Title:
ALPHA ACYLOXYACETAMIDES FOR KALLIKREIN AND UROKINASE INHIBITION
Document Type and Number:
WIPO Patent Application WO2003101941
Kind Code:
A3
Abstract:
Disclosed herein is a compound represented by Structural Formula (I). R1 is a substituted or unsubstituted aryl group or alkyl group; R2 is a substituted or unsubstituted aryl group or cycloalkyl group; Ar is a substituted or unsubstituted aryl group; X is a -CH2-, -O-, -S- or -CO-, m is an integer from zero to two; n is an integer from 0-2 when X is -O-, -S- and 1-2 when X is -CH2- or -CO-. Also disclosed are methods of inhibiting kallikrein activity or urokinase activity in subject in need of such inhibition by administering a compound represented by Structural Formula (I).
Inventors:
STAVESKI MARK M (US)
SNEDDON SCOTT F (US)
SNEDDON SCOTT F (US)
Application Number:
PCT/US2003/016665
Publication Date:
September 01, 2005
Filing Date:
May 28, 2003
Export Citation:
Assignee:
GENZYME CORP (US)
STAVESKI MARK M (US)
SNEDDON SCOTT F (US)
STAVESKI MARK M (US)
SNEDDON SCOTT F (US)
International Classes:
C07C235/34; C07C235/36; C07C235/38; C07C237/30; C07C255/57; C07C323/25; C07D209/18; C07D215/12; C07D239/38; C07D317/58; C07D405/12; C07D495/04; (IPC1-7): C07C235/34; C07C317/46; C07D215/38; C07C235/36; C07C323/62; C07D495/04; C07C235/38; C07D209/18; C07C323/41; C07C237/30; C07D239/38; C07D405/12; C07C255/57; C07D317/58
Domestic Patent References:
| WO2000041531A2 | 2000-07-20 |
Foreign References:
| JPH01253742A | 1989-10-11 |
Other References:
BAKER, R.H. ET AL.: "The Passerini Reaction. II. Optically active anilides", J. AM. CHEM. SOC., vol. 70, no. 11, 1948, pages 3721 - 3723, XP002253870
TENO N ET AL: "DEVELOPMENT OF ACTIVE CENTER-DIRECTED PLASMIN AND PLASMA KALLIKREIN INHIBITORS AND STUDIES ON THE STRUCTURE-INHIBITORY ACTIVITY RELATIONSHIP", CHEMICAL AND PHARMACEUTICAL BULLETIN, PHARMACEUTICAL SOCIETY OF JAPAN. TOKYO, JP, vol. 41, no. 6, June 1993 (1993-06-01), pages 1079 - 1090, XP001007888, ISSN: 0009-2363
OKADA Y ET AL: "Development of plasmin and plasma kallikrein selective inhibitors and their effect on M1 (melanoma) and ht29 cell lines", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 10, no. 19, 2 October 2000 (2000-10-02), pages 2217 - 2221, XP004212007, ISSN: 0960-894X
TENO N ET AL: "DEVELOPMENT OF ACTIVE CENTER-DIRECTED PLASMIN AND PLASMA KALLIKREIN INHIBITORS AND STUDIES ON THE STRUCTURE-INHIBITORY ACTIVITY RELATIONSHIP", CHEMICAL AND PHARMACEUTICAL BULLETIN, PHARMACEUTICAL SOCIETY OF JAPAN. TOKYO, JP, vol. 41, no. 6, June 1993 (1993-06-01), pages 1079 - 1090, XP001007888, ISSN: 0009-2363
OKADA Y ET AL: "Development of plasmin and plasma kallikrein selective inhibitors and their effect on M1 (melanoma) and ht29 cell lines", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 10, no. 19, 2 October 2000 (2000-10-02), pages 2217 - 2221, XP004212007, ISSN: 0960-894X
Download PDF: