@@Update 4-14

Publications

  1. Akama, T.; Dong, C.; Virtucio, C.; Sullivan, D.; Zhou, Y.; Zhang, Y-K.; Rock, F.; Freund, Y. R.; Bu, W.; Wu, A.; Liu L.; Fan, X-Q.; Jarnagin, K.  Linking phenotype to kinase: Identification fo a novel benzoxaborole hinge binding motif for kinase inhibition and the development of high potency rho-kinase inhibitors.  J. Phram. Exp. Ther. 2013, 347(3), 615625. 

  2. Akama, T.; Dong, C.; Virtucio, C.; Freund, Y. R.,; Chen, D.; Orr, M.D.; Jacobs, R.T.; Zhang, Y-K.; Hernandez, V.; Liu, Y.; Wu, A.; Liu L.; Jarnagin, K.; Plattner, J. J.  Discovery and structure–activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents.  Bioorg. Med. Chem. Lett.  2013, 23, 5870–5873.

  3. Hernandez, V.; Crepin, T.; Palencia, A.; Cusack, S.; Akama, T.; Baker, S. J.; Bu .W.; Feng, L.; Freund, Y. R.; Liu, L.; Meewan, M.; Mohan, M.; Mao, W.; Rock, F. L.; Sexton, H.; Sheoran, A.; Zhang, Y.; Zhang, Y-K.; Zhou, Y.; Nieman, J. A.; Anugula, M. R.; Keramane, E. M.; Savariraj, K.; Redy, D. S.; Sharma, R.; Subedi, R.; Singh, R.; OfLeary, A.; Simon, N. L.; De Marsh, P. L.; Mushtag, S.; Warner, M.; Livermore, D. M.; Alley, M. R. K.; Plattner, J. J.  Discovery of a novel class of boron-based antibacterials with activity against gram-negative bacteria.  Antimicrob. Agents Chemither.  2013, 57(3), 1394–1403.

  4. Akama, T.; Virtucio, C.; Dong, C.; Kimura, R.; Zhang, Y-K.; Nieman, J. A.; Shamra, R.; Lu, X.; Sales, M.; Singh, R.; Wu, A.; Fan, X-Q.; Liu, L.; Plattner, J. J.; Jarnagin, K.; Freund, Y. R.  Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent.  Bioorg. Med. Chem. Lett.  2013, 23, 1680–1683.

  5. Freund, Y. R.; Akama, T.; Alley, M. R. K.; Antunes, J.; Dong, C.; Jarnagin, K.; Kimura, R.; Nieman, J. A.; Maples, K. R.; Plattner, J. J.; Rock, F.; Sharma, R.; Singh, R.; Sanders, V.; Zhou, Y.; Boron-based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center.  FEBS Lett.  2012, 586, 3410–3414.

  6. Bu, W.; Akama, T.; Chanda, S.; Sullivan, D.; Ciaravino, V.; Jarnagin, K.; Freund, Y.; Sanders, V.; Chen, C-W.; Fan, X.; Heyman, I.; Liu, L.  Early rapid identification of in vivo rat metabolism of AN6414, a novel boron-containing PDE4 inhibitor by QTRAP LC/MS/MS to support drug discovery.  J. Pharm. Biomed. Anal.  2012, 70, 344–353.

  7. Jacobs, R. T.; Nare, B.; Wring, S. A.; Orr, M. D.; Chen, D.; Sliger, J. M.; Jenks, M. X.; Noe, R. A.; Bowling, T. S.; Mercer, L. T.; Rewerts, C.; Gaukel, E.; Owens, J.; Parham, R.; Randolph, R.; Beaudet, B.; Bacchi, C. J.; Yarlett, N.; Plattner, J. J.; Freund, Y.; Ding, C.; Akama, T.; Zhang, Y-K.; Brun, R.; Kaiser, M.; Scandale, I.; Don, R.  SCYX-7157, an Orally- Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosimiasis.  PLoS Negrected Tropical Diseases, 2011, 5(6), e1151.

  8. Zhang, Y-K.; Plattner, J. J.; Akama, T.; Baker, S. J.; Hernandez, V. S.; Sanders, V.; Freund, Y.; Kimura, R.; Bu W.; Hold, K. M.; Lu, X-S.  Design and synthesis of boron-containing PDE4 inhibitors using soft-drug strategy for potential dermatologic anti-inflammatory application.  Bioorg. Med. Chem. Lett.  2010, 20, 22702274.

