Preparation of Novel Pyridopyrimidine Derivatives as PI3K Inhibitors, Gyorkos, Albert C.,
Lee, G., Lim, C., Cho, H.W., Seo, J.B., Cho, S.Y., Choi, E.K., Kim, C.S., Hwang, J.J.,
US20150158874.

Preparation of Novel Pyridopyrimidine Derivatives as PI3K Inhibitors, Gyorkos, Albert
Charles, Lee, G., Lim, C., Cho, H.W., Seo, J.B., Cho, S.Y., Choi, E.K., Kim, C.S., Hwang, J.J.,
WO2013141586.

Preparation of Novel Pyridopyrimidine Derivatives as PI3K Inhibitors, Gyorkos, Albert
Charles, Lee, G., Lim, C., Cho, H.W., Seo, J.B., Cho, S.Y., Choi, E.K., Kim, C.S., Hwang, J.J.,
US20120238587.

Preparation of Heterocyclic Compounds as MEK Inhibitors, Gyorkos, A.C., Lee, G., Cho, H.W.,
Song, E. J., Jeon, H., Kim, M., Seo, J., Cho, S.Y., US20120238599.

Preparation of Heterocyclic Cyclohexane Analogues as GPR119 Agonists for Treating Metabolic
Disorders and Complications of Metabolic Disorders, Gyorkos, A.C., Kang, S.U., Kim., M.J.,
Kang, B.N., Tan, W., Cho, S.Y., US20120053180.

Fused Heterocyclic Compounds, Gyorkos, A.C., ., Corrette,C. Cho, S., Young, T., Aso, K,
Michiyo, M., Siedem, C.; United States Patent 8163935. Issued April 24, 2012

Preparation of Enantiomeric Heterocyclic Compounds with Antibacterial Activity, Gyorkos,
A.C., Guiles, J., Strong, S., Sun X., Janjic, N. PCT Int. Appl. 2008 WO2008039640.

Preparation of Benzimidazole Derivatives as CRF Receptor Antagonists. Aso, K, Mochizuki,
M., Kojima, T., Kobayashi, K, Pratt, S., Gyorkos, A.C., Corrette, C.P.,Cho, S. WO2008051533
Issued May 2, 2008.

Preparation of Fused Heterocyclic Compounds like Benzimidazoles as CRF Receptor
Antagonists, Gyorkos, A.C., Corrette, C., Cho, S., Siedem, C. Aso, K, Gyoten, M, PCT Int.
Appl. 2006 WO2006116412.

Preparation of Cyclic Compounds as CRF Antagonists, Gyorkos, A.C., Corrette,C. Cho, S.,
Young, T., Aso, K, Kori, M, Gyoten, M., Condtoski, K, Siedem, C. Boyd, S., PCT Int. Appl.
2005 WO2005099688.

Preparation of Nitrogen Containing Fused Heterocyclic Compounds like Benzimidazoles and
Benzothiazoles as CRF Antagonists, Gyorkos, A.C., Corrette, C., Cho, S. Turner, T., Pratt, S.,
Aso, K., Gyoten, M., PCT. Int. Appl. 2005 WO2005044793.

Preparation of Pyrazolopyrimidines as Calcium Receptor Modulators, Gyorkos, A.C.,. Yasuma,
T., Akira, K., Masahiro, K., Hiroyuki, T., Pratt, S. Corrette, C. PCT. Int. Appl. 2004
WO2004017908.

Nitrogen Containng Fused Heterocyclic Compounds, Gyorkos, A.C., Pratt, S.A., Corrette, C.P.,
Cho, S.Y., Turner, T., International Patent Application filed October , 2004.
Calcium Receptor Modulating Compounds and Use Thereof Gyorkos, A.C., Pratt, S.A.,
Corrette, C.P., Yoshida, M., Kimura, H., Kawase, M., Mori, A.,Yasuma, T. International Patent
WO2004/017908. Issued March 4, 2004.

Regioselective Synthesis of DTPA Derivatives. Gyorkos, A.C., LeBarre, M., Ruhl, S.,
Ryskamp, T. International Patent WO2000/051976.

Preparation of Heterocyclic Compounds as Serine Protease Inhibitors. Gyorkos, A., Spruce,
L.W. United States Patent 6015791. Issued Jan 18, 2000.

Human Neutrophil Elastase Inhibitors. Gyorkos, A.C., Spruce, L.W. United States Patent
5,618,792. Issued Apr. 8, 1997. International Patent Application WO96/16080. Issued May
30, 1996.

