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(11)

EP 1 083 897 A1

(12)

(43) Date of publication: 21.03.2001 Bulletin 2001/12 (21) Application number: 99926096.1 (22) Date of filing: 01.06.1999

(51) International Patent Classification (IPC)7: A61K 31/40, A61K 31/415, A61K 31/445, C07D 207/30, C07D 207/333, C07D 209/04, C07D 209/12, C07D 211/18, C07D 211/26, C07D 211/28, C07D 211/32, C07D 211/40, C07D 231/10, C07D 231/12, C07D 233/54, C07D 233/64, C07D 401/04 (86) International application number: PCT/US9912/095 (87) International publication number: WO 9962/513 (09.12.1999 Gazette 1999/49)

(84) Designated Contracting States: AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU NL PT SE Designated Extension States: AL LT LV MK RO SI (30) Priority: 03.06.1998 US 87845 P 09.07.1998 GB 9814930 (71) Applicants: MERCK & CO., INC. Rahway, New Jersey 07065 (US) Tularik Inc. South San Francisco, CA 94080 (US)

(72) Inventors: SELNICK, Harold, G. Rahway, NJ 07065 (US) HAZUDA, Daria, Jean Rahway, NJ 07065 (US) EGBERTSON, Melissa Rahway, NJ 07065 (US) GUARE, James, P., Jr. Rahway, NJ 07065 (US) WAI, John, S. Rahway, NJ 07065 (US) YOUNG, Steven, D. Rahway, NJ 07065 (US) CLARK, David, L. South San Francisco, CA 94080 (US) MEDINA, Julio, C. South San Francisco, CA 94080 (US) (74) Representative: Horgan, James Michael Frederic  Merck & Co., Inc.,Terlings Park,Eastwick Road Harlow,Essex CM20 2QR Harlow,Essex CM20 2QR (GB)