(19)

(11)

EP 1 175 422 A2

(12)

(88) Date of publication A3: 08.02.2001 (43) Date of publication: 30.01.2002 Bulletin 2002/05 (21) Application number: 00926495.3 (22) Date of filing: 01.05.2000

(51) International Patent Classification (IPC)7: C07D 498/04, A61K 31/5383, A61P 35/00, A61P 5/32 (86) International application number: PCT/US0011/750 (87) International publication number: WO 0066/590 (09.11.2000 Gazette 2000/45)

(84) Designated Contracting States: AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE Designated Extension States: AL LT LV MK RO SI (30) Priority: 04.05.1999 US 304614 19.04.2000 US 552353 (71) Applicants: LIGAND PHARMACEUTICALS INCORPORATED San Diego, California 92121 (US) American Home Products Corporation Madison, New Jersey 07840 (US)

(72) Inventors: ZHI, Lin San Diego, CA 92129 (US) JONES, Todd, K. Solana Beach, CA 92075 (US) TEGLEY, Christopher, M. Thousand Oaks, CA 91360 (US) FENSOME, Andrew Wayne, PA 19087 (US) ZHANG, Puwen Audubon, PA 19403 (US) WROBEL, JAY,E Lawrenceville, NJ 08648 (US) EDWARDS, James, P San Diego, CA 92129 (US) (74) Representative: Hale, Stephen Geoffrey  JY & GW Johnson, Kingsbourne House, 229-231 High Holborn London WC1V 7DP London WC1V 7DP (GB)