Platelet aggregation inhibitors

US5968902A · kind A · utility

Assignee

• COR Therapeutics, Inc. · US

Inventors

• Robert M. Scarborough · Belmont, US
• David L. Wolf · Palo Alto, US
• Israel Charo · Lafayette, US

Key dates

• Filing date: Jun 7, 1995
• Grant date: Oct 19, 1999
• Expiry date: Jun 7, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K14/78
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The isolated and purified PAI from several active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K* -(G/Sar)-D wherein K* is a modified lysyl residue of the formula EQU R.sup.1.sub.2 N(CH .sub.2).sub.4 CHNHCO-- wherein each R.sup.1 is independently H, alkyl(1-6C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6C), phenyl or benzyl, or is NR.sup.4 .sub.2 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3 is H, alkyl(1-6C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.5 is independently H or alkyl(1-6C); PA1 and wherein one or two (CH.sub.2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom PA1 are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.