C5a receptor antagonists

Details C5a receptor antagonists C5a receptor antagonists

C - Chemistry, Metallurgy

07

K

C07K 7/00 (2006.01)

Patent

CA 2532994

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.

L'invention concerne un antagoniste du récepteur de C5A, de structure (I), dans laquelle X1 désigne un radical d'une masse d'environ 1-300 et signifie R5-, R5-CO-, R5-N(R6)-CO-, R5-O-CO-, R5-SO¿2?-, R5-N(R6)-SO¿2?-, R5-N(R6)-, R5-N(R6)-CS-, R5-N(R6)-C(NH)-, R5-CS-, R5-P(O)OH-, R5-B(OH), ou R5-CH=N-O-CH¿2?-CO-, où R5 / R6 désigne H, F, un hydroxy, un alkyle, un alkyle substitué, un cycloalkyle, un cycloalkyle substitué, un hétérocyclyle, un hétérocyclyle substitué, un arylalkyle, un arylalkyle substitué, un aryle, un aryle substitué, un hétéroaryle, un hétéroaryle substitué, un acyle, un acyle substitué , un alcoxy, un alcoxyalkyle, un alcoxyalkyle substitué, un aryloxyalkyle ou un aryloxyalkyle substitué, X2 = radical (propriétés biologiques d'un motif phynylalanine mimétisant), X3 / X4 = espaceur (aminoacides, analogues d'aminoacides ou dérivés d'aminoacides), X5 = radical (propriétés de liaison biologiques d'un motif cyclohexylalanine ou homoleucine mimétisant), X6 = radical (propriétés biologiques d'un motif tryptophane mimétisant), X7 = radical (propriétés biologiques d'un motif norleucine ou phénylalanine mimétisant), une liaison chimique étant formée entre X3 et X7.

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