

Young SC, Fabio KM, Guillon C, Mohanta P, Halton TA, Heck DE, Flowers RA, Laskin JD, Heindel ND, Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction, Biorg and Med Chem Lett. 2010, 20:2987-2990. PMID: 20347302 doi:10.1016/j.bmcl.2010.02.102

Shakarjian MP, Heck DE, Gray JP, Sinko PJ, Gordon MK, Casillas RP, Heindel ND, Gerecke DR, Laskin DL, Laskin JD. Mechanisms mediating the vesicant actions of sulfur mustard after cutaneous exposure. Toxicol Sci. 2010, 114(1):5-19. PMID: 19833738

Gordon MK, DeSantis A, Deshmukh M, Lacey CJ, Hahn RA, Beloni J,  Anumolu SS, Schlager JJ, Gallo MA, Gerecke DR, Heindel ND, Svoboda KKH, Babin MC and Sinko PJ, Doxycycline Hydrogels as a Potential Therapy for Ocular Vesicant Injury, Journal of Ocular Pharmacology and Therapeutics, 2010, 5: 407-419.

Fabio K, Guillon CD, Lu S-F, Heindel ND, Miller MJ, Ferris CF, Brownstein MJ, Garripa C, Steiner M, Coccaro E, Damiano E, Koppel GA, Simon NG, Vasopressin Antagonists as Anxiolytics and Antidepressants: Recent Developments. Frontiers in CNS Drug Discovery, 2010, 1, 156-183.

Laskin JD, Heck DE, Huang M-T, Fabio K, Lacey CJ, Young S, Mohanta P, Guillon CD,  Heindel ND,  Preparation of phenyl carbonate derivatives as reversible inhibitors of acetylcholinesterase, PTC Int, Appl. (2010) WO Patent No. 2010051044 A1 20100506. Accession Number 2010:563796; CAN 152:501184

Laskin JD, Black AT, Jan YH, Sinko PJ, Heindel ND, Sunil V, Heck DE, Laskin DL. Oxidants and antioxidants in sulfur mustard-induced injury. Ann N Y Acad Sci., 2010, 1203:92-100. PMID: 20716289

Jeffrey D. Laskin, Diane E. Heck, C. Jeffrey Lacey, Erik Aponte, Mou-Tuan Huang, and Ned D. Heindel,  Vanilloid Carbamates of Pharmacological Utility as Inhibitors of Fatty Acid Amide Hydrolase, Modulators of TRPV1, and Suppressors of Inflammation,  Patent Pending, #RWJ 09-52, September 14, 2009.

Laskin JD, Heindel N, Heck D,  Vetrano AM, Guillon C, DeMatteo P,

Fluorescent Fused-Ring Triazoles that Inhibit Cell Proliferation and Uses Thereof,  U.S.Patent 7,598,238 (2009)

M. P. Shakarjian, D. E. Heck, J. Gray, P. J. Sinko, M. K. Gordon, R.P. Casillas, N. D. Heindel, D. R. Gerecke, D.L. Laskin, and J. D. Laskin, Mechanisms mediating the vesicant actions of sulfur mustard after cutaneous exposure, Tox. Sci. Advanced Access, 108: 15 October 2009, pp 1-43.

N. G. Simon, C. Guillon, K. Fabio,  N. D. Heindel, S.F. Lu, M. Miller, C.F. Ferris, M.J. Brownstein, C. Garripa, G.A. Koppel. Vasopressin antagonists as anxiolytics and antidepressants: recent developments. Recent Patents CNS Drug Discov., 2008, 3:77-93.


Robert F. Bruns, Jr., Christophe D. Guillon,  Ned D. Heindel, Gary A. Koppel, Shifang Lu, Marvin J. Miller, Neal G. Simon,  Preparation of Peptidyl Beta-lactamyl Vasopressin V1a Antagonists, US Patent 7,268,125 (2007).   

C. Guillon, G. Koppel, N. Heindel et al. “Azetidinones as vasopressin V1a antagonists,” Bioorg. & Med. Chem., 15 (2007) 2054-2080.

