Recent patents in antifungal agent discovery

Expert Opinion on Therapeutic Patents

Volumn 18, Issue 3, 2008, Pages 275-292

  Di Santo, Roberto ^a  

^a SAPIENZA UNIVERSITY OF ROME   (Italy)

Author keywords

(13) D glucan synthase; 14 lanosterol demethylase; Antifungal agent; Azole; CYP51; Echinocandin; Efflux pump; Geranylgeranyl transferase; Macrolide; Natural product; Peptide; Pmt; Polyene macrolide; Protein mannosyl transferase; Sordarin; Translation elongation factor 2

Indexed keywords

AEROTHRICINE DERIVATIVE; ALBACONAZOLE; AMPHOTERICIN B DEOXYCHOLATE; AMPHOTERICIN B LIPID COMPLEX; ANTIFUNGAL AGENT; ANTIINFECTIVE AGENT; ANTIRETROVIRUS AGENT; BERBERINE; BIFONAZOLE; CLOTRIMAZOLE; CYCLOHEXAPEPTIDYL BISAMINE DERIVATIVE; ECHINOCANDIN; ECHINOCANDIN B; ECONAZOLE; FLUCONAZOLE; IMIDAZOLE DERIVATIVE; ITRACONAZOLE; KETOCONAZOLE; MACROLIDE; MICONAZOLE; MORINIAFUNGIN; NEOPELTOLIDE; POSACONAZOLE; PYRROLE DERIVATIVE; RAVUCONAZOLE; SORDARIN DERIVATIVE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VORICONAZOLE; ZOFIMARIN;

ACQUIRED IMMUNE DEFICIENCY SYNDROME; ANTIFUNGAL ACTIVITY; ASPERGILLUS; CANDIDIASIS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DOSAGE FORM COMPARISON; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; EUKARYOTE; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; MINIMUM INHIBITORY CONCENTRATION; MYCOSIS; NEPHROTOXICITY; NONHUMAN; PATENT; REVIEW; UNSPECIFIED SIDE EFFECT;

EID: 42549146640     PISSN: 13543776     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543776.18.3.275     Document Type: Review

References (96)

