C07K5/062

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.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

Prodrugs of glutamine analogs

The disclosure provides compounds having formula (I): ##STR00001##
and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

N-acyldipeptide Derivatives and Their Uses
20200237637 · 2020-07-30 ·

Methods of treating aging related skin changes and of increasing skin thickness with topical administration of N-acyldipeptide derivatives are described. Compositions comprising N-acyldipeptide derivatives, are therapeutically effective for increasing skin thickness, and for treating extrinsic and intrinsic aging and aging related skin changes, such as fine lines, wrinkles, photoaging, hyperpigmentation, laxity, age spots, lentigines, mottled skin, and cellulite.

PPAR AGONISTS AND METHODS OF USE THEREOF

Provided herein are deuterated compounds and compositions useful in increasing PPAR activity. The compounds have a formula

##STR00001##

where L.sup.5 comprises at least one deuterium. Exemplary species include

##STR00002##

The compounds and compositions provided herein are useful for the treatment of PPAR related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS
20200207809 · 2020-07-02 ·

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X):

##STR00001##

and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

PH-sensitive linkers for delivering a therapeutic agent

The invention provides a pH-sensitive linker that can simultaneously bind metallic nanoparticles and one or more agents with various molecular size. The linker of the invention can deliver the agents into cells involved in disease processes or close to cells so that the agents can selectively target and effect on the cells. The target delivery provided by the linker of the invention can be used for example for disease sensing, imaging, drug delivery, and therapy.

ADJUVANT COMPOUNDS

Adjuvant compounds are described, as well as their conjugates comprising peptide antigens or other immunomodulatory moieties. Also described are methods of modulating immune responses in a subject in need thereof, as well as methods of treating cancer, viral or bacterial infections comprising administering the adjuvant compounds or the conjugates to a subject in need thereof.

Method for preparing largazole analogs and uses thereof

Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.

Cystargolide compounds and uses thereof

There is provided herein compounds of formula I, wherein R.sub.1 is H or linear or branched C.sub.1-C.sub.6 lower alkyl; R.sub.2 is H, linear or branched C.sub.1-C.sub.6 lower alkyl, or a proteinogenic amino acid side chain; R.sub.3 is H, linear or branched C.sub.1-C.sub.6 lower alkyl, or a proteinogenic amino acid side chain; R.sub.4 is OH or OR.sub.5 wherein R.sub.5 is linear or branched C.sub.1-C.sub.6 lower alkyl; and each R.sub.6 is independently H or CH.sub.3; or a pharmaceutically acceptable prodrug, salt, or ester thereof. Compositions containing said compounds, and uses thereof, are also provided. ##STR00001##