Patents

1. Pyridoza Prostacyclin Analogues and N-Oxides Thereof, K. C. Nicolaou, W. E. Barnette, R. L. Magolda; Serial No. 06/20,543; U.S. Patent No. 4,256,883 issued Mar. 17, 1981.

2. Method for Preparing Cyclic Ethers and Thioethers Including Oxygen Isomers and Sulfur Analogs of Prostacyclin, K. C. Nicolaou, W. E. Barnette, R. L. Magolda, Z. Lysenko; Serial No. 05/886,143; U.S. Patent No. 4,258,199 issued Mar. 24, 1981.

3. Carbocyclic Thromboxane A₂ Analogues, K. C. Nicolaou, R. L. Magolda, D. A. Claremon, Serial No. 06/87,678; U.S. Patent No. 4,260,806 issued Apr. 7, 1981.

4. Pharmaceutically Active 6,9-Thiaprostacyclin Analogs and Derivatives Thereof, K. C. Nicolaou, W. E. Barnette, R. L. Magolda; Serial No. 05/886,141; U.S. Patent No. 4,291,166 issued Sept. 22, 1981.

5. Thromboxane A₂ Analogues, K. C. Nicolaou, R. L. Magolda; Serial No. 06/19,932; U.S. Patent No. 4,308,396 issued Dec. 29, 1981.

6. Bicyclo Aldehyde and Process for Preparation, K. C. Nicolaou, R. L. Magolda, D. A. Claremon; Serial No. 06/194,399; U.S. Patent No. 4,317,935 issued Mar. 2, 1982.

7. Method of Preparing Bicyclo(3.1.1)Hept-2-One, K. C. Nicolaou, R. L. Magolda, D. A. Claremon; Serial No. 06/289,965; U.S. Patent No. 4,429,166 issued Jan. 31, 1984.

8. Leukotriene Analogues, K. C. Nicolaou, N. A. Petasis, S. P. Seitz; Serial No. 06/325,553; U.S. Patent No. 4,442,099 issued Apr. 10, 1984.

9. Leukotriene Analogues, K. C. Nicolaou, N. A. Petasis, S. P. Seitz; Serial No. 06/528,733; U.S. Patent No. 4,567,290 issued Jan. 28, 1986.

10.Alkanoarachidonic Acids, K. C. Nicolaou, N. A. Petasis, W. S. Li, T. Ladduwahetty, J. L. Randall, S. E. Webber, P. E. Hernandez; Serial No. 06/655,196; U.S. Patent No. 4,759,880 issued July 26, 1988.

11. Method of Synthesizing Leukotriene B₄ and Derivatives Thereof, Y. Abe, K. C. Nicolaou; Serial No. 06/165,521; U.S. Patent No. 4,873,024 issued Oct. 10, 1989.

12. Glycolipids, K. C. Nicolaou, T. J. Caulfield; Serial No. /07242,723; U.S. Patent No. 4,977,286 issued Dec. 11, 1990.

13. Sesquiterpene Epoxides and Process for Their Preparation, J. R. Aldrich, J. E. Oliver, K. C. Nicolaou, B. E. Marron; Serial No. 07/168,047; U.S. Patent No. 4,981,981 issued Jan. 1, 1991.

14. Cyclic Conjugated Enediynes, K. C. Nicolaou, G. Zuccarello, Y. Ogawa; Serial No. 07/214,019; U.S. Patent No. 5,097,062 issued Mar. 17, 1992.

15. Method of Synthesizing Leukotriene B₄ and Derivatives Thereof, Y. Abe, K. C. Nicolaou; Serial No. 07/388,990; U.S. Patent No. 5,110,949 issued May 5, 1992.

16. Golfomycin Derivatives: Fused Ring Cyclodecadiyne Derivatives Having DNA-Cleaving Properties and Antitumor Activity, G. Skokotas, K. C. Nicolaou; Serial No. 07/561,964; U.S. Patent No. 5,136,099 issued Aug. 4, 1992.

17. Ten-Membered Ring Enediynediols and Enediynediones Having DNA Cleaving Properties, K. C. Nicolaou, E. Sorensen, C.-K Hwang, R. Discordia, R. G. Bergman, R. E. Minto; Serial No. 07/788,161; U.S. Patent No. 5,183,942 issued Feb. 2, 1993.

18. Phosphene Oxide-Terminated Allene-Ene-Yne DNA Cleaving, Antitumor and Antibiotic Molecules, P. E. Maligres, K. C. Nicolaou; Serial No. 07/561,455; U.S. Patent No. 5,229,375 issued Jul. 20, 1993.

19. Propargylic and Allenic Sulfones, K. C. Nicolaou, G. Zuccarello, S. Skokotas, P. Maligres; Serial No. 07/470,814; U.S. Patent No. 5,237,101 issued Aug. 17, 1993.

