A61K49/005

BLOOD-BRAIN BARRIER PERMEABLE PEPTIDE COMPOSITIONS
20210017262 · 2021-01-21 ·

Blood-brain barrier permeable peptide compositions that contain variable antigen binding domains from camelid and/or shark heavy-chain only single-domain antibodies are described. The variable antigen binding domains of the peptide compositions bind to therapeutic and diagnostic biomarkers in the central nervous system, such as the amyloid-beta peptide biomarker for Alzheimer's disease. The peptide compositions contain constant domains from human IgG, camelid IgG, and/or shark IgNAR. The peptide compositions include heavy-chain only single-domain antibodies and compositions with one or more variable antigen binding domain bound to one or more constant domains.

Super-resolution fluorescent imaging probe

[Problem] To provide a novel fluorescent probe for super-resolution imaging that uses fluorescent light emission characteristics that originate from an intermolecular nucleophilic addition-dissociation equilibrium reaction, and to provide a super-resolution fluorescent imaging method that uses the probe. [Solution] A fluorescent probe for super-resolution imaging that comprises a compound represented by formula (I) or a salt thereof [in the formula, X represents an oxygen atom, C(R.sup.a)(R.sup.b), or Si(R.sup.a)(R.sup.b) (wherein R.sup.a and R.sup.b each independently represent a hydrogen atom or an alkyl group), R.sup.1 represents a hydrogen atom or an optionally substituted aryl (provided that, if R.sup.1 is a phenyl group, the benzene ring of the phenyl group does not have a substituent at position 2 or position 6), R.sup.2 and R.sup.3 each independently represent 1-3 identical or differing substituents that are independently selected from the group that consists of hydrogen atoms, hydroxyl groups, halogen atoms, optionally substituted alkyl groups, optionally substituted sulfo groups, optionally substituted carboxyl groups, optionally substituted ester groups, optionally substituted amide groups, and optionally substituted azide groups, R.sup.4 and R.sup.5 each independently represent a hydrogen atom or an optionally substituted alkyl group or N(R.sup.4)(R.sup.5) forms an amide group or a carbamate group (provided that, if R.sup.4 or R.sup.5 is an alkyl group, each may form, together with R.sup.2, a ring structure that contains the nitrogen atom that is bonded thereto), and R.sup.6 and R.sup.7 each independently represent a hydrogen atom or an optionally substituted alkyl group or N(R.sup.6)(R.sup.7) forms an amide group or a carbamate group (provided that, if R.sup.6 or R.sup.7 is an alkyl group, each may form, together with R.sup.3, a ring structure that contains the nitrogen atom that is bonded thereto)], the fluorescent probe for super-resolution imaging being characterized in that the compound represented by formula (I) or the salt thereof undergoes a nucleophilic addition-dissociation equilibrium reaction with a nucleophilic compound that contains an SH group.

NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises

##STR00001##

wherein R is H or CH.sub.3, wherein R is NR.sup.1R.sup.2, wherein R.sup.1 and R.sup.2 are alkyl groups, wherein R.sup.1 and R.sup.2 are the same or different, wherein R.sup.1 and R.sup.2 together have from 5 to 16 carbons, wherein R.sup.1 and R.sup.2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises

##STR00001##

wherein R is H or CH.sub.3, wherein R is NR.sup.1R.sup.2, wherein R.sup.1 and R.sup.2 are alkyl groups, wherein R.sup.1 and R.sup.2 are the same or different, wherein R.sup.1 and R.sup.2 together have from 5 to 16 carbons, wherein R.sup.1 and R.sup.2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

NOVEL BLOCK COPOLYMER AND MICELLE COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises

##STR00001##

wherein R is H or CH.sub.3, wherein R is NR.sup.1R.sup.2, wherein R.sup.1 and R.sup.2 are alkyl groups, wherein R.sup.1 and R.sup.2 are the same or different, wherein R.sup.1 and R.sup.2 together have from 5 to 16 carbons, wherein R.sup.1 and R.sup.2 may optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

Blood-brain barrier permeable peptide compositions comprising a VAB domain of an anti-amyloid-beta camelid single-domain heavy-chain only antibody
10738109 · 2020-08-11 · ·

Blood-brain barrier permeable peptide compositions that contain variable antigen binding domains from camelid and/or shark heavy-chain only single-domain antibodies are described. The variable antigen binding domains of the peptide compositions bind to therapeutic and diagnostic biomarkers in the central nervous system, such as the amyloid-beta peptide biomarker for Alzheimer's disease. The peptide compositions contain constant domains from human IgG, camelid IgG, and/or shark IgNAR. The peptide compositions include heavy-chain only single-domain antibodies and compositions with one or more variable antigen binding domain bound to one or more constant domains.

EDIBLE PLANT-DERIVED MICROVESICLE COMPOSITIONS FOR DIAGNOSIS AND TREATMENT OF DISEASE

Compositions comprising a therapeutic agent encapsulated by an edible plant-derived microvesicle are provided. Methods of treating an inflammatory disorder and methods of treating a cancer are further provided and include administering an effective amount of a composition comprising a therapeutic agent encapsulated by an edible plant-derived microvesicle to a subject. Further provided are methods of diagnosing a colon cancer that include the steps of administering an edible plant-derived microvesicle incorporating a detectable label to a subject and then determining an amount of the detectable label in an intestine of the subject.

PHTHALOCYANINE PROBES AND USES THEREOF
20200179514 · 2020-06-11 · ·

The present invention relates to compositions and methods for destroying target cells in a patient using photodynamic therapy. In particular, the present invention provides a photosensitizing agent based on a small molecular weight (<50 kDa) protein or peptide or a small molecule that is conjugated to a phthalocyanine dye, such as IRDye 700DX.

Cathepsin-binding compounds bound to a carrier and their diagnostic use

The invention relates to Cathepsin-binding compounds bound to a carrier comprising a diagnostic moiety, for use in the diagnosis of inflammatory diseases, and/or for use in the diagnosis of neoplastic diseases, wherein the Cathepsin-binding compound binds to inflammatory cells of the tumour stroma. The invention also relates to Cathepsin B-targeting compounds and Cathepsin B-binding and liposome-binding compounds.

Compound and contrast agent for optical imaging having the compound

To provide a compound having high T/B and a contrast agent for optical imaging. The compound has a molecular weight of a specific range, the compound in which two polyethylene glycols are bonded to a specific cyanine pigment through a linker. The present invention provides a compound which has a high T/B and which can be used as a contrast agent capable of imaging a tumor portion with high contrast.