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GREGORY S. HAMILTON, Ph.D.
BIBLIOGRAPHY
Journal publications
1. Sundberg, R.J.; Hamilton, G.S.; Trindle, C. Synthesis and Diels-Alder reactions of N-
carboalkoxy dihydropyridines. Substituent effects on the regiochemistry of reduction of N-
carboalkoxy pyridinium ions. J. Org. Chem. 1986, 51, 3672.
2. Sundberg, R.J.; Hamilton, G.S.; Laurino, J.P. 3-(3-Pyrrolyl)thiopyrrolidones as precursors of
benzo [1,2-b:4,3-b’]dipyrroles. Synthesis of intermediates and analogs related to the
phosphodiesterase inhibitors PDE-I and PDE-II and the antitumor antibiotic CC-1065. J. Org.
Chem. 1988, 53, 976.
3. Zimmerman, S.C.; Van Zyl, C.M.; Hamilton, G.S. Rigid molecular tweezers: preorganized hosts
for electron donor-acceptor complexation in organic solvents. J. Am. Chem. Soc. 1989, 111,
1373.
4. Hamilton, G.S.; Huang, Z.; Patch, R.J.; Guzewska, M.E.; Elliott, R.L.; Borosky, S.A.; Bednar,
D.L.; Ferkany, J.W.; Karbon, E.W. Phosphonoethylphenylalanine derivatives as novel antagonists
of non-NMDA ionotropic glutamate receptors. Bioorg. Med. Chem. Lett. 1992, 2, 1269.
5. Ferkany, J.W.; Hamilton, G.S.; Patch, R.J.; Huang, Z.; Borosky, S.; Bednar, D.; Karbon, E.W.
Pharmacological profile of NPC 17742 [(2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-
phosphonoheptanoic acid], a potent and selective NMDA antagonist. J. Pharmacol. Exp. Ther.
1993, 264, 256.
6. Hamilton, G.S.; Huang, Z.; Patch, R.J.; Narayanan, B.A.; Ferkany, J.W. Enzymatic asymmetric
synthesis of (2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid, a potent
selective and competitive NMDA antagonist. Bioorg. Med. Chem. Lett. 1993, 3, 27.
7. Ferkany, J.W.; Hamilton, G.S.; Patch, R.J.; Huang, Z.; Borosky, S.A.; Bednar, D.L.; Jones,
B.E.; Zubrowski, R.; Willetts, J.; Karbon, E.W. Pharmacology of NPC 17742 [(2R, 4R, 5S)-2-
amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid], a potent selective and competitive
NMDA receptor antagonist. Bioorg. Med. Chem. Lett. 1993, 3, 33.
8. Willetts, J.; Clissold, D.B.; Hartman, T.L.; Brandsgaard, R.R.; Hamilton, G.S.; Ferkany, J.W.
Behavioral pharmacology of NPC 17742, a competitive NMDA antagonist. J. Pharm. Exp. Ther.
1993, 265, 1055.
9. Hamilton, G.S.; Huang, Z.; Yang, X.; Patch, R.J.; Narayanan, B.A.; Ferkany, J.W. Asymmetric
synthesis of a potent and selective competitive NMDA antagonist. J. Org. Chem. 1993, 58, 7263.
10. Hamilton, G.S.; Bednar, D.L.; Borosky, S.A.; Huang, Z.; Zubrowski, R.; Ferkany, J.W.;
Karbon, E.W. Synthesis and glutamate antagonist activity of 4-phosphonoalkyl-
quinoline derivatives: a novel class of non-NMDA antagonist. Bioorg. Med. Chem. Lett. 1994, 4,
2035.
11. Mewshaw, R.E.; Bryant, C.M.; Endemann, G.; Feng, Y.; Madden, K.; Perumattam, J.;
Stanton, L.W.; Yang, X.Y.; Yin, Z.; Venkataramen, B.; Liu, D.Y.; Hamilton, G.S. Fluorenyl alkanoic
1
and benzoic acids as novel inhibitors of cell adhesion processes in leukocytes. J. Med. Chem.
1995, 38, 1650.
12. Endemann, G.; Feng, Y.; Bryant, C.M.; Hamilton, G.S.; Perumattam, J.; Mewshaw, R.E.; Liu,
D.Y. Novel antiinflammatory compounds prevent Mac-1 dependent neutrophil adhesion without
blocking activation induced changes in level or conformation of Mac-1. J. Pharmacol. Exp. Ther.
1996, 276, 5.
13. Steiner, J.P.; Hamilton, G.S.; Ross, D.T.; Valentine, H.L.; Guo, H.; Connolly, M.A.; Liang, S.;
Ramsey, C.; Li, J.; Huang, W.; Howorth, P.; Soni, R.; Fuller, M.; Sauer, H.; Nowotnick, A.C.;
Suzdak, P.D. Neurotrophic immunophilin ligands stimulate structural and functional recovery in
neurodegenerative animal models. Proc. Natl. Acad. Sci. USA 1997, 94, 2019.
14. Steiner, J.P.; Connolly, M.A.; Valentine, H.L.; Hamilton, G.S.; Dawson, T.M.; Hester, L.;
Snyder, S.H. Neurotrophic actions of nonimmunosuppressive analogues of immunosuppressive
drugs FK506, rapamycin and cyclosporin A. Nature Medicine 1997, 3, 421.
15. Hamilton, G.S.; Huang, W.; Connolly, M.A.; Ross, D.T.; Guo, H.; Valentine, H.L.; Suzdak,
P.D.; Steiner, J.P. FKBP12-binding domain analogues of FK506 are potent,
nonimmunosuppressive neurotrophic agents in vitro and promote recovery in a mouse model of
Parkinson’s Disease. Bioorg. Med. Chem. Lett. 1997, 7, 1785.
16. Sauer, H.; Francis, J.; Jiang, H.; Hamilton, G.S.; Steiner, J.P. Systemic treatment with GPI
1046 improves spatial memory and reverses cholinergic neuron atrophy in the medial septal
nucleus of aged mice. Brain Res. 1999, 842, 109.
17. Wu, Y.; Limburg, D.C.; Wilkinson, D.; Hamilton, G.S. 1-Cyanoimidazole as a mild and efficient
electrophilic cyanating agent. Organic Letters, 2000, 2, 795-797.
18. Wu, Y.; Limburg, D.C.; Wilkinson, D.; Vaal, M.J.; Hamilton, G.S. A mild deprotection
procedure for tert-butyl esters and tert-butyl ethers using ZnBr2 in methylene chloride.
Tetrahedron Letters, 2000, 41, 2847-2849.
19. Ross, D.T.; Guo, H.; Howorth, P.; Chen, Y.; Hamilton, G.S.; Steiner, J.P. The small molecule
FKBP ligand GPI 1046 induces partial striatal re-innervation after intranigral 6-hydroxydopamine
lesion in rats. Neurosci. Lett. 2001, 297, 113-116.
20. Emborg, M.E.; Shin, P.; Roitberg, B.; Sramek, J.G.; Chu, Y.; Stebbins, G.T.; Hamilton, G.S.;
Suzdak, P.D.; Steiner, J.P.; Kordower, J.H. Systemic adnistration of the immunophilin ligand GPI
1046 in MPTP-treated monkeys. Exp. Neurol. 2001, 168, 171-182.
21. Zhang, C., Steiner, J. P., Hamilton, G. S., Hicks, T. P., and Poulter, M.O.
Regeneration of dopaminergic function in 6-hydroxydopamine-lesioned rats by
neuroimmunophilin ligand treatment. J. Neurosci. 2001, 21, RC156.
22. Wei, L.; Wu, Y.-Q.; Wilkinson, D.E.; Chen, Y.; Soni, R.; Scott, C.; Ross, D.T.; Guo, H.;
Howorth, P.; Valentine, H.L.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.P.; Hamilton, G.S.
Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl and pipecolyl
amides. Bioorg. Med. Chem. Lett. 2002, 12, 1429-1433.
23. Choi, C.; Li, J.-H.; Vaal, M.; Thomas, C.; Limburg, D.C.; Wu, Y.-Q.; Chen, Y.; Soni, R.; Scott,
C.; Ross, D.T.; Guo, H.; Howorth, P.; Valentine, H.L.; Liang, S.; Spicer, D.; Fuller, M.;
Steiner, J.P.; Hamilton, G.S. Use of parallel synthesis combinatorial libraries for rapid
identification of potent FKBP12 inhibitors. Bioorg. Med. Chem. Lett. 2002, 12, 1421-1428.
2
24. Hamilton, G.S.; Wu, Y.-Q.; Limburg, D.C.; Wilkinson, D.E.; Vaal, M.J.; Li, J.-H.; Thomas, C.;
Huang, W.; Sauer, H.; Ross, D.T.; Soni, R.; Chen, Y.; Guo, H.; Howorth, P.; Valentine, H.L.;
Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.P. Synthesis of N-glyoxyl and pipecoly amides and
thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. J. Med. Chem.
2002, 45. 3549-3557
25. Wu, Y.-Q.; Wilkinson, D.E.; Limburg, D.C.; Li, J.-H.; Sauer, H.; Ross, D.T.; .; Liang, S.;
Spicer, D.; Valentine, H.L.; Fuller, M.; Guo, H.; Howorth, P.; Soni, R.; Chen, Y.; Steiner, J.P.;
Hamilton, G.S. Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. J.
Med. Chem. 2002, 45, 3558-3568.
26. Khan, Z.; Ferrari, G.; Kasper, M.; Tonge, D. A.; Steiner, J. P.; Hamilton, G. S.; Gordon-
Weeks, P. R. The non-immunosuppressive immunophilin ligand GPI-1046 potently stimulates
regenerating axon growth from adult mouse dorsal root ganglia cultured in Matrigel.
Neuroscience 2002, 114, 601-609.
27. Wu, Yong-Qian; Hamilton, Sean K.; Wilkinson, Douglas E.; Hamilton, Gregory S.. Direct
synthesis of guanidines using di(imidazol-1-yl)methanimine. J. Org. Chem. 2002, 67, 7553-
7556.
28. Wu, Yong-Qian; Belyakov, Sergei; Choi, Chi; Limburg, David; Thomas, Bert E., IV; Vaal,
Mark; Wei, Ling; Wilkinson, Douglas E.; Holmes, Agnes; Fuller, Mike; McCormick, Jocelyn;
Connolly, Maureen; Moeller, Tim; Steiner, Joseph; Hamilton, Gregory S. Synthesis and biological
evaluation of non-peptidic cyclophilin ligands. J. Med. Chem. 2003, 46, 1112-1115.
29. Wu, Yong-Qian; Limburg, David C.; Wilkinson, Douglas E.; Hamilton, Gregory S.. Formation
of nitrogen-containing heterocycles using di(imidazole-l-yl)methanimine. J. Het. Chem. 2003,
40, 191-193.
30. Limburg, D.C.; Thomas, B.E.; Li, J.-H.; Fuller, M.; Spicer, D.; Chen, Y.; Guo, H.; Steiner, J.P.;
Hamilton, G.S.; Wu, Y.-Q. “Synthesis and evaluation of chiral bicyclic proline FKBP12 ligands”.
