Dual neurokinin NK1/NK2 receptor antagonists

Drugs of the Future

Volumn 24, Issue 8, 1999, Pages 883-892

  Gerspacher, Marc ^a   Von Sprecher, Andreas ^b  

^a NOVARTIS PHARMA AG   (Switzerland)

^b ACTELION PHARMACEUTICALS LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

1' [4 (N BENZOYL N METHYLAMINO) 3 (3,4 DICHLOROPHENYL)BUTYL]SPIRO[BENZO[C]THIOPHENE 1(3H) 4' PIPERIDINE] 2 OXIDE; 2 BENZHYDRYL 3 (2 METHOXYBENZYLAMINO) 1 AZABICYCLO[2.2.2]OCTANE; 2 BENZYL 1 (3,5 DIMETHYLBENZOYL) 4 (4 QUINOLINYLMETHYLAMINO)PIPERIDINE; 3 (2 METHOXYBENZYLAMINO) 2 PHENYLPIPERIDINE; FK 224; L 743986; LANEPITANT; MDL 105172A; MDL 105212A; MEN 10627; N BENZYL N2 [4 HYDROXY 1 [(1 METHYL 1H INDOL 3 YL)CARBONYL]PROLYL] N METHYL 3 (2 NAPHTHYL)ALANINAMIDE; NEUROKININ 1 RECEPTOR; NEUROKININ 2 RECEPTOR; NOLPITANTIUM; S 16474; SAREDUTANT; TACHYKININ RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG; YM 44778;

ANTIINFLAMMATORY ACTIVITY; BRONCHODILATATION; BRONCHOSPASM; CYTOKINE RELEASE; DRUG EFFECT; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SPECIFICITY; GUINEA PIG; MUCUS SECRETION; NONHUMAN; RECEPTOR AFFINITY; REVIEW;

EID: 0032856478     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1999.024.08.858627     Document Type: Review

References (69)

