(19)

(11)

EP 0 497 835 A1

(12)

(43) Date of publication: 12.08.1992 Bulletin 1992/33 (21) Application number: 90915950.0 (22) Date of filing: 16.10.1990

(51) International Patent Classification (IPC):  A61K 31/ 13( . ) A61K 31/ 16( . ) A61K 31/ 275( . ) A61K 38/ 55( . ) C07C 237/ 22( . ) C07D 233/ 64( . ) C07K 5/ 06( . ) A61K 31/ 155( . ) A61K 31/ 215( . ) A61K 38/ 00( . ) A61P 31/ 12( . ) C07D 213/ 89( . ) C07K 5/ 02( . ) C07K 14/ 81( . ) (86) International application number: PCT/US1990/005818 (87) International publication number: WO 1991/006561 (16.05.1991 Gazette 1991/11)

(84) Designated Contracting States: AT BE CH DE DK ES FR GB GR IT LI LU NL SE (30) Priority: 27.10.1989 US 19890428291 (71) Applicant: THE UPJOHN COMPANY Kalamazoo, Michigan 49001 (US)

(72) Inventors: HEINRIKSON, Robert, Leroy Kalamazoo, MI 49008 (US) TOMASSELLI, Alfredo, Guiseppe Kalamazoo, MI 49009 (US) SAWYER, Tomi, Kim Portage, MI 49002 (US) SCHOSTAREZ, Heinrich, Josef Portage, MI 49002 (US) THAISRIVONGS, Suvit Portage, MI 49002 (US) HESTER, Jackson, B., Jr. Galesburg, MI 49053 (US) HUI, John, On-Ting Portage, MI 49002 (US) TARPLEY, William, Gary Omaha, NB 68124 (US) TEN BRINK, Ruth, Elizabeth Richland, MI 49083 (US) (74) Representative: Perry, Robert Edward, et al  GILL JENNINGS & EVERY Broadgate House 7 Eldon Street London EC2M 7LH London EC2M 7LH (GB)