Bioorg. Med. Chem. Lett. 2003, 13, 3867-3870.
31. Wilkinson, D.E.; Thomas, B.E.; Limburg, D.C.; Holmes, A.; Sauer, H.; Ross, D.T.; Soni, R.;
Chen, Y.; Guo, H.; Howorth, P.; Valentine, H.; Spicer, D.; Fuller, M.; Steiner, J.P.; Hamilton, G.S.;
Wu, Y.-Q. “Synthesis, molecular modeling and biological evaluation of aza-proline and aza-
pipecolic derivatives as FKBP12 ligands and their in vivo neuroprotective effects.” Bioorg. Med.
Chem. 2003, 11, 4815-4825.
32. Wei; L.; Steiner, J.P.; Hamilton, G.S.; Wu, Y.-Q. “Synthesis and neurotrophic activity of
nonimmunosuppressant cyclosporine A derivatives.” Bioorg. Med. Chem. Lett. 2004, 14, 4549-
4551.
33. Hamilton, S.; Wilkinson, D.E.; Hamilton, G.S.; Wu, Y.-Q. “Microwave assisted synthesis of
N,N’-diaryl cyanoguanidines.” Org. Lett. 2005, 2429-2431.
34. Caporella, E.; Nath, A.; Slevin, J.; Galey, D.; Hamilton, G.; Williams, L.; Steiner, J.P.;
Haughey, N.J. “The immunophilin ligand GPI1046 protects neurons from the lethal effects of the
HIV-1 proteins gp120 and Tat by modulating endoplasmic reticulum calcium load.” J. Neurochem.
2006, 98, 146-155.
3
Abstracts
1. Zimmerman, S.C.; Hamilton, G.S.; Finney, N.F. Complexation chemistry of a rigid molecular
tweezer. 195th
American Chemical Society National Meeting. 1988.
2. Hamilton, G.S.; Huang, Z.; Patch, R.J. Asymmetric synthesis of NPC 17742: a potent and
selective competitive NMDA antagonist. 202nd
American Chemical Society National Meeting.
1991.
3. Hamilton, G.S.; Huang, Z.; Wu, J.; Borosky, S.A.; Bednar, D.L.; Ferkany, J.W.; Karbon, E.W.
Phosphonoethylphenylalanine derivatives as novel antagonists of non-NMDA ionotropic
glutamate receptors. 204th
American Chemical Society National Meeting. 1992.
4. Karbon, E.W.; Bednar, D.L.; Bailey, M.A.; Borosky, S.A.; Zubrowski, R.A.; Ferkany, J.W.;
Huang, Z.; Hamilton, G.S. 2-Phosphonoethylphenylalanine derivatives as novel antagonists of
kainic acid/AMPA receptors. Soc. Neurosci. Abstr. 613.3, 1992.
5. Perumattam, J.; Hamilton, G.S.; Wu, J.P.; Confer, W.L.; Shao, C.; Hatoum, H.N.;
Venkataramen, B.; Blok, N.; Yang, X.Y.; Lowe, V.C.; Laemont, K.; Endemann, G.; Bryant, C.M.;
Feng, Y. New orally active leukocyte recruitment inhibitors as antiinflammatory agents. 208th
American Chemical Society National Meeting. 1994.
6. Steiner, J.P.; Dawson, T.M.; Connolly, M.A.; Hamilton, G.S.; Suzdak, P.D.; Snyder, S.H.
Neuroimmunophilin ligands are neurotrophic for PC12 cells and sensory neuronal cultures. Soc.
Neurosci. Abstr. 699.4, 1995.
7. Hamilton, G.S.; Huang, W.; Connolly, M.A.; Suzdak, P.D.; Steiner, J.P. FKBP12-binding
domain analogues of immunosuppressive drug FK506 are potent, nonimmunosuppressive
neurotrophic agents in vitro. Soc. Neurosci. Abstr. 297.12, 1996.
8. Steiner, J.P.; Connolly, M.A.; Valentine, H.L.; Hamilton, G.S.; Dawson, T.M.; Hester, L.;
Snyder, S.H.; Nonimmunosuppressive ligands for neuroimmunophilins promote nerve extension
in vitro and in vivo. Soc. Neurosci. Abstr. 297.13, 1996.
9. Ross, D.T.; Valentine, H.L.; Guo, H.; Hamilton, G.S.; Huang, W.; Suzdak, P.D.; Steiner, J.P.
Novel neuroimmunophilin ligands for FKBP12 possess potent neurotrophic activity in the mouse
MPTP model of Parkinson’s Disease. Soc. Neurosci. Abstr. 297.14, 1996.
10. Hamilton, G.S.; Ross, D.T.; Valentine, H.L.; Guo, H.; Connolly, M.A.; Liang, S.; Ramsey, C.;
Li, J.; Huang, W.; Wei, L.; Howorth, P.; Soni, R.; Fuller, M.; Sauer, H.; Nowotnick, A.; Suzdak,
P.D.; Steiner, J.P. Neuroimmunophilins as novel targets for CNS drug discovery. 213th
American
Chemical Society National Meeting. 1997, Abstract MEDI 172.
11. Hamilton, G.S.; Huang, W.; Li, J.; Connolly, M.A.; Ross, D.T.; Guo, H.; Valentine, H.L.;
Steiner, J.P. (N-Glyoxyl)pipecolate esters are potent neurotrophic agents in vitro and promote
recovery in a mouse model of Parkinson’s Disease. 214th
American Chemical Society National
Meeting. 1997, Abstract MEDI 142.
12. Li, J.; Hamilton, G.S.; Huang, W.; Connolly, M.A.; Ross, D.T.; Guo, H.; Valentine, H.L.;
Steiner, J.P. In vitro and in vivo neurotrophic effects of (N-sulfonyl) and (N-carbamoyl) pipecolate
esters. 214th
American Chemical Society National Meeting. 1997, Abstract MEDI 183.
13. Ross, D.T.; Guo, H.; Howorth, P.; Fuller, M.; Nowotnick, A.; Hamilton, G.S.; Suzdak, P.D.;
Steiner, J.P. The novel neuroimmunophilin ligand GPI 1046 stimulates morphological,
biochemical, and behavioral recovery in the rat intranigral 6-OHDA Parkinson’s Disease model.
Soc. Neurosci. Abstr. 677.7, 1997.
4
14. Liang, S.; Valentine, H.L.; Ross, D.T.; Huang, W.; Suzdak, P.D.; Hamilton, G.S.; Steiner, J.P.
Neuroimmunophilin ligands augment serotonin fiber protection following lesions with para-
chloroamphetamine (PCA). Soc. Neurosci. Abstr. 677.10, 1997.
15. Valentine, H.L.; Liang, S.; Suzdak, P.D.; Hamilton, G.S.; Steiner, J.P. The neuroimmunophilin
ligand GPI 1046 stimulates recovery following sciatic nerve injury. Soc. Neurosci. Abstr. 677.9,
1997.
16. Connolly, M.A.; Ramsey, C.; Hamilton, G.S.; Steiner, J.P. GPI 1046 elicits neurite outgrowth
of primary sensory neuronal cultures. Soc. Neurosci. Abstr. 677.13, 1997.
17. Steiner, J.P.; Ross, D.T.; Valentine, H.L.; Liang, S.; Guo, H.; Huang, W.; Suzdak, P.D.;
Hamilton, G.S. The orally active neuroimmunophilin ligand GPI 1046 promotes structural and
functional recovery in the mouse MPTP model of Parkinson’s Disease. Soc. Neurosci. Abstr.
677.6, 1997.
18. Guo, H.; Spicer, D.M.; Howorth, P.; Hamilton, G.S.; Suzdak, P.D.; Steiner, J.P.; Ross, D.T.
The novel small molecule immunophilin ligand GPI 1046 stimulates cholinergic reinnervation of
deafferented hippocampal regions after fimbria-fornix transection. Soc. Neurosci. Abstr. 677.12,
1997.
19. Wu, Y-Q., Wilkinson, D.; Soni, R.; Scott, C.; Ross, D.T.; Guo, H.; Howorth, P.; Chen, Y.;
Valentine, H.; Liang, S.; Spicer, D.; Steiner, J.; Hamilton, G.S. N-Glyoxyl prolyl and pipecolyl
amide FKBP12 ligands: potent neurotrophic agents in an animal model of Parkinson’s Disease.
216th
American Chemical Society National Meeting. 1998, Abstract MEDI 103.
20. Choi, C.; Li, J.-H.; Vaal, M.; Thomas, C.; Limburg, D.; Chen, Y.; Soni, R.; Scott, C.; Ross,
D.T.; Guo, H.; Howorth, P.; Valentine, H.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.; Hamilton,
G.S. Use of parallel synthesis combinatorial libraries for rapid identification of potent FKBP12
inhibitors. 216th
American Chemical Society National Meeting. 1998, Abstract MEDI 157.
21. Wei, L.; Wu, Y.-Q.; Wilkinson, D.; Chen, Y.; Soni, R.; Scott, C.; Ross, D.T.; Guo, H.; Howorth,
P.; Valentine, H.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.; Hamilton, G.S. Solid-phase
synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoyl prolyl and pipecolyl amides. 216th
American Chemical Society National Meeting. 1998, Abstract MEDI 158.
22. Valentine, H.L.; Spicer, D.; Fuller, M.; Hamilton, G.S.; Steiner, J.P. Neuroimmunophilin
ligands promote recovery from the peripheral sensory neuropathy associated with streptozotocin-
induced diabetes. Soc. Neurosi. Abstr. 185.9, 1998.
23. Kordower, J.H.; Emborg, M.E.; Shin, P.; Roitberg, B.; Sramek, J.; Chu, Y.-P.; Hamilton, G.S.;
Suzdak, P.D.; Steiner, J.P. Systemic administration of the immunophilin ligand GPI 1046 in
MPTP-treated monkeys. Soc. Neurosci. Abstr. 324.7, 1998.
24. Structural analysis of the binding of neurotrophic ligands for FK506-binding protein (FKBP).
Holmes, A.F.; Thomas, C.; Wei, L.; Soni, R.; Connolly, M.; Steiner, J.P.; Hamilton, G.S. 217th
American Chemical Society National Meeting, 1999, Abstract MEDI 238.
25. Synthesis of thioester FKBP12 ligands and evaluation of their in vitro and in vivo nerve
regenerative effects. Limburg, D.C.; Vaal, M.J.; Li, J.-H.; Wu, Y.-Q.; Thomas, C.; Sauer, H.; Ross,
D.T.; Soni, R.; Chen, Y.; Guo, H.; Howorth, P.; Valentine, H.; Liang, S.; Spicer, D.; Fuller, M.;
Steiner, J.P.; Hamilton, G.S. 217th
American Chemical Society National Meeting, 1999, Abstract
MEDI 237.
5
26. Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. Wu, Y.-Q.;
Wilkinson, D.; Limburg, D.C.; Li, J.-H.; Sauer, H.; Ross, D.T.; Liang, S.; Spicer, D.; Valentine, H.;
Fuller, M.; Guo, H.; Howorth, P.; Soni, R.; Chen, Y.; Steiner, J.P.; Hamilton, G.S. 218th
American
Chemical Society National Meeting, 1999, Abstract MEDI 69.