C. F. Ferris, S-f Lu, T. Messenger, C. D. Guillon, N. Heindel, M. Miller, G. Koeppel, F. R. Bruns, and N. G. Simon, “Orally active vasopressin V1a receptor antagonist, SRX251, selectively blocks aggressive behavior,” Pharmacology, Biochemistry and Behavior, 83 (2006) 169-174.

J. D. Laskin,  C. Martey, N. D. Heindel, M. Whittemore, and D. Heck,    “Fluorescent Tags for Amino Acid and Nucleic Acid Analysis,”    U.S. Patent 7,150,967 (2006)

J. D. Laskin, D. Heck, N. D. Heindel, A. M. Vetrano, C. Guillon, P. DeMatteo, “Fluorescent Fused-Ring Triazoles that Inhibit Cell Proliferation,” U.S. Patent 7,105,511 (2006)

R. F. Bruns, C. Guillon, N. D. Heindel, G. A. Koppel, M. Miller, ‘Beta-Lactamyl Vasopressin Antagonists,”   U.S.Patent 7,119,083 (2006).

N. D. Heindel, Tina Masciangioli, and Eva von Schaper, eds., “Are Chemistry Journals too Expen-sive and Inaccessible?,”  National Academies Press, ISBN 0-309-09590-5, Washington, DC, 2005.

N. D. Heindel, M. A. Portz, Peggy Kane, “Mainstreaming Distance Education at Lehigh University: From Satellite to Online and Still Evolving”  Sloan-C Conference Proceedings, Session 4-2,  Orlando, FL, November 15, 2003

T. M. Mariano, A. M. Vetrano, S. L. Gentile, D. E. Heck, M. S. Whittemore, C. D. Guillon, I. Jabin, R. D. Rapp, N. D. Heindel, and J. D. Laskin, “Cell-Impermeant Pyridinium Derivatives of Psoralens Retain Activity as Inhibitors of Keratinocyte Growth,” Biochemical Pharmacology, 63, 31-39 (2002)

N. D. Heindel, “The Unexpected Book on the Shelf,”  Boltonia, 3, 1-2 (2002).

C. A. Martey, A. M. Vetrano, M. S. Whittemore, T. M. Mariano, S. L. Gentile, D. E. Heck, D. L. Laskin, N. D. Heindel, and J. D. Laskin, “Mechanisms of Growth Inhibition in Keratinocytes by Mercurio-Substituted 4’,5’-Dihydropsopralens,”  Biochemical Pharmacology,  7242, 1-9 (2002)

M.S. Whittemore, N.D. Heindel,  I. Jabin,  C. Guillon,  T. E. McNeel,  R. D. Rapp, D.E. Heck, J.D. Laskin,   “Synthetic approaches to 4,8-dimethyl-5'-(N-pyridiniummethyl)-4',5'-dihydropsoralens and 4,8-dimethyl-5'-(N-aminomethyl)-4',5'-dihydropsoralens,” J. Heterocyclic Chem., 38 (4),  909-916 (2001)

M. S. Whittemore, N. D. Heindel, C. Guillon, T. McNeel, R. D. Rapp, J. Laskin, T. Marino, and D. Heck, “Synthetic Approaches to 4,8-Dimethyl-4’-(N-Pyridiniummethyl)-4’,5’-Dihydropsoralens and their Activity against PAM 212 Keratinocytes,”  Heterocycles, 55, 1081-1093 (2001)

N. D. Heindel, J. D. Laskin, D. E. Heck, R. D. Rapp, M.S. Whittemore, T. E. McNeel, and I. Jabin, “Amino-and Mercurio-Substituted 4’,5’-Dihydropsoralen and Therapeutic Uses Thereof,”  U. S. Patent 6,255,324 (July 3, 2001).

N. D. Heindel, J. D. Laskin, M. Whittemore, T. McNeel, C. Guillon, D. Heck, and R. D. Rapp. “Syntheses and Therapeutic Uses of 4’-Substituted-4’,5’-Dihydropsoralens,”  U. S. Patent 6,177,424 (January 23, 2001)

H. Zeng, N. D. Heindel, P. A. Rea, and G. D. Kruh, “Transport of Folates and Antifolates: Mechanism of MRP3 Mediated Antifolate Resistance,”  PharmSci, 2 (#4), 4146 (2000).