C5a receptor antagonists

US7727960B2 · kind B2 · utility

Assignee

• Jerini AG · DE

Inventors

• Gerd Hummel · Berlin, DE
• Elsa Locardi · Berlin, DE
• Thomas Polakowski · Berlin, DE
• Dirk Scharn · Wien, AT
• Karsten Schnatbaum · Berlin, DE

Key dates

• Filing date: Jul 19, 2004
• Grant date: Jun 1, 2010
• Expiry date: Jul 19, 2024

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K14/705
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to a C5a receptor antagonist of structure (I), wherein X1 is a radical having a mass of about 1-300 and stands for R5-, R5-CO—, R5-N(R6)-CO—, R5-O—CO—, R5-SO2—, R5-N(R6)-SO2—, R5-N(R6)-, R5-N(R6)-CS—, R5-N(R6)-C(NH)—, R5-CS—, R5-P(O)OH—, R5-B(OH)— or R5-CH═N—O—CH2—CO—, wherein R5/R6 represent H, F, hydroxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, arylalkyl, substituted arylalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl, substituted acyl, alkoxy, alkoxyalkyl, substituted alkoxyalkyl, aryloxyalkyl or substituted aryloxyalkyl; X2=radical (biological bonding properties of a mimicrying phenylalanine unit); X3/X4=spacer (amino acids, amino-acid analogs and amino-acid derivatives); X5=radical (biological bonding properties of a mimicrying cyclohexylalanine or homoleucine unit); X6=radical (biological bonding properties of a mimicrying tryptophan unit); X7=radical (biological bonding properties of a mimicrying norleucine or phenylalanine unit), a chemical bond being formed between X3 and X7.