27. Thioester FKBP12 ligands: evaluation of their in vitro and in vivo nerve regenerative effects.
Guo, H.; Limburg, D.C.; Vaal, M.J.; Li, J.-H.; Wu, Y.-Q.; Thomas, C.; Sauer, H.; Ross, D.T.; Soni,
R.; Chen, Y.; Howorth, P.; Valentine, H.; Moeller, T.; Spicer, D.; Fuller, M.; Wood, S.; Hamilton,
G.S.; Steiner, J.P. Soc. Neurosci. Abstr. 88.20, 1999.
28. Structural analysis of the binding of neurotrophic ligands for FK506-binding protein (FKBP).
Hamilton, G.S.; Holmes, A.F.; Thomas, C.; Wei, L.; Soni, R.; Connolly, M.; Summers, M.F.;
Steiner, J.P. Soc. Neurosci. Abstr. 88.17, 1999.
29. N-glyoxyl prolyl and pipecolyl amide FKBP12 ligands: potent neurotrophic agents in an animal
model of Parkinson’s Disease. Ross, D.T.; Wu, Y.-Q.; Wilkinson, D.; Soni, R.; Scott, C.; Guo, H.;
Howorth, P.; Chen, Y.; Valentine, H.; Spicer, D.; Hamilton, G.S.; Steiner, J.P. Soc. Neurosci.
Abstr. 88.19, 1999.
30. Neurotrophic ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. Steiner, J.P.;
Wu, Y.-Q.; Wilkinson, D.; Limburg, D.C.; Li, J.-H.; Sauer, H.; Ross, D.T.; Liang, S.; Spicer, D.;
Valentine, H.; Fuller, M.; Howorth, P.; Soni, R.; Chen, Y.; Hamilton, G.S. Soc. Neurosci. Abstr.
88.18, 1999.
31. Protection of optic nerve axons by representatives of different classes of Guilford FKBP
immunophilin ligands. D.T. Ross, H. Guo, Y. Chen, P. Howorth, C. Thomas, A. Holmes, C. Choi,
M. Vaal, W. Huang, Y. Wu, D. Limburg, D. Wilkinson, G.S. Hamilton and J.P Steiner. Soc.
Neurosci. Abstr. 29.18, 2000.
32. FKBP protein distribution in the optic nerve. Y. Chen, H. Guo, P. Howorth, J.P.Steiner, G.S.
Hamilton, P.Suzdak, and D.T. Ross. Soc. Neurosci. Abstr. 29.17, 2000.
33. Structural and biochemical analysis of neurotrophic FKBP ligands. G. S. Hamilton, A. Holmes,
C. Thomas, L. Wei, T. Ho, J. Rothstein, and J. P. Steiner. Soc. Neurosci. Abstr. 216.1, 2000.
34. Synthesis of chiral asymmetric bicyclic proline FKBP12 ligands and in vivo evaluation in
Parkinson’s Disease. D. Limburg, J.-H. Li, D. Ross, D. Spicer, P. Howorth, Y. Chen, H. Guo, J.
Steiner and G. Hamilton. 220th
American Chemical Society National Meeting, 2000, Abstract
MEDI 200.
35. GPI-1046 stimulation of axon growth from embryonic dorsal root ganglia may require non-
neuronal cells. Ferrari, G., Khan, Z., Steiner, J. P., Hamilton, G. S., Gordon-Weeks, P. 31st
Society for Neuroscience Meeting in San Diego, 2001.
36. Regenerative effects of neuroimmunophilin ligands. Steiner, J. P., Wu, Y. and Hamilton, G.
S. Immunophilins in the Brain II mini-symposium Nov. 10, 2001.
37. Synthesis, Molecular Modeling and Biological Evaluation of Aza-proline and Aza-pipecolic
Derivatives as FKBP12 Ligands and their In Vivo Nerve Regenerative Effects Wu, Y.Q.,
Wilkinson, D., Limburg, D., Sauer, H., Ross, D.T., Soni, R., Chen, Y., Guo, H., Howorth, P.,
Valentine, H., Spicer, D., Fuller, M., Steiner, J., Hamilton, G. Presented at the 223rd National
Meeting of the American Chemical Society, April 10-14, 2002 in Orlando, FL
38. Neuroimmunophilin Ligands Protect Against Post Prostaecomy-Induced Erectile Dysfunction.
Steiner, J., Wu, Y. Q., Burnett, A. L., Hamilton, G. S. 5th
International Neurodegeneration in AD,
PD and Related Disorders, June 24-25, 2002, Princeton, NJ.
6
39. Synthesis and biological evaluation of non-peptidic cyclophilin ligands and their in vivo
neuroprotective effects. Wu, Y.-Q.; Belyakov, S.; Choi, Chi; Wilkinson, D.; Limburg, D.; Vaal, M.;
Thomas, B.; Holmes, A.; Chen, Y.; Gio, H.; Howorth, P.; Valentine, H.; Spicer, D.; Fuller, M.;
Steiner, J.; Hamilton, G. S. Presented at the 224th
National Meeting of the American Chemical
Society, August 18-22, 2002 in Boston, MA.
40. Neuroprotective effects of inhibitors of dipeptidyl peptidase-IV in vitro and in vivo. Wu, Y.Q.;
Hamilton, G.S.; Limburg, D.C.; Wilkinson, D.E.; Jackson, P.; Steiner, J.P.; Belyakov, S.A.
Presented at the First International Conference “Dipeptidyl Aminopeptidases: Basic Science and
Clinical Applications” Berlin, September 2002.
41. Structure-based design of potent small molecule cyclophilin ligands. Belyakov, S.A.;
Hamilton, S.; Limburg, D.C.; Thomas, B.; Vaal, M.; Wei, L.; Wilkinson, D.E.; Fuller, M.; Steiner,
J.P.; Hamilton, G.S.; Wu, Y.Q. Presented at the 225th
National Meeting of the American Chemical
Society, March 23-27, 2003 in New Orleans, LA.
42. Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporine A derivatives.
Wei, L.; Hamilton, G.S.; Steiner, J.P.; Wu, Y.Q. Presented at the 225th
National Meeting of the
American Chemical Society, March 23-27, 2003 in New Orleans, LA.
43. Microwave assisted synthesis of aryl cyanoguanidines. Hamilton, S.; Wilkinson, D.E.;
Hamilton, G.S.; Wu, Y.Q. Presented at the 229th
National Meeting of the American Chemical
Society, March 13-17, 2005, in San Diego, CA.
44. Design and synthesis of arylsulfonyl thioureas as novel potent cyclophilin ligands. Serdyuk,
L.E.; Wilkinson, D.E.; Hamilton, S.; Belyakov, S.A.; Wei, L.; Thomas B.E., Hamilton, G.S.;
Massuda, E.; Stathis, M.; Fuller, M.; Rojas, C.; Steiner, J.P.; Huang, S; Liu, G.; and Wu, Y.Q.
Presented at the 230th
National Meeting of the American Chemical Society, August 28, 2005, in
Washington, DC.
45. Design and synthesis of arylsulfonylthiosemicarbazides as potent, nonpeptidic cyclophilin
ligands. Wu, Y.Q.; Wilkinson, D.E.; Hamilton, G.S.; Steiner, J.P.; Hamilton, S.; Thomas B.E.,
Massuda, E.; Fuller, M.; Stathis, M.; and Belyakov, S.A. Presented at the 230th
National Meeting
of the American Chemical Society, August 28, 2005, in Washington, DC.
46. Small molecule inhibitors against mitochondrial permeability transition pore (mPTP). Wu, Y.-
Q.; Wilkinson, D.; Hamilton, S.; Wei, L.; Serdyuk, L.; Fuller, M.; Alt, J.; Steiner, J.P.; Williams, L.;
Rojas, C.; Hamilton, G.S. Presented at the 230th
National Meeting of the American Chemical
Society, August 31, 2005, in Washington, DC.
Reviews and book chapters
Hamilton, G.S.; Steiner, J.P. Neuroimmunophilin ligands as novel therapeutics for the treatment
of degenerative disorders of the nervous system. Curr. Pharm. Design 1997, 3, 405-428.
Snyder, S.H.; Sabatini, D.E.M.; Lai, M.M.; Steiner, J.P.; Hamilton, G.S.; Suzdak, P.D. Neural
actions of immunophilin ligands. Trends Pharm. Sci. 1998, 19, 21-26.
Hamilton, G.S. Emerging therapeutic agents for Parkinson’s Disease. Chem. Ind. 1998, 127-132.
Hamilton, G.S. Immunophilin ligands for the treatment of neurological disorders. Exp. Opin. Ther.
Patents 1998, 8, 1109-1123.
7
Hamilton, G.S.; Steiner, J.P. Immunophilins: Beyond Immunosuppression. J. Med. Chem. 1998,
41, 5119-5143.
Hamilton, G.S.; Thomas, C. Immunophilins: The Next Generation. IN Advances in Med. Chem.
Vol. 5, JAI Press, 2000.
Steiner, J.P.; Valentine, H.; Morrow, T.; Hamilton, G.S. Neuroimmunophilin ligands stimulate
recovery of injured sciatic nerves. IN Immunosuppressants and Neurological Disorders, Ed. by
C.V. Borlongan, Humana Press, 2001.
Steiner, J.P.; Ross, D.T.; Sauer, H.; Morrow, T.; Hamilton, G.S. Effects of neuroimmunophilin
ligands on Parkinson's Disease and cognition. IN Immunosuppressants and Neurological
Disorders, Ed. by C.V. Borlongan, Humana Press, 2001.
Wu, Y.-Q.; Limburg, D.C.; Wilkinson, D.E.; Jackson, P.; Steiner, J.P.; Hamilton, G.S.; Belyakov,
S.A. Neuroprotective effects of inhibitors of dipeptidyl peptidase-IV in vitro and in vivo. IN
Dipeptidyl Aminopeptidases in Health and Disease, Ed. by Hildebrandt et al. Kluwer
Academic/Plenum Publishers, New York, 2003.
Williams, L.; Wu, F.; Hamilton, G. Mitochondrial permeability as a target for neurodegenerative
disorders. Drugs of the Future 2006, 31, 1083-1098.
Hamilton, G.S. Antibody-drug conjugates for cancer therapy: The technological and regulatory
challenges of developing drug-biologic hybrids. Biologicals 2015, in press.
Patents
1. Hamilton, G.S. Excitatory amino acid antagonists. US Patent 5,256,814.
2. Hamilton, G.S. ω-[2-(Tetrazolylalkyl)cyclohexyl]-2-aminoalkanoic acids as antagonists of
excitatory amino acid receptors. US Patent 5,331,001.
3. Hamilton, G.S. Phosphonoalkylquinolin-2-ones as novel antagonists of non-NMDA ionotropic
excitatory amino acid receptors. US Patent 5,342, 946.