  9. Baker, S. J.; Ding, C. Z.; Akama, T.; Zhang, Y-K.; Hernandez, V. S.; Xia, Y.  Therapeutic potential of boron-containing compounds. (Review)  Future Med. Chem. 2009, 1(7), 1275–1288.

  10. Akama, T.; Baker, S. J.; Zhang, Y-K.; Hernandez, V. S.; Zhou, H.; Sanders, V.; Freund, Y.; Kimura, R.; Maples, K. R..; Plattner, J. J.  Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the topical treatment of psoriasis and atopic dermatitis.  Bioorg. Med. Chem. Lett.  2009, 19(8), 2129–2132.

  11. Hui, X.; Baker, S. J.; Wester, R. C.; Barbadillo, S.; Cashmore, A. K.; Sanders, V.; Hold, K. M.; Akama, T.; Zhang, Y-K.; Plattner, J. J.; Maibach, H. I.  In vitro penetration of a novel oxaborole antifungal (AN2690) into the human nail plate.  J. Pharm. Sci.  2007, 96, 2622–2631.

  12. Baker, S. J.; Zhang, Y-K.; Akama, T.; Wheeler, C.; Plattner, J. J.; Rosser, R. M.; Reid, R. P.; Nixon, N. S.  Synthesis of isotopically labeled (3-14C)- and (3,3-2H2)-5-fluoro, 1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), a new antifungal agent for the potential treatment of onychomycosis.  J. Label. Compd. Radiopharm., 2007, 50, 245–250.

  13. Rock, F. L.; Mao, W.; Yaremchuk, A.; Tukalo, M.; Crépin, T.; Zhou, H.; Zhang, Y-K.; Hernandez, V.; Akama, T.; Baker, S. J.; Plattner, J. J.; Shapiro, L.; Martinis, S.; Benkovic, S. J.; Alley, M. R. K.  An Antifungal Agent Inhibits an Aminoacyl-tRNA Synthase by Trapping tRNA in the Editing Site.  Science, 2007, 316, 1759-1761.

  14. Baker, S. J.; Akama, T.; Zhang, Y-K.; Sauro, V.; Pandit, C.; Singh, R.; Kully, M.; Khan, J.; Plattner, J. J.; Benkovic, S. J.; Lee, V.; Maples, K.  Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases.  Bioorg. Med. Chem. Lett.  2006, 16, 5963–5967.

  15. Baker, S. J.; Zhang, Y-K.; Akama, T.; Lau A.; Zhou, H.; Hernandez, V.; Mao, W.; Alley, M. R. K.; Sanders, V.; Plattner, J. J.  Discovery of a New Boron-Containing Antifungal Agent, 5-Fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), for the Potential Treatment of Onychomycosis.  J. Med. Chem.  2006, 49, 4447–4450.

  16. Benkovic, S. J.; Baker, S. J.; Alley, M. R. K.; Woo, Y-H.; Zhang, Y-K.; Akama, T.; Mao, W.; Bavoval, J.; Rajagopalan, P. T. R.; Wall, M.; Kahng, L. S.; Tavassoli, A.; Shapiro, L.  Identification of Borinic Esters as Inhibitors of Bacterial Cell Growth and Bacterial Methyltransferases, CcrM and MenH.  J.  Med. Chem.  2005, 48, 7468–7476.

  17. Agatsuma, T.; Akama, T.; Nara, S.; Matsumiya, S.; Nakai, R.; Ogawa, H.; Otaki, S.; Ikeda, S.; Saitoh, Y.; Kanda, Y.  UCS1025A and B, New Antitumor Antibiotics from the Fungus Acremonium Species.  Org. Lett.  2002, 12, 4387–4390.

  18. Akama, T.; Ishida H.; Kimura, U.; Gomi, K.; Saito, H.  Structure­-Activity Relationships of the 7-Substituents of 5,4f-Diamino-6,8,3f-triflioroflavone, A Potent Antitumor Agent.  J. Med. Chem.  1998, 41, 2056-2067.

  19. Akama, T.; Ueno, K.; Saito, H.; Kasai, M.  Synthesis of an Ethyl 6-Amino-3,5-difluorosalicylate Derivative by Sequential Regioselective Directed ortho-Metalation; A Practical Synthesis of 4f,5-Amino-3f,6,8-trifluoroflavone, A Potent Antitumor Agent.  Synthesis, 1997, 1446-1450.

