Non-peptidic GnRH receptor antagonists

Current Medicinal Chemistry

Volumn 11, Issue 22, 2004, Pages 3017-3028

  Armer, Richard E ^a   Smelt, Kathryn H ^b  

^a Ardana   (France)

^b BioFocus DPI   (United Kingdom)

Author keywords

Agonist; Antagonists; GnRH; LHRH; Non peptidic

Indexed keywords

2 (3,4 DIMETHOXYPHENYL)INDOLE; A 198401; ABARELIX; BENZIMIDAZOLE DERIVATIVE; BUSERELIN; CETRORELIX; DESLORELIN; DIAZEPINE DERIVATIVE; ERYTHROMYCIN DERIVATIVE; FOLLITROPIN; GANIRELIX; GONADORELIN; GONADORELIN AGONIST; GONADORELIN ANTAGONIST; GOSERELIN; HISTRELIN; HYPOTHALAMUS HORMONE; KETOCONAZOLE; LEUPRORELIN; LONG ACTING DRUG; NAFARELIN; NBI 42902; PEPTIDE HORMONE ANTAGONIST; SHORT ACTING DRUG; STEROID; T 98457; TEVERELIX; TK 013; TRIPTORELIN; UNCLASSIFIED DRUG; UNINDEXED DRUG;

BREAST TUMOR; CLINICAL TRIAL; CONTRACEPTION; DRUG BIOAVAILABILITY; DRUG FORMULATION; DRUG MECHANISM; DRUG RECEPTOR BINDING; ENDOMETRIOSIS; GENITAL SYSTEM; HORMONE ACTION; HORMONE RELEASE; HUMAN; INFERTILITY; INFERTILITY THERAPY; NONHUMAN; OVARY DEVELOPMENT; OVARY FOLLICLE; PRECOCIOUS PUBERTY; PREMENSTRUAL SYNDROME; PROSTATE TUMOR; REVIEW; SPERMATOGENESIS; STEROIDOGENESIS; STRUCTURE ACTIVITY RELATION; UTERUS MYOMA;

EID: 5644242134     PISSN: 09298673     EISSN: None     Source Type: Journal    
DOI: 10.2174/0929867043363983     Document Type: Review

References (151)

1. Sealfon, S.C.; Weinstein, H.; Millar, R.P. Endocrine Rev. 1997, 18, 180.
2. Cheng, K.W.; Leung, P.C.K. Can. J. Phys. Pharmacol., 2000, 78, 1029.
3. Conn, P.M.; Crowley Jr W.F. Annu. Rev. Med., 1994 45, 391.
4. Filicori, M. Drugs, 1994, 48, 41.
5. Barbieri, R.L. J. Reprod. Med., 1998, 43, 287.
6. Rivier, C.; Wylie, V.; Rivier, J. J. Med. Chem., 1983, 26(11), 1545.
7. Nestor Jr., J.J.; Vickery, B.H. Ann. Rep. Med. Chem., 1988, 23, 211.
8. Wojciechowski, N.J.; Carter, C.A.; Skoutakis, V.A.; Bess, D.T.; Falbe, W.J.; Mickle, T.R. Drug Intelligence and Clinical Pharmacy, 1986, 20(10), 746.
9. Santen, R.J.; Warner, B.; Demers, L.M.; Dufau, M.; Smith Jr., J.A. LHRH and Its Analogues, 1984, 351.
10. Anon. Drugs in R&D, 1999, 2(6), 420.
11. Chardonnens, D.; Sylvan, K.; Walker, D.; Bischof, P.; Sakkas, D.; Campana, A. Eur. J. of Obs. & Gyn. and Repr. Biol., 1998, 80(2), 143.
12. Chrisp, P.; Goa, K. Drugs, 1990, 39(4), 523.
13. Barradell, L,B,; McTavish, D. Drugs, 1993, 45(4), 570.
14. Perry, C.M.; Brogden, R.N. Drugs, 1996, 51(2) 319.
15. Goulet, M.T. Ann. Rep. Med. Chem., 1995, 30 169.
16. Rabasseda, X.; Leeson, P.; Castaner, J. Drugs of the Future, 1999, 24(4), 393.
17. Gillies, P.S.; Faulds, D.; Barman-Balfour, J.A.; Perry, C.M. Drugs, 2000, 59(1), 107.
18. Reissmann, T.; Schally, A.V.; Bouchard, P.; Riethmuller, H.; Engel, J. Human Reproduction Update, 2000, 6(4), 322-331.