1. Maggi, C.A., Patacchini, R., Rovero, P., Giachetti, A. Tachykinin receptors and tachykinin receptor antagonists. J Auton Pharmacol 1993, 13: 23-93.
2. Regoli, D., Boudon, A., Fauchére, J-L. Receptors and antagonists for substance P and related peptides. Pharmacol Rev 1994, 46: 551-99.
3. Maggio, J.E., Mantyh, P.W. History of tachykinin peptides. In: The Tachykinin Receptors. Buck, S.H. (Ed.). Humana: Totowa 1994, 1-21.
4. Nakanishi, S. Mammalian tachykinin receptors. Ann Rev Neurosci 1994, 14: 123-36.
5. Burcher, E., Mussap, C.J., Stephenson, J.A. Autoradiographic localization of receptors in peripheral tissues. In: The Tachykinin Receptors. Buck, S.H. (Ed.). Humana: Totowa 1994, 125-63.
6. Krause, J.E., Blount, P., Sachais, B.S. Molecular biology of receptors. In: The Tachykinin Receptors. Buck, S.H. (Ed.). Humana: Totowa 1994, 165-218.
7. Longmore, J., Swain, C.J., Hill, R.G. Neurokinin receptors. Drug News Perspect 1995, 8: 5-23.
8. Kucharczyk, N. Tachykinin antagonists in development. Exp Opin Invest Drugs 1995, 4: 299-311.
9. Elliott, J., Seward, E.M. Neurokinin receptor antagonists. Exp Opin Ther Patents 1997, 7: 43-54.
10. Longmore, J., Hill, R.G., Hargreaves, R.J. Neurokinin receptor antagonists: Pharmacological tools and therapeutic drugs. Can J Physiol Pharmacol 1997, 75: 612-21.
11. von Sprecher, A., Gerspacher, M., Anderson, G.P. Neurokinin antagonists as potential therapies for inflammation and rheumatoid arthritis. I Drugs 1998, 1: 73-91.
12. Ford-Hutchinson, A.W., Rodger, I.W., Jones, T.R. Novel therapeutic strategies for the treatment of human bronchial asthma. Drug News Perspect 1992, 5: 542-9.
13. Geppetti, P., Bertrand, C., Ricciardolo, F.M.L., Nadel, J.A. New aspects on the role of kinins in neurogenic inflammation. Can J Physiol Pharmacol 1995, 73: 843-7.
14. Advenier, C., Lagente, V., Boichot, E. The role of tachykinin receptor antagonists in the prevention of bronchial hyperresponsiveness, airway inflammation and cough. Eur Respir J 1997, 10: 1892-906.
15. Chapman, R.W., Hey, J.A., McLeod, R., Minnicozzi, M., Rizzo, Ch. Tachykinins in the lungs. Drug News Perspect 1998, 11:480-9.
16. Murai, M., Morimoto, H., Maeda, Y., Kiyotoh, S., Nishikawa, M., Fujii, T. Effects of FK-224, a novel compound NK-1 and NK-2 receptor antagonist, on airway constriction and airway edema induced by neurokinins and sensory nerve stimulation in guinea-pigs. J Pharmacol Exp Ther 1992, 262: 403-8.
17. Joos, G.F., van Schoor, J., Kips, J.C., Pauwels, R.A. The effect of inhaled FK-224, a tachykinin NK-1 and NK-2 receptor antagonist on neurokinin A-induced bronchoconstriction in asthmatics. Am J Respir Crit Care Med 1996, 153: 1781-4.
18. Barnes, P.J., Baraniuk, J.M., Belvisi, M.G. Neuropeptides in the respiratory tract. Am Rev Respir Dis 1991, 144: 1187-98.
19. Martling, C.R., Theodorsson-Norheim, E., Lundberg, J.M. Occurrence and effects of multiple tachykinins: Substance P, neurokinin A and neuropeptide K in human lower airways. Life Sci 1987, 40: 1633-43.
20. Holgate, ST., Djukanovic, R., Wilson, J., Roche, W., Howarth, P.M. Inflammatory processes and bronchial hypperresponsiveness. Clin Exp Allergy 1991, 21 (Suppl. 1): 30-6.
21. 1 receptor antagonist. Br J Pharmacol 1992, 105: 261-2.
22. 2 receptors by CP 99,994 and SR 48968 prevents airway hyperresponsiveness in primates. Am J Respir Crit Care Med 1996, 153: A160.
23. Fujii, T. Discovery and pharmacological properties of selective neurokinin receptor antagonists, FK-224 and FK-888. Folia Pharmacol Jpn 1995, 106: 193-204.
24. Hirayama, Y., Lei, Y-H., Barnes, P.J., Rogers, D.F. Effects of novel tachykinin antagonists, FK-224 and FK-888, on neurogenic airway plasma exudation, bronchoconstriction and systemic hypotension in guinea pigs in vivo. Br J Pharmacol 1993, 108: 844-51.
25. 1 receptor antagonist SR 140333 produces long lasting inhibition of neurogenic inflammation, but does not influence acute chemo-or thermonociception in rats. Arch Pharmacol 1995, 352: 201-5.
26. 2 receptor. Drugs Fut 1995, 20: 701-7.
27. 2 receptors. J Pharmacol Exp Ther 1994, 271: 1489-500.
28. Kudlacz, E.M., Scott, A., Shatzer, S.A. et al. In vitro and in vivo characterisation of MDL 105,212A, a nonpeptide NK-1/NK-2 tachykinin receptor antagonist. J Pharmacol Exp Ther 1996, 277: 840-51.
29. 2 receptor antagonist. Eur J Pharmacol 1995, 294: 677-84.
30. van Schoor, J., Joos, G., Chasson, B., Brouard, R., Pauwels, R. The effect of the oral nonpeptide NK2 receptor antagonist SR 48968 on neurokinin A-induced bronchoconstriction in asthmatics. Eur Resp J 1996, 9 (Suppl. 23): 289S.
