C07K5/1021

Cytotoxic benzodiazepine derivatives

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Lipid assemblies and uses thereof and some pH and electrostatic modulating lipids to be used in said assemblies

Provided are modified lipid compounds and their use in the formation of lipid assemblies. Also provided are lipid assemblies including (a) an amphoteric lipid including in covalent association with (i) one or more acyl chains; (ii) one or more weak base moiety; (iii) one or more weak acid moiety; the lipid assembly also including (b) one or more additional lipids, at least one of which being a zwitterionic lipid. In some embodiments, the amphoteric lipid is a compound including (a) a tri-functional moiety; (b) two non-phosphate lipid chains associated with two of the functional moieties of said tri-functional moiety; (c) optionally a spacer moiety associated with the third of the functional moieties of said tri-functional moiety; and (d) a polyalkylamine optionally including a short peptide with one to several carboxylic acid residues. Further provided are the uses of the lipid assembly, inter alia, for transfection or cancer treatment.

Prodrugs of peptide epoxy ketone protease inhibitors

This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.

PROBIOTIC BACTERIAL MOLECULES AND THEIR USE IN METHODS TO TREAT/PREVENT INFECTION BY HARMFUL BACTERIA AND TO PROVIDE NUTRITIONAL HEALTH

This invention provides isolated and characterized secreted molecules from probiotic bacteria for use in compositions and methods for the treatment and/or prevention of infection by harmful pathogenic bacteria. The isolated secreted molecules can also be used in nutritional or medical food products which provide probiotics to the gastrointestinal tract of a mammal.

PEPTIDE

A novel substance which adds body to a food product, and a body-adding agent for food products that uses said substance are provided. More specifically, the body adding agent for food products is characterized by having as an active component a peptide, or a salt thereof, that is characterized in that the -glutamyl bond number is 2-4 and the peptide chain length is the -glutamyl bond number +1 to +2, a food product manufacturing method that uses said peptide, and a method for adding body to a food product, characterized by adding said peptide are provided.

SAPOSIN-A DERIVED PEPTIDES AND USES THEREOF

Disclosed herein are polypeptides and fusion polypeptides that have anti-angiogenic activity that can be used to inhibit tumor growth and tumor metastasis. The polypeptide consists of 9 or less consecutive amino acid residues (e.g., 8, 7, 6, 5, or 4) comprising the active core amino acid sequence DWLP, or an amino acid substitution variant thereof. Specific amino acid substitutions are disclosed herein. In some embodiments, the peptide consists essentially of 4-6 mers identified as exhibiting the activity of prosaposin A. Also disclosed herein are therapeutic compositions comprising the polypeptides and fusion polypeptides, and their use in the treatment, prevention, and inhibition of angiogenesis-related diseases and disorders such as cancer and cancer metastasis.

A PEPTIDE CAPABLE OF FORMING A GEL FOR USE IN TISSUE ENGINEERING AND BIOPRINTING
20200148720 · 2020-05-14 ·

The present invention relates to peptides capable of forming a gel and to their use in tissue engineering and bioprinting. The present invention furthermore relates to a gel comprising a peptide in accordance with the present invention, to a method of preparing such gel and to the use of such gel. In one embodiment, such gel is a hydrogel. The present invention furthermore relates to a wound dressing or wound healing agent comprising a gel according to the present invention and to a surgical implant or stent comprising a peptide scaffold formed by a gel according to the present invention. Moreover, the present invention also relates to a pharmaceutical and/or cosmetic composition, to a biomedical device or an electronic device comprising the peptide according to the present invention.

THERANOSTIC CAPTURE AGENTS, COMPOSITIONS, AND METHODS OF USING AND MAKING
20200147244 · 2020-05-14 ·

Disclosed are compounds, compositions, and methods involving theranostic capture agent for a target where the capture agent is (a) a precursor that can be loaded with a detectable moiety, a therapeutic moiety, or both, (b) loaded with a detectable moiety, (c) loaded with a therapeutic moiety, or (d) loaded with both a detectable moiety and a therapeutic moiety. Also disclosed are stable peptide-based PSMA capture agents and methods of use as detection agents.

Cage-like bifunctional chelators, copper-64 radiopharmaceuticals and PET imaging using the same

Disclosed is a class of versatile Sarcophagine based bifunctional chelators (BFCs) containing a hexa-aza cage for labeling with metals having either imaging, therapeutic or contrast applications radiolabeling and one or more linkers (A) and (B). The compounds have the general formula ##STR00001## where A is a functional group selected from group consisting of an amine, a carboxylic acid, an ester, a carbonyl, a thiol, an azide and an alkene, and B is a functional group selected from the group consisting of hydrogen, an amine, a carboxylic acid, and ester, a carbonyl, a thiol, an azide and an alkene. Also disclosed are conjugate of the BFC and a targeting moiety, which may be a peptide or antibody. Also disclosed are metal complexes of the BFC/targeting moiety conjugates that are useful as radiopharmaceuticals, imaging agents or contrast agents.

SMALL MOLECULE DCN1 INHIBITORS AND THERAPEUTIC METHODS USING THE SAME

Compounds of formula (I) as inhibitors of DCN1 and compositions containing the same are disclosed. Methods of using the DCN1 inhibitors in the treatment of diseases and conditions wherein inhibition of DCN1 provides a benefit, like oxidative stress-related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.

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