Cyclopeptide derivatives

US6566491B2 · kind B2 · utility

Assignee

• Merck Patentgesellschaft · DE

Inventors

• Alfred Jonczyk · Darmstadt, DE
• Simon Goodman
• Beate Diefenbach · Darmstadt, DE
• Arne Sutter · Darmstadt, DE
• Horst Kessler · Schwalbach, DE

Key dates

• Filing date: Aug 18, 1998
• Grant date: May 20, 2003
• Expiry date: Aug 18, 2018

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to compounds of the formula (I) R1—Q1—X—Q2—R2, in which: Q1, Q2, each independent of one another, are missing or are —NH—(CH2)n—CO—; R1, R2, each independent of one another, are missing or are cyclo-(Arg-Gly-Asp-Z), wherein Z is missing in side chain of Q1 or Q2 of if Q1 and/or Q2 missing, is bound to X, at least one of the groups R1 or R2 always having to be included; X is —CO—R18—CO—, and if R1—Q1— or R2—Q2— are missing is R10, R13, Het-CO or a flourescent pigment residue linked through a —CONH—, —COO—, NH—C(═S)—N—, —NH—C(═O)—NH—, —SO2 NH—or —NHCO— bond; and Z, R10, R13, R16, R18, Het and n have the meaning given in claim 1. The invention also relates to the salts of said compounds. These compounds and their salts can be used as integrin inhibitors, in particular for the prevention and treatment of circulatory diseases, thrombosis, heart infarct, coronary heart diseases, arteriosclerosis, angiogenic diseases and in tumor therapy.