Baxalta Gmbh

Shire Orphan Therapies Gmbh

Baxter International Inc.

Baxter Healthcare Sa

3B Pharmaceuticals Gmbh

Takeda Pharmaceutical Company Limited

Alcon Research, Ltd.

Jerini Ag

Shire Orphan Thereapies Gmbh

Tmd Friction Services Gmbh

Ulrich Reineke

Frank Osterkamp

Thomas Polakowski

Friedrich Scheiflinger

Michael Dockal

Gerd Hummel

Ulf Reimer

Hartmut Ehrlich

Rudolf Hartmann

Uwe Richter

Edgar Specker

Bernadett Simon

Tobias Knaute

Heiko Hawlisch

Markus Woischnik

Mark R Hellberg

Markus Fries

Dirk Scharn

Eberhard Schneider

Gunther Zischinsky

Matthias Paschke

Roland Stragies

Christian Haase

Christiane Smerling

Grit Zahn

Karsten Schnatbaum

Elsa Locardi

Jan Ungewiß

Holger Kalkhof

Doerte Vossmeyer

Claudia Christner-Albrecht

Sascha Birkner

Christoph Gibson

Dirk Zboralski

Wolfgang Hogenkamp

Jochen Pfeifer

Jan Ungewiss

Anne Bredenbeck

Aileen Höhne

Thomas Tradler

Jochen Knolle

Mark R Helberg

Paul Wahle

Helmuth Wensch

The present invention is related to a compound comprising a cyclic peptide and a chelator, and its use.

Compounds comprising a fibroblast activation protein ligand and use thereof

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 present invention is related to a compound of formula (I) wherein Ris selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting of 2-amino-2-adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9-carboxylic acid; Ris selected from the group consisting of (C-C)alkyl, (C-C)cycloalkyl, (C-C)cycloalkylmethyl, halogen, nitro and trifluoromethyl; ALK is (C-C)alkylidene; R, Rand Rare each and independently selected from the group consisting of hydrogen and (C-C)alkyl under the proviso that one of R, Rand Ris of the formula (II) wherein ALK' is (C-C)alkylidene; Ris selected from the group consisting of hydrogen and (C-C)alkyl; and Ris selected from the group consisting of H and an Effector moiety; or a pharmacologically acceptable salt, solvate or hydrate thereof. 

Neurotensin receptor ligands

The present invention is related to a conjugate comprising a structure of general formula (1) [TM1]-[AD1]-[LM]-[AD2]-[TM2] (1), wherein TM1 is a first targeting moiety, wherein the first targeting moiety is capable of binding to a first target, AD1 is a first adapter moiety or is absent, LM is a linker moiety or is absent, AD2 is a second adapter moiety or is absent, and TM2 is a second targeting moiety, wherein the second targeting moiety is capable of binding to a second target; wherein the first targeting moiety and/or the second targeting moiety is a compound of formula (2): wherein Ris selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting of 2-amino-2 adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9 carboxylic acid; Ris selected from the group consisting of (C-C)alkyl, (C-C)cycloalkyl, (CC)cycloalkylmethyl, halogen, nitro and trifluoromethyl; ALK' is (C-C)alkylidene; R, Rand Rare each and independently selected from the group consisting of hydrogen and (C-C)alkyl under the proviso that one of R, Rand Ris of the following formula (3) wherein ALK&#x2032; is (C-C)alkylidene; Ris selected from the group consisting of hydrogen and (C-C)alkyl; and Ris a bond; or a pharmacologically acceptable salt, solvate or hydrate thereof. 

Conjugate comprising a neurotensin receptor ligand and use thereof

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.

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

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.

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

Growing community of inventors

Berlin, Germany

Ulrich Reineke