C07K5/09

METHOD FOR THE STEREOISOMERIZATION OF CHIRAL COMPOUNDS

The present invention provides a novel method for the controlled stereoisomerization (comprising the stereo-conversion of chiral compounds to racemates, non-racemic mixtures and mixtures of epimers). The method of the invention provides the fully controlled generation of mixtures of different ratios of (S) and (R) stereoisomers, both enantiomers and diastereomers, of a given compound or a mixture of compounds. Such mixtures and isotopically labeled variants of said mixtures provided by the present invention are useful as an authenticity or external or internal standards in various biochemical and medical applications. Further, with the method of the invention it is possible to generate specific stereoisomers from some amino acids as well as degradation and oxidation products thereof which were previously not available. Thence, the invention provides in additional aspects the generation of a group of previously unavailable stereoisomers (enantiomers, epimers, and mixtures thereof such as a racemate) with amino acid type structures.

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.

INHIBITORS OF GROWTH FACTOR ACTIVATION ENZYMES

The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.

PEPTIDE FOR REDUCING HAIR LOSS AND PROMOTING HAIR GROWTH, AND COSMETIC COMPOSITION AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
20220160608 · 2022-05-26 ·

The present invention relates to a peptide for reducing hair loss or promoting hair growth, and a cosmetic composition and a pharmaceutical composition comprising the same, and specifically, a cosmetic composition, and a pharmaceutical composition for treatment may be provided, which are capable of reducing hair loss and promoting hair growth by activating a Wnt/β-catenin signaling pathway, and at the same time, promoting the activity of the collagenase MMP-2 and ALP proteins and growth hormones needed for hair growth.

Crystalline salt forms of SBT-20
11325943 · 2022-05-10 · ·

Disclosed are various crystalline salt forms of L-Phe-D-Arg-L-Phe-L-Lys-NH.sub.2.

NANOBARCODE FOR CONTROLLING CELL ADHESION AND DIFFERENTIATION OF STEM CELLS, PREPARATION METHOD THEREOF, AND METHOD OF CONTROLLING ADHESION AND DIFFERENTIATION OF STEM CELLS BY USING THE SAME

Disclosed are a nanobarcode for controlling adhesion and differentiation of stem cells and a method of controlling adhesion and differentiation of stem cells by using nanobarcodes. The method of controlling adhesion and differentiation of stem cells of the present invention may efficiently control adhesion and differentiation of stem cells in vivo or in vitro by tuning periodicity and sequences of a ligand peptide (RGD) of a nanobarcode.

NANOBARCODE TO CONTROL CELL ADHESION AND POLARIZATION OF MACROPHAGE, PREPARATION METHOD THEREOF, AND METHOD OF CONTROLLING CELL ADHESION AND POLARIZATION OF MACROPHAGE BY USING THE SAME

Disclosed are a nanobarcode for controlling adhesion and polarization of macrophages and a method of controlling adhesion and polarization of macrophages by using nanobarcodes. The method of controlling adhesion and polarization of macrophages of the present invention may efficiently control adhesion and phenotypic polarization of macrophages in vivo or in vitro by tuning periodicity and sequences of ligand peptide (RGD) of a nanobarcode.

GEMINOID LIPOPEPTIDE COMPOUNDS AND THEIR USES

Disclosed are geminoid peptide-like compound according to Formula I:


R.sup.1—C(═O)—Z.sub.n—NR.sup.3-R.sup.2  (I)

in which R.sup.1 and R.sup.2 are each independently saturated, partly saturated or unsaturated, straight, branched or cyclic alkyl chains, wherein R.sup.1 has a number of C atoms of 11 or more, preferably 11 to 19, and R.sup.2 has a number of C atoms of 12 or more, preferably 12 to 20; R.sup.3 is hydrogen or C.sub.1-C.sub.6 alkyl; n is an integer from 1-15;
each Z independently is an amino acid residue, wherein Z.sub.n comprises an N-terminus attached to C(═O) and a C-terminus that is attached to NR.sup.3, for use as a medicament.

PEPTIDE INHIBITORS OF TIGHT JUNCTION PERMEABILITY

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.

TRANSITION METAL CHELATING BEADS
20220009963 · 2022-01-13 ·

The present invention relates to a complex comprising a transition metal cation (i); a ligand (ii) comprising at least one chelating group, preferably from 1 to 4 chelating groups, more preferred 2 or 3 chelating groups, wherein the chelating group(s) is/are selected from hydroxamate group —N(O″)—C(═O)—R, catechol ate group, carboxyl ate group, partly or totally protonated forms of these chelating groups and mixtures of these chelating groups and/or their partly or totally protonated forms, wherein R is hydrogen or a C1 to C5 alkyl group; and a magnetic bead (iii); wherein the magnetic bead (iii) and the ligand (ii) are covalently bonded. The invention also relates to the use of the complex for reduction of the content of at least one phosphor-oxy-substance, which preferably comprises a structural element —O—P(O″)(═O)—O— within its structure, in a fluid sample, as well as to a method for decreasing the content of at least one phosphor-oxy-substance, preferably a phospholipid, in a fluid sample, comprising a step of adding the complex. The invention further relates to a supernatant obtained or obtainable from this method and to the use of a supernatant obtained or obtainable from the method for qualitative and/or quantitative determination of at least one analyte in said supernatant. Furthermore, the invention relates to a method for qualitative and/or quantitative determination of at least one analyte in a fluid sample and to a method for determining the kind and/or amount of at least one phosphor-oxy-substance in a fluid sample.