1. Vicente MF, Basilio A, Cabello A, Pelaez F. Microbial natural products as a source of antifungals. Clin Microbiol Infect 2003;9:15-32
2. Chakrabarti A. Microbiology of systemic fungal infections. J Postgrad Med 2005;51:16-20
3. Martin GS, Mannino DM, Eaton S, Moss M. The epidemiology of sepsis in the United States from 1979 through 2000. N Engl J Med 2003;348:1546-54
4. Zacchino S, Yunes R, Cechinel Filho V, et al. The need for new antifungal drugs: screening for antifungal compounds with a selective mode of action with emphasis on the inhibitors of the fungal cell wall. In: Rai M, Mares D, editors. Plant-Derived Antimycotics: Current Trends and Future Prospects. Haworth Press, New York; 2003. p. 1-48
5. Ablordeppey S, Fan P, Ablordeppey J, Mardenborough L. Systemic antifungal agents against AIDS-related opportunistic infections: current status and emerging drugs in development. Curr Med Chem 1999;6:1151-95
6. Li D, Calderone R. Antifungal drugs, targets and target discovery. In: San-Blas G, Calderone R, editors. Pathogenic Fungi, Host Interaction and Emerging Strategies for Control. Caister Academic Press, Norfolk; 2004. p. 335-56
7. Boo TW, O'Reilly B, O'Leary J, Cryan B. Candidaemia in an Irish tertiary referral hospital: epidemiology and prognostic factors. Mycoses 2005;48:251-9
8. Groll AH, Mickiene D, Petraitiene R, et al. Pharmacokinetic and pharmacodynamic modeling of anidulafungin (LY303366): reappraisal of its efficacy in neutropenic animal models of opportunistic mycoses using optimal plasma sampling. Antimicrob Agents Chemother 2001;45:2845-55
9. Singh N. Changing spectrum of invasive candidiasis and its therapeutic implications. Clin Microbiol Infect 2001;7(S2):1-7
10. Hazen KC. New and emerging yeast pathogens. Clin Microbiol Rev 1995;8:462-78
11. Hossain MA, Ghannoum MA. New investigational antifungal agents for treating invasive fungal infections. Expert Opin Investig Drugs 2000;9:1797-813
12. Hossain MA, Ghannoum MA. New developments in chemotherapy for non-invasive fungal infections. Expert Opin Investig Drugs 2001;10:1501-11
13. Ng AWK, Wasan KM, Llopez-Berestein G. Development of liposomal polyene antibiotics: an historical perspective. J Pharm Pharm Sci 2003;6:67-83
14. Andes D. In vivo pharmacodynamics of antifungal drugs in treatment of candidiasis. Antimicrob Agents Chemother 2003;47:1179-86
15. Zotchev SB. Palyene macrolide antibiotics and their applications in human therapy. Curr Med Chem 2003;10:211-23
16. Gibbs WJ, Drew RH, Perfect JR. Liposomal amphotericin B: clinical experience and perspectives. Expert Rev Antiinfect Ther 2005;3:167-81
17. Eth Zurich. Preparation of macrolide amphotericin derivatives as antifungal agents. WO07096137 (2007)
18. Vanden Bossche H, Koymans L, Moereels H. P450 inhibitors of use in medical treatment: focus on mechanisms of action. Pharmacol Ther 1995;67:79-100
19. Podust LM, Poulos TL, Waterman MR. Crystal structure of cytochrome P450 14-alpha-sterol demethylase (CYP51) from Mycobacterium tuberculosis in complex with azole inhibitors. Proc Natl Acad Sci USA 2001;98:3068-73
20. Adams JL, Metcalf BW. Therapeutic consequences of the inhibition of sterol metabolism. In: Comprehensive Medicinal Chemistry. Hansch C. Sammes PG. Taylor JB, editors. Pergamon Press, Oxford; 1990. p. 333-64
21. Asai K, Tsuchimori N, Okonogi K, et al. Formation of azole-resistant Candida albicans by mutation of sterol 14-demethylase P450. Antimicrob Agents Chemother 1999;43:1163-9
22. Dawson JH, Sono MI. Cytochrome P-450 and chloroperoxidase: thiolate-ligated heme enzymes. Spectroscopic determination of their active-site structures and mechanistic implications of thiolate ligation. Chem Rev 1987;87:1255-76
23. Odds FC, Brown AJ, Gow NA. Antifungal agents: mechanisms of action. Trends Microbiol 2003;11:272-9
24. Sheehan DJ, Hitchcock CA, Sibley CM. Current and emergine azole antifungal agents. Clin Microbiol Rev 1999;12:40-79
25. Di Santo R. Recent developments in antifungal drug discovery. Ann Rep Med Chem 2006;41:299-315
26. Pitisuttithum P, Negroni R, Graybill JR, et al. Activity of posaconazole in the treatment of central nervous system fungal infections. J Antimicrob Chemother 2005;56:745-55