19. Graul, A.; Rabasseda, X.; Castaner, J. Drugs of the Future 1998, 23(10), 1057.
20. De, B.; Plattner, J.J.; Bush, E.N.; Jae, H-S.; Diaz, G.; Johnson, E.S.; Perun, T.J. J. Med. Chem., 1989, 32, 2038.
21. De, B.; Plattner, J.J.; Jae, H-S. US-04992421, 1991 (Abbott Laboratories)
22. Kato, K.; Kato K.; Nagai, Y. EP-00679642, 1995. (Takeda Chemical Industries Ltd.)
23. Kato, K.; Kato K.; Sugiura, Y. EP-00712845, 1996. (Takeda Chemical Industries Ltd.)
24. Kato, K.; Doi, T.; Sugiura Y.; Kawada, M. WO-09802432, 1998. (Takeda Chemical Industries Ltd.)
25. Suzuki, N.; Takekawa, S.; Kubo, T.; Imaeda, Y. JP-12095767 2000. (Takeda Chemical Industries Ltd.)
26. Matsutani, E.; Naito, K.; Asahina, T. WO-00020034, 2000. (Takeda Chemical Industries Ltd.)
27. Ohkawa, S.; Fujii, N.; Kato, K.; Miyamoto, M. WO-09529900 1995. (Takeda Chemical Industries Ltd.)
28. Ohkawa, S.; Fujii, N.; Kato, K. WO-09638438, 1996 (Takeda Chemical Industries Ltd.)
29. Ohkawa, S.; Fujii, N.; Kato, K. JP-09048777, 1997 (Takeda Chemical Industries Ltd.)
30. Furuya, S.; Choh, N.; Sasaki, S. WO-09714682, 1997 (Takeda Chemical Industries Ltd.)
31. Furuya, S.; Choh, N.; Kato, K.; Hinuma, S. WO-09528405, 1995. (Takeda Chemical Industries Ltd.)
32. Furuya, S.; Choh, N.; Fiarada, M.; Sasaki, S. WO-09714697 1997. (Takeda Chemical Industries Ltd.)
33. Furuya, S.; Matsumoto, H.; Hayase, Y.; Suzuki, N.; Imada, T. WO-09741126, 1997. (Takeda Chemical Industries Ltd.)
34. Furuya, S.; Choh, N.; Suzuki, N.; Imada, T. WO-00000493 2000. (Takeda Chemical Industries Ltd.)
35. Furuya, S.; Nagai, N.; Suzuki, N.; Imada, T. JP-12219690 2000. (Takeda Chemical Industries Ltd.)
36. Furuya, S.; Choh, N.; Suzuki, N.; Imada, T. US-6329388, 2001. (Takeda Chemical Industries Ltd.)
37. Miki, S.; Fukuoka, K.; Akita, M.; Kawakami, J., Furuya, S.; Ishimaru, Y. US-6313301, 2001. (Takeda Chemical Industries Ltd.)
38. Furuya, S.; Suzuki, N.; Hinoshita, M.; Imada, T.; Harada, S. JP-14030087, 2002. (Takeda Chemical Industries Ltd.)
39. Miki, S.; Fukuoka, K.; Akita, M.; Kawakami, J.; Furuya, S.; Ishimaru, Y. WO-020198384, 2002. (Takeda Chemical Industries Ltd.)
40. Cho, N.; Harada, M.; Imaeda, T.; Imada, T., Matsumoto, H.; Hayase, Y.; Sasaki, S.; Furuya, S.; Suzuki, N.; Okubo, S.; Ogi, K.; Endo, S.; Onda, H.; Fujino, M. J. Med. Chem., 1998, 41, 4190.
