Baxalta Gmbh

Shire Orphan Therapies Gmbh

Baxter International Inc.

Baxter Healthcare Sa

3b Pharmaceuticals Gmbh

Takeda Pharmaceutical Company Limited

Alcon Research, Ltd.

Jpt Peptide Technologies Gmbh

Shire Orphan Thereapies Gmbh

Frank Osterkamp

Ulrich Reineke

Friedrich Scheiflinger

Michael Dockal

Thomas Polakowski

Gerd Hummel

Rudolf Hartmann

Ulf Reimer

Uwe Richter

Edgar Specker

Markus Woischnik

Heiko Hawlisch

Tobias Knaute

Bernadett Simon

Mark R Hellberg

Hartmut Ehrlich

Markus Fries

Matthias Paschke

Gunther Zischinsky

Dirk Scharn

Roland Stragies

Christian Haase

Christiane Smerling

Grit Zahn

Bettina Hartlieb

Jan Ungewiß

Holger Kalkhof

Doerte Vossmeyer

Claudia Christner-Albrecht

Sascha Birkner

Dirk Zboralski

Jens Schneider-Mergener

Mark R Helberg

Jan Ungewiss

Anne Bredenbeck

Aileen Höhne

Eberhard Schneider

Laurence Jobron

Soren Panse

Liying Dong

Mike Schutkowski

Jochen Knolle

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 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, 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.

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

Frank Osterkamp