27. Edmond MB, Wallace SE, Mcclish DK, et al. Nosocomial bloodstream infections in United States hospitals: a three-year analysis. Clin Infect Dis 1999;29:239-44
28. Trick WE, Fridkin SK, Edwards JR, et al. Secular trend of hospital-acquired candidemia among intensive care unit patients in the United States during 1989-1999. Clin Infect Dis 2002;35:627-30
29. Yamazaki T, Kume H, Murase S, et al. Epidemiology of visceral mycoses: analysis of data in annual of the pathological autopsy cases in Japan. J Clin Microbiol 1999;37:1732-8
30. Takeda Chemical Industry Ltd. Preparation of water-soluble triazolium compounds and their use as antifungal agents. JP00086655 (2000)
31. Hoffmann-La Roche AG. N-Substituted carbamoyloxyalkyl-azolium derivatives. WO0132652 (2001)
32. Sankyo Co. Ltd. Pharmaceuticals and antifungal agents containing water-soluble triazoles. JP05263636 (2005)
33. The Board of Governors for Higher Education State of Rhode Island and Providence Plantations. Preparation of azole monosaccharide as antifungal agents. WO05006860 (2005)
34. Korea Research Institute of Chemical Technology. Preparation of triazolylmethanol derivatives as antifungal agents. WO05014583 (2005)
35. Aventis Pharma SA. Novel azole or triazole derivatives, method for preparing same and use thereof as antifungal medicines. WO02090350 (2002)
36. Aventis Pharma SA. Novel azole or triazole derivatives, method for preparing same and use thereof as fungicides. WO02090354 (2002)
37. Ranbaxy Lab Ltd. Azole derivatives as antifungal agents. WO03086271 (2003)
38. Ranbaxy Lab Ltd. Azole compounds as antifungal agents. WO03008391 (2003)
39. Faming Zhuanli Shenqing Gongkai Shuomingshu. Preparation of piperidinyl triazoleethanols as antifungal agents. CN1557808 (2004)
40. SSP Co. Ltd. Novel azole derivative having antifungal activity. WO04108684 (2004)
41. Meiji Seika Kaisha Ltd. Triazole derivatives and antifungal agents containing the same. WO04067537 (2004)
42. Ranbaxy Lab Ltd. Azole derivatives as antifungal agents. WO04018485 (2004)
43. Valgus JM. What's new in antifungals? Curr Infect Dis Rep 2003;5:16-21
44. Groll AH, Walsh TJ. Antifungal chemotherapy: advances and perspectives. Swiss Med Wkly 2002;132:303-11
45. Andes D, Marchillo K, Lowther J, et al. In vivo pharmacodynamics of HMR 3270, a glucan synthase inhibitor, in a murine candidiasis model. Antimicrob Agents Chemother 2003;47:1187-92
46. Debono M, Gordee RS. Antibiotics that inhibit fungal cell wall development. Ann Rev Microbiol 1994;48:471-97
47. Tortes-Rodriguez JM, Carrillo-Muñoz A, Gallach-Bau C, Madrenys N. Susceptibility of Candida species to cilofungin (LY-121019). Mycoses 1989;32:316-8
48. Keating G, Figgitt D. Caspofungin: a review of its use in oesophageal candidiasis, invasive candidiasis and invasive aspergillosis. Drugs 2003;63:2235-63
49. Fromtling RA. Micafungin sodium (FK-463). Drugs Today 2002;38:245-57
50. Arévalo MP, Carrillo-Muñoz A-J, Salgado J, et al. Antifungal activity of the echinocandin anidulafungin (VER002, LY-303366) against yeast pathogens: a comparative study with M27-A microdilution method. J Antimicrob Chemother 2003;51:163-6
51. Eli Lilly & Co. Ring modified cyclic peptide analogs. WO0011023 (2000)
52. Eli Lilly & Co. Preparation of cyclic peptide antifungal agents. US6384013 (2002)
53. Merck & Co. Preparation of cyclohexapeptidyl bisamines as antifungal agents. US6030944 (2000)
54. Cambas Co. Ltd. Preparation of ring modified cyclic peptide analogs as antifungal agents. WO0011023 (2004)
55. Adaptive Therapeutics, Inc. Antifungal therapeutic agents. WO04050685 (2004)
56. Hoffman-La Roche AG. Aerothricin analogs, their preparation and use. WO0005251 (2000)
57. Basilea Pharmaceutica AG. Novel cyclic compounds. WO0153322 (2001)
58. Dominguez JM, Martin JJ. Identification of elongation factor 2 as the essential protein targeted by sordarins in Candida albicans. Antimicrob Agents Chemother 1998;42:2279-83
59. Gómez-Lorenzo MG, García-Bustos JF. Ribosomal P-protein stalk function is targeted by sordarin antifungals. J Biol Chem 1998;273:25041-4
60. Kamai Y, Kakuta M, Shibayama T, et al. Antifungal activities of R-135853, a sordarin derivative, in experimental candidiasis in mice. Antimicrob Agents Chemother 2005;49:52-6
