C07K5/083

PEPTIDE DERIVATIVE WITH COLLAGENASE INHIBITORY ACTIVITY, AND USE THEREOF

The present invention relates to a peptide derivative, having collagenase inhibitory activity, or a use thereof and has the effects of increasing a percutaneous absorption rate, inhibiting collagenase activity, and reducing wrinkles.

Inhibitors of NF kappa-B activity for treatment of diseases and disorders
11773135 · 2023-10-03 ·

Peptides and methods of use thereof, are disclosed for use in treating various disease and disorders, including inflammation, pain, oral mucositis, oral lesions, and cancer. The Peptides modulate the activity of the transcription factor NF κB.

SOLUTION PHASE ROUTES FOR WNT HEXAPEPTIDES
20230295232 · 2023-09-21 ·

The present disclosure relates generally to the field of polypeptide synthesis, and more particularly, to the solution phase synthesis of the Wnt hexapeptide Foxy-5 and protected derivatives and peptide fragments thereof.

TETRAHYDRONAPHTHALENE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS

The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Bioactive Collagen Peptides, Method Of Production Thereof, And Use Thereof
20230374112 · 2023-11-23 ·

The invention provides a composition comprising one or more bioactive peptides from collagen hydrolysate and use thereof for reducing joint and/or bone pain such as in arthritis or osteoarthritis. The invention also provides a use of the composition for inhibiting the activity and/or expression of osteoclasts, increasing the activity and/or expression of osteoblasts, or for the treatment and/or prevention of osteoclast-related diseases. The invention also provides a method for generating bioactive peptides from collagen hydrolysate in vitro.

SMALL MOLECULE DRUG CONJUGATES

A binding moiety (B) for Carbonic Anhydrase IX (CAIX), the binding moiety comprising:

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The binding moiety is univalent, bivalent, or multivalent. A targeted therapeutic agent may comprise the binding moiety. The invention also includes a method for treating a disease expressing elevated levels of CAIX by administering the targeted therapeutic agent.

RILUZOLE PRODRUGS AND THEIR USE

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

RILUZOLE PRODRUGS AND THEIR USE

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

METHOD OF ENHANCING A BRAIN OR COGNITIVE FUNCTION
20220296673 · 2022-09-22 · ·

A composition for improving memory, learning ability, and cognitive ability and a method of enhancing a brain or cognitive function by administering the composition to a subject in need thereof. It has been confirmed that a peptide having a C-terminal region ended to GAG had an effect of improving the memory. In order for the peptide to have the effect, it has been confirmed that the peptide should be a peptide of which the length consists of at least 4 amino acids. Further, it has been confirmed that a peptide of which the length of the peptide having the C-terminal region ended to GAG consists of 5 to 9 amino acids has the same effect. As a result, the peptide of the present invention can be used as the composition for improving memory, learning ability, and cognitive ability, and the method of enhancing a brain or cognitive function.

Methods of preparing cytotoxic benzodiazepine derivatives

The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.