(19)

(11)

EP 1 224 316 A2

(12)

(88) Date of publication A3: 13.12.2001 (43) Date of publication: 24.07.2002 Bulletin 2002/30 (21) Application number: 00966129.9 (22) Date of filing: 06.10.2000

(51) International Patent Classification (IPC)7: C12P 17/16, C12P 17/18, C12P 41/00, C12N 9/00, C07K 16/44, C07D 277/24, C07D 277/36, C07D 277/34, C07D 417/06, C07D 493/04, A61K 31/427, A61P 35/00 // (C07D493/04, 313:00, 277:00) (86) International application number: PCT/EP0009/817 (87) International publication number: WO 0127/308 (19.04.2001 Gazette 2001/16)

(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: 08.10.1999 US 415453 21.06.2000 US 213064 P (71) Applicants: Novartis AG 4056 Basel (CH) The Scripps Research Institute La Jolla, CA 92037 (US)	(72) Inventors: SINHA, Subhash, C. San Diego, CA 92130 (US) LERNER, Richard, A. La Jolla, CA 92037 (US) BARBAS, Carlos, F. Solana Beach, CA 92075 (US) SUN, Jian San Diego, CA 92122 (US) (74) Representative: Fisher, Adrian John et al CARPMAELS & RANSFORD43 Bloomsbury Square London WC1A 2RA London WC1A 2RA (GB)