Baxalta Gmbh

Baxter International Inc.

Baxter Healthcare Sa

Takeda Pharmaceutical Company Limited

Jerini Ag

Thomas Polakowski

Friedrich Scheiflinger

Michael Dockal

Ulrich Reineke

Frank Osterkamp

Rudolf Hartmann

Hartmut Ehrlich

Markus Fries

Eberhard Schneider

Ulf Reimer

Gerd Hummel

Dirk Scharn

Matthias Paschke

Karsten Schnatbaum

Elsa Locardi

Bettina Hartlieb

Uwe Richter

The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, an identify a TFPI-binding compound.

TFPI inhibitors and methods of use

The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, and/or treat a blood coagulation disorder in a subject.

The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. Peptide complexes also are provided. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.

The invention provides peptides, including peptides that bind and, optionally, inhibit Protein S, and compositions thereof. The peptides may be used to, e.g., inhibit Protein S activity, enhance thrombin formation in a subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify Protein S, and identify a Protein S binding compound.

Peptides and methods of use

The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.

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.

Growing community of inventors

Berlin, Germany

Thomas Polakowski