Discovery of CS-0777: A potent, selective, and orally active S1P 1 agonist

ACS Medicinal Chemistry Letters

Volumn 2, Issue 5, 2011, Pages 368-372

  Nishi, Takahide ^a   Miyazaki, Shojiro ^a   Takemoto, Toshiyasu ^a   Suzuki, Keisuke ^a   Iio, Yukiko ^a   Nakajima, Katsuyoshi ^a   Ohnuki, Takashi ^a   Kawase, Yumi ^a   Nara, Futoshi ^a   Inaba, Shinichi ^a   Izumi, Takashi ^a   Yuita, Hiroshi ^a   Oshima, Keiko ^a   Doi, Hiromi ^a   Inoue, Ryotaku ^a   Tomisato, Wataru ^a   Kagari, Takashi ^a   Shimozato, Takaichi ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

agonist; CS 0777; EAE; lymphocyte; MS; S1P1

Indexed keywords

CS 0777; CS 0777 P; IMMUNOMODULATING AGENT; SPHINGOSINE 1 PHOSPHATE RECEPTOR; UNCLASSIFIED DRUG;

ALLERGIC ENCEPHALOMYELITIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE COMPARISON; DRUG HALF LIFE; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; FEMALE; IN VITRO STUDY; LYMPHOCYTE COUNT; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PERIPHERAL LYMPHOCYTE; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; RAT; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION;

RATTUS;

EID: 79956068785     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml100301k     Document Type: Article

References (23)

1. Cyster, J. G. Annu. Rev. Immunol. 2005, 23, 127
2. Kihara, A.; Igarashi, Y. Biochim. Biophys. Acta 2008, 1781, 496
3. Mandala, S.; Hajdu, R.; Bergstrom, J.; Quackenbush, E.; Xie, J.; Milligan, J.; Thornton, R.; Shei, G.-J.; Card, D.; Keohane, C.; Rosenbach, M.; Hale, J.; Lynch, C. L.; Rupprecht, K.; Parsons, W.; Rosen, H. Science 2002, 296, 346
4. Rivera, J; Proia, R. L.; Olivera, A. Nat. Rev. Immunol. 2008, 8, 753
5. Brinkmann, V.; Davis, M. D.; Heise, C. E.; Albert, R.; Cottens, S.; Hof, R.; Bruns, C.; Prieschl, E.; Baumruker, T.; Hiestand, P.; Foster, C. A.; Zollinger, M.; Lynch, K. R. J. Biol. Chem. 2002, 277, 21453
6. Chiba, K. Pharmacol. Ther. 2005, 108, 308
7. Brinkmann, V. Pharmacol. Ther. 2007, 115, 84
8. Hale, J. J.; Yan, L.; Neway, W. E.; Hajdu, R.; Bergstrom, J. D.; Milligan, J. A.; Shei, G.-J.; Chrebet, G. L.; Thornton, R. A.; Card, D.; Rosenbach, M.; Rosen, H.; Mandala, S. Bioorg. Med. Chem. 2004, 12, 4803
9. Kiuchi, M.; Adachi, K.; Tomatsu, A.; Chino, M.; Takeda, S.; Tanaka, Y.; Maeda, Y.; Sato, N.; Mitsutomi, N.; Sugahara, K.; Chiba, K. Bioorg. Med. Chem. 2005, 13, 425
10. Kappos, L.; Radue, E.-W.; O'Conner, P.; Polman, C.; Hohlfeld, R.; Calabresi, P.; Selmaj, K.; Agoropoulou, C.; Leyk, M.; Zhang-Auberson, L.; Burtin, P. N. Engl. J. Med. 2010, 362, 387
11. Cohen, J. A.; Barkhof, F.; Comi, G.; Hartung, H.-P.; Khatri, B. O.; Montalban, X.; Pelletier, J.; Capra, R.; Gallo, P.; Izquierdo, G.; Tiel-Wilck, K.; de Vera, A.; Jin, J.; Stites, T.; Wu, S.; Aradhye, S.; Kappos, L. N. Engl. J. Med. 2010, 362, 402
12. Brinkmann, V.; Cyster, J. G.; Hla, T. Am. J. Transplant. 2004, 4, 1019
13. Matloubian, M.; Lo, C. G.; Cinamon, G.; Lesneski, M. J.; Xu, Y.; Brinkmann, V.; Allende, M. L.; Proia, R. L.; Cyster, J. G. Nature 2004, 427, 355
14. Forrest, M.; Sun, S.-Y.; Hajdu, R.; Bergstrom, J.; Card, D.; Doherty, G.; Hale, J.; Keohane, C.; Meyers, C.; Milligan, J.; Mills, S.; Nomura, N.; Rosen, H.; Rosenbach, M.; Shei, G.-J.; Singer, I. I.; Tian, M.; West, S.; White, V.; Xie, J.; Proia, R. L.; Mandala, S. J. Phamacol. Exp. Ther. 2004, 309, 758
15. Sanna, M. G.; Liao, J.; Jo, E.; Alfonso, C.; Ahn, M.-Y.; Peterson, M. S.; Webb, B.; Lefebvre, S.; Chun, J.; Gray, N.; Rosen, H. J. Biol. Chem. 2004, 279, 13839
16. Kappos, L.; Antel, J.; Comi, G.; Montalban, X.; O'Conner, P.; Polman, C. H.; Haas, T.; Korn, A. A.; Karlsson, G.; Radue, E. W. N. Engl. J. Med. 2006, 355, 1124
17. Brinkmann, V. Pharmacol. Ther. 2007, 115, 84
18. Nakamura, T.; Tsuji, T.; Iio, Y.; Miyazaki, S.; Takemoto, T.; Nishi, T. Tetrahedron: Asymmetry 2006, 17, 2781
19. Ohnuki, T.; Tsuji, T.; Miyazaki, S.; Moriguchi, T.; Nishi, T. Synlett 2009, 910
20. Endo, A.; Yamashita, H.; Naoki, H.; Iwashita, T.; Mizukawa, Y. J. Antibiot. 1985, 38, 328
21. Shimozato, T.; Tomisato, W.; Doi, H.; Kagari, T.; Inoue, R.; Yuita, H.; Oshima, K.; Makino, T.; Suzuki, K.; Sato, S.; Tamura, M.; Kawase, Y.; Yonesu, K.; Nara, F. Eur. J. Pharmacol. 2011, in press.
22. Inaba, S.; Goto, M.; Yabe, Y.; Tanaka, H.; Takahashi, M.; Ikeda, T.; Iwabuchi, H.; Izumi, T. Drug Metab. Dispos. 2011, in press.
23. Moberly, J.; Rohatagi, S.; Zahir, H.; Hsu, C.; Noveck, R.; Truitt, K. J. Clin. Pharmacol. 2011, in press.