4. Hamilton, G.S. ω-[2-Alkylphenyl]-2-aminoalkanoic acids as antagonists of excitatory amino
acid receptors. US Patent 5,364,876.
5. Hamilton, G.S.; Ferkany, J.W.; Rzeszotarki, W.J.; Ellenberger, S.R.; Guzewska, M.E.; Patch,
R.J.; Karbon, E.W. . ω-[2-(Phosphonoalkyl)phenyl]-2-aminoalkanoic acids as antagonists of
excitatory amino acid receptors. US Patent 5,395,827.
6. Hamilton, G.S. ω-[2-(Tetrazolylalkyl)cyclohexyl]-2-aminoalkanoic acids as antagonists of
excitatory amino acid receptors. US Patent 5,426,114.
7. Hamilton, G.S. Phosphonoalkylquinolin-2-ones as novel antagonists of non-NMDA ionotropic
excitatory amino acid receptors. US Patent 5,510,338.
8. Mewshaw, R.E.; Hamilton, G.S. Antiinflammatory benzoic acid derivatives. US Patent
5,530,157.
9. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent
5,614,547.
8
10. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S. Inhibitors of rotamase enzyme activity. US Patent
5,696,135.
11. Hamilton, G.S.; Li, J.-H.; Steiner, J.P. Method of using neurotrophic sulfonamide compounds.
US Patent 5,721,256.
12. Hamilton, G.S.; Li, J.-H. Heterocyclic thioesters. US Patent 5,786,378.
13. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US
Patent 5,795,908.
14. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T. Inhibitors of rotamase enzyme
activity. US Patent 5,798,355.
15. Li, J.-H.; Hamilton, G.S. Heterocyclic esters and amides. US Patent 5,801,187.
16. Steiner, J.P.; Hamilton, G.S. Rotamase enzyme activity inhibitors. US Patent 5,801,197.
17. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T. Inhibitors of rotamase enzyme
activity. US Patent 5,843,960.
18. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxides of heterocyclic esters, amides, thioesters
and ketones. US Patent 5,846,979.
19. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T.M. Inhibitors of rotamase enzyme
activity. US Patent 5,846,981.
20. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US
Patent 5,859,031.
21. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked sulfonamides of heterocyclic thioesters. US
Patent 5,874,449.
22. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked ureas and carbamates of piperidyl thioesters.
US Patent 5,935,989.
23. Steiner, J.P.; Hamilton, G.S. Pyrrolidine carboxylate hair revitalizing agents. US Patent
5,945,441.
24. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked ureas and carbamates of piperidyl thioesters.
US Patent 5,958,949.
25. Hamilton, G.S.; Li, J.-H.; Steiner, J.P. Method of using neurotrophic sulfonamide compounds.
US Patent 5,968,957.
26. Hamilton, G.S.; Li, J.-H. Heterocyclic thioesters and ketones. US Patent 5,990,131.
27. Steiner, J.P.; Hamilton, G.S.; N-linked sulfonamides of heterocyclic thioester hair growth
compounds and uses. US Patent 6,004,993.
28. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T.M. Inhibitors of rotamase enzyme
activity. US Patent 6,022,878.
29. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxides of heterocyclic esters, amides, thioesters,
and ketones. US Patent 6,054,452.
9
30. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked sulfonamides of heterocyclic thioesters. US
Patent 6,121,273.
31. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US
Patent 6,140,357.
32. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxide of heterocyclic ester, amide, thioester, or
ketone hair growth compositions and uses. US Patent 6,172,087.
33. Steiner, J.P.; Hamilton, G.S. Pyrrolidine derivative hair growth compositions and uses. US
Patent 6,177,455.
34. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked ureas and carbamates of heterocyclic thioesters.
US Patent 6,184,243.
35. Steiner, J.P.; Hamilton, G.S. Pipecolic acid derivative hair growth compositions and uses. US
Patent 6,187,784.
36. Steiner, J.P.; Hamilton, G.S. Sulfone hair growth compositions and uses. US Patent
6,187,796.
37. Steiner, J.P.; Hamilton, G.S. N-linked sulfones of heterocyclic thioester hair growth
compositions and uses. US Patent 6,187,806.
38. Steiner, J.P.; Hamilton, G.S. Small molecule pipecolic acid derivative hair growth
compositions and uses. US Patent 6,191,125.
39. Steiner, J.P.; Hamilton, G.S. Small molecule carbamate or urea hair growth compositions
and uses. US Patent 6,194,440.
40. Li, J.-H.; Hamilton, G.S. Heterocyclic esters and amides. US Patent 6,200,972.
41. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Pyrrolidine derivatives for vision and
memory disorders. US Patent 6,218,423.
42. Hamilton, G.S.; Li, J.-H. Heterocyclic ketone and thioester compounds and uses. US Patent
6,218,424.
43. Li, J.-H.; Hamilton, G.S. Heterocyclic esters and amides. US Patent 6,218,544.
44. Hamilton, G.S.; Steiner, J.P. Pyrrolidine carboxylate and pyrrolidine amide hair revitalizing
agents. US Patent 6,239,164.
45. Li, J.-H.; Steiner, J.P.; Hamilton, G.S.; Carbamate and urea compositions and neurotrophic
uses. US Patent 6,242,468.
46. Hamilton, G.S.; Li, J.-H.; Steiner, J.P. Method of using neurotrophic sulfonamide compounds.
US Patent 6,245,783.
47. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxides of heterocyclic esters, amides, thioesters
and ketones. US Patent 6,251,892.
48. Steiner, J.P.; Hamilton, G.S. N-Linked urea or carbamate of heterocyclic thioester hair growth
compositions and uses.US Patent 6,271,244.
10
49. Steiner, J.P.; Hamilton, G.S. Heterocyclic thioester and ketone hair growth compositions and
uses. US Patent 6,274,602.
50. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked ureas and carbamates of heterocyclic
thioesters. US Patent 6,274,607.
51. Steiner, J.P.; Hamilton, G.S. Heterocyclic ester and amide hair growth compositions and
uses. US Patent 6,274,617.
52. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US
Patent 6,291,510.
53. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked sulfonamides of heterocyclic thioesters. US
Patent 6,294,551.
54. Hamilton, G.S.; Norman, M.H.; Wu, Y.-Q. Carboxylic acids and carboxylic acid isosteres of
N-heterocyclic compounds. US Patent 6,331,537.
55. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Small molecule sulfonamides for vision
and memory disorders. US Patent 6,333,340.
56. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Nitrogen-containing linear and azepinyl
compositions and uses for vision and memory disorders. US Patent 6,335,348.
57. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Carboxylic acids and isosteres of
heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders. US
Patent 6,337,340.
58. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. N-linked sulfonamides of N-heterocyclic
carboxylic acids or isosteres for vision and memory disorders. US Patent 6,339,101.
59. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Pipecolic acid derivatives for vision and
memory disorders. US Patent 6,376,517.
60. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Heterocyclic thioesters or ketones for
vision and memory disorders. US Patent 6,384,056.
61. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Small molecule carbamates or ureas for
vision and memory disorders. US Patent 6,395,758.
62. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. N-oxides of heterocyclic ester, amide,
thioester, or ketones for vision and memory disorders. US Patent 6,399,648.
63. Wu, Y.-Q.; Hamilton, G.S.; Huang, W. AZA compounds, pharmaceutical compositions, and
methods of use. US Patent 6,417,189.
64. Hamilton, G.S.; Li, J.-H. Heterocyclic ketone and thioester compounds and uses. US Patent
6,417,209.
65. Steiner, J.P.; Hamilton, G.S. N-oxides of heterocyclic ester, amide, thioester, or ketone hair
growth compositions and uses. US Patent 6,429,215.
66. Steiner, J.P.; Hamilton, G.S.; Snyder, S.H. Methods of using inhibitors of cyclophilin
rotamase activity to affect neurological activity. US Patent 6,444,643.
67. Hamilton, G.S.; Limburg, D.C. Cyclic ester or amide derivatives. US Patent 6,462,072.
11
68. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxides of heterocyclic esters, amides, thioesters,
and ketones. US Patent 6,486,151.
69. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T. Inhibitors of rotamase enzyme
activity. US Patent 6,500,843.
70. Hamilton, G.S.; Steiner, J.P. Pyrrolidine derivatives and processes for preparing same. US
Patent 6,500,959.
71. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. N-linked urea or carbamate of
heterocyclic thioesters for vision and memory disorders. US Patent 6,506,788.
72. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US
Patent 6,509,477.
73. Steiner, J.P.; Hamilton, G.S. Non-peptidic cyclophilin binding compounds and their use. US
Patent 6,593,362.
74. Wu, Y.-Q.; Belyakov, S.; Hamilton, G.S.; Limburg, D.; Steiner, J.P.; Vaal, M.; Wei, L.;
Wilkinson, D. Trisubstituted carbocyclic cyclophilin binding compounds and their use. US Patent
6,656,971.
75. Hamilton, G.S.; Steiner, J.P.; Vaal, M.J.; Choi, C.; Wei, L. Non-peptidic cyclophilin binding
compounds and their use. US Patent 6,677,376.
76. Steiner, J.P.; Hamilton, G.S. Pyrrolidine derivative hair growth compositions and uses. US
Patent 6,943,187.
77. Hamilton, G.S. Hydantoin derivative compounds, pharmaceutical compositions, and methods
of using same. US Patent 6,974,823.
78. Hamilton, G.S.; Li, J.-H. Heterocyclic ketone and thioester compounds and uses. US
6,984,639.
79. Steiner, J.P., Hamilton, G.S. Rotamase enzyme activity inhibitors. US Patent 7,056,935.
80. Hamilton, G.S.; Norman, M.H.; Wu, Y.-Q. N-linked sulfonamides of N-heterocyclic acids or
carboxylic acid isosteres. US Patent 7,078,424.
81. Hamilton, G.S., Leighton, H.J. Compounds having simultaneous ability to block L-type
calcium channels and to inhibit phosphodiesterase type 3 activity. US Patent 7,098,211.
82. Hamilton, G.S.; Norman, M.H.; Wu, Y.-Q. Carboxylic acids and carboxylic acid isosteres of
N-heterocyclic compounds. US Patent 7,153,883.
83. Wu, Y.-Q., Huang, W., Hamilton, G.S. Aza compounds, pharmaceutical compositions and
methods of use. US Patent 7,253,169.
84. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Carboxylic acids and carboxylic acid
isosteres of N-heterocyclic compounds for vision and memory disorders. US Patent 7,265,150.
85. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US
Patent 7,282,510.
12
86. Ross, D.T.; Hamilton, G.S.; Steiner, J.P. Heterocyclic esters or amides for vision and memory
disorders. US Patent 7,338,976.
87. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. N-linked sulfonamide of heterocyclic
thioesters for vision and memory disorders. US Patent 7,410,995.
88. Hamilton, G.S.; Norman, M.H.; Wu, Y.-Q. N-linked sulfonamides of N-heterocyclic acids or
carboxylic acid isosteres. US Patent 7,459,473.
89. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US
Patent 7,652,060.
90. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US
Patent 7,960,570.
