C07K5/0821

USE OF PEPTIDES AS THERAPEUTIC AGENT FOR AUTOIMMUNE DISEASES AND BONE DISEASES

The present invention relates to use of peptides as a therapeutic agent, wherein it has been confirmed that the peptides of the present invention significantly inhibit the activity of T cells and the differentiation of T helper 17 cells (Th17 cells), which are associated with autoimmune disease, and have remarkable effects of treating and improving arthritis in an animal model of arthritis. Therefore, the peptides may be used as an active ingredient in therapeutic agents for various autoimmune diseases such as bone disease, inflammatory disease or rheumatoid arthritis.

Method for preparing natural bioactive peptide Tubulysin U

A preparation method of a novel natural bioactive peptide Tubulysin U includes: dissolving a compound 2 in trifluoroacetic acid, heating under reflux to prepare an intermediate, reacting with a compound 3 and N,N-diisopropylethylamine to obtain a product, reacting the product with 2, 6-dimethylpyridine and tert-butyldimethylsilyl trifluoromethanesulfonate, adding sodium hydroxide after the reaction to prepare an intermediate acid, reacting the intermediate acid with a compound 6, HATU and N,N-diisopropylethylamine to obtain a product, adding triphenylphosphine to prepare an intermediate amine, adding a compound 8 and HATU to react, adding ammonium fluoride to prepare a first intermediate, adding sodium hydroxide to the first intermediate to prepare a second intermediate, adding acetic anhydride to the second intermediate to prepare a third intermediate, adding trifluoroacetic acid to the third intermediate to prepare a fourth intermediate, and adding formaldehyde and sodium cyanoborohydride to the fourth intermediate to react, thereby obtaining a target product.

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.

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.

METHOD FOR PREPARING NATURAL BIOACTIVE PEPTIDE TUBULYSIN U
20230099436 · 2023-03-30 ·

A preparation method of a novel natural bioactive peptide Tubulysin U includes: dissolving a compound 2 in trifluoroacetic acid, heating under reflux to prepare an intermediate, reacting with a compound 3 and N,N-diisopropylethylamine to obtain a product, reacting the product with 2, 6-dimethylpyridine and tert-butyldimethylsilyl trifluoromethanesulfonate, adding sodium hydroxide after the reaction to prepare an intermediate acid, reacting the intermediate acid with a compound 6, HATU and N,N-diisopropylethylamine to obtain a product, adding triphenylphosphine to prepare an intermediate amine, adding a compound 8 and HATU to react, adding ammonium fluoride to prepare a first intermediate, adding sodium hydroxide to the first intermediate to prepare a second intermediate, adding acetic anhydride to the second intermediate to prepare a third intermediate, adding trifluoroacetic acid to the third intermediate to prepare a fourth intermediate, and adding formaldehyde and sodium cyanoborohydride to the fourth intermediate to react, thereby obtaining a target product.

MELANOMA THERAPEUTICS
20230100707 · 2023-03-30 ·

Two therapeutics, oligopeptides P5 and P14, which have proven to be selectively cytotoxic towards multiple melanoma cell lines in vitro. These oligopeptides offer an efficacious treatment for all types of pathogenic melanocytes and stages of melanoma, and a cost effective prophylactic to all individuals who are at high risk of developing skin cancer. In addition, these oligopeptides can be formulated into a sunscreen to serve as a prophylactic against any precancerous lesion or dysplastic nevi that might develop in high risk groups.

INHIBITORS OF HSP70 PROTEINS
20230091297 · 2023-03-23 ·

Provided are compounds useful for selectively inhibiting HSP70 isoforms. Also provided are methods of inhibiting HSP70 proteins and methods of treating a disease characterized by overexpression of a HSP70, such as cancer. In particular embodiments, the disclosed compounds may be used as potent inhibitors for HSPA5 and may display greater than 20-fold selectivity over other HSP70 isoforms.

Inhibitors of blood coagulation factor XIII

The invention relates to a compound of general formula (I) as novel inhibitor of blood coagulation factor XIII, methods for synthesis thereof and to use thereof for the prophylaxis or treatment of diseases associated with blood coagulation factor XIII. ##STR00001##

Use of peptides as therapeutic agent for autoimmune diseases and bone diseases

The present invention relates to use of peptides as a therapeutic agent, wherein it has been confirmed that the peptides of the present invention significantly inhibit the activity of T cells and the differentiation of T helper 17 cells (Th17 cells), which are associated with autoimmune disease, and have remarkable effects of treating and improving arthritis in an animal model of arthritis. Therefore, the peptides may be used as an active ingredient in therapeutic agents for various autoimmune diseases such as bone disease, inflammatory disease or rheumatoid arthritis.

COLLAGEN MIMICS

Novel collagen mimics are disclosed with a tripeptide unit having the formula (Xaa-Yaa-Gly).sub.n, where one of the positions Xaa or Yaa is a bulky, non-electron withdrawing proline derivative. By substituting a proline derivative at either the Xaa or Yaa position in the native collagen helix, the stability of the helix is increased due solely to steric effects relative to prior known collagen-related triple helices. Methods are also disclosed for making the novel collagen mimics.