Method for inhibiting blood vessel blockage using octapeptide compositions

US5147856A · kind A · utility

Assignee

• Société de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S) SAS · FR

Inventors

• Peter W. Ramwell · McLean, US
• Pierre Braquet · Garches, FR

Key dates

• Filing date: Mar 28, 1989
• Grant date: Sep 15, 1992
• Expiry date: Mar 28, 2009

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A method for inhibiting blood vessel blockage in a mammal particularly after a procedure such as angioplasty, an arterial bypass operation or an allograft transplant operation which comprises: administering to a mammal before, during and/or after the procedure an effective blood vessel blockage inhibiting amount of an octapeptide having the formula ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o-, m- or, more preferably, p-substituted X-Phe (where X is a halogen, H, NH.sub.2, NO.sub.2, OH , or C.sub.1-13 alkyl), pentafluoro-Phe, or .beta.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile; A.sub.7 is Thr, Trp, or .beta.-Nal (and can be either the D- or L-isomer); and Z is NH.sub.2 or OH; or a pharm…