Shire Orphan Therapies Gmbh

Jerini Ag

Boehringer Ingelheim International Gmbh

Jpt Peptide Technologies Gmbh

Dirk Scharn

Georg Dahmann

Gerd Hummel

Ulrich Reineke

Frank Osterkamp

Karsten Schnatbaum

Elsa Locardi

Thomas Polakowski

Ulf Reimer

Uwe Richter

Gunther Zischinsky

Roland Stragies

Grit Zahn

Holger Kalkhof

Doerte Vossmeyer

Claudia Christner-Albrecht

Tobias Wunberg

Harald Engelhardt

Juergen Ramharter

Ulrich Reiser

Christoph Gibson

Matthias Paschke

Mark Petronczki

Dietrich Boese

Jens Schneider-Mergener

Heinz Stadtmueller

Thomas Tradler

Jochen Pfeifer

Mike Schutkowski

Liying Dong

Soren Panse

Laurence Jobron

Sebastian Carotta

Matthias Treu

Birgit Wilding

Ralph Neumueller

Julian Fuchs

Heribert Arnhof

Marc Kerenyi

Marco Hofmann

Marco Hans Hofmann

The present invention encompasses compounds of formula (I) wherein the groups Rto Rand Xto Xhave the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

Substituted 1H-pyrazolo[4,3-c]pyridines and derivatives as EGFR inhibitors

The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; &#x3a8; is a radical of formula (II), Ris 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. 

Compounds for the inhibition of integrins and use thereof

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 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 &#x3a8; is a radical of formula (II) and their use for the inhibition of integrin. 

Heterocyclic compounds for the inhibition of integrins and use thereof

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 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 immobilized; 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 immobilized 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.

Method for determining the substrate specificity of an enzyme

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

Dirk Scharn