41. Furuya, S.; Choh, N.; Kato, K.; Hinuma, S. WO-09624597, 1996. (Takeda Chemical Industries Ltd.)
42. Ishiguro, T.; Koya, S.; Suzuki, N. JP-09208496, 1997 (Takeda Chemical Industries Ltd.)
43. Furuya, S.; Suzuki, N.; Choh, N.; Nara, Y. WO-00056739, 2000. (Takeda Chemical Industries Ltd.)
44. Fukuoka, K.; Yamamoto, H.; Kimura, K.; Kawakami, J.; Miki, S. WO-00164683, 2001. (Takeda Chemical Industries Ltd.)
45. Furuya, S.; Suzuki, N. WO-00178780, 2001. (Takeda Chemical Industries Ltd.)
46. Nakano, Y.; Yoneyama, S.; Ochi, M. WO-00224230, 2002 (Takeda Chemical Industries Ltd.).
47. Fukuoka, K.; Yamamoto, H.; Kimura, K.; Kawakami, J.; Miki, S. EP-01266898, 2002. (Takeda Chemical Industries Ltd.)
48. Sasaki, S.; Cho, N.; Nara, Y.; Harada, M.; Endo, S.; Suzuki, N.; Furuya, S.; Fujino, M. J. Med. Chem., 2003, 46, 113.
49. Sorbera, L.S.; Castaner, J.; Leeson, P.A. Drugs of the Future, 2003, 28(2), 121.
50. Furuya, S.; Imaeda, T.; Sasaki, S. WO-09933831, 1999 (Takeda Chemical Industries Ltd.)
51. Furuya, S.; Imaeda, T.; Sasaki, S. JP-11315079, 1999 (Takeda Chemical Industries Ltd.)
52. Sasaki, S.; Imaeda, T.; Hayase, Y.; Shimizu, Y.; Kasai, S.; Cho, N.; Harada, M.; Suzuki, N.; Furuya, S.; Fujino, M. Bioorg. Med. Chem. Letts., 2002, 12, 2073.
53. Zhu, Y-F.; Wilcoxen, K.M.; Struthers, R.S.; Chen, C.; Connors Jr., P.; Gao, Y.; Tucci, F.C. WO-00069859, 2000. (Neurocrine Biosciences Inc.)
54. Zhu, Y-F.; Gross, T.D.; Gao, Y.; Connors Jr., P.J.; Guo, Z.; Chen, C. WO-00129044, 2001. (Neurocrine Biosciences Inc.)
55. Zhu, Y-F.; Gross, T.D.; Gao, Y.; Connors Jr., P.J.; Guo, Z.; Chen, C. US-6537998, 2003. (Neurocrine Biosciences Inc.)
56. Zhu, Y-F.; Struthers, R.S.; Connors Jr., P.J.; Gao, Y.; Gross, T.D.; Saunders, J.; Wilcoxen, K.; Reinhart, G.J.; Ling, N.; Chen, C. Bioorg. Med. Chem. Letts., 2002, 12, 399.
57. Zhu, Y-F.; Wilcoxen, K.; Saunders, J.; Guo, Z.; Gao, Y.; Connors Jr., P.J.; Gross, T.D.; Tucci, F.C.; Struthers, R.S.; Reinhart, G.J.; Xie, Q.; Chen, C. Bioorg. Med. Chem. Letts., 2002, 12, 403.
58. Tucci, F.C.; Zhu, Y-F.; Guo, Z.; Gross, T.D.; Connors Jr., P.J.; Struthers, R.S.; Reinhart, G.J.; Wang, X.; Saunders, J.; Chen, C. Bioorg. Med. Chem. Letts., 2002, 12, 3491.
59. Wilcoxen, K.M.; Zhu, Y-F.; Connors Jr., P.J.; Saunders, J.; Gross, T.D.; Gao, Y.; Reinhart, G.J.; Struthers, R.S.; Chen, C. Bioorg. Med. Chem. Letts., 2002, 12, 2179.
60. Gross, T.D.; Zhu, Y-F.; Saunders, J.; Wilcoxen, K.M.; Gao, Y.; Connors Jr., P.J.; Guo, Z.; Struthers, R.S.; Reinhart, G.J.; Chen, C. Bioorg. Med. Chem. Letts., 2002, 12, 2185.