Preparation of Peptoid and Nonpeptoid Containing a-Keto Oxadiazoles as Serine Protease
Inhibitors. Gyorkos, A., Spruce, L., Ohmoto, K., Kawabata, K. United States Patent 6255453.
Issued July 3, 2001.

Serine Protease Inhibitors -Tripeptoid Analogs Gyorkos, A.C., Spruce, L.W. United States
Patent 5807829. Issued Sept. 15, 1998.

Serine Protease Inhibitors -Proline Analogs. Gyorkos, A.C., Spruce, L.W. United States Patent
5801148. Issued Sept. 01, 1998.

Serine Protease Inhibitors-Keto and Di-Keto Containing Ring Systems. Gyorkos, A.C., Spruce,
L.W., Leimer, A. United States Patent 5861380. Issued Jan. 19, 1999.

Serine Protease Inhibitors -N-Substituted Derivatives. Gyorkos, A.C., Spruce, L.W., Leimer, A.
United States Patent 5869455. Issued Feb. 09, 1999.

Substituted Heterocyclic Compounds Useful as Inhibitors of (Serine Proteases) Human
Neutrophil Elastase. Gyorkos, A.C., Spruce, L.W. United States Patent 5874585. Issued Feb.
23, 1999.

Serine Protease Inhibitors -Cycloheptane Derivatives. Gyorkos, A.C., Spruce, L.W., Leimer, A.
United States Patent 5891852. Issued Apr. 06, 1999.

Preparation of a-Keto Heterocycles as Serine Protease Inhibitors. Gyorkos, A.C., Spruce,
L.W., Leimer, A.H., Cheronis, J.C. United States Patent 6159938 Issued Dec. 12, 2000.

Preparation of Indoles and Tetrahydroisoquinolines Containing a-Keto Oxadiazoles as Serine
Protease Inhibitors. Gyorkos, A.C., Spruce, L.W.. United States Patent 6100238. Issued
August 8, 2000.

Preparation of N-substituted Prolinyl Peptide Analogs as Serine Protease Inhibitors. Gyorkos,
A., Spruce, L.W. United States Patent 6001811 Issued Dec. 14, 1999.

Serine Protease Inhibitors Comprising a-Keto Heterocycles. Gyorkos, A.C., Spruce, L.W.,
Leimer, A. CIP of U.S. Serial No. 08/345,820 filed November, 21, 1994.

Preparation of Heterocyclyl Peptide Derivatives as Cysteine Protease Inhibitors Spruce, L.W.,
Gyorkos, A.C., Cheronis, J.C., Goodfellow, V.S., Leimer, A.H.,Young, J.M., Gerrity, J.I.
WO9954317 Issued Oct. 10, 1999.

Preparation of Oxadiazolylcarbonylmethylaminomethylpyrimidinones as Serine Protease
Inhibitors. Gyorkos, A.C., Spruce, L.W. United States Patent 6001814 Issued Dec. 14, 1999.

Preparation of Val-Pro Containing Oxadiazoles as Serine Protease Inhibitors. Gyorkos, A.C.,
Spruce, L.W. United States Patent 6001813 Issued Dec. 14, 1999.

Preparation of Substituted Oxadiazole Peptide Derivatives as Cysteine Protease Inhibitors.
Gyorkos, A.C., Spruce, L.W. , Goodfellow V.S., Leimer, A., Cheronis, J.C., Young, J.M.,
Gerrity, J.I. United States Patent 6004933. Issued December 21, 1999.

Preparation of N-substituted Derivatives of Azole Heterocyclic Peptoids as Serine Protease
Inhibitors. Gyorkos, A.C., Spruce, L.W. United States Patent 5869455 Issued Feb. 9, 1999.

Preparation of Fused Cycloheptane Azole Heterocyclic Peptoids as Serine Protease Inhibitors.
Gyorkos, A.,. Spruce, L.W. United States Patent 5891852 Issued April 6, 1999.

Preparation of Peptidyl a-Keto Oxadiazoles as Serine Protease Inhibitors. Gyorkos, A., Spruce,
L. WO9962538 Issued Dec. 9, 1999.

Preparation of Azole Heterocyclic Peptoids as Serine Protease Inhibitors. Gyorkos, A., Spruce,
L.W. United States Patent 5807829 Issued Sept. 15, 1998.

Preparation of Tripeptoid Analogs as Serine Protease Inhibitors. Gyorkos A.C., Spruce, L.W.
United States Patent 6150334 Issued Nov. 21, 2000.