  20. Akama, T.; Ishida, H.; Shida, Y.; Kimura, U.; Gomi, K.; Saito, H.; Fuse, E.; Kobayashi, S.; Yoda, N.; Kasai, M.  Design and Synthesis of Potent Antitumor 5,4f- Aminoflavone Derivatives Based on Metabolic Considerations.  J. Med. Chem.  1997, 40, 1894-1900.

  21. Akama, T.; Shida, Y.; Sugaya, T.; Ishida, H.; Gomi, K.; Kasai, M.  Novel 5-Aminoflavone Derivatives as Specific Antitumor Agents in Breast Cancer.  J. Med. Chem.  1996, 39(18), 3461-3469.

  22. Hagiwara, H.; Akama, T.; Okano, A.; Uda, H.  Annulation by Sequential Double Michael Reaction; Synthesis of Decalones and Its Application to the Synthesis of e-Cadinene, Khusitone, and Khusilal.  J. Chem. Soc., Perkin Trans. 1 1993, 2173-2184.

  23. Hagiwara, H; Akama, T.; Okano, A.; Uda, H.  Assymmetric Two-fold Michael Reaction.  Synthesis of Optically Active 4-Substituted 1-Decalones from Trimethylsilyl Enol Ether of 1-Acetylcyclohexene.  Chem. Lett.  1989, 2149-2152.

  24. Hagiwara, H; Akama, T.; Okano, A.; Uda, H.  Synthesis of (})-Khusial.  Chem. Lett.  1988, 2067-2068.

  25. Hagiwara, H; Akama, T.; Okano, A.; Uda, H.  Synthesis of Substituted 2-Decalones from 1-Acetylcyclohexenes and a-Trimethylsilyl ab-Unsaturated Carbonyl Compounds by Two-fold Michael Reactions.  Synthesis of (})-Khusitone.  Chem. Lett.  1988, 1793-1796.

  26. Hagiwara, H.; Okano, A.; Akama, T.; Uda, H.  Lewis Acid Assisted Annelation of Trimethylsilyl Enol Ethers of 1-Acetylcyclohexenes with ab-Unsaturated Carbonyl Compounds to Give Substituted 2-Decalones; Synthesis of (})-e-Cadinene.  J. Chem. Soc., Chem. Commun.  1987, 1333-1335.

 

Patents

  1. Akama, T.; Balko, T. W.; Defauw, J. M.; Plattner, J. J.; White, W. H.; Winkle, J. R.; Zhang, Y-K.; Zhou, Y.  Boron-containing small molecules.  US2013/0131017 A1, 2013.

  2. Akama, T.; Balko, T. W.; Defauw, J. M.; Plattner, J. J.; White, W. H.; Winkle, J. R.; Zhang, Y-K.; Zhou, Y.  Boron-containing small molecules.  US2013/0131016 A1, 2013.  

  3. Jarnagin, K.; Akama, T.  Boron-containing small molecules. WO 2011094450, 2011.

  4. Hernandez, V. S.; Li, X.; Zhang, S.; Akama, T.; Zhang, Y.; Liu, Y.; Plattner, J. J.; Alley, M. R. K.; Zhou, Y.; Nieman, J. A.  Boron-containing small molecules.  US2011/0172187 A1, 2011.

  5. Zhou, Y.; Zhang, Y-K.; Akama, T.; Jarangin, K.  Boron-containing small molecules.  US2011/0166104 A1, 2011

  6. Hernandez, V. S.; Li, X; Zhang, S.; Akama, T.; Zhang, Liu., Y., Plattner, J. J.; Alley, M. K. R.; Zhou, Y.; Nieman, J.  Preparation of Boron-containing small molecules useful for treating bacterial infections.  WO 2011069196, 2011

  7. Hernandez, V. S.; Li, X; Zhang, S; Akama, T.; Zhang, Liu, Y., Y.; Plattner, J. J.; Alley, M. K. R.; Zhou, Y.; Nieman, J.  Boron-containing small molecules.  WO 2011060199, 2011

  8. Zhou, Y.; Zhang, Y-K.; Akama, T.; Jarnagin, K.  Preparation of 6-((aminomethyl)phenoxy)-1,3-dihydro-1-hydroxybenzoxaborole derivatives as inhibitors of pro-inflammatory cytokines and phosphodiesterases useful in the treatment of inflammatory diseases.  WO 2010028005 A1, 2010

  9. Akama, T.; Plattner, J. J.  Preparation of 5-amino-1,3-dihydro-1-hydroxybenzoxaborole derivatives as inhibitors of pro-inflammatory cytokines and phosphodiesterases useful in the treatment of inflammatory diseases.  WO 2010027975 A1, 2010.

