C07K5/0808

GRANZYME B INHIBITOR COMPOSITIONS AND METHODS FOR THE PREVENTION AND/OR TREATMENT OF SKIN BLISTERING AND/OR PEELING

Methods for using compositions comprising a Granzyme B inhibitor and a pharmaceutically acceptable carrier for treating and/or preventing blistering and/or peeling of a skin of a subject are provided. Also provided are methods for using the compositions to improve the healing of a blistered or area of peeled skin of a subject. The compositions can be formulated for oral administration, nasal administration, topical administration, subcorneal administration, intra-epidermal administration, sub-epidermal administration, or for administration by injection.

METHOD FOR PRODUCING PEPTIDE COMPOUND COMPRISING HIGHLY STERICALLY HINDERED AMINO ACID
20230026641 · 2023-01-26 ·

It was found that a peptide compound that has an N-substituted-α,α-disubstituted amino acid residue at the N-terminus and containing a dipeptide residue in which the N-substituted-α,α-disubstituted amino acid residue and an N-substituted amino acid residue are linked together, can be efficiently produced by linking an N-unsubstituted-α,α-disubstituted amino acid whose amino group is protected with an electron-withdrawing protecting group to an N-substituted amino acid or a peptide compound having an N-substituted amino acid residue at the N-terminus, and then allowing a substituent-introducing agent to act in the presence of a specific base to selectively introduce a substituent to the amino group at the N-terminus.

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.

SARS-COV-2 MAIN PROTEASE INHIBITORS

The present disclosure relates to certain molecules, pharmaceutical compositions containing them, and methods of using them to treat viral infections.

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.

LABYRINTHIN-BASED PEPTIDES FOR CANCER IMMUNOTHERAPIES AND USES THEREOF
20220409709 · 2022-12-29 ·

Antigenic compositions comprising one or more labyrinthin-derived peptides are described herein. In some embodiment, each peptide of the antigenic composition comprises a T-cell epitope and/or a B-cell epitope. In other aspects, the present disclosure provides, e.g., vaccine compositions comprising tin antigenic composition disclosed herein, including kits, medicines, and compositions (such as pharmaceutical compositions and unit dosages) thereof. Also provided are methods of using the compositions disclosed herein, such as methods of treatment thereof and methods of producing antibodies, and antibody compositions thereof, against the one or more labyrinthin-derived peptides or a portion thereof.

PRODRUGS OF RILUZOLE AND THEIR METHOD OF 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.

Ultrasound-assisted simulated digestion method of milk protein active peptide and application thereof in health foods

An ultrasound-assisted simulated digestion method of a milk protein active peptide and an application thereof in health foods, pertaining to the technical field of intensive processing of dairy products and preparation of health foods. The method firstly employs ultrasonic pretreatment of casein and β-lactoglobulin, followed by enzymatic hydrolysis with a protease to prepare casein and ρ-lactoglobulin polypeptide, and traces the activity of the polypeptide by simulating gastrointestinal digestion, and then simulates absorption by intestinal epithelial cells with Caco-2 cells, to characterize a highly active milk protein polypeptide digested by the gastrointestinal tract and absorbed by the Caco-2 cells simulating absorption by the inner wall of the small intestine. The method has identified five such highly active milk protein polypeptides.

METHOD FOR PRODUCING PEPTIDE COMPOUND

An object of the present invention is to provide a method for producing a peptide with high efficiency, and a method for producing a peptide which comprises the following steps (1) and (2): (1) a step of mixing an N-protected amino acid or an N-protected peptide with a carboxylic acid halide represented by the formula (I)

##STR00001##

(wherein X represents a halogen atom,
R.sup.1, R.sup.2 and R.sup.3 each independently represent an aliphatic hydrocarbon group which may have a substituent, and a total number of the carbon atoms in R.sup.1, R.sup.2 and R.sup.3 is 3 to 40); and (2) a step of mixing the product obtained in the step (1) and a C-protected amino acid or a C-protected peptide
is provided.

Peptide macrocycles against <i>Acinetobacter baumannii</i>

The present invention provides compounds of formula (I) ##STR00001## wherein X, L.sup.1 and R.sup.1 to R.sup.10 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.