61. Zhu, Y-F.; Guo, Z.; Gross, T.D.; Gao, Y.; Connors Jr., P.J.; Struthers, R.S.; Xie, Q.; Tucci, F.C.; Reinhart, G.J.; Wu, D.; Saunders, J.; Chen, C. J. Med. Chem., 2003, 46, 1769.
62. Zhu, Y-F.; Chen, C.; Tucci, F.; Guo, Z.; Gross, T.D.; Rowbottom, M.; Struthers, R.S. WO-00155119, 2001. (Neurocrine Biosciences Inc.)
63. Zhu, Y-F.; Guo, Z.; Gross, T.D.; Guo, Z.; Connors Jr., P.J.; Gao, Y.; Tucci, F.C.; Struthers, R.S.; Reinhart, Saunders, J.; Chen, T.K.; Killam Bonneville A.L.; Chen, C. J. Med. Chem., 2003, 46, 2023.
64. Pontillo, J.; Chen, C. WO-03011870, 2003. (Neurocrine Biosciences Inc.)
65. Pontillo, J.; Chen, C. US-2003/0109535, 2003. (Neurocrine Biosciences Inc.)
66. Guo, Z.; Zhu, Y-F.; Tucci, F.C.; Gao, Y.; Struthers, R.S.; Saunders, J.; Gross, T.D.; Xie, Q.; Reinhart, G.J.; Chen, C. Bioorg. Med. Chem. Letts., 2003, 13, 3311.
67. Tucci, F.C.; Zhu, Y-F.; Guo, Z.; Gross, T.D.; Connors Jr., P.J.; Struthers, R.S.; Reinhart, G.J.; Saunders, J.; Chen, C. Bioorg. Med. Chem. Letts., 2003, 13, 3317.
68. Chen, C.; Wu, D.; Guo, Z.; Rowbottom, M. WO-03011293, 2003. (Neurocrine Biosciences Inc.)
69. Chen, C.; Wu, D.; Guo, Z.; Rowbottom, M. US-2003/0073693 2003. (Neurocrine Biosciences Inc.)
70. Tucci, F.; Connors Jr., P.J.; Zhu, Y-F.; Chen, C. WO-03013528, 2003. (Neurocrine Biosciences Inc.)
71. Tucci, F.; Connors Jr., P.J.; Zhu, Y-F.; Chen, C. US-2003/0119878, 2003. (Neurocrine Biosciences Inc.)
72. Guo, Z.; Wu, D.; Chen, C.; Tucci, F.C.; Regan, C. WO-03011839, 2003. (Neurocrine Biosciences Inc.)
73. Pontillo, J.; Guo, Z.; Wu, D. WO-03011841, 2003. (Neurocrine Biosciences Inc.)
74. Pontillo, J.; Guo, Z.; Wu, D. US-2003/0114455, 2003 (Neurocrine Biosciences Inc.)
75. Goulet, M.; Bugianesi, R.L.; Ashton, W.T.; Chu, L.; Fisher, M.H.; Lin, P.; Smith, R.G.; Ponpipom, M.M. WO-09721435, 1997. (Merck & Co Inc.)
76. Goulet, M.; Chu, L.; Fisher, M.H.; Girotra, N.N.; Lin, P.; Walsh, T.F.; Wyvratt, M.J. WO-09721703, 1997. (Merck & Co Inc.)
77. Goulet, M.; Ashton, W.T.; Chu, L.; Fisher, M.H.; Girotra, N.N.; Lin, P.; Wyvratt, M.J. WO-09721704, 1997. (Merck & Co Inc.)
78. Goulet, M.; Ashton, W.T.; Chu, L.; Fisher, M.H.; Wyvratt, M.J. WO-09721707, 1997. (Merck & Co Inc.)
79. Goulet, M.; Chu, L.; Ashton, W.T.; Fisher, M.H.; Wyvratt, M.J.; Smith, R.G.; Bugianesi, R.L.; Ponpipom, M.M.; Yang, Y.T.; Lin, P. WO-05756507, 1998. (Merck & Co Inc.)