  10. Xia, Y.; Alley, M. R. K.; Zhou, Y.; Hernandez, V. S.; Plattner, J. J.; Ding, C. Z.; Cao, K.; Zhang, Y-K.; Akama, T.; Sliger, J.; Benowits, A.; Jia, G.; Ou, L.; Saraswat, N.; Ramachandran, S.; Diaper, C.; Zhang, Y.; Banda, G. G.; Nieman, J.; Keramane, M.; Mohammad, R.; Subedi, R.; Liang, H.; Singh, R.  Boron-containing small molecules for treating bacterial infections.  WO 2009140309 A2, 2009.

  11. Akama, T.; Zhang, Y-K.; Ding, C. Z.; Plattner, J. J.; Maples, K. R.; Freund, Y.; Sanders, V.; Xia, Y.; Baker, S. J.; Nieman, J. A.; Lu, X.; Sales, M.; Sharma, R.; Singh, R.; Jacobs, R.; Chen, D.; Alley, M. R. K.  Preparation of boron-containing small molecules as anti-inflammatory agents.  WO 2009111676 A2, 2009.

  12. Baker, S. J.; Akama, T.; Bellinger-Kawahara, C.; Hernandez, V. S.; Hold, K. M.; Leiden, J. J.; Maples, K. R.; Plattner, J. J.; Sanders, V.; Zhang, Y-K.  Boron-containing small molecules for topical treatment of fungal infections.  U.S. Pat. 7,582,621 B2, 2009.

  13. Baker, S. J.; Hernandez, V. S; Sharma, R.; Nieman, J. A.; Akama, T.; Zhang, Y-K.; Plattner, J. J.; Alley, M. R. K.; Singh, R.; Rock, F.; Boron-containing small molecules  WO 2008157726 A1, 2008.

  14. Akama, T.; Baker, S. J.; Hernandez, V. S.; Plattner, Jacob, J.; Zhang, Y-K.; Zhou, H.;  Microorganism killing compounds.  WO 2008064345 A2, 2008.

  15. Lee, V.; Plattner, J. J.; Benkovic, S. J.; Baker, S. J.; Maples, K. R.; Bellinger-Kawahara, C.; Akama, T.; Zhang, Y-K.; Singh, R.; Sauro, V. A.  Hydrolytically-resistant boron containing therapeutics and methods of use.  US Pat. 7,465,836 B2, 2008.

  16. Lee, V.; Benkovic, S. J.; Baker, S. J.; Maples, K. R.; Akama, T.; Zhang, Y-K.; Singh, R.; Sauro, V. A.; Pandit, C.; Su, Z.; Yang, Z.  Antibiotics containing borinic acid complexes and methods of use.  U.S. Pat. 7,390,806 B2, 2008. 

  17. Baker, S. J.; Sanders, V.; Akama, T.; Bellinger-Kawahara, C., Freund, Y.; Maples, K. R.; Plattner, J. J.; Zhang, Y-K.; Zhou, H.; Hernandez, V. S.  Boron-containing small molecules as anti-inflammatory agents.  WO 2007095638 A2, 2007.

  18. Baker, S. J.; Akama, T.; Alley, M. R. K.; Benkovic, S. J.; DiPierro, M.; Hernandez, V. S.; Hold, K. M.; Kennedy, I.; Likhotvorik, I.; Mao, W.; Maples, K. R.; Plattner, J. J.; Rock, F.; Sanders, V.; Stemphoski, A. M.; Yiannikouros, G. P.; Zegar, S.; Zhang, Y-K.; Zhou, H.;  Boron-containing small molecules.  WO 2006089067 A2, 2007.

  19. Harley, C. B.; Chin, A. C.; Akama, T.; Ip, N. Y.; Wong, Y.; Miller-Martini, D. M.  Comositions and Methods for Skin Conditioning Using Astragenols, Cycloastragenols, and/or Protopanaxatriols.  WO 2005000248, 2005.

  20. Harley, C. B.; Chin, A. C.; Akama, T.; Ip, N. Y.; Wong, Y.; Miller-Martini, D. M.  Compositions and Methods for Increasing Telomerase Activity.  WO 2005000245, 2005.

