A novel orally active inhibitor of HLE

European Journal of Medicinal Chemistry

Volumn 38, Issue 4, 2003, Pages 421-425

  Varga, Márton ^a   Kapui, Zoltán ^a   Bátori, Sándor ^a   Nagy, Lajos T ^a   Vasvári Debreczy, Lelle ^a   Mikus, Endre ^a   Urbán Szabó, Katalin ^a   Arányi, Péter ^a  

^a Chinoin Pharmaceutical and Chemical Works Ltd   (Hungary)

Author keywords

Adult respiratory distress syndrome; Bronchoalveolar lavage; Chronic obstructive pulmonary disease; Human leucocyte elastase; Polymorphonuclear leukocyte; 1 Protease inhibitor

Indexed keywords

2 [(4 ISOPROPYL 6 METHOXY 1,1 DIOXIDO 3 OXO 1,2 BENZISOTHIAZOL 2(3H) YL)METHOXY] 9 (2 PIPERIDIN 1 YLETHOXY) 4H PYRIDO[1,2 A]PYRIMIDIN 4 ONE; LEUKOCYTE ELASTASE INHIBITOR; SSR 69071; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; CHRONIC OBSTRUCTIVE LUNG DISEASE; CONFERENCE PAPER; CONTROLLED STUDY; CYSTIC FIBROSIS; DOSE RESPONSE; DRUG EFFICACY; DRUG THERAPY; EMPHYSEMA; ENZYME INHIBITION; LUNG HEMORRHAGE; LUNG LAVAGE; MOUSE; NONHUMAN;

EID: 0038393251     PISSN: 02235234     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0223-5234(03)00046-1     Document Type: Conference Paper

References (20)

1. P. Arányi, S. Batori, S. Dessilla, I. Hermecz, Z. Kapui, F. Levai, E. Mikus, M. Pascal, L. T. Nagy, B. Simonot, K. Urban-Szabo, M. Varga, L. Vasvari-Debreczy, Saccharin derivatives as orally active elastase inhibators, WO 01/44245 A1 (Priority date. 17-12-1999).
2. Kapui Z., Varga M., Urban-Szabo K., Mikus E., Szabó T., Szeredi J., Finance O., Arányi P. J. Pharm. Exp. Ther. 305:2003;1-9.
3. Delclaux C., Delacourt C., d'Ortho M., Boyer V., Lafuma C., Harf A. Am. J. Respir. Cell Mol. Biol. 14:1996;288-295.
4. Skiles J.W., Jeng A. Exp. Opin. Ther. Patents. 9:1999;869-895.
5. Vogelmeier C., Hubbard R.C., Fells G.A., Schnebli H.P., Thompson R.C., Fritz H., Crystal R.G. J. Clin. Invest. 87:1991;482-488.
6. Janoff A. Am. Rev. Respir. Dis. 132:1985;417-433.
7. Lee C.T., Fein A.M., Lippmann M., Holzmann H., Kimbel P., Weinbaum G. N. Eng. J. Med. 304:1981;192-196.
8. Llewellyn-Jones C.G., Harris T.A., Stockley R.A. Am. J. Respir. Crit. Care Med. 153:1996;616-621.
9. Piccioni P.D., Kramps J.A., Rudolphus A., Bulgheroni A., Luisetti M. Chest. 102:1992;1470-1476.
10. Cowan K.N., Heilbut A., Humpl T., Lam C., Ito S., Rabinovitsch M. Nat. Med. 6:2000;698-702.
11. Adeyemi E.O., Neumann S., Chadwik V.S., Hodgson H.J.F., Prepys M.B. Gut. 26:1985;1306-1311.
12. Veale C.A., Bernstein P.R., Bohnert C.M., Brown F.J., Bryant C., Damewood J.R., Earley R., Feeney S.W., Edwards P.D., Gomes B., Hulsizer J.M., Kosmider B.J., Krell R.D., Moore G., Wolanin D.J., Woolson S. J. Med. Chem. 40:1997;3173-3181.
13. Hlasta D.J., Bell M.R., Boaz N.W., Court J.J., Desai R.C., Franke C.A., Mura A.J., Subramanyam C., Dunlap R.P. Bioorg. Med. Chem. Lett. 4:1994;1801-1806.
14. Hlasta D.J., Ackerman J.H., Court J.J., et al. J. Med. Chem. 38:1995;4687-4692.
15. Desai R.C., Hlasta D.J., Monsour G., et al. J. Org. Chem. 59:1994;7161-7163. EP 550111 A1.
16. Shinguh Y., Yamazaki A., Inamura N., Fujie K., Okamoto M., Nakahara K., Notsu Y., Okuhara M., Ono T. Eur. J. Pharmacol. 345:1998;299-308.
17. Gütschow M., Kuerschner L., Neumann U., Pietsch M., Löser R., Koglin N., Eger K. J. Med. Chem. 42:1999;5437-5447.
18. Mitsuhashi H., Asano S., Nonaka T., Masuda K., Kiyoki M. J. Pharm. Exp. Ther. 282:1997;1005-1010.
19. Kawabata K., Suzuki M., Sugitani M., Imaki K., Toda M., Miyamoto T. Biochem. Biophys. Res. Comm. 177:1991;814-820.
20. Norman P. Drug News Perspect. 11:1998;431-437.