C5a receptor antagonists

Details C5a receptor antagonists C5a receptor antagonists

2004-07-19

2010-06-01

Gupta, Anish (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C530S329000

Reexamination Certificate

active

07727960

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.

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Demartino et al., “Arginine 206 of the C5a receptor is critical for ligand recognition and receptor activation by C-terminal hexapeptide analogs”, Journal of Biological Chemistry, vol. 270, No. 27, 1995, pp. 15966-15969.
March, Darren R. et al., “Potent Cyclic Antagonists of the Complement C5a Receptor on Human Polymorphonuclear Leukocytes. Relationships between Structures and Activity,” Institute for Molecular Bioscience and School of Biomedical Sciences, vol. 65, No. 4, Jan. 7, 2004, pp. 868-879.
DeMartino, Julie A. et al., “Arginine 206 of the C5a Receptor is Critical for Ligand Recognition and Receptor Activation by C-terminal Hexapeptide Analogs,” The Journal of Biological Chemistry, vol. 270, No. 27, Jul. 7, 1995, pp. 15966-15969.

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