31. Ichinose, M., Miura, M., Yamauchi, H. et al. A neurokinin-1 receptor antagonist improves exercise-induced airway narrowing in asthmatic patients. Am J Respir Crit Care Med 1996, 153: 936-41.
32. 1 receptors mediate leukocyte adhesion in neurogenic inflammation in the rat trachea. Am J Physiol 1995, 268: L263-9.
33. 1 receptor antagonist (CP-99,994) on hypertonic saline-induced bronchoconstriction and cough in male asthmatic subjects. Am J Respir Crit Care med 1995, 152: 879-84.
34. Ellis, J.L., Undem, B.J., Kays, J.S., Ghanekar, S.V., Barthlow, H.G., Buckner, C.K. Pharmacological examination of receptors mediating contractile responses to tachykinins in airways isolated from human, guinea pig and hamster. J Pharmacol Exp Ther 1993, 267: 95-101.
35. 2-receptor. Neuropeptides 1995, 29: 281-92.
36. Sherwood, J.E., Mauser, P.J., Chapman, R.W. Bronchoconstrictor and respiratory effects of neurokinin A in dogs. J Pharmacol Exp Ther 1997, 283: 788-93.
37. 3 receptor. Life Sci 1995, 56: PL27-32.
38. 3 antagonist, SR 142801, of substance P-induced microvascular leakage hypersensitivity and airway hyperresponsiveness in guinea-pigs. Am J Respir Crit Care 1996, 153: A163.
39. 2 dual antagonist) on the knee joint inflammation induced by carrageenin, substance P, serotonin and antigen. Regul Pep 1992, Suppl. 1: Abst S59.
40. Schmidt, D., Jorres, R.A., Rabe, K.F., Magnussen, H. Reproducibility of airway response to inhaled bradykinin and effect of the neurokinin receptor antagonist FK-224 in asthmatic subjects. Eur J Clin Pharmacol 1996, 50: 269-73.
41. Ichinose, M., Nakajima, N., Takahashi, T., Yamauchi, H., Inoue, H., Takishima, T. Protection against bradykinin-induced bronchoconstriction in asthmatic patients by neurokinin receptor antagonist. Lancet 1992, 340: 1248-51.
42. 2 receptors. Bioorg Med Chem Lett 1996, 6: 951-6.
43. Kudlacz, E.M., Knippenberg, R.W., Logan, D.E., Burkholder, T.P. Effect of MDL-105212, a non-peptide NK-1/NK-2 receptor antagonist in allergic guinea pig model. J Pharmacol Exp Ther 1996, 279: 732-9.
44. Kudlacz, E.M., Knippenberg, R.W., Shatzer, S.A., Kehne, J.H., McCloskey, T.C., Burkholder, T.P. The peripheral NK-1/NK-2 receptor antagonist MDL-105172A inhibits tachykinin-mediated respiratory effects in guinea pigs. J Auton Pharmacol 1997, 17: 109-19.
45. Burkholder, T.P., Maynard, G.D., Kudlacz, E.M. WO 9827085.
46. Burkholder, T.P., Maynard, G.D., Kudlacz, E.M. WO 9827086.
47. 2 receptors. 212th ACS Natl Meet (Aug 25-29, Orlando) 1996, MEDI 136.
48. Mills, S.G. et al. William Harvey Res Inst Conf Tachykinins and their Antagonists (Oct 10-11, London) 1996, P5.
49. Chiang, Y-C.P., Finke, P.E., MacCoss, M. et al. WO 9610568.
50. Kubota, H., Kakefuda, A., Nagaoka, H., Yamamoto, O., Ikeda, K., Shibanuma, T. AFMC Int Med Chem Symp/AEWECS 95 (Sept 3-8, Tokyo) 1995, P6M139 (Derwent Conf Fast Track 3 (14) 96, 1995).
51. 2 dual antagonistic activities. Chem Pharm Bull 1998, 46: 1538-44.
52. Bernstein, P.R., Dembofsky, B.T., Jacobs, R.T. WO 9624582.
53. Carruthers, N.I., Alaimo, C.A. WO 9639386.
54. Shanker, B.B. WO 9818785.
55. McCormick, K.D., Lupo, A.T. WO 9639383.
56. Monaghan, S.M., Alker, D., Burns, C.J. WO 9807722.
57. Nishi, T., Ishibashi, K., Nakajima, K., Fukazawa, T., Kurata, H., Yamaguchi, T., Ito, K. EP 776893.
58. 2 dual antagonists. 25th Natl Med Chem Symp, Univ Michigan (June 18-22, Ann Arbor) 1996, Poster 94.
59. Yang, L., Guo, L., Pasternak, A. et al. Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype (sst2) agonists. J Med Chem 1998, 41: 2175-9.
60. 1 antagonist. Bioorg Med Chem Lett 1996, 6: 1623-8.
61. 2 antagonists. 216th ACS Natl Meet (Aug 23-27, Boston) 1998, MEDI 52.
62. Hipskind, P.A., Howbert, J.J., Bruns, R.F. et al. 3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists. J Med Chem 1996, 39: 736-48.
63. Cho, S-S.Y., Hipskind, P.A., Howbert, J.J., Muehl, B.S., Nixon, J.A. WO 9631214.
64. Hipskind, P.A. EP 714891.
65. Natsugari, H., Ishimaru, T., Doi, T., Ikeura, Y., Kimura, C. EP 733632.
66. Natsugari, H., Ikeura, Y., Kiyota, Y. et al. Novel, potent and orally active substance P antagonists: Synthesis and antagonist activity of N-benzylcarboxamide derivatives of pyrido[3,4-b]pyridine. J Med Chem 1995, 38: 3106-20.
67. Burkholder, T.P., Le, T-B., Kudlacz, E.M. WO 9632385.
68. Shue, H-J., Shih, N-Y., Blythin, D.J., Chen, X., Piwinski, J.J., McCormick, K.D. WO 9808826.
69. Gitter, B.D., Iyengar, S. WO 9731635.