Shire Orphan Therapies Gmbh

Jerini Ag

Alcon Research, Ltd.

Jpt Peptide Technologies Gmbh

Shire Orphan Thereapies Gmbh

Takeda Pharmaceutical Company Limited

Gerd Hummel

Ulrich Reineke

Frank Osterkamp

Ulf Reimer

Uwe Richter

Edgar Specker

Dirk Scharn

Markus Woischnik

Tobias Knaute

Heiko Hawlisch

Bernadett Simon

Mark R Hellberg

Gunther Zischinsky

Roland Stragies

Karsten Schnatbaum

Elsa Locardi

Grit Zahn

Thomas Polakowski

Claudia Christner-Albrecht

Doerte Vossmeyer

Holger Kalkhof

Sascha Birkner

Christoph Gibson

Matthias Paschke

Jens Schneider-Mergener

Jochen Knolle

Thomas Tradler

Jochen Pfeifer

Mark R Helberg

Mike Schutkowski

Liying Dong

Soren Panse

Laurence Jobron

Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.

NPR-B agonists

Disclosed are cyclic, peptide-based novel compounds having NPR-B agonistic activity. Preferred compounds are cyclic peptides containing conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds. In some embodiments, provided herein are a cyclic peptide compound with a ring size that is significantly reduced as compared to known NPR-B agonists, such as CNP.

Cyclic peptide-based NPR-B agonists

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

This invention is directed to compounds of structure (I). Particularly this invention is directed to compounds of structure (VIII) wherein the variables are defined as in the description. These compounds are integrin inhibitors and are useful in the treatment of diseases in which an inhibition of angiogenesis is desired. 

Compounds for the inhibition of angiogenesis 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

Gerd Hummel