N-terminal site selective inhibitors of human angiotensin conversion enzyme (ACE)

US6482797B1 · kind B1 · utility

Assignees

• COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES · FR
• Institut National de la Sante et de la Recherche Medicale (INSERM) · FR

Inventors

• Vincent Dive · Palaiseau, FR
• Joel Cotton · Orsay, FR
• Philippe Cuniasse · Montrouge, FR
• Athanasios Yiotakis · Athens, GR
• Pierre Corvol · Paris, FR
• Annie Michaud · Le Touquet-Paris-Plage, FR
• Marie-Thérèse Chauvet · Chaumont, FR
• Joël Menard · Paris, FR
• Eric Ezan · Malakoff, FR

Key dates

• Filing date: Jan 30, 2001
• Grant date: Nov 19, 2002
• Expiry date: Jan 30, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/572
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to peptide derivatives that can be used as selective inhibitors of the N-terminal site of human angiotensin-converting enzyme.The derivatives comprise the amino acid sequence with the following formula:-Asp-Phe-&PSgr;(PO2CH2)-Ala-Xaa′-  (I)wherein:&PSgr;(PO2CH2) indicates that the peptide bond (CONH) between Phe and Ala has been replaced by the phosphonic bond PO2CH2, andXaa′ represents an amino acid residue.They can be used in pharmaceutical formulations, particularly to protect haematopoietic strain cells of patients undergoing aggressive chemotherapy or radiotherapy treatment.