91. Hamilton, G.S.; Tsukamoto, T.; Ferraris, D.; Duvall, B.; Lapidus, R. Certain compounds,
compositions and methods. US Patent 8,268,800.
92. Belyakov, S.; Duvall, B.; Ferraris, D.; Hamilton, G.S.; Vaal, M. Compositions and methods for
treating cancer. US Patent 8,329,665.
93. Hamilton, G.S.; Tsukamoto, T.; Ferraris, D.; Duvall, B.; Lapidus, R. Certain compounds,
compositions and methods. US Patent 8,951,987.
13

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G.S. Hamilton Bibliography June 2015

  • 1. GREGORY S. HAMILTON, Ph.D. BIBLIOGRAPHY Journal publications 1. Sundberg, R.J.; Hamilton, G.S.; Trindle, C. Synthesis and Diels-Alder reactions of N- carboalkoxy dihydropyridines. Substituent effects on the regiochemistry of reduction of N- carboalkoxy pyridinium ions. J. Org. Chem. 1986, 51, 3672. 2. Sundberg, R.J.; Hamilton, G.S.; Laurino, J.P. 3-(3-Pyrrolyl)thiopyrrolidones as precursors of benzo [1,2-b:4,3-b’]dipyrroles. Synthesis of intermediates and analogs related to the phosphodiesterase inhibitors PDE-I and PDE-II and the antitumor antibiotic CC-1065. J. Org. Chem. 1988, 53, 976. 3. Zimmerman, S.C.; Van Zyl, C.M.; Hamilton, G.S. Rigid molecular tweezers: preorganized hosts for electron donor-acceptor complexation in organic solvents. J. Am. Chem. Soc. 1989, 111, 1373. 4. Hamilton, G.S.; Huang, Z.; Patch, R.J.; Guzewska, M.E.; Elliott, R.L.; Borosky, S.A.; Bednar, D.L.; Ferkany, J.W.; Karbon, E.W. Phosphonoethylphenylalanine derivatives as novel antagonists of non-NMDA ionotropic glutamate receptors. Bioorg. Med. Chem. Lett. 1992, 2, 1269. 5. Ferkany, J.W.; Hamilton, G.S.; Patch, R.J.; Huang, Z.; Borosky, S.; Bednar, D.; Karbon, E.W. Pharmacological profile of NPC 17742 [(2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7- phosphonoheptanoic acid], a potent and selective NMDA antagonist. J. Pharmacol. Exp. Ther. 1993, 264, 256. 6. Hamilton, G.S.; Huang, Z.; Patch, R.J.; Narayanan, B.A.; Ferkany, J.W. Enzymatic asymmetric synthesis of (2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid, a potent selective and competitive NMDA antagonist. Bioorg. Med. Chem. Lett. 1993, 3, 27. 7. Ferkany, J.W.; Hamilton, G.S.; Patch, R.J.; Huang, Z.; Borosky, S.A.; Bednar, D.L.; Jones, B.E.; Zubrowski, R.; Willetts, J.; Karbon, E.W. Pharmacology of NPC 17742 [(2R, 4R, 5S)-2- amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid], a potent selective and competitive NMDA receptor antagonist. Bioorg. Med. Chem. Lett. 1993, 3, 33. 8. Willetts, J.; Clissold, D.B.; Hartman, T.L.; Brandsgaard, R.R.; Hamilton, G.S.; Ferkany, J.W. Behavioral pharmacology of NPC 17742, a competitive NMDA antagonist. J. Pharm. Exp. Ther. 1993, 265, 1055. 9. Hamilton, G.S.; Huang, Z.; Yang, X.; Patch, R.J.; Narayanan, B.A.; Ferkany, J.W. Asymmetric synthesis of a potent and selective competitive NMDA antagonist. J. Org. Chem. 1993, 58, 7263. 10. Hamilton, G.S.; Bednar, D.L.; Borosky, S.A.; Huang, Z.; Zubrowski, R.; Ferkany, J.W.; Karbon, E.W. Synthesis and glutamate antagonist activity of 4-phosphonoalkyl- quinoline derivatives: a novel class of non-NMDA antagonist. Bioorg. Med. Chem. Lett. 1994, 4, 2035. 11. Mewshaw, R.E.; Bryant, C.M.; Endemann, G.; Feng, Y.; Madden, K.; Perumattam, J.; Stanton, L.W.; Yang, X.Y.; Yin, Z.; Venkataramen, B.; Liu, D.Y.; Hamilton, G.S. Fluorenyl alkanoic 1
  • 2. and benzoic acids as novel inhibitors of cell adhesion processes in leukocytes. J. Med. Chem. 1995, 38, 1650. 12. Endemann, G.; Feng, Y.; Bryant, C.M.; Hamilton, G.S.; Perumattam, J.; Mewshaw, R.E.; Liu, D.Y. Novel antiinflammatory compounds prevent Mac-1 dependent neutrophil adhesion without blocking activation induced changes in level or conformation of Mac-1. J. Pharmacol. Exp. Ther. 1996, 276, 5. 13. Steiner, J.P.; Hamilton, G.S.; Ross, D.T.; Valentine, H.L.; Guo, H.; Connolly, M.A.; Liang, S.; Ramsey, C.; Li, J.; Huang, W.; Howorth, P.; Soni, R.; Fuller, M.; Sauer, H.; Nowotnick, A.C.; Suzdak, P.D. Neurotrophic immunophilin ligands stimulate structural and functional recovery in neurodegenerative animal models. Proc. Natl. Acad. Sci. USA 1997, 94, 2019. 14. Steiner, J.P.; Connolly, M.A.; Valentine, H.L.; Hamilton, G.S.; Dawson, T.M.; Hester, L.; Snyder, S.H. Neurotrophic actions of nonimmunosuppressive analogues of immunosuppressive drugs FK506, rapamycin and cyclosporin A. Nature Medicine 1997, 3, 421. 15. Hamilton, G.S.; Huang, W.; Connolly, M.A.; Ross, D.T.; Guo, H.; Valentine, H.L.; Suzdak, P.D.; Steiner, J.P. FKBP12-binding domain analogues of FK506 are potent, nonimmunosuppressive neurotrophic agents in vitro and promote recovery in a mouse model of Parkinson’s Disease. Bioorg. Med. Chem. Lett. 1997, 7, 1785. 16. Sauer, H.; Francis, J.; Jiang, H.; Hamilton, G.S.; Steiner, J.P. Systemic treatment with GPI 1046 improves spatial memory and reverses cholinergic neuron atrophy in the medial septal nucleus of aged mice. Brain Res. 1999, 842, 109. 17. Wu, Y.; Limburg, D.C.; Wilkinson, D.; Hamilton, G.S. 1-Cyanoimidazole as a mild and efficient electrophilic cyanating agent. Organic Letters, 2000, 2, 795-797. 18. Wu, Y.; Limburg, D.C.; Wilkinson, D.; Vaal, M.J.; Hamilton, G.S. A mild deprotection procedure for tert-butyl esters and tert-butyl ethers using ZnBr2 in methylene chloride. Tetrahedron Letters, 2000, 41, 2847-2849. 19. Ross, D.T.; Guo, H.; Howorth, P.; Chen, Y.; Hamilton, G.S.; Steiner, J.P. The small molecule FKBP ligand GPI 1046 induces partial striatal re-innervation after intranigral 6-hydroxydopamine lesion in rats. Neurosci. Lett. 2001, 297, 113-116. 20. Emborg, M.E.; Shin, P.; Roitberg, B.; Sramek, J.G.; Chu, Y.; Stebbins, G.T.; Hamilton, G.S.; Suzdak, P.D.; Steiner, J.P.; Kordower, J.H. Systemic adnistration of the immunophilin ligand GPI 1046 in MPTP-treated monkeys. Exp. Neurol. 2001, 168, 171-182. 21. Zhang, C., Steiner, J. P., Hamilton, G. S., Hicks, T. P., and Poulter, M.O. Regeneration of dopaminergic function in 6-hydroxydopamine-lesioned rats by neuroimmunophilin ligand treatment. J. Neurosci. 2001, 21, RC156. 22. Wei, L.; Wu, Y.-Q.; Wilkinson, D.E.; Chen, Y.; Soni, R.; Scott, C.; Ross, D.T.; Guo, H.; Howorth, P.; Valentine, H.L.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.P.; Hamilton, G.S. Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl and pipecolyl amides. Bioorg. Med. Chem. Lett. 2002, 12, 1429-1433. 23. Choi, C.; Li, J.-H.; Vaal, M.; Thomas, C.; Limburg, D.C.; Wu, Y.-Q.; Chen, Y.; Soni, R.; Scott, C.; Ross, D.T.; Guo, H.; Howorth, P.; Valentine, H.L.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.P.; Hamilton, G.S. Use of parallel synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors. Bioorg. Med. Chem. Lett. 2002, 12, 1421-1428. 2
  • 3. 24. Hamilton, G.S.; Wu, Y.-Q.; Limburg, D.C.; Wilkinson, D.E.; Vaal, M.J.; Li, J.-H.; Thomas, C.; Huang, W.; Sauer, H.; Ross, D.T.; Soni, R.; Chen, Y.; Guo, H.; Howorth, P.; Valentine, H.L.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.P. Synthesis of N-glyoxyl and pipecoly amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects. J. Med. Chem. 2002, 45. 3549-3557 25. Wu, Y.-Q.; Wilkinson, D.E.; Limburg, D.C.; Li, J.-H.; Sauer, H.; Ross, D.T.; .; Liang, S.; Spicer, D.; Valentine, H.L.; Fuller, M.; Guo, H.; Howorth, P.; Soni, R.; Chen, Y.; Steiner, J.P.; Hamilton, G.S. Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. J. Med. Chem. 2002, 45, 3558-3568. 26. Khan, Z.; Ferrari, G.; Kasper, M.; Tonge, D. A.; Steiner, J. P.; Hamilton, G. S.; Gordon- Weeks, P. R. The non-immunosuppressive immunophilin ligand GPI-1046 potently stimulates regenerating axon growth from adult mouse dorsal root ganglia cultured in Matrigel. Neuroscience 2002, 114, 601-609. 27. Wu, Yong-Qian; Hamilton, Sean K.; Wilkinson, Douglas E.; Hamilton, Gregory S.. Direct synthesis of guanidines using di(imidazol-1-yl)methanimine. J. Org. Chem. 2002, 67, 7553- 7556. 28. Wu, Yong-Qian; Belyakov, Sergei; Choi, Chi; Limburg, David; Thomas, Bert E., IV; Vaal, Mark; Wei, Ling; Wilkinson, Douglas E.; Holmes, Agnes; Fuller, Mike; McCormick, Jocelyn; Connolly, Maureen; Moeller, Tim; Steiner, Joseph; Hamilton, Gregory S. Synthesis and biological evaluation of non-peptidic cyclophilin ligands. J. Med. Chem. 2003, 46, 1112-1115. 29. Wu, Yong-Qian; Limburg, David C.; Wilkinson, Douglas E.; Hamilton, Gregory S.. Formation of nitrogen-containing heterocycles using di(imidazole-l-yl)methanimine. J. Het. Chem. 2003, 40, 191-193. 30. Limburg, D.C.; Thomas, B.E.; Li, J.-H.; Fuller, M.; Spicer, D.; Chen, Y.; Guo, H.; Steiner, J.P.; Hamilton, G.S.; Wu, Y.-Q. “Synthesis and evaluation of chiral bicyclic proline FKBP12 ligands”. Bioorg. Med. Chem. Lett. 2003, 13, 3867-3870. 31. Wilkinson, D.E.; Thomas, B.E.; Limburg, D.C.; Holmes, A.; Sauer, H.; Ross, D.T.; Soni, R.; Chen, Y.; Guo, H.; Howorth, P.; Valentine, H.; Spicer, D.; Fuller, M.; Steiner, J.P.; Hamilton, G.S.; Wu, Y.-Q. “Synthesis, molecular modeling and biological evaluation of aza-proline and aza- pipecolic derivatives as FKBP12 ligands and their in vivo neuroprotective effects.” Bioorg. Med. Chem. 2003, 11, 4815-4825. 32. Wei; L.; Steiner, J.P.; Hamilton, G.S.; Wu, Y.-Q. “Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporine A derivatives.” Bioorg. Med. Chem. Lett. 2004, 14, 4549- 4551. 33. Hamilton, S.; Wilkinson, D.E.; Hamilton, G.S.; Wu, Y.-Q. “Microwave assisted synthesis of N,N’-diaryl cyanoguanidines.” Org. Lett. 2005, 2429-2431. 34. Caporella, E.; Nath, A.; Slevin, J.; Galey, D.; Hamilton, G.; Williams, L.; Steiner, J.P.; Haughey, N.J. “The immunophilin ligand GPI1046 protects neurons from the lethal effects of the HIV-1 proteins gp120 and Tat by modulating endoplasmic reticulum calcium load.” J. Neurochem. 2006, 98, 146-155. 3
