Patent classifications
C07K5/0815
Peptide macrocycles and use thereof in the treatment of bacterial infections
The present invention provides compounds of formula (I) ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.8′, R.sup.9, R.sup.9′, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, X.sup.7, X.sup.8, X.sup.9 and X.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 baurnannii.
Anti-bacterial peptide macrocycles and use thereof
The present invention relates to 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 for the use in the treatment or prevention of infections and resulting diseases caused by Pseudomonas aeruginosa.
AROMATIC-CATIONIC PEPTIDES AND USES OF SAME
The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.
Trifluoromethylpropanamide derivatives as HTRA1 inhibitors
The invention provides novel compounds having the general formula (I) ##STR00001##
wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.3, R.sup.8, R.sup.10, R.sup.11 and R.sup.23 are as described herein, compositions including the compounds and methods of using the compounds.
Self-assembling peptide polymer
A self-assembling peptide is provided that is enzymatically oxidized to form a polymeric pigment. The monomeric peptide has three amino acids (tyrosine (Y), one phenylalanine (F), and one aspartic acid (D) or one lysine (K)) and, following self-assembly and treatment with a tyrosinase enzyme oxidizes and polymerizes into a material with predetermined properties.
Peptide, composition comprising said peptide and uses thereof, in particular cosmetic uses
The peptide has from 3 to 10 amino acids comprising at least the sequence K*(Ac)GH or K*(Ac)HG and may further comprise an N-terminus modification, preferably an acylation, and/or a C-terminus modification; K* is selected from the group consisting of lysine, ornithine, diaminobutyric acid, diaminopropionic acid and a hydroxylated derivative thereof; K*(Ac) corresponds to a lysine, ornithine, diaminobutyric acid, diaminopropionic acid or a hydroxylated derivative thereof, acetylated on the amine of their lateral hydrocarbon chain. The two preferred peptides are Pal-K(Ac)GH and Pal-K(Ac)HG. This peptide can be used for a cosmetic treatment, in particular anti-aging, anti-wrinkle and fine lines, to improve the mechanical properties of the skin, firmness/tonicity/elasticity/flexibility, to increase the density and volume of the skin, for a restructuring, healing effect, and/or to fight stretch marks.
BIFUNCTIONAL CYTOTOXIC AGENTS CONTAINING THE CTI PHARMACOPHORE
The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula:
F.sup.1-L.sup.1-T-L.sup.2-F.sup.2
where F.sup.1, L.sup.1, T, L.sup.2 and F.sup.2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.
AROMATIC-CATIONIC PEPTIDES AND USES OF SAME
The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.
Antibacterial agents
The invention concerns agents with antibacterial activity, their production and use in the treatment of bacterial infections in animals, including man. The agents are derivatives of vancomycin-type antibiotics, of structure XW-L-V, wherein X is hydrogen, acetyl or a lipophilic membrane-insertive element, W is a basic peptide or basic amino acid; L is a linking group and V is a glycopeptide moiety which inhibits peptidoglycan biosynthesis in bacteria.
Anti-inflammatory tripeptides
The present invention relates to tripeptide compounds according to the general formula (1) and their use as a medicament, in particular as anti-inflammatory agents. ##STR00001##