80. Goulet, M; Ujjainwalla, F; Walsh, T.F., Wyvratt, M.J. WO-09855116, 1998. (Merck & Co. Inc.)
81. Goulet, M; Ujjainwalla, F; Walsh, T.F., Wyvratt, M.J.; Young, J.R.; Chu, L. WO-09855119, 1998. (Merck & Co. Inc.)
82. Goulet, M.; Wyvratt, M.J.; Chu, L.; Girrotra, N.N.; Lin, P. WO-09855123, 1998. (Merck & Co Inc.)
83. Goulet, M.; Ujjainwalla, F.; Walsh, T.F.; Wyvratt, M.J.; Young, J.R.; Chu, L. WO-09855470, 1998. (Merck & Co Inc.)
84. Goulet, M; Ujjainwalla, F; Walsh, T.F., Wyvratt, M.J. WO-09855479, 1998. (Merck & Co. Inc.)
85. Goulet, M; Chu, L.; Walsh, T.F.; Fisher, M.H.; Giotra, N.N.; Wyvratt, M.J.; Lin, P.; Ashton, W.T. US-05849764, 1998. (Merck & Co. Inc.)
86. Chu, L.; Goulet, M.T.; Walsh, T.F.; Witkin, S.L.; Wyvratt, M.J. WO-09921553, 1999. (Merck & Co Inc)
87. Chu, L.; Goulet, M.T.; Walsh, T.F.; Witkin, S.L.; Wyvratt, M.J. WO-09921557, 1999. (Merck & Co Inc)
88. Young, J.R.; Goulet, M.T.; Walsh, T.F.; Fisher, M.H. WO-09941251, 1999. (Merck & Co Inc)
89. Young, J.R.; Goulet, M.T.; Walsh, T.F.; Fisher, M.H. WO-09941252, 1999. (Merck & Co Inc)
90. Walsh, T.F., Ujjainwalla, F.; Goulet, M.T.; Young, J.R. WO-09951231, 1999. (Merck & Co. Inc.)
91. Walsh, T.F., Ujjainwalla, F.; Goulet, M.T. WO-09951232, 1999. (Merck & Co. Inc.)
92. Walsh, T.F., Ujjainwalla, F.; Goulet, M.T. WO-09951233, 1999. (Merck & Co. Inc.)
93. Walsh, T.F., Ujjainwalla, F.; Goulet, M.T.; Young, J.R. WO-09951234, 1999. (Merck & Co. Inc.)
94. Walsh, T.F., Ujjainwalla, F.; Goulet, M.T. WO-09951595, 1999. (Merck & Co. Inc.)
95. Walsh, T.F., Ujjainwalla, F.; Goulet, M.T.; Bugianesi, R.L. WO-09951596, 1999. (Merck & Co. Inc.)
96. Goulet, M.; Ashton, W.T.; Chu, L.; Fisher, M.H.; Lin, P.; Ponpipom, M.M.; Wyvratt, M.J.; Giotra, N.N.; Young, J. WO-00004013, 2000. (Merck & Co Inc.)