  • 4. Abstracts 1. Zimmerman, S.C.; Hamilton, G.S.; Finney, N.F. Complexation chemistry of a rigid molecular tweezer. 195th American Chemical Society National Meeting. 1988. 2. Hamilton, G.S.; Huang, Z.; Patch, R.J. Asymmetric synthesis of NPC 17742: a potent and selective competitive NMDA antagonist. 202nd American Chemical Society National Meeting. 1991. 3. Hamilton, G.S.; Huang, Z.; Wu, J.; Borosky, S.A.; Bednar, D.L.; Ferkany, J.W.; Karbon, E.W. Phosphonoethylphenylalanine derivatives as novel antagonists of non-NMDA ionotropic glutamate receptors. 204th American Chemical Society National Meeting. 1992. 4. Karbon, E.W.; Bednar, D.L.; Bailey, M.A.; Borosky, S.A.; Zubrowski, R.A.; Ferkany, J.W.; Huang, Z.; Hamilton, G.S. 2-Phosphonoethylphenylalanine derivatives as novel antagonists of kainic acid/AMPA receptors. Soc. Neurosci. Abstr. 613.3, 1992. 5. Perumattam, J.; Hamilton, G.S.; Wu, J.P.; Confer, W.L.; Shao, C.; Hatoum, H.N.; Venkataramen, B.; Blok, N.; Yang, X.Y.; Lowe, V.C.; Laemont, K.; Endemann, G.; Bryant, C.M.; Feng, Y. New orally active leukocyte recruitment inhibitors as antiinflammatory agents. 208th American Chemical Society National Meeting. 1994. 6. Steiner, J.P.; Dawson, T.M.; Connolly, M.A.; Hamilton, G.S.; Suzdak, P.D.; Snyder, S.H. Neuroimmunophilin ligands are neurotrophic for PC12 cells and sensory neuronal cultures. Soc. Neurosci. Abstr. 699.4, 1995. 7. Hamilton, G.S.; Huang, W.; Connolly, M.A.; Suzdak, P.D.; Steiner, J.P. FKBP12-binding domain analogues of immunosuppressive drug FK506 are potent, nonimmunosuppressive neurotrophic agents in vitro. Soc. Neurosci. Abstr. 297.12, 1996. 8. Steiner, J.P.; Connolly, M.A.; Valentine, H.L.; Hamilton, G.S.; Dawson, T.M.; Hester, L.; Snyder, S.H.; Nonimmunosuppressive ligands for neuroimmunophilins promote nerve extension in vitro and in vivo. Soc. Neurosci. Abstr. 297.13, 1996. 9. Ross, D.T.; Valentine, H.L.; Guo, H.; Hamilton, G.S.; Huang, W.; Suzdak, P.D.; Steiner, J.P. Novel neuroimmunophilin ligands for FKBP12 possess potent neurotrophic activity in the mouse MPTP model of Parkinson’s Disease. Soc. Neurosci. Abstr. 297.14, 1996. 10. Hamilton, G.S.; Ross, D.T.; Valentine, H.L.; Guo, H.; Connolly, M.A.; Liang, S.; Ramsey, C.; Li, J.; Huang, W.; Wei, L.; Howorth, P.; Soni, R.; Fuller, M.; Sauer, H.; Nowotnick, A.; Suzdak, P.D.; Steiner, J.P. Neuroimmunophilins as novel targets for CNS drug discovery. 213th American Chemical Society National Meeting. 1997, Abstract MEDI 172. 11. Hamilton, G.S.; Huang, W.; Li, J.; Connolly, M.A.; Ross, D.T.; Guo, H.; Valentine, H.L.; Steiner, J.P. (N-Glyoxyl)pipecolate esters are potent neurotrophic agents in vitro and promote recovery in a mouse model of Parkinson’s Disease. 214th American Chemical Society National Meeting. 1997, Abstract MEDI 142. 12. Li, J.; Hamilton, G.S.; Huang, W.; Connolly, M.A.; Ross, D.T.; Guo, H.; Valentine, H.L.; Steiner, J.P. In vitro and in vivo neurotrophic effects of (N-sulfonyl) and (N-carbamoyl) pipecolate esters. 214th American Chemical Society National Meeting. 1997, Abstract MEDI 183. 13. Ross, D.T.; Guo, H.; Howorth, P.; Fuller, M.; Nowotnick, A.; Hamilton, G.S.; Suzdak, P.D.; Steiner, J.P. The novel neuroimmunophilin ligand GPI 1046 stimulates morphological, biochemical, and behavioral recovery in the rat intranigral 6-OHDA Parkinson’s Disease model. Soc. Neurosci. Abstr. 677.7, 1997. 4
  • 5. 14. Liang, S.; Valentine, H.L.; Ross, D.T.; Huang, W.; Suzdak, P.D.; Hamilton, G.S.; Steiner, J.P. Neuroimmunophilin ligands augment serotonin fiber protection following lesions with para- chloroamphetamine (PCA). Soc. Neurosci. Abstr. 677.10, 1997. 15. Valentine, H.L.; Liang, S.; Suzdak, P.D.; Hamilton, G.S.; Steiner, J.P. The neuroimmunophilin ligand GPI 1046 stimulates recovery following sciatic nerve injury. Soc. Neurosci. Abstr. 677.9, 1997. 16. Connolly, M.A.; Ramsey, C.; Hamilton, G.S.; Steiner, J.P. GPI 1046 elicits neurite outgrowth of primary sensory neuronal cultures. Soc. Neurosci. Abstr. 677.13, 1997. 17. Steiner, J.P.; Ross, D.T.; Valentine, H.L.; Liang, S.; Guo, H.; Huang, W.; Suzdak, P.D.; Hamilton, G.S. The orally active neuroimmunophilin ligand GPI 1046 promotes structural and functional recovery in the mouse MPTP model of Parkinson’s Disease. Soc. Neurosci. Abstr. 677.6, 1997. 18. Guo, H.; Spicer, D.M.; Howorth, P.; Hamilton, G.S.; Suzdak, P.D.; Steiner, J.P.; Ross, D.T. The novel small molecule immunophilin ligand GPI 1046 stimulates cholinergic reinnervation of deafferented hippocampal regions after fimbria-fornix transection. Soc. Neurosci. Abstr. 677.12, 1997. 19. Wu, Y-Q., Wilkinson, D.; Soni, R.; Scott, C.; Ross, D.T.; Guo, H.; Howorth, P.; Chen, Y.; Valentine, H.; Liang, S.; Spicer, D.; Steiner, J.; Hamilton, G.S. N-Glyoxyl prolyl and pipecolyl amide FKBP12 ligands: potent neurotrophic agents in an animal model of Parkinson’s Disease. 216th American Chemical Society National Meeting. 1998, Abstract MEDI 103. 20. Choi, C.; Li, J.-H.; Vaal, M.; Thomas, C.; Limburg, D.; Chen, Y.; Soni, R.; Scott, C.; Ross, D.T.; Guo, H.; Howorth, P.; Valentine, H.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.; Hamilton, G.S. Use of parallel synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors. 216th American Chemical Society National Meeting. 1998, Abstract MEDI 157. 21. Wei, L.; Wu, Y.-Q.; Wilkinson, D.; Chen, Y.; Soni, R.; Scott, C.; Ross, D.T.; Guo, H.; Howorth, P.; Valentine, H.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.; Hamilton, G.S. Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoyl prolyl and pipecolyl amides. 216th American Chemical Society National Meeting. 1998, Abstract MEDI 158. 22. Valentine, H.L.; Spicer, D.; Fuller, M.; Hamilton, G.S.; Steiner, J.P. Neuroimmunophilin ligands promote recovery from the peripheral sensory neuropathy associated with streptozotocin- induced diabetes. Soc. Neurosi. Abstr. 185.9, 1998. 23. Kordower, J.H.; Emborg, M.E.; Shin, P.; Roitberg, B.; Sramek, J.; Chu, Y.-P.; Hamilton, G.S.; Suzdak, P.D.; Steiner, J.P. Systemic administration of the immunophilin ligand GPI 1046 in MPTP-treated monkeys. Soc. Neurosci. Abstr. 324.7, 1998. 24. Structural analysis of the binding of neurotrophic ligands for FK506-binding protein (FKBP). Holmes, A.F.; Thomas, C.; Wei, L.; Soni, R.; Connolly, M.; Steiner, J.P.; Hamilton, G.S. 217th American Chemical Society National Meeting, 1999, Abstract MEDI 238. 25. Synthesis of thioester FKBP12 ligands and evaluation of their in vitro and in vivo nerve regenerative effects. Limburg, D.C.; Vaal, M.J.; Li, J.-H.; Wu, Y.-Q.; Thomas, C.; Sauer, H.; Ross, D.T.; Soni, R.; Chen, Y.; Guo, H.; Howorth, P.; Valentine, H.; Liang, S.; Spicer, D.; Fuller, M.; Steiner, J.P.; Hamilton, G.S. 217th American Chemical Society National Meeting, 1999, Abstract MEDI 237. 5
  • 6. 26. Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. Wu, Y.-Q.; Wilkinson, D.; Limburg, D.C.; Li, J.-H.; Sauer, H.; Ross, D.T.; Liang, S.; Spicer, D.; Valentine, H.; Fuller, M.; Guo, H.; Howorth, P.; Soni, R.; Chen, Y.; Steiner, J.P.; Hamilton, G.S. 218th American Chemical Society National Meeting, 1999, Abstract MEDI 69. 27. Thioester FKBP12 ligands: evaluation of their in vitro and in vivo nerve regenerative effects. Guo, H.; Limburg, D.C.; Vaal, M.J.; Li, J.-H.; Wu, Y.-Q.; Thomas, C.; Sauer, H.; Ross, D.T.; Soni, R.; Chen, Y.; Howorth, P.; Valentine, H.; Moeller, T.; Spicer, D.; Fuller, M.; Wood, S.; Hamilton, G.S.; Steiner, J.P. Soc. Neurosci. Abstr. 88.20, 1999. 28. Structural analysis of the binding of neurotrophic ligands for FK506-binding protein (FKBP). Hamilton, G.S.; Holmes, A.F.; Thomas, C.; Wei, L.; Soni, R.; Connolly, M.; Summers, M.F.; Steiner, J.P. Soc. Neurosci. Abstr. 88.17, 1999. 29. N-glyoxyl prolyl and pipecolyl amide FKBP12 ligands: potent neurotrophic agents in an animal model of Parkinson’s Disease. Ross, D.T.; Wu, Y.-Q.; Wilkinson, D.; Soni, R.; Scott, C.; Guo, H.; Howorth, P.; Chen, Y.; Valentine, H.; Spicer, D.; Hamilton, G.S.; Steiner, J.P. Soc. Neurosci. Abstr. 88.19, 1999. 30. Neurotrophic ketone analogues of prolyl and pipecolyl ester FKBP12 ligands. Steiner, J.P.; Wu, Y.-Q.; Wilkinson, D.; Limburg, D.C.; Li, J.-H.; Sauer, H.; Ross, D.T.; Liang, S.; Spicer, D.; Valentine, H.; Fuller, M.; Howorth, P.; Soni, R.; Chen, Y.; Hamilton, G.S. Soc. Neurosci. Abstr. 