C07K5/1027

Peptidomimetics for imaging the ghrelin receptor

The present invention concerns compositions comprising and methods of identification and use of imaging agents. The imaging agents comprise a growth hormone secretagogues having a conjugated fluoride. The imaging agents of the present invention may be used for detection, diagnosis and/or staging of prostate or other forms of cancer, and may also be used for cardiac disease.

NOVEL AGENTS TARGETING INHIBITOR OF APOPTOSIS PROTEINS

Disclosed herein, inter alia, are methods of use and composition of novel inhibitors that target the Smac binding site of a variety of inhibitor of apoptosis proteins that contain a Bir domain, including XIAP, cIAP1, cIAP2, or other IAP proteins.

PROCESS AND INTERMEDIATES FOR SYNTHESIS OF PEPTIDE COMPOUNDS
20200199173 · 2020-06-25 ·

Disclosed is a new process and intermediates for preparing dipyrrolidine peptide compounds such as, for example, rapastinel. Advantageously, the process may be industrially scalable and cost-effective and use less toxic reagents and/or solvents. Further, the process may be used to prepare peptide compounds having improved purity.

ANTIMICROBIAL PEPTIDOMIMETICS
20200157144 · 2020-05-21 ·

The present invention relates to peptides containing guanidine and halogenated biphenyl moieties of the formula (I), and to salts and solvates of each of these peptides and to processes for the preparation thereof, compositions containing them and the uses of such compounds. It has been found that the compounds have a high microbicide activity and are suited to combat resistant bacteria, such as Methicillin-resistant Staphylococcus aureus (MRSA) strains, at very low concentrations.

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METHOD FOR ENHANCING EXTRACELLULAR VESICLE PRODUCTION
20190316163 · 2019-10-17 ·

A method for enhancing extracellular vesicle production is described. A peptide that induces polymer formation is incubated with a cell culture which results in enhanced EV production. The peptide penetrates the cells and subsequently polymerizes upon exposure to enzymes (e.g. phosphatase) within the cell. The cells that contain the newly formed polymers have an increased production of EVs. These EVs can be harvested using centrifugation techniques.

18F LABELED AMINO ACIDS, DERIVATIVES THEREOF AND METHOD OF MAKING SAME

The present invention provides .sup.18F-labeled amino acids or derivatives thereof having formula (I) and methods of making same, which can be suitable for PET imaging:

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SOLUTION PHASE SYNTHESIS AND CRYSTALLIZATION OF BETA-TURN PEPTIDOMIMETIC CYCLIC SALTS
20190194251 · 2019-06-27 ·

The present disclosure relates to methods of preparing and crystallizing -turn cyclic peptidomimetic salts of formula I:

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where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.10, X, Y and n are as defined in the specification.

The present disclosure provides a more efficient route for preparing a crystalline form of -turn cyclic peptidomimetic compounds and salts thereof.

PROTEASOME INHIBITORS
20190161516 · 2019-05-30 ·

Unique epoxyketone compounds useful for inhibiting a proteasome in a cell, pharmaceutical compositions and methods of their use are provided herein.

RETRO-INVERSO PEPTIDE INHIBITORS OF CELL MIGRATION, EXTRACELLULAR MATRIX AND ENDOTHELIAL INVASION BY TUMOR CELLS

The present invention discloses retro-inverso peptides and pharmaceutical composition containing them. The peptides of the invention prevent key events occurring during the metastatic process, i.e. invasion of the extracellular matrix, formation of a capillary network, and the entry into bloodstream. They are therefore useful in the treatment of diseases and conditions that are sustained by an increase of cell motility, cell invasion, and/or angiogenesis, such as tumors and chronic inflammation.

USE OF ANTI-AGING GLYCOPROTEIN FOR ENHANCING SURVIVAL OF NEUROSENSORY PRECURSOR CELLS
20190046582 · 2019-02-14 ·

The present disclosure relates to an in vitro method for enhancing engraftment of neurosensory precursor cell comprising the step of contacting an isolated neurosensory precursor cell prior to a transplantation in a subject in need thereof, with a gem-difluorinated C-glycopeptide compound of general formula I, or a pharmaceutically acceptable base, addition salt with an acid, hydrate or solvate thereof: (I).