Substituted azetidin-2-ones as cysteine protease inhibitors

US6569847B1 · kind B1 · utility

Assignee

• Naeja Pharmaceutical Inc. · CA

Inventors

• Rajeshwar Singh · Edmonton, CA
• Andhe V. Narender Reddy · Swan Hills, CA
• Jadwiga Kaleta · Edmonton, CA
• Ronald G. Micetich · Edmonton, CA
• Mark Whittaker · Felton, GB
• Philip Huxley · Felton, GB

Key dates

• Filing date: Oct 5, 2001
• Grant date: May 27, 2003
• Expiry date: Oct 5, 2021

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention relates to substituted azetidin-2-ones and to pharmaceutical compositions containing such compounds. Their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins is also described. The invention includes a compound of formula (I), Y represents —C(O)— or —S(O2)—; R represents an allyl (ie CH2═CHCH2—) group or a radical. R1 represents —OCOR5, —OR5, —SR5, —S(O)R5, or —S(O)2R5; R2 represents a radical. R3 represents —OR5 or R5; or a pharmaceutically acceptable salt, hydrate or solvate thereof.