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Recent US Patents in which Dr MacCoss is an inventor (of 108 total)

posted Feb 3, 2013, 10:14 AM by Malcolm MacCoss   [ updated Feb 21, 2018, 4:59 PM ]

U.S. Patent No. 7,534,767.  “C-purine nucleoside analogs as inhibitors of RNA-dependent RNA viral polymerase”, issued May 19, 2009

U.S. Patent No. 7,632,821.  “Ribonucleoside cyclic acetal derivatives for the treatment of RNA-dependent RNA viral infection” issued December 15, 2009

U.S. Patent No. 7,879,815.  “Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection” issued February 1, 2011

U.S. Patent No. 8,168,637.  “Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of diabetes” issued May 1, 2012

U.S. Patent No. 8,735,414.  “Indole derivatives and methods for antiviral treatment” issued May 27, 2014

U.S. Patent No. 8,809,318.  “Gamma secretase modulators” issued August 19, 2014

U.S. Patent No. 8,859,776 “Substituted piperidines that increase p53 activity and the uses thereof”, issued October 14, 2014

U.S. Patent No. 9,433,621  “Substituted pyridine and pyrimidine derivatives and their use in treating viral infections”, issued September 6, 2016

U.S. Patent No. 9,593,108  “Compounds and methods for antiviral treatment”, issued March 14, 2017

U.S. Patent No. 9,890,174 “Fused tricyclic benzimidazole derivatives as modulators of TNF activity”, issued February 13, 2018

WO 2016/050975  “Fused pentacyclic imidazole derivatives”, published April 7, 2016.

WO 2017/020010  “Bis-Heteroaryl derivatives as modulators of protein aggregation”, published February 2, 2017


Recent publications authored or co-authored by Dr. MacCoss (of 177 in total)

posted Jul 18, 2012, 6:31 PM by Malcolm MacCoss   [ updated Feb 21, 2018, 5:52 PM ]

Carroll, S.S., Koeplinger, K., Vavrek, M., Zhang, N.R., Handt, L., MacCoss, M., Olsen, D.B., Reddy, K.R., Sun, Z., van Poelje, P.D., Fujitaki, J.M., Boyer, S.H., Linemeyer, D.L., Hecker, S.J., and Erion, M.D.  Antiviral efficacy upon administration of a HepDirect prodrug of 2’-C-methylcytidine to Hepatitis C virus-infected chimpanzees.  Antimicrobial Agents and Chemotherapy, 55: 3854 (2011)


Sun, Z.Y., Asberom, T., Bara, T., Bennett, C., Burnett, D.A., Chou, I., Clader, J., Cohen-Williams, M., Cole, D., Czarniecki, M., Durkin, J., Gallo, G., Greenlee, W.J., Josien, H., Huang, X., Hyde, L., Jones, N., Kazakevich, I., Li, H., Liu, X., Lee, J., MacCoss, M., McCracken, T., Nomeir, A., Mazzola, R., Palani, A., Parker, E.M., Pissarnitski, D., Qin, J., Song, L., Terracina, G., Vicarel, M., Voigt, J.H., Xu, R., Zhang, L., Zhang, Q., Zhao, Z., Zhu, X., and Zhu, Z.  Cyclic hydroxyamidines as amide isosteres:  Discovery of oxadiazolines and oxadiazines as potent and highly efficacious g-secretase modulators in vivo.  J. Med. Chem., 55: 489 (2012)


Huang, Y., Bennett, F., Verma, V., Njoroge, F.G., and MacCoss, M.  A notable conversion of a thioacetate to it’s corresponding sulfonyl chloride.  Tetrahedron Letters, 53: 3203 (2012)


Arasappan, A., Bennett, F., Girijavallabhan, V., Huang, Y., Huelgas, R.,Alvarez, C., Chen, L., Gavalas, S., Kim, S-H., Kosinski, A., Pinto, P., Rizvi, R., Rossman, R., Shankar, B., Tong, L., Velazquez, F., Venkatraman, S., Kozlowski, J., Shih, N-Y., Piwinski, J.J., MacCoss, M., Kwong, C.D., Clark, J.L., Fowler, A.T., Geng, F., Kezar III, H.S., Roychowdhury, A., Reynolds, R.C., Maddry, J.A., Ananthan, S., Secrist III, J.A., Cheng, L., Chase, R., Curry, S., Huang, H-C., Tong, X. and Njoroge, G.  5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.  Bioorganic & Med. Chem. Letters, 22: 3229 (2012)