Preparation of Proline Analog Peptides as Serine Protease Inhibitors. Gyorkos, A., Spruce,
L.W. United States Patent 5801148 Issued Sept. 1, 1998.

Preparation of Oxadiazole Peptide Analogs as Serine Protease Inhibitors. Gyorkos, A., Spruce,
L.W. WO9824806 Issued June 11, 1998.

Preparation of Prolinyl Peptide Analogs as Serine Protease Inhibitors. Gyorkos, A., Spruce,
L.W. United States Patent 5998379. Issued Dec. 7, 1999.

Preparation of Azole Containing Peptide Analogs as Human Neutrophil Elastase Inhibitors.
Gyorkos, A., Spruce, L.W. WO9616080 Issued May 30, 1996.

Preparation of Bradykinin Antagonists Component Covalently Linked to a-Opiod Agonists.
Cheronis, J.C., Gyorkos, A.C., Spruce, L.W., Whalley, E.T. CIP of U.S. Serial No. 296,185.

Compounds Having Bradykinin Antagonistic Activity and a-Opiod Agonistic Activity.
Cheronis, J.C., Gyorkos, A., Spruce, L.W., Whalley, E.T. WO9639425 Issued Dec. 12, 1996.

Bradykinin Antagonists in Human Systems: Correlation Between Receptor Binding, Calcium
Signaling in Isolated Cells, and Functional Activity in Isolated Ileum. Wieczorek, M.;
Pilyavskaya, A.; Burkard, M.; Zuzack, J.; Jones, S.; Francis, M.; Beckey, V.; Ross, S.; Selig,
W.; John, M.; Gera, L.; Whalley, E.; Spruce, L.; Gyorkos, A. Biochem. Pharmacol. 1997,
54(2), 283.

Biochemical Characterization of a-Ketooxadiazole Inhibitors of Elastases. Gyorkos, A.;
Wieczorek, M.; Spruce, L.; Ettinger, A; Ross, S.; Kroona, H.; Burgos-Lepley, C.; Bratton, L.;
Drennan, T.; Garnert, D.; Von Burg, G.; Pilkington, C.; Cheronis, J.C., Archives of Biochemistry
and Biophysics 1999, 367, 193.

Preparation of N,N-Bis[2-[N’,N’-bis[(tert-butoxycarbonyl)methyl]-amino]ethyl]-L-aspartic acid:
an Intermediate in the Synthesis of MRI Contrast Agents, Amedio, J.C.; Van Wagenen, G.;
Zavlin, G.; Gyorkos, A.; Peterson, S. Synthetic Communications 2000, 30, 3755.

Design and Synthesis of New Orally Active Nonpeptidic Inhibitors of Human Neutrophil
Elastase. Ohmoto, K.; Yamamoto, T.; Horiuchi, T.; Imanishi, H.; Odagaki, Y.; Kawabata, K.;
Sekioka, T.; Hiroto, Y.; Matsuoka, S.; Nakai, H.; Toda, M.; Cheronis, J.C.; Spruce, L.W.;
Gyorkos, A.; Wieczorek, M. J. Med. Chem. 2000, 43, 4927.

Development of Orally Active Nonpeptidic Inhibitors of Human Neutrophil Elastase. Ohmoto,
K.; Yamamoto, Okuma; M., Horiuchi; T.,Imanishi; H., Odagaki, Y.; Kawabata, K.; Sekioka, T.;,
Tomohiko, H.; Yasushi, M.; Matsuoka, S.; Nakai, H.; Toda, M.; Cheronis, J.; Spruce, L.;
Gyorkos, A.; Wieczorek M. J. Med. Chem. 2001, 44, 1268.

Design and Synthesis of Benzimidazoles as Novel Corticotropin Releasing Factor 1 Receptor
Antagonists, Mochizuki, M.; Kori, M.; Kobayashi, K.; Yano, T.; Sako, Y.; Tanaka, M.; Kanzaki,
N.; Gyorkos, A.C.; Corrette, C.P.; Cho, S. J. Med. Chem. 2016, 59, 2551.

Discovery of a 7-Arylaminobenzimidazole Series as Novel CRF 1 Receptor Antagonists,
Mochizuki, M.; Kori, M.; Kono, M.; Yano, T.; Sako, Y.; Tanaka, M.; Kanzaki, N.; Gyorkos, A.;
Corrette, C.; Aso, K. Biorg. Med. Chem., 2016, 24, 4675..