97. Walsh, T.F., Ujjainwalla, F. WO-00053178, 2000. (Merck & Co. Inc.)
98. Walsh, T.F., Ujjainwalla, F. WO-00053179, 2000. (Merck & Co. Inc.)
99. Walsh, T.F., Ujjainwalla, F. WO-00053180, 2000. (Merck & Co. Inc.)
100. Walsh, T.F., Ujjainwalla, F. WO-00053181, 2000. (Merck & Co. Inc.)
101. Walsh, T.F., Ujjainwalla, F. WO-00053185, 2000. (Merck & Co. Inc.)
102. Walsh, T.F., Ujjainwalla, F. WO-00053602, 2000. (Merck & Co. Inc.)
103. Goulet, M.T.; Walsh, T.F., Ujjainwalla, F.; Wyvratt, M.J. WO-0069433, 2000. (Merck & Co. Inc.)
104. Goulet, M.T.; DeVita, R.J.; Wyvratt, M.J.; Young, J.R. WO-09744037, 1997. (Merck & Co Inc)
105. Goulet, M.T.; DeVita, R.J.; Wyvratt, M.J.; Young, J.R. WO-09744041, 1997. (Merck & Co Inc)
106. Goulet, M.T.; Allen, E.E.; Jiang, J.; Smith, R.G.; Walsh, T.F.; Wyvratt, M.J.; Yang, Y.T.; Young, J.R.; DeVita, R.J. WO-09744321 1997. (Merck & Co Inc)
107. Goulet, M.T.; Allen, E.E.; DeVita, R.J.; Jiang, J.; Walsh, T.F.; Young, J.R.; Wyvratt, M.J.; Toupence, R.B.; Ujjainwalla, F. WO-09744339, 1997. (Merck & Co Inc)
108. DeVita, R.J.; Goulet, M.T.; Parikh, M. WO-00170227, 2001, (Merck & Co. Inc.)
109. DeVita, R.J.; Goulet, M.T.; Parikh, M. WO-00170228, 2001, (Merck & Co. Inc.)
110. Chung, J.L.Y.; Farr, R.N.; Humphrey, G.R. WO-03013876, 2002, (Merck & Co. Inc.)
111. Chu, L.; Hutchins, J.E.; Weber, A.E.; Lo, J-L.; Yang, Y.T.; Cheng, K.; Smith, R.G; Fisher, M.H.; Wyvratt, M.J.; Goulet, M.T. Bioorg. Med. Chem. Letts., 2001, 11, 509.
112. Lin, P.; Marino, D.; Lo, J-L.; Yang, Y.T.; Cheng, K.; Smith, R.G; Fisher, M.H.; Wyvratt, M.J.; Goulet, M.T. Bioorg. Med. Chem. Letts., 2001, 11, 1073.
113. Lin, P.; Parikh, M.; Lo, J-L.; Yang, Y.T.; Cheng, K.; Smith, R.G.; Fisher, M.H.; Wyvratt, M.J.; Goulet, M.T. Bioorg. Med. Chem. Letts., 2001, 11, 1077.
114. Chu, L.; Lo, J-L.; Yang, Y.T.; Cheng, K.; Smith, R.G; Fisher, M.H.; Wyvratt, M.J.; Goulet, M.T. Bioorg. Med. Cheng. Letts., 2001, 11, 515.
115. Ashton, W.T.; Sisco, R. M.; Yang, Y.T.; Lo, J-L.; Yudkovitz, J.B.; Cheng, K.; Goulet, M.T. Bioorg. Med. Chem. Letts., 2001 11, 1723.
116. Ashton, W.T.; Sisco, R. M.; Yang, Y.T.; Lo, J-L.; Yudkovitz, J.B.; Gibbons, P.H.; Mount, G.R.; Ren, R.N.; Butler, B.S.; Cheng, K., Goulet, M.T. Bioorg. Med. Chem. Letts., 2001, 11, 1727.
117. Simeone, J.P.; Bugianesi, R.L.; Ponpipom, M.M.; Goulet, M.T., Levorse, M.S., Desia, R.C. Tetrahedron Letts., 2001, 42 6459.
118. Ashton, W.T.; Sisco, R. M.; Kieczykowski, G.R; Yang, Y.T.; Yudkovitz, J.B.; Cui, J.; Mount, G.R.; Ren, R.N.; Wu, T-J.; Shen, X.; Lyons, K.A.; Mao, A-H.; Carlin, J.R.; Karanam, B.V.; Vincent, S.H.; Cheng, K.; Goulet, M.T. Bioorg. Med. Chem. Letts., 2001, 11, 2597.
119. Young, J.R.; Huang, S.X.; Walsh, T.F.; Wyvratt, M.J.; Yang, Y.T.; Yudkovitz, J.B.; Cui, J.; Mount, G.R.; Ren, R.N.; Wu, T-J.; Shen, X.; Lyons, K.A.; Mao, A-H.; Carlin, J.R.; Karanam, B.V.; Vincent, S.H.; Cheng, K.; Goulet, M.T. Bioorg. Med. Chem. Letts., 2002, 12, 827.
120. Simeone, J.P.; Bugianesi, R.L.; Ponpipom, M.M.; Yang, Y.T.; Lo, J-L.; Yudkovitz, J.B.; Cui, J.; Mount, G.R.; Ren, R.N.; Creighton, M.; Mao, A-H.; Vincent, S.H.; Cheng, K.; Goulet, M.T. Bioorg. Med. Chem. Letts., 2002, 12, 3329.