Bennett, F., Kezar III, H.S., Girijavallabhan, V., Huang, Y., Huelgas, R., Rossman, R., Shih, N-Y., Piwinski, J.J., MacCoss, M., Kwong, C.D., Clark, J.L., Fowler, A.T., Geng, F., Roychowdhury, A., Reynolds, R.C., Maddry, J.A., Ananthan, S., Secrist III, J.A., Li, C., Chase, R., Curry, S., Huang, H-C., Tong, X., Njoroge, G. and Arasappan, A.  Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.  Bioorganic & Med. Chem. Letters, 22: 5144 (2012)


Girijavallabhan, V., Alvarez, C., Bennett, F., Chen, L., Gavalas, S., Huang, Y., Kim, S-H., Kosinski, A., Pinto, P., Rizvi, R., Rossman, R., Shankar, B., Tong, L., Velazquez, F., Venkatraman, S., Verma, V.A., Kozlowski, J., Shih, N-Y., Piwinski, J.J., MacCoss, M., Kwong, C.D., Bansal, N., Clark, J.L., Fowler, A.T., Kezar III, H.S., Valiyaveettil, J., Reynolds, R.C., Maddry, J.A., Ananthan, S., Secrist III, J.A., Cheng, L., Chase, R., Curry, S., Huang, H-C., Tong, X., Njoroge, G. and Arasappan, A.  Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors.  Bioorganic & Med. Chem. Letters, 22: 5652 (2012)


Verma, V.A., Rossman, R., Bennett, F., Chen, L., Gavalas, S., Girijavallabhan, V., Huang, Y., Kim, S-H., Kosinski, A., Pinto, P., Rizvi, R., Shankar, B., Tong, L., Velazquez, F., Venkatraman, S., Kozlowski, J., MacCoss, M., Kwong, C.D., Bansal, N., Kezar III, H.S., Reynolds, R.C., Maddry, J.A., Ananthan, S., Secrist III, J.A., Cheng, L., Chase, R., Curry, S., Huang, H-C., Tong, X., Njoroge, G. and Arasappan, A.  Synthesis and SAR of germinal substitutions at the C5’ carbosugar position of pyrimidine-derived HCV inhibitors.  Bioorganic & Med. Chem. Letters, 22: 6967 (2012).


M. MacCoss, “Introduction: Drug Discovery in Difficult Times” in “Case Studies in Modern Drug Discovery and Development”, editors: Xianhai Huang and Robert Aslanian, John Wiley & Sons, Inc, Hoboken, NJ, 2012.


M. MacCoss, “A Career in Medicinal Chemistry - A Journey in Drug Discovery“, Annual Reports in Medicinal Chemistry, 23-34, 48, 2013.


Taylor, R., MacCoss, M. and Lawson, A.  Rings in drugs.  J. Med. Chem., 57: 5845 (2014)

Taylor, R., MacCoss, M. and Lawson, A.  Combining Molecular Scaffolds from FDA Approved Drugs: Application to Drug DiscoveryJ. Med. Chem., 60: 1638 (2016)

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Elbert, B.L., Farley, A.J.M., Gorman, T.W., Johnson, T.C., Genicot, C., Lallemand, B., Pasau, P., Flasz, J., Castro, L., MacCoss, M., Paton, R., Schofield, C.J., Smith, M.D., and Dixon, D.J., Willis, M.C.  A General C-H Cyanation of 6-Ring N-containing Heteroaromatics.  Chemistry – a European J., 23: 14,733 (2017).

 Johnson, T.C., Elbert, B.L., Farley, A.J.M., Gorman, Genicot, C., T.W., Lallemand, B., Pasau, P., Flasz, J., Castro, L., MacCoss, M., Dixon, D.J.,  Paton, R., Schofield, C.J., Smith, M.D., and Willis, M.C.  Direct Sulphonylation of Anilines Mediated by Visible Light.  Chemical Science, 9: 629 (2018).

 Lawson, A.D.G., MacCoss, M., and Heer, J.P.  On the Importance of Rigidity in Designing Small Molecules to Tackle the Problem of Inhibution of Protein-Protein Interactions (PPIs).  J. Med. Chem., doi: 10.1021/acs.jmedchem.7b01120. (2017) 

 

 


Dr. MacCoss awarded the 2010 ACS Division of Medicinal Chemistry National Award

posted Feb 9, 2012, 8:48 AM by Malcolm MacCoss   [ updated Feb 3, 2013, 10:02 AM ]


Dr. MacCoss inducted into the ACS Hall of Fame, 2009

posted Feb 8, 2012, 10:19 AM by Michael MacCoss   [ updated Feb 9, 2012, 8:51 AM by Malcolm MacCoss ]

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