  21. Chin, A. C.; Holcomb, R.; Piatyszek, M.; Singh, U.; Tolman, R.; Akama, T.; Kanda, Y.; Asai, A.; Yamashita, Y.; Endo, K.; Yamaguchi, H.  Telomerase Inhibitors and Methods of Their Use.  US 6518268, 2003.

  22. Snader, K. M.; Vishnuvajjala, R. B.; Akama, T.  Aminoflavone Compounds, Compositions, and Methods of Use Thereof.  WO 02/081462, 2002.

  23. Akama, T.; Holcomb, R.; Tolman, R.  Telomerasee Inhibitors and Methods of Their Use.  WO 02/51409, 2002.

  24. Akama, T.; Kanda, Y.; Asai, A.; Yamashita, Y.; Kitamura, Y.; Murakata C.; Komatsu, K.; Kishikawa, K.; Kobayashi, Y.; Sasho, S.  Thiazolidinedione Derivatives.  WO 01/30771, 2001.

  25. Akama, T.; Asai, A.; Nara, S.; Yamashita, Y.; Agatsuma, T.; Mizukami, T.; Ikeda, S.; Saitoh, Y.  UCS1025 Derivatives.  WO 01/29043, 2001.

  26. Yamashita, Y.; Asai, A.; Hasegawa, A.; Yamaguchi, H.; Akama, T.; Endo, K.; Akinaga, S.; Ishida, H.; Nara, S.; Kanda, Y.; Mizukami, T.  Telomerase Inhibitors.  WO 00/41689, 2000.

  27. Akama, T.; Nagata, H.; Takahashi, I.; Ikeda, S.  2-Acylquinoline Derivatives.  JP2000–128866, 2000.

  28. Akama, T.; Nagata, H.; Hasegawa, A.; Ue, H.; Takahashi, I.; Saitoh, Y.; Mochida, K.; Ikeda, S.; Kanda, Y.  LK6-A Derivatives.  WO 00/02879, 2000.

  29. Akama, T.; Miyata, M.; Ishida, H.; Akinaga, S.; Gomi, K.; Saito, H.  Preparation of Pyranoazine Derivatives Showing Antibacterial, Antiestrogen, and Antitumor Activities.  JP 10–287678, 1998.

  30. Ino, Y.; Kanai, F.; Shiotsu, Y.; Murakami, S.; Murakata, C.; Akama, T.; Yamashita, K.; Akinaga, S.; Tamaoki, T.  Pyrrolocarbazole Derivatives.  WO 98/099.

  31. Kanai, F.; Ikuina, Y.; Murakata, C.; Akama, T.; Shiotsu, Y.; Yamashita, K.; Akinaga, S.; Tamaoki, T.  Preparation of Pyrolophenanthridines and Their Use for Treatment of Thrombocytopenia.  JP 10–­­212289, 1998.

  32. Ikuina, Y.; Kanai, F.; Murakami, S.; Murakata, C.; Akama, T.; Shiotsu, Y.; Yamashita, K.; Akinaga, S.; Tamaoki, T.  Preparation of Pyrolocarbazole Derivatives for the Treatment of Thrombocytopenia.  WO 98/09967, 1998.

  33. Akama, T.; Ikeda, S.; Ishida, H.; Kimura, U.; Gomi, K.; Saito, H.; Ueno, K.  5-Aminoflavone Derivatives with Antiestrogenic, Antibacterial, and Antitumor Activity.  US 5539112, 1996.

  34. Akama, T.; Ikeda, S.; Ishida, H.; Kimura, U.; Gomi, K.; Saito, H.  Preparation of 5-Aminoflavone Derivatives as Antiestrogenic and Antitumor Agents.  EP 638566, 1995.

  35. Akama, T.; Shida, Y.; Ikeda, S.; Kasai, M.; Ishida, H.; Kimura, U.; Gomi, K.; Saito, H.; Ueno K.  5-Aminoflavone Derivative Antibiotics and Antitumor Agents.  EP 556720, 1993.

  36. Shida, Y.; Akama, T.; Ikeda, S.; Kasai, M.; Kamitori, S.; Hirayama, Y.; Ishida, H.; Gomi, K.  Preparation of 5-Aminochromone Derivatives as Neoplasm Inhibitors.  JP 04282380, 1992.

 

 

 

Top