Patent classifications
C07K5/081
Tripeptide Propylene Oxide Derivative and Preparation Method and Application thereof
The present invention discloses a tripeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The structure of the tripeptide propylene oxide derivative is shown in formula I. Compared with the prior art, the present invention provides tripeptide epoxy ketone compounds with a novel structure and a function of inhibiting proteasome. As 20S proteasome inhibitors, the tripeptide epoxy ketone compounds can block tumor cell proliferation and induce tumor cell apoptosis, so the tripeptide epoxy ketone compounds can be used for the treatment and prevention of a plurality of human and animal diseases such as malignant tumors, and the effect is significantly better.
NOVEL DOPAMINE PRECURSORS
The invention disclosed herein concerns a novel class of compounds suitable for the treatment of neurodegenerative diseases, such as Parkinson’s Disease.
Caspase-3-triggered molecular self-assembling PET probes and uses thereof
Embodiments of the synthesis, radiolabeling and biological applications of an activatable tracer that undergoes intramolecular cyclization and aggregation upon activation by cleavage of a blocking moiety are provided. The probes of the disclosure allow for target-controlled self-assembly of small molecules in living subjects for imaging and drug delivery. The aggregated nanoprobes of the disclosure may be detectable optically, by PET detection, magnetic resonance imaging, and the like depending on the detectable reporter attached to the nanoprobe.
Methods of treating depression and other related diseases
The invention relates to methods for treating depression, anxiety, and other related diseases by administering a peptide NMDAR partial agonist.
Process for the manufacture of degarelix and its intermediates
The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula II: (P.sub.1)AA.sub.1-AA.sub.2-AA.sub.3-AA.sub.4(P.sub.4)-AA.sub.5-AA.sub.6(P.sub.6)-AA.sub.7-AA.sub.8(P.sub.8)-AA.sub.9-AA.sub.10-NH.sub.2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P.sub.1 is an amino protecting groups; preferably acetyl; P.sub.4 is hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group; P.sub.6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P.sub.8 is an amino protecting group.
PEPTIDE MACROCYCLES AGAINST ACINETOBACTER BAUMANNII
The present invention provides compounds of formula (I)
##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
Methods And Compositions For Stimulating Collagen Synthesis In Skin Cells
A composition comprising a first peptide selected from tripeptide, tetrapeptide and mixtures thereof; a second peptide selected from pentapeptide, hexapeptide, and mixtures thereof; an extract from the Laminaria genus, and whey protein, and a method for stimulating collagen synthesis in skin cells.
PEPTIDE EPOXYKETONE PROTEASOME INHIBITORS IN COMBINATION WITH PIM KINASE INHIBITORS FOR TREATMENT OF CANCERS
This disclosure provides methods of treating a cancer in a patient using a peptide epoxyketone proteasome inhibitor in combination with a PIM kinase inhibitor.
Skin treatment devices and methods with pre-stressed configurations
Devices, bandages, kits and methods are described that can control or regulate the mechanical environment of a wound to ameliorate scar and/or keloid formation. The mechanical environment of a wound includes stress, strain, and any combination of stress and strain. The control of a wound's mechanical environment can be active, passive, dynamic, or static. The devices are configured to be removably secured to a skin surface in proximity to the wound site and shield the wound from endogenous and/or exogenous stress.
COMPUNDS FOR ENZYME INHIBITION
Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.