20. Cyclic Conjugated Enediynes, K. C. Nicolaou, G. Zuccarello, Y. Ogawa; Serial No. 07/803,618; U.S. Patent No. 5,239,118 issued Aug. 24, 1993.

21. Analogs of Calicheamicin γ₁^I, Method of Making and Using the Same, K. C. Nicolaou, A. L. Smith, C.-K. Hwang, E. Pitsinos; Serial No. 07/915,071, U.S. Patent No. 5,264,586 issued Nov. 23, 1993.

22. Intermediates for Preparation of Taxols, K. C. Nicolaou, C.-K. Hwang, E. J. Sorenson, J.-J. Liu; Serial No. 07/902,390; U.S. Patent No. 5,274,137 issued Dec. 28, 1993.

23. Designed Quinone- and Hydroquinone-Containing Cyclic Enediyneols and Enediyneones Having DNA Cleaving and Cytotoxic Properties, K. C. Nicolaou, A. Liu; Serial No. 07/938,756; U.S. Patent No. 5,274,141 issued Dec. 28, 1993.

24. Dynemicin Analogs: Syntheses, Methods of Preparation and Use, A. L. Smith, C.-K. Hwang, S. Wendeborn, K. C. Nicolaou, E. P. Schreiner, W. Stahl, W.-M. Dai, P. E. Maligres, T. Suzuki; Serial No. 07/886,984; U.S. Patent No. 5,276,159 issued Jan. 4, 1994.

25. Dynemicin Analogs: Synthesis, Methods of Preparation and Use, A. L. Smith, C.-K. Hwang, S. V. Wendeborn, K. C. Nicolaou, E. P. Schreiner, W. Stahl, W.-M. Dai, P. E. Maligres, T. Suzuki; Serial No. 07/939,104; U.S. Patent No. 5,281,710 issued Jan. 25, 1994.

26. Open Chain Enediyne Dihydroperoxides Having DNA Cleaving Properties, K. C. Nicolaou, E. Sorensen, C.-K Hwang, R. Discordia, R. G. Bergman, R. E. Minto; Serial No. 08/010,639; U.S. Patent No. 5,288,761 issued Feb. 22, 1994.

27. Saccharide Intermediates in the Formation of the Calicheamicin and Esperamicin Oligosaccharides, K. C. Nicolaou, R. D. Groneberg, E. P. Schreiner, W. Stahl; Serial No. 07/972,246; U.S. Patent No. 5,384,412 issued Jan. 24, 1995.

28. Daunomycin Derivative with Reduced Cytotoxicity Toward Normal Cells, K. C. Nicolaou, W. A. Wrasidlo, P. E. Maligres; Serial No. 07/922,834, U.S. Patent No. 5,413,992 issued May 9, 1995.

29. Water Soluble Taxol Derivatives, K. C. Nicolaou, C. G. Riemer, M. A. Kerr; Serial No. 08/122,722; U.S. Patent No. 5,422,364 issued Jun. 6, 1995.

30. Access to Taxol Analogs, K. C. Nicolaou, P. G. Nantermet, R. K. Guy, H. Ueno; Serial No. 08/110,095; U.S. Patent No. 5,440,057 issued Aug. 8, 1995.

31. Total Synthesis of Taxol and Taxol Analogs, K. C. Nicolaou, Z. Yang, J.-J. Liu, H. Ueno, P. G. Nantermet; Serial No. 08/197,637; U.S. Patent No. 5,461,169 issued Oct. 24, 1995.

32. Taxoid Synthesis, K. C. Nicolaou, C. F. Claiborne, P. G. Nantermet, E. A. Couladouros, E. J. Sorensen; Serial No. 08/201,926; U.S. Patent No. 5,481,007 issued Jan. 2, 1996.

33. Induction and Inhibition of Apoptosis, K. C. Nicolaou, W. Wrasidlo, A. Hiatt; Serial No. 08/046,626; U.S. Patent No. 5,500,432 issued Mar. 19, 1996.

34. Formation of Esperamicin Precursors, K. C. Nicolaou, D. A. Clark, Serial No. 08/312,106; U.S. Patent No. 5,504,206 issued Apr. 2, 1996.

35. Transformations of Taxol, K. C. Nicolaou, P. G. Nantermet, R. K. Guy, H. Ueno; Serial No. 08/193,263; U.S. Patent No. 5,504,222 issued Apr. 2, 1996.

36. Dynemicin Analogs: Syntheses, Methods of Preparation and Use, A. L. Smith, C.-K. Hwang, S. V. Wendeborn, K. C. Nicolaou, E. P. Schreiner, W. Stahl, W.-M. Dai, P. E. Maligres, T. Suzuki; Serial No. 08/184,580; U.S. Patent No. 5,527,805 issued June 18, 1996.