61. Basilio A, Justice M, Harris G, et al. The discovery of moriniafungin, a novel sordarin derivative produced by Morinia pestalozzioides. Bioorg Med Chem 2006;14:560-6
62. Sankyo Co. Ltd. Preparation of oxazepane ring-containing zofimarin derivatives and their use as antifungal agents. JP2003261450 (2003)
63. Sankyo Co. Ltd. Preparation of zofimarin derivatives and their use as antifungal agents. JP2003089684 (2003)
64. Bristol-Myers Squibb Co. Novel thio derivatives of sordarin as antifungal agents. WO0222567 (2002)
65. Glaxo Wellcome SA. Carbocyclic derivatives. WO0134582 (2001)
66. Glaxo Wellcome SA. Antifungal sordaricin derivatives. WO0134583 (2001)
67. Kolman A. Activity of epothilones. Curr Opin Investig Drugs 2005;6:616-22
68. Harbor Branch Oceanographic Institution, Inc. Biologically active neopeltolide compounds. US2004266847 (2004)
69. Kitasato Institute. Novel macrolide derivatives having effect of potentiating antifungal acdvity WO04039823 (2004)
70. Luzhetskyy A, Pelzer S, Bechthold A. The future of natural products as a source of new antibiotics. Curr Opin Investig Drugs 2007;8:608-13
71. Banyu Pharmaceutical Co. Ltd. Sesterpene derivatives exhibiting antifungal activities. WO0008010 (2000)
72. Pfizer Pharmaceutical Co. Ltd. Antifungal agents containing terpenoid lactone, and its manufacture with Codiniaea talboti. JP20000086651 (2000)
73. Toa Gosei Chemical Industry Co. Ltd. Preparation of hydronaphthalenes as antifungal agents and drug intermediates. JP2001026564 (2001)
74. Mercian Co./Eisai Co. Ltd. Novel polycyclic compounds, their use as antifungal agents, and their manufacture with Fumicola species. JP20010354693 (2001)
75. Cernáková M, Kostálová D. Antimicrobial activity of berberine a constituent of Mahonia aquifolium. Folia Microbiol 2002; 47:375-8
76. Newtreeindustry Co. Ltd. New derivatives of berberrubine and their salts for antibiotics and antifungal agents. WO03051875 (2003)
77. Daiichi Seiyaku Co. Ltd. Preparation of tricyclic heterocyclic compounds as antimycotic or antifungal agents. JP2007204458 (2007)
78. Daiichi Seiyaku Co. Ltd. Preparation of bicyclo heterocyclic compounds as antimycotic or antifungal agents. WO07020936 (2007)
79. F2G Ltd. Antifungal agents. WO05092304 (2005)
80. Anadys Pharmaceuticals, Inc. Hydrazone, hydrazine and thiosemicarbazone derivatives as antifungal agents. US6329378 (2001)
81. Bayer Cropscience SA. Mèdicaments antifongiques à base de derives d'arylamidine. EP1413301 (2004)
82. Isis Pharmaceuticals, Inc. Novel pyranosyl cytosines: pharmaceutical formulations and methods. WO03066633 (2003)
83. Kurtz MB, Douglas CM. Lipopeptide inhibitors of fungal glucan synthase. J Med Vet Mycol 1997;35:79-86
84. Willer T, Valero MC, Tanner W, et al. O-mannosyl glycans: from yeast to novel associations with human disease. Curr Opin Struct Biol 2003;13:621-30
85. Oxford Glycosciences (UK) Ltd. Thiazolidine derivatives and its use as antifungal agent WO0222612 (2002)
86. Oxford Glycosciences (UK) Ltd. Thiazolidine antifungal agents. WO03070238 (2003)
87. Oxford Glycosciences (UK) Ltd. Benzylidene thiazolidinediones and their use as antimycotic agents. WO03070239 (2003)
88. Johnston SRD. Farnesyl transferase inhibitors: a novel targeted therapy for cancer. Lancet Oncol 2001;2:18-26
89. Bell IM. Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy? J Med Chem 2004;47:1869-78
90. Banyu Pharmaceutical Co. Ltd. Inhibitor against geranylgeranyltransferase, I-type protein. JP2000204087 (2000)
91. Banyu Pharmaceutical Co. Ltd. Type I protein, geranylgeranyltransferase inhibitory compound. JP2000204078 (2000)
92. Gottesman MM, Pastan I. Biochemistry of multidrug resistance mediated by the multidrug transporter. Ann Rev Biochem 1993;62:385-427
93. Albertson GD, Niimi M, Cannon RD, Jenkinson HF. Multiple efflux mechanisms are involved in Candida albicans fluconazole resistance. Antimicrob Agents Chemother 1996;40:2835-41
94. Parkinson T, Falconer DJ, Hitchcock CA. Fluconazole resistance due to energy-dependent drug efflux in Candida glabrata. Antimicrob Agents Chemother 1995;39:1696-9
95. Essential Therapeutics, Inc. Fungal efflux pump inhibitors. US2003229097 (2003)
96. Essential Therapeutics, Inc. Fungal efflux pump inhibitors. US6596723 (2003)