121. DeVita, R.J.; Hollings, D.D.; Goulet, M.T.; Wyvratt, M.J.; Fisher, M.H.; Lo, J-L.; Yang, Y.T.; Cheng, K.; Smith, R.G. Bioorg. Med. Chem. Letts., 1999, 9, 2615.
122. DeVita, R.J.; Goulet, M.T.; Wyvratt, M.J.; Fisher, M.H.; Lo, J-L.; Yang, Y.T.; Cheng, K.; Smith, R.G. Bioorg. Med. Chem. Letts., 1999, 9, 2621.
123. Walsh, T.F.; Toupence, R.B.; Young, J.R.; Huang, S.X.; Ujjainwalla, F.; DeVita, R.J.; Goulet, M.T.; Wyvratt, M.J.; Fisher, M.H.; Lo, J-L.; Ren, N.; Yudkovitz, J.B.; Yang, Y.T.; Cheng, K.; Smith, R.G. Bioorg. Med. Chem. Letts., 2000, 10, 443.
124. Young, J.R.; Huang, S.X.; Chen, I.; Walsh, T.F.; DeVita, R.J.; Wyvratt, M.J.; Goulet, M.T.; Ren, N.; Lo, J-L.; Yang, Y.T.; Yudkovitz, J.B.; Cheng, K.; Smith, R.G. Bioorg. Med. Chem. Letts., 2000, 10, 1723.
125. DeVita, R.J.; Walsh, T.F.; Young, J.R.; Jiang, J.; Ujjainwalla, F.; Toupence, R.B.; Parikh, M.; Huang, S.X.; Fair, J.A.; Goulet, M.T.; Wyvratt, M.J.; Lo, J-L.; Ren, N.; Yudkovitz, J.B.; Yang, Y.T.; Cheng, K.; Cui, J.; Mount, G.; Rohrer, S.P.; Schaeffer, J.M.; Rhodes, L.; Drisko, J.E.; McGowan, E.; MacIntyre, D.E.; Vincent, S.; Carlin, J.; Cameron, J.; Smith, R.G. J. Med. Chem. 2001, 44, 917.
126. Luthin, D.R.; Hong, Y.; Pathak, V.P.; Paderes, G.; Nared-Hood, K.D.; Castro, M.A.; Vazir, H.; Li, H.; Tompkins, E.; Christie, L.; May, J.M.; Anderson, M.B. Bioorg. Med. Chem. Letts., 2002, 12, 3467.
127. Anderson, M.; Polinsky, A.; Hong, Y.; Gregor, V. WO-09944987, 1999, (Alanex Corp - now Pfizer)
128. Anderson, M.B.; Vazir, H.N.; Luthin, D.R.; Paderes, G.D.; Pathak, V.P.; Christie, L.C.; Hong, Y.; Tompkins, E.V.; Li, H.; Faust, J. WO-00020358, 2000, (Agouron Pharmaceuticals Inc. - now Pfizer)
129. Sun, E.T.; Anderson, M.B.; Anderes, K.L.; Christie, L.; Do, Q-Q.T.; Feng, J.; Goetzen, T.; Hong, Y.; latsimirskaia, E.A.; Li, H.; Luthin, D.R.; Paderes, G.D.; Pathak V.P.; Rajapakse, R.J.; Shakelford, S.; Tompkins, E.V.; Truesdale, L.K.; Vazir, H. WO-02098363, 2002 (Agouron Pharmaceuticals Inc. - now Pfizer)
130. Anderson, M.B.; Christie, L.C.; Feng, J.; Hong, Y.; Li, H.; Pathak, V.P.; Rajapakse, R.; Tompkins, E.; Vazir, H.N. EP-01334972, 2003, (Pfizer Inc.)
131. Luthin, D.R.; Hong, Y.; Tompkins, E.; Anderes, K.L.; Paderes, G.; Kraynov, E.A.; Castro, M.A.; Nared-Hood, K.D.; Castillo, R.; Gregory, M.; Vazir, H.; May, J.M.; Anderson, M.B. Bioorg. Med. Chem. Letts., 2002, 12, 3635.
