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

Abstract: The present invention relates to compounds of formula (I) wherein: A is a radical selected from the group comprising aromatic heterocyclic 5-membered ring systems; Ar is a radical selected from the group comprising optionally substituted 5- and 6-membered aromatic ring systems, whereby the ring system contains 0, 1, 2 or 3 heteroatoms selected from the group comprising N, O and S; Z is a linker and ? is a radical of formula (II) and their use for the inhibition of integrin.

Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.

Abstract: The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21 and R22 are individually and independently selected from the group comprising H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl, substituted arylalkyl, heteroarylalkyl, substituted heteroarylalkyl, alkoxyl, substituted alkoxyl, aryloxy, substituted aryloxy, arylalkyloxy, substituted arylalkyloxy, acyloxy, substituted acyloxy, halogen, hydroxyl, nitro, cyano, acyl, substituted acyl, mercapto, alkylthio, substituted alkylthio, amino, substituted amino, alkylamino, substituted alkylamino, bisalkyl amino, substituted bisalkyl amino, cyclic amino, substituted cyclic amino, carbamoyl (—CONH2), substituted carbamoyl, carboxyl

Abstract: The present invention is related to a compound, preferably a C5a receptor antagonist, having the following structure: (I), whereby X1 is a radical having a mass of about 1-300, whereby X1 is preferably selected from the group comprising 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-5 R5-B(OH)—, and R5-CH?N—O—CH2—CO—, whereby R5 and R6 are individually and independently selected from the group comprising 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 and substituted aryloxyalkyl, X2 is a radical that mimics the biological binding characteristics of a phenylalanine unit, X3 and X4 are individually and independently a spacer, whereby the spacer is preferably selected from the group comprising ami

Abstract: The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and —S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y.

Abstract: The invention relates to a method for determining the substrate specificity of an enzymatic activity comprising the following steps: providing an assembly comprising a plurality of amino acid sequences on a planar surface of a support material, whereby the amino acids are directionally immobilised; contacting and/or incubating of an enzymatic activity with the assembly; and detection of a reaction between one of the amino acid sequences that are immobilised on the assembly and the enzymatic activity. According to the invention, during the reaction of the enzymatic activity with the assembly, a change in the molecular weight of at least one of the amino acid sequences takes place.

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

Abstract: The invention relates to a method for determining the substrate specificity of an enzymatic activity comprising the following steps: providing an assembly comprising a plurality of amino acid sequences on a planar surface of a support material, whereby the amino acids are directionally immobilised; contacting and/or incubating of an enzymatic activity with the assembly; and detection of a reaction between one of the amino acid sequences that are immobilised on the assembly and the enzymatic activity. According to the invention, during the reaction of the enzymatic activity with the assembly, a change in the molecular weight of at least one of the amino acid sequences takes place.