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EP 1 204 640 A2

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(88) Date of publication A3: 05.07.2001 (43) Date of publication: 15.05.2002 Bulletin 2002/20 (21) Application number: 00952261.6 (22) Date of filing: 28.07.2000

(51) International Patent Classification (IPC)7: C07D 211/52, A61K 31/497, A61K 31/4523, A61P 29/00, C07D 405/06, C07D 493/04, C07D 409/06, C07D 495/04, C07D 491/04, C07D 401/06, C07D 401/14, C07D 471/04, C07D 519/00, C07D 313/12 // (C07D493/04, 317:00), C07D313:00,(C07D495/04, 333:00), C07D313:00,(C07D491/04, 313:00), C07D221:00,(C07D471/04, 223:00) (86) International application number: PCT/US0020/607 (87) International publication number: WO 0109/094 (08.02.2001 Gazette 2001/06)

(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: 28.07.1999 US 362807 (71) Applicants: Millennium Pharmaceuticals, Inc. Cambridge,Massachusetts 02139 (US) KYOWA HAKKO KOGYO CO., LTD. Chiyoda-ku,Tokyo 100-8185 (JP)

(72) Inventors: LULY, Jay, R. Wellesley, MA 02481 (US) NAKASATO, Yoshisuke Sunto-gun,Shizuoka 411 (JP) OHSHIMA, Etsuo Nagareyama-shi,Chiba 270-0115 (JP) SONE, Hiroki Sunto-gun,Shizuoka 411 (JP) KOTERA, Osamu Sunto-gun,Shizuoka 411 (JP) HARRIMAN, Geraldine, C., B. Charlestown, RI 02813 (US) CARSON, Kenneth, G. Needham, MA 02492 (US) (74) Representative: Keen, Celia Mary  J.A. Kemp & Co.14 South SquareGray's Inn London WC1R 5JJ London WC1R 5JJ (GB)