132. Hoeger, C.; Rivier, J.; Porter, J. WO-09500474, 1995 (Sibia Neurosciences Inc.)
133. Haviv, F.; Dwight, W.J.; Crawford, B.W.; Swenson, R.E.; Bruncko, M.; Kaminski, M.A.; Frey, L.M.; Demattei, J.; Greer, J. US-05981521, 1999. (Abbott Laboratories)
134. Haviv, F.; Dwight, W.J.; Crawford, B.W.; Swenson, R.E.; Bruncko, M.; Kaminski, M.A.; Frey, L.M.; Demattei, J.; Greer, J. WO-0029380, 2000. (Abbott Laboratories)
135. Sauer, D.R.; Haviv, F.; Randolph, J.; Mort, N.A.; Dalton, C.R.; Bruncko, M.; Kaminski, M.A.; Crawford, B.W.; Frey, L.M.; Greer, J. US-05955440, 1999. (Abbott Laboratories)
136. Sauer, D.R.; Haviv, F.; Randolph, J.; Mort, N.A.; Dalton, C.R.; Bruncko, M.; Kaminski, M.A.; Crawford, B.W.; Frey, L.M.; Greer, J. WO-09950276, 1999. (Abbott Laboratories)
137. Dalton, C.R.; Bruncko, M.; Kaminski, M.A.; Frey, L.M.; Sauer, D.R.; Haviv, F. WO-00012521, 2000. (Abbott Laboratories)
138. Randolph, J.; Haviv, F.; Sauer, D.; Waid, P.; Nichols, C.J.; Mort, N.A.; Dalton, C.R.; Greer, J. US-06020521, 2000. (Abbott Laboratories)
139. Besecke, L.M.; Diaz, G.J.; Segreti, J.A.; Mohning, K.M.; Cybulski, V.A.; Rao, M.; Bush, E.N.; Randolph, J.T.; Waid, P.L.; Haviv, F., Wegner, C.D.; Greer, J. Drug Dev. Res., 2001, 52, 485.
140. Hirano, M.; Kawaminami, E.; Toyoshima, A.; Moritomo, H.; Seki, N.; Wakayama, R.; Okada, M.; Kusayama, T. WO-00202533, 2002. (Yamanouchi Pharmaceutical Co, Ltd.)
141. Strehlke, P.; Droescher, P.; Buehmann, U.; Schmees, N.; Muhn, P.; Hess-Stump, H.; Kuehne, R.; Guenther, E.; Polymeropoulos, E.; Ter Laak, A.M. WO-02066437, 2002. (Schering AG)
142. Peng, G.; Gallop, M.A.; Chernov-Rogan, T.; Yanovsky, S.; Pelletier, J.C.; Green, D.M. WO-00211732, 2002. (Glaxo Wellcome plc)
143. Sui, Z.; Macielag, M.; Lanter, J.C. WO-00248112, 2002. (Ortho-McNeil Pharmaceutical Inc.)
144. Sui, Z.; Macielag, M.; Lanter, J.C. US-6583153, 2003 (Ortho-McNeil Pharmaceutical Inc.)
145. Ho, C.H. US-4678784, 2003 (McNeilab Inc.)
146. Wardleworth, M.; Dossetter, A.G.; Halsall, C.T. WO-02066459, 2002. (AstraZeneca AB)
147. Dossetter, A.G.; Kenny, P.; Mckerrecher, D.; Wardleworth, M. WO-02066478, 2002. (AstraZeneca AB)
148. Dossetter, A.G.; Kenny, P.; Mckerrecher, D.; Wardleworth, M. WO-02066477, 2002. (AstraZeneca AB)
149. Wardleworth, M.; Dossetter, A.G.; Halsall, C.T. WO-02092565, 2002. (AstraZeneca AB)
150. Koppitz, M.; Muhn, H.P.; Shaw, K.; Hess-Stump, H.; Paulini, K. WO-03051837, 2003. (Zentaris AG)
151. Poitout, L.; Brault, V.; Ferrandis, E.; Thurieau, C. WO-03053939, 2003.(S.C.R.A.S.)