37. Calicheamicin Mimics, K. C. Nicolaou, E. N. Pitsinos, Serial No. 08/301,968; U.S. Patent No. 5,550,246 issued Aug. 27, 1996.

38. Non-Peptide Peptidomimetics, R. F. Hirschmann, K. C. Nicolaou, S. Pietranico, T. R. Reisine, J. M. Salvino, P. Sprengeler, C. D. Strader; Serial No. 08/144,660; U.S. Patent No. 5,552,534 issued Sept. 3, 1996.

39. Water Soluble Taxol Derivatives, K. C. Nicolaou, C. G. Riemer, M. A. Kerr; Serial No. 08/395,169; U.S. Patent No. 5,608,087 issued Mar. 4, 1997.

40. Daunomycin Derivative with Reduced Cytotoxicity Toward Normal Cells, K. C. Nicolaou, W. A. Wrasidlo, P. E. Maligres; Serial No. 08/423,266, U.S. Patent No. 5,643,887 issued Jul. 1, 1997.

41. Access to Taxol Analogs, K. C. Nicolaou, P. G. Nantermet, R. K. Guy, H. Ueno; Serial No. 08/512,229; U.S. Patent No. 5,750,691 issued May 12, 1998.

42. Taxoid Synthesis, K. C. Nicolaou, C. F. Claiborne, P. G. Nantermet, E. A. Couladouros, E. J. Sorensen; Serial No. 08/527,377; U.S. Patent No. 5,760,240 issued Jun. 2, 1998.

43. Transformations of Taxol, K. C. Nicolaou, P. G. Nantermet, R. K. Guy, H. Ueno; Serial No. 08/626,112; U.S. Patent No. 5,786,489 issued Jul. 28, 1998.

44. Water Soluble Taxol Derivatives, K. C. Nicolaou, C. G. Riemer, M. A. Kerr; Serial No. 08/811,522; U.S. Patent No. 5,817,840 issued Oct. 6, 1998.

45. Analogs of Sarcodictyin and Eleutherobin, K. C. Nicolaou, F. Van Delft, S. Hosokawa, S. Kim, T. Li, T. Ohshima, J. Pfefferkorn, D. Vourloumis, J.-Y. Xu, N. Winssinger; Serial No. 09/145,376; U.S. Patent No. 5,965,718 issued Oct. 12, 1999.

46. Water Soluble Onium Salt of Taxo-Deterpenoid, K. C. Nicolaou, W. Wrasidlo, R. K. Guy, E. Pitsinos; Serial No. 08/817,890; U.S. Patent No. 6,025,491 issued Feb. 15, 2000.

47. Transformations of Taxol, K. C. Nicolaou, P. G. Nantermet, R. K. Guy, H. Ueno; Serial No. 09/123,504; U.S. Patent No. 6,043,382 issued Mar. 28, 2000.

48. Carbopeptoids and Carbonucleotoids, K. C. Nicolaou; Serial No. 08/913,035; U.S. Patent No. 6,204,376 issued Mar. 20, 2001.

49. Chemical Switching of Taxo-Diterpenoids Between Low Solubility Active Forms and High Solubility Inactive Forms, K. C. Nicolaou, W. Wrasidlo, R. K. Guy, E. Pitsinos; Serial No. 08/750,638; U.S. Patent No. 6,252,094 B1, issued Jun. 26, 2001.

50. Self-Assembled Taxo-Deterpenoid Nanostructures, K. C. Nicolaou, W. Wrasidlo, R. K. Guy, E. Pitsinos; Serial No. 08/913,744; U.S. Patent No. 6,271,384 B1, issued Aug. 7, 2001.

51. Epothilone Analogs, K. C. Nicolaou, N. P. King, M. R. Finlay, Y. He, F. Roschangar, D. Vourloumis, S. Ninkovic, D. Hepworth, T. Li; Serial No. 09/102,602; U.S. Patent No. 6,380,394 B1 issued Apr. 30, 2002.

52. Carbopeptoids and Carbo-nucleotoids, K. C. Nicolaou; Serial No. 09/417,877; U.S. Patent No. 6,384,211 B1 issued May 7, 2002.

53. Epothilone Analogs, K. C. Nicolaou, Y. He, S. Ninkovic, J. Pastor, F. Roschangar, F. Sarabia, H. Vallberg, D. Vourloumis, N. Winssinger, Z. Yang, N. P. King, M. R. Finlay; Serial No. 08/923,869; U.S. Patent No. 6,441,186 B1, issued Aug. 27, 2002.

