Jerini Ag

Shire Orphan Therapies Gmbh

Elsa Locardi

Gerd Hummel

Dirk Scharn

Karsten Schnatbaum

Ulrich Reineke

Thomas Polakowski

Uwe Richter

Ulf Reimer

Christoph Gibson

Matthias Paschke

Thomas Tradler

Jochen Pfeifer

The present invention is related to compound of the formula (I): or a pharmacologically acceptable salt, solvate, or hydrate thereof, wherein A is a 6-membered heteroaryl having from 1 to 3 heteroatoms, each independently selected from N or O and the other substituents are defined as in the claims. 

8-oxy-quinoline derivatives as bradykinin B2 receptor modulators

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 (&#x2014;CONH), substituted carbamoyl, carboxyl, carbamate, alkoxycarbonyl, substituted alkoxycarbonyl, acylamino, substituted acylamino, sulfamoyl (&#x2014;SONH), substituted sulfamoyl, haloalkyl, haloalkyloxy, &#x2014;C(O)H, trialkylsilyl and azido. 

C5a receptor antagonists

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&#x2014;, R5-N(R6)-CO&#x2014;, R5-O&#x2014;CO&#x2014;, R5-SO&#x2014;, R5-N(R6)-SO&#x2014;, R5-N(R6)-, R5-N(R6)-CS&#x2014;, R5-N(R6)-C(NH)&#x2014;, R5-CS&#x2014;, R5-P(O)OH&#x2014;, R5-B(OH)&#x2014; or R5-CH&#x2550;N&#x2014;O&#x2014;CH&#x2014;CO&#x2014;, 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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Berlin, Germany

Elsa Locardi