C07K5/087

Pro-Pigmenting Peptides
20200253852 · 2020-08-13 · ·

The invention is directed to the use of at least one peptide of formula: X-(Xaa.sub.1).sub.n-Pro*-(Xaa.sub.2).sub.m-Y (I) With: -n=0, 1 or 2; -m=0 or 1 and if m=0 then n0 -Xaa.sub.1 is: -An hydrophobic aminoacid selected from Alanine (Ala, A), Valine (Val, V), Methionine (Met, M), Leucine (Leu, L), Isoleucine (Ile, I), Phenylalanine (Phe, F), Proline (Pro, P) and analogues and derivatives thereof; -A polar aminoacid selected from Serine (Ser, S), Threonine (Thr, T), Tyrosine (Tyr, Y), Asparagine (Asn, N), Glutamine (Gln, Q) and analogues and derivatives thereof; -or Glycine (Gly, G); When n=2 the two aminoacids Xaa.sub.1 can be the same or different; -Xaa.sub.2 is: -An hydrophobic aminoacid selected from Alanine (Ala, A), Valine (Val, V), Methionine (Met, M), Leucine (Leu, L), Isoleucine (Ile, I), Phenylalanine (Phe, F), Proline (Pro, P) and analogues and derivatives thereof; -A basic aminoacid selected from Arginine (Arg, R), Lysine (Lys, K) and Histidine (His, H) and analogues and derivatives thereof; -Glycine (Gly, G) or Serine (Ser, S); -At the N terminal end of the peptide, X is selected from H, COR.sub.1 and SO.sub.2R.sub.1; -At the C terminal end of the peptide, Y is selected from OH, OR.sub.1, NH.sub.2, NHR.sub.1 or NR.sub.1R.sub.2, R.sub.1 and R.sub.2 being independently from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group, that can be linear, branched, cyclic, poly-cyclic, non-saturated, hydroxylated, carbonylated, phosphorylated and/or sulphured, with the possibility to have in said group skeleton a O, S and/or N heteroatom; -Pro* corresponding to a Proline, an analogue or derivative thereof; Excluding the peptides where X=H and Y=OH, for a non therapeutical cosmetic pro-pigmenting treatment of skin. The invention also encompasses new tripeptides of formula (I) suitable for a non therapeutical cosmetic treatment of skin.

INHIBITION OF GLIADIN PEPTIDES

Novel compounds and methods for the inhibition of biological barrier permeability and for the inhibition of peptide translocation across biological barriers are identified. Assays for determining modulators of biological barrier permeability and for peptide translocation across biological barriers are provided. Methods for treating diseases relating to aberrant biological barrier permeability and peptide translocation across biological barriers are provided. Such diseases include celiac disease, necrotizing enterocolitis, diabetes, cancer, inflammatory bowel diseases, asthma, COPD, excessive or undesirable immune response, gluten sensitivity, gluten allergy, food allergy, rheumatoid arthritis, multiple sclerosis, immune-mediated or type 1 diabetes mellitus, systemic lupus erythematosus, psoriasis, scleroderma and autoimmune thyroid diseases.

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.

COMPOUNDS FOR PROTEASOME
20200071356 · 2020-03-05 ·

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. 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.

THERAPEUTIC PEPTIDES
20200071355 · 2020-03-05 ·

The present invention provides peptides, salts thereof, peptide conjugates, and salts thereof having an anxiolytic-like effect, for example a peptide comprising any amino acid sequence selected from (i) an amino acid sequence SYLPPLTT (SEQ ID NO: 1), (ii) an amino acid sequence YHIEPV (SEQ ID NO: 2), (iii) an amino acid sequence YLLVK (SEQ ID NO: 3), (iv) an amino acid sequence SYLPPLT (SEQ ID NO: 4), (v) an amino acid sequence FLLVK (SEQ ID NO: 5), and (vi) an amino acid sequence WLLVK (SEQ ID NO: 6).

Therapeutic compositions including frataxin, lactoferrin, and mitochondrial energy generating enzymes, and uses thereof
10576124 · 2020-03-03 · ·

Disclosed herein are methods and compositions for the treatment and/or prevention of diseases or conditions comprising administration of a therapeutic biological molecule, and/or naturally or artificially occurring derivatives, analogues, or pharmaceutically acceptable salts thereof, alone or in combination with one or more active agents (e.g., an aromatic-cationic peptide). The present technology provides compositions related to aromatic-cationic peptides linked to a therapeutic biological molecule and uses of the same. In some embodiments, the aromatic-cationic peptide comprises 2,6-dimethyl-Tyr-D-Arg-Phe-Lys-NH.sub.2, Phe-D-Arg-Phe-Lys-NH.sub.2, or D-Arg-2,6-Dmt-Lys-Phe-NH.sub.2.

AZAINDOLINE COMPOUNDS AS GRANZYME B INHIBITORS
20200062803 · 2020-02-27 · ·

Azaindoline compounds as granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Methods for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.

COMPOUNDS USEFUL FOR THE TREATMENT AND/OR CARE OF THE SKIN, HAIR, NAILS AND/OR MUCOUS MEMBRANES

A peptide has the formula (I) R.sub.1W.sub.mX.sub.n-AA.sub.1-AA.sub.2-AA.sub.3-Y.sub.pZ.sub.qR.sub.2, where AA.sub.1 is Tyr or Trp, AA.sub.2 is Val, Ile, Leu or Met, AA.sub.3 is Tyr, Phe or Trp, W, X, Y and Z are amino acids, m, n, p and q are each 0 or 1, and m+n+p+q is less than or equal to 2. R.sub.1 is H, a polymer derived from polyethylene glycol, a non-cyclic aliphatic group, alicyclyl, heterocyclyl, heteroarylalkyl, aryl, aralkyl, or R.sub.5CO. R.sub.5 is H, a non-cyclic aliphatic group, alicyclyl, aryl, aralkyl, heterocyclyl or heteroarylalkyl. R.sub.2 is NR.sub.3R.sub.4, OR.sub.3, or SR.sub.3. R.sub.3 and R.sub.4 are each H, a polymer derived from polyethylene glycol, a non-cyclic aliphatic group, alicyclyl, heterocyclyl, heteroarylalkyl, aryl, or aralkyl. R.sub.1 and R.sub.2 are not amino acids. Cosmetic or pharmaceutical compositions may include the peptide. It find use in reduction of lipid accumulation in the skin, treatment of cellulite, and treatment of symptoms of skin aging.

NOVEL COMPOSITION FOR ORGAN PRESERVATION
20200045954 · 2020-02-13 ·

The present invention relates to a peptide and solutions for preservation, perfusion, and/or reperfusion of an organ, especially the heart, for transplantation or after coronary angioplasty/coronary arterial bypass. The peptide contains the amino acid sequence of the sequence Phe-D-Arg-Phe-Amide (SEQ ID NO: 1), and the solution contains the peptide dissolved therein.

Process for the preparation of (2S)-N-((S)-1-((S)-4-methyl-1-((R)-2-methyl oxiran-2-yl)-1-oxopentan-2-ylcarbamoyl)-2-phenylethyl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)-4-methylpentanamide

The present invention relates to process for the preparation of (2S)-N-((S)-1-((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-ylcarbamoyl)-2-phenyethyl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)-4- methylpentanamide represented by the following structural formula-1. ##STR00001##