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EP 0 552 309 A1

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(43) Date of publication: 28.07.1993 Bulletin 1993/30 (21) Application number: 92901105.0 (22) Date of filing: 19.09.1991

(51) International Patent Classification (IPC):  A61K 31/ 675( . ) C07F 9/ 09( . ) C07F 9/ 59( . ) C07F 9/ 655( . ) C07K 7/ 56( . ) A61K 38/ 00( . ) A61P 37/ 00( . ) C07F 9/ 117( . ) C07F 9/ 6533( . ) C07H 19/ 01( . ) C12P 9/ 00( . ) C12R 1/ 845( . ) (86) International application number: PCT/US1991/006816 (87) International publication number: WO 1992/006992 (30.04.1992 Gazette 1992/10)

(84) Designated Contracting States: AT BE CH DE DK ES FR GB GR IT LI LU NL SE (30) Priority: 09.10.1990 US 19900594500 09.10.1990 US 19900594214 11.10.1990 US 19900595894 26.04.1991 US 19910691606 26.04.1991 US 19910691607 16.05.1991 US 19910701387 25.07.1991 US 19910735963 (71) Applicant: MERCK & CO. INC. Rahway New Jersey 07065-0900 (US)

(72) Inventors: CHEN, Shieh-Shung, Tom Morganville, NJ 07751 (US) PETUCH, Brian, R. Florence, NJ 08518 (US) HSU, Annjia, T. Columbus, OH 43220 (US) ARISON, Byron, H. Watchung, NJ 07060 (US) DUMONT, Francis Rahway, NJ 07065 (US) WHITE, Raymond, F. Englishtown, NJ 07726 (US) MATHRE, David, J. Edison, NJ 08817 (US) WU, Jane, T. Scotch Plains, NJ 07076 (US) SO, Lydia, T. Maywood, NJ 07607 (US) REAMER, Robert, A. Bloomfield, NY 07003 (US) (74) Representative: Quillin, Helen Kaye, et al  European Patent Department, Merck & Co., Inc., Terlings Park, Eastwick Road Harlow, Essex CM20 2QR Harlow, Essex CM20 2QR (GB)