88.18, 1999. 31. Protection of optic nerve axons by representatives of different classes of Guilford FKBP immunophilin ligands. D.T. Ross, H. Guo, Y. Chen, P. Howorth, C. Thomas, A. Holmes, C. Choi, M. Vaal, W. Huang, Y. Wu, D. Limburg, D. Wilkinson, G.S. Hamilton and J.P Steiner. Soc. Neurosci. Abstr. 29.18, 2000. 32. FKBP protein distribution in the optic nerve. Y. Chen, H. Guo, P. Howorth, J.P.Steiner, G.S. Hamilton, P.Suzdak, and D.T. Ross. Soc. Neurosci. Abstr. 29.17, 2000. 33. Structural and biochemical analysis of neurotrophic FKBP ligands. G. S. Hamilton, A. Holmes, C. Thomas, L. Wei, T. Ho, J. Rothstein, and J. P. Steiner. Soc. Neurosci. Abstr. 216.1, 2000. 34. Synthesis of chiral asymmetric bicyclic proline FKBP12 ligands and in vivo evaluation in Parkinson’s Disease. D. Limburg, J.-H. Li, D. Ross, D. Spicer, P. Howorth, Y. Chen, H. Guo, J. Steiner and G. Hamilton. 220th American Chemical Society National Meeting, 2000, Abstract MEDI 200. 35. GPI-1046 stimulation of axon growth from embryonic dorsal root ganglia may require non- neuronal cells. Ferrari, G., Khan, Z., Steiner, J. P., Hamilton, G. S., Gordon-Weeks, P. 31st Society for Neuroscience Meeting in San Diego, 2001. 36. Regenerative effects of neuroimmunophilin ligands. Steiner, J. P., Wu, Y. and Hamilton, G. S. Immunophilins in the Brain II mini-symposium Nov. 10, 2001. 37. Synthesis, Molecular Modeling and Biological Evaluation of Aza-proline and Aza-pipecolic Derivatives as FKBP12 Ligands and their In Vivo Nerve Regenerative Effects Wu, Y.Q., Wilkinson, D., Limburg, D., Sauer, H., Ross, D.T., Soni, R., Chen, Y., Guo, H., Howorth, P., Valentine, H., Spicer, D., Fuller, M., Steiner, J., Hamilton, G. Presented at the 223rd National Meeting of the American Chemical Society, April 10-14, 2002 in Orlando, FL 38. Neuroimmunophilin Ligands Protect Against Post Prostaecomy-Induced Erectile Dysfunction. Steiner, J., Wu, Y. Q., Burnett, A. L., Hamilton, G. S. 5th International Neurodegeneration in AD, PD and Related Disorders, June 24-25, 2002, Princeton, NJ. 6
  • 7. 39. Synthesis and biological evaluation of non-peptidic cyclophilin ligands and their in vivo neuroprotective effects. Wu, Y.-Q.; Belyakov, S.; Choi, Chi; Wilkinson, D.; Limburg, D.; Vaal, M.; Thomas, B.; Holmes, A.; Chen, Y.; Gio, H.; Howorth, P.; Valentine, H.; Spicer, D.; Fuller, M.; Steiner, J.; Hamilton, G. S. Presented at the 224th National Meeting of the American Chemical Society, August 18-22, 2002 in Boston, MA. 40. Neuroprotective effects of inhibitors of dipeptidyl peptidase-IV in vitro and in vivo. Wu, Y.Q.; Hamilton, G.S.; Limburg, D.C.; Wilkinson, D.E.; Jackson, P.; Steiner, J.P.; Belyakov, S.A. Presented at the First International Conference “Dipeptidyl Aminopeptidases: Basic Science and Clinical Applications” Berlin, September 2002. 41. Structure-based design of potent small molecule cyclophilin ligands. Belyakov, S.A.; Hamilton, S.; Limburg, D.C.; Thomas, B.; Vaal, M.; Wei, L.; Wilkinson, D.E.; Fuller, M.; Steiner, J.P.; Hamilton, G.S.; Wu, Y.Q. Presented at the 225th National Meeting of the American Chemical Society, March 23-27, 2003 in New Orleans, LA. 42. Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporine A derivatives. Wei, L.; Hamilton, G.S.; Steiner, J.P.; Wu, Y.Q. Presented at the 225th National Meeting of the American Chemical Society, March 23-27, 2003 in New Orleans, LA. 43. Microwave assisted synthesis of aryl cyanoguanidines. Hamilton, S.; Wilkinson, D.E.; Hamilton, G.S.; Wu, Y.Q. Presented at the 229th National Meeting of the American Chemical Society, March 13-17, 2005, in San Diego, CA. 44. Design and synthesis of arylsulfonyl thioureas as novel potent cyclophilin ligands. Serdyuk, L.E.; Wilkinson, D.E.; Hamilton, S.; Belyakov, S.A.; Wei, L.; Thomas B.E., Hamilton, G.S.; Massuda, E.; Stathis, M.; Fuller, M.; Rojas, C.; Steiner, J.P.; Huang, S; Liu, G.; and Wu, Y.Q. Presented at the 230th National Meeting of the American Chemical Society, August 28, 2005, in Washington, DC. 45. Design and synthesis of arylsulfonylthiosemicarbazides as potent, nonpeptidic cyclophilin ligands. Wu, Y.Q.; Wilkinson, D.E.; Hamilton, G.S.; Steiner, J.P.; Hamilton, S.; Thomas B.E., Massuda, E.; Fuller, M.; Stathis, M.; and Belyakov, S.A. Presented at the 230th National Meeting of the American Chemical Society, August 28, 2005, in Washington, DC. 46. Small molecule inhibitors against mitochondrial permeability transition pore (mPTP). Wu, Y.- Q.; Wilkinson, D.; Hamilton, S.; Wei, L.; Serdyuk, L.; Fuller, M.; Alt, J.; Steiner, J.P.; Williams, L.; Rojas, C.; Hamilton, G.S. Presented at the 230th National Meeting of the American Chemical Society, August 31, 2005, in Washington, DC. Reviews and book chapters Hamilton, G.S.; Steiner, J.P. Neuroimmunophilin ligands as novel therapeutics for the treatment of degenerative disorders of the nervous system. Curr. Pharm. Design 1997, 3, 405-428. Snyder, S.H.; Sabatini, D.E.M.; Lai, M.M.; Steiner, J.P.; Hamilton, G.S.; Suzdak, P.D. Neural actions of immunophilin ligands. Trends Pharm. Sci. 1998, 19, 21-26. Hamilton, G.S. Emerging therapeutic agents for Parkinson’s Disease. Chem. Ind. 1998, 127-132. Hamilton, G.S. Immunophilin ligands for the treatment of neurological disorders. Exp. Opin. Ther. Patents 1998, 8, 1109-1123. 7
  • 8. Hamilton, G.S.; Steiner, J.P. Immunophilins: Beyond Immunosuppression. J. Med. Chem. 1998, 41, 5119-5143. Hamilton, G.S.; Thomas, C. Immunophilins: The Next Generation. IN Advances in Med. Chem. Vol. 5, JAI Press, 2000. Steiner, J.P.; Valentine, H.; Morrow, T.; Hamilton, G.S. Neuroimmunophilin ligands stimulate recovery of injured sciatic nerves. IN Immunosuppressants and Neurological Disorders, Ed. by C.V. Borlongan, Humana Press, 2001. Steiner, J.P.; Ross, D.T.; Sauer, H.; Morrow, T.; Hamilton, G.S. Effects of neuroimmunophilin ligands on Parkinson's Disease and cognition. IN Immunosuppressants and Neurological Disorders, Ed. by C.V. Borlongan, Humana Press, 2001. Wu, Y.-Q.; Limburg, D.C.; Wilkinson, D.E.; Jackson, P.; Steiner, J.P.; Hamilton, G.S.; Belyakov, S.A. Neuroprotective effects of inhibitors of dipeptidyl peptidase-IV in vitro and in vivo. IN Dipeptidyl Aminopeptidases in Health and Disease, Ed. by Hildebrandt et al. Kluwer Academic/Plenum Publishers, New York, 2003. Williams, L.; Wu, F.; Hamilton, G. Mitochondrial permeability as a target for neurodegenerative disorders. Drugs of the Future 2006, 31, 1083-1098. Hamilton, G.S. Antibody-drug conjugates for cancer therapy: The technological and regulatory challenges of developing drug-biologic hybrids. Biologicals 2015, in press. Patents 1. Hamilton, G.S. Excitatory amino acid antagonists. US Patent 5,256,814. 2. Hamilton, G.S. ω-[2-(Tetrazolylalkyl)cyclohexyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors. US Patent 5,331,001. 3. Hamilton, G.S. Phosphonoalkylquinolin-2-ones as novel antagonists of non-NMDA ionotropic excitatory amino acid receptors. US Patent 5,342, 946. 4. Hamilton, G.S. ω-[2-Alkylphenyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors. US Patent 5,364,876. 5. Hamilton, G.S.; Ferkany, J.W.; Rzeszotarki, W.J.; Ellenberger, S.R.; Guzewska, M.E.; Patch, R.J.; Karbon, E.W. . ω-[2-(Phosphonoalkyl)phenyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors. US Patent 5,395,827. 6. Hamilton, G.S. ω-[2-(Tetrazolylalkyl)cyclohexyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors. US Patent 5,426,114. 7. Hamilton, G.S. Phosphonoalkylquinolin-2-ones as novel antagonists of non-NMDA ionotropic excitatory amino acid receptors. US Patent 5,510,338. 8. Mewshaw, R.E.; Hamilton, G.S. Antiinflammatory benzoic acid derivatives. US Patent 5,530,157. 9. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 5,614,547. 8
  • 9. 10. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S. Inhibitors of rotamase enzyme activity. US Patent 5,696,135. 11. Hamilton, G.S.; Li, J.-H.; Steiner, J.P. Method of using neurotrophic sulfonamide compounds. US Patent 5,721,256. 12. Hamilton, G.S.; Li, J.-H. Heterocyclic thioesters. US Patent 5,786,378. 13. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 5,795,908. 14. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T. Inhibitors of rotamase enzyme activity. US Patent 5,798,355. 15. Li, J.-H.; Hamilton, G.S. Heterocyclic esters and amides. US Patent 5,801,187. 16. Steiner, J.P.; Hamilton, G.S. Rotamase enzyme activity inhibitors. US Patent 5,801,197. 17. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T. Inhibitors of rotamase enzyme activity. US Patent 5,843,960. 18. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxides of heterocyclic esters, amides, thioesters and ketones. US Patent 5,846,979. 19. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T.M. Inhibitors of rotamase enzyme activity. US Patent 5,846,981. 20. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 5,859,031. 21. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked sulfonamides of heterocyclic thioesters. US Patent 5,874,449. 22. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked ureas and carbamates of piperidyl thioesters. US Patent 5,935,989. 23. Steiner, J.P.; Hamilton, G.S. Pyrrolidine carboxylate hair revitalizing agents. US Patent 5,945,441. 24. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked ureas and carbamates of piperidyl thioesters. US Patent 5,958,949. 25. Hamilton, G.S.; Li, J.-H.; Steiner, J.P. Method of using neurotrophic sulfonamide compounds. US Patent 5,968,957. 26. Hamilton, G.S.; Li, J.-H. Heterocyclic thioesters and ketones. US Patent 5,990,131. 27. Steiner, J.P.; Hamilton, G.S.; N-linked sulfonamides of heterocyclic thioester hair growth compounds and uses. US Patent 6,004,993. 28. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T.M. Inhibitors of rotamase enzyme activity. US Patent 6,022,878. 29. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxides of heterocyclic esters, amides, thioesters, and ketones. US Patent 6,054,452. 9