54. Epothilone Derivatives and Their Synthesis and Use, K .C. Nicolaou, N. P. King, M. R. V. Finlay, Y. He, F. Roschangar, D. Vourloumis, H. Vallberg, A. Bigot; Serial No. 09/720,070; U.S. Patent No. 6,531,497 B1 issued Mar. 11, 2003.

55. Epothilone Analogs, K. C. Nicolaou, Y. He, S. Ninkovic, J. Pastor, F. Roschangar, F. Sarabia, H. Vallberg, D. Vourloumis, N. Winssinger, Z. Yang, N. P. King, M. R. Finlay; Serial No. 09/319,885; U.S. Patent No. 6,660,758 B1 issued Dec. 9, 2003.

56. Synthesis of Non-Symmetrical Sulfamides Using Burgess-Type Reagents, K. C. Nicolaou, D. Longbottom, S. A. Snyder, X. Huang; Serial No.10/685,658; U.S. Patent No. 7,015,321 B2 issued Mar. 21, 2006.

57. Analogs of Epothilones, K. C. Nicolaou, A. Ritzén, K. Namoto; Serial No. 10/634,537; U.S. Patent No. 7,169,930 B2 issued Jan. 30, 2007.

58. Epothilone Analogs, K. C. Nicolaou, Y. He, S. Ninkovic, J. Pastor, F. Roschangar, F. Sarabia, H. Vallberg, D. Vourloumis, N. Winssinger, Z. Yang, N. P. King, M. R. V. Finlay; Serial No. 10/732,698; U.S. Patent No. 7,173,137 B2 issued Feb. 6, 2007.

59. Cyclopropyl and Cyclobutyl Epothilone Analogs, K. C. Nicolaou, K. Namoto, A. Ritzén, M. Shoji, T. Ulven, K.-H. Altmann; Serial No. 10/227,073; U.S. Patent No. 7,358,266 B2 issued Apr. 15, 2008.

60. Inhibitors of NADH:Ubiquinone Oxidoreductase, K. C. Nicolaou, J. Pfefferkorn, G.-Q. Cao, A. J. Roecker; Serial No. 10/363,181, U.S. Patent No. 7,410,998 B2, issued Aug. 12, 2008.

61. Epothilone Derivatives and Their Synthesis and Use, K. C. Nicolaou, N. P. King, M. R. V. Finlay, Y. He, F. Roschangar, D. Vourloumis, H. Vallberg, A. Bigot; Serial No. 10/386,999; U.S. Patent No. 7,579,366 B2, issued Aug. 25, 2009.

62. HIF-1 Inhibitors, E. G. Van Meir, C. Tan, A. J. Roecker, K. C. Nicolaou; Serial No. 10/550,286; U.S. Patent No. 7,652,033 issued Jan. 26, 2010.

63. Chemical Synthesis of a Highly Potent Epothilone, K. C. Nicolaou, B. Pratt, S. Arseniyadis; Serial No. 12/092,038; U.S. Patent No. 8,003,801 issued Aug. 23, 2011.

64. HIF-1 Inhibitors, E. G. Van Meir, K. C. Nicolaou; Serial No. 11/977,809; U.S. Patent No. 8,071,795 B2 issued Dec. 6, 2011.

[many of the above patents were also filed in various other countries, as follows: Australia, Canada, Czech Republic, China, Hong Kong, Indonisia, Israel, Japan, Norway, Poland, Russia, Slovak Republic, Spain, and several other European countries].

International PCT Applications

65. Novel Derivatives of Uncialamycin and Methods of Synthesis, K. C. Nicolaou, M. Lu, D. Mandal; International Application No. PCT/US2014/51127, filed August 14, 2014.

66. Synthesis of Δ¹²-PGJ₃ and Related Compounds, K. C. Nicolaou, P. M. Heretsch, C. R. H. Hale, A. El Marrouni El Ghzaoui, K. K. Pulukuri, R. Yu, C. Grove; International Publication No. WO 2015/048268 (based on PCT/US2014/057426, filed September 25, 2014), published April 2, 2015.

67. Preparation of (S,S)-Secoisolariciresinol Diglucoside and (R,R)-Secoisolariciresinol Diglucoside, M. Christofidou-Solomidou, K. C. Nicolaou, R. A. Valiulin, N. Simmons, P. M. Heretsch, International Publication No. WO 2014/200964 (based on PCT/US2014/041636, filed June 10, 2014), published December 18, 2014.

68. Preparation and Biological Evaluation of Viridicatumtoxin Analogs, K. C. Nicolaou, C. R. H. Hale, C. Nilewski, H. A. Ioannidou, A. El Marrouni, International Publication No. PCT/US2015/041494 (based on U.S. Provisional Appl. No. 62/027,500), filed July 22, 2015.

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