  • 10. 30. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked sulfonamides of heterocyclic thioesters. US Patent 6,121,273. 31. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 6,140,357. 32. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxide of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses. US Patent 6,172,087. 33. Steiner, J.P.; Hamilton, G.S. Pyrrolidine derivative hair growth compositions and uses. US Patent 6,177,455. 34. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked ureas and carbamates of heterocyclic thioesters. US Patent 6,184,243. 35. Steiner, J.P.; Hamilton, G.S. Pipecolic acid derivative hair growth compositions and uses. US Patent 6,187,784. 36. Steiner, J.P.; Hamilton, G.S. Sulfone hair growth compositions and uses. US Patent 6,187,796. 37. Steiner, J.P.; Hamilton, G.S. N-linked sulfones of heterocyclic thioester hair growth compositions and uses. US Patent 6,187,806. 38. Steiner, J.P.; Hamilton, G.S. Small molecule pipecolic acid derivative hair growth compositions and uses. US Patent 6,191,125. 39. Steiner, J.P.; Hamilton, G.S. Small molecule carbamate or urea hair growth compositions and uses. US Patent 6,194,440. 40. Li, J.-H.; Hamilton, G.S. Heterocyclic esters and amides. US Patent 6,200,972. 41. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Pyrrolidine derivatives for vision and memory disorders. US Patent 6,218,423. 42. Hamilton, G.S.; Li, J.-H. Heterocyclic ketone and thioester compounds and uses. US Patent 6,218,424. 43. Li, J.-H.; Hamilton, G.S. Heterocyclic esters and amides. US Patent 6,218,544. 44. Hamilton, G.S.; Steiner, J.P. Pyrrolidine carboxylate and pyrrolidine amide hair revitalizing agents. US Patent 6,239,164. 45. Li, J.-H.; Steiner, J.P.; Hamilton, G.S.; Carbamate and urea compositions and neurotrophic uses. US Patent 6,242,468. 46. Hamilton, G.S.; Li, J.-H.; Steiner, J.P. Method of using neurotrophic sulfonamide compounds. US Patent 6,245,783. 47. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxides of heterocyclic esters, amides, thioesters and ketones. US Patent 6,251,892. 48. Steiner, J.P.; Hamilton, G.S. N-Linked urea or carbamate of heterocyclic thioester hair growth compositions and uses.US Patent 6,271,244. 10
  • 11. 49. Steiner, J.P.; Hamilton, G.S. Heterocyclic thioester and ketone hair growth compositions and uses. US Patent 6,274,602. 50. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked ureas and carbamates of heterocyclic thioesters. US Patent 6,274,607. 51. Steiner, J.P.; Hamilton, G.S. Heterocyclic ester and amide hair growth compositions and uses. US Patent 6,274,617. 52. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 6,291,510. 53. Hamilton, G.S.; Li, J.-H.; Huang, W. N-linked sulfonamides of heterocyclic thioesters. US Patent 6,294,551. 54. Hamilton, G.S.; Norman, M.H.; Wu, Y.-Q. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds. US Patent 6,331,537. 55. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Small molecule sulfonamides for vision and memory disorders. US Patent 6,333,340. 56. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Nitrogen-containing linear and azepinyl compositions and uses for vision and memory disorders. US Patent 6,335,348. 57. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders. US Patent 6,337,340. 58. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. N-linked sulfonamides of N-heterocyclic carboxylic acids or isosteres for vision and memory disorders. US Patent 6,339,101. 59. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Pipecolic acid derivatives for vision and memory disorders. US Patent 6,376,517. 60. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Heterocyclic thioesters or ketones for vision and memory disorders. US Patent 6,384,056. 61. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Small molecule carbamates or ureas for vision and memory disorders. US Patent 6,395,758. 62. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. N-oxides of heterocyclic ester, amide, thioester, or ketones for vision and memory disorders. US Patent 6,399,648. 63. Wu, Y.-Q.; Hamilton, G.S.; Huang, W. AZA compounds, pharmaceutical compositions, and methods of use. US Patent 6,417,189. 64. Hamilton, G.S.; Li, J.-H. Heterocyclic ketone and thioester compounds and uses. US Patent 6,417,209. 65. Steiner, J.P.; Hamilton, G.S. N-oxides of heterocyclic ester, amide, thioester, or ketone hair growth compositions and uses. US Patent 6,429,215. 66. Steiner, J.P.; Hamilton, G.S.; Snyder, S.H. Methods of using inhibitors of cyclophilin rotamase activity to affect neurological activity. US Patent 6,444,643. 67. Hamilton, G.S.; Limburg, D.C. Cyclic ester or amide derivatives. US Patent 6,462,072. 11
  • 12. 68. Hamilton, G.S.; Steiner, J.P.; Burak, E.S. N-oxides of heterocyclic esters, amides, thioesters, and ketones. US Patent 6,486,151. 69. Steiner, J.P.; Snyder, S.H.; Hamilton, G.S.; Dawson, T. Inhibitors of rotamase enzyme activity. US Patent 6,500,843. 70. Hamilton, G.S.; Steiner, J.P. Pyrrolidine derivatives and processes for preparing same. US Patent 6,500,959. 71. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. N-linked urea or carbamate of heterocyclic thioesters for vision and memory disorders. US Patent 6,506,788. 72. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 6,509,477. 73. Steiner, J.P.; Hamilton, G.S. Non-peptidic cyclophilin binding compounds and their use. US Patent 6,593,362. 74. Wu, Y.-Q.; Belyakov, S.; Hamilton, G.S.; Limburg, D.; Steiner, J.P.; Vaal, M.; Wei, L.; Wilkinson, D. Trisubstituted carbocyclic cyclophilin binding compounds and their use. US Patent 6,656,971. 75. Hamilton, G.S.; Steiner, J.P.; Vaal, M.J.; Choi, C.; Wei, L. Non-peptidic cyclophilin binding compounds and their use. US Patent 6,677,376. 76. Steiner, J.P.; Hamilton, G.S. Pyrrolidine derivative hair growth compositions and uses. US Patent 6,943,187. 77. Hamilton, G.S. Hydantoin derivative compounds, pharmaceutical compositions, and methods of using same. US Patent 6,974,823. 78. Hamilton, G.S.; Li, J.-H. Heterocyclic ketone and thioester compounds and uses. US 6,984,639. 79. Steiner, J.P., Hamilton, G.S. Rotamase enzyme activity inhibitors. US Patent 7,056,935. 80. Hamilton, G.S.; Norman, M.H.; Wu, Y.-Q. N-linked sulfonamides of N-heterocyclic acids or carboxylic acid isosteres. US Patent 7,078,424. 81. Hamilton, G.S., Leighton, H.J. Compounds having simultaneous ability to block L-type calcium channels and to inhibit phosphodiesterase type 3 activity. US Patent 7,098,211. 82. Hamilton, G.S.; Norman, M.H.; Wu, Y.-Q. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds. US Patent 7,153,883. 83. Wu, Y.-Q., Huang, W., Hamilton, G.S. Aza compounds, pharmaceutical compositions and methods of use. US Patent 7,253,169. 84. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds for vision and memory disorders. US Patent 7,265,150. 85. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 7,282,510. 12
  • 13. 86. Ross, D.T.; Hamilton, G.S.; Steiner, J.P. Heterocyclic esters or amides for vision and memory disorders. US Patent 7,338,976. 87. Ross, D.T.; Sauer, H.; Hamilton, G.S.; Steiner, J.P. N-linked sulfonamide of heterocyclic thioesters for vision and memory disorders. US Patent 7,410,995. 88. Hamilton, G.S.; Norman, M.H.; Wu, Y.-Q. N-linked sulfonamides of N-heterocyclic acids or carboxylic acid isosteres. US Patent 7,459,473. 89. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 7,652,060. 90. Hamilton, G.S.; Steiner, J.P. Small molecule inhibitors of rotamase enzyme activity. US Patent 7,960,570. 91. Hamilton, G.S.; Tsukamoto, T.; Ferraris, D.; Duvall, B.; Lapidus, R. Certain compounds, compositions and methods. US Patent 8,268,800. 92. Belyakov, S.; Duvall, B.; Ferraris, D.; Hamilton, G.S.; Vaal, M. Compositions and methods for treating cancer. US Patent 8,329,665. 93. Hamilton, G.S.; Tsukamoto, T.; Ferraris, D.; Duvall, B.; Lapidus, R. Certain compounds, compositions and methods. US Patent 8,951,987. 13