196 results about "Moiety" patented technology

The present application provides SOX9 inhibitor compounds and compositions and methods of use thereof. In certain aspects, the SOX9 inhibitor is a peptide comprising a portion of the SOX9 dimerization motif. In other aspects, the SOX9 inhibitor is a compound of the general formula Iwhere one A is H and the other is:and the remaining substituents are as defined in the application.

A method for determining soluble aldehydes in a composition comprising one or more of (a) 2,5-furan dicarboxylic acid (FDCA), (b) terephthalic acid (TPA), (c) an ester of 2,5-furan dicarboxylic acid, and (d) an ester of terephthalic acid is described. The method can indicate even very low levels of soluble aldehydes associated with unacceptable color development in a) the composition, b) a portion of the composition, or c) a prepolymer, oligomer, or polymer at least partially prepared directly or indirectly from the composition or a portion of the composition, so that mitigating or improving measures can be taken in response.

The present invention provides a method for screening for a candidate peptide capable of binding to a target molecule, the method including the steps of: (1) preparing a plurality of nucleic acid display libraries containing a barcoded peptide-nucleic acid complex, wherein the barcoded peptide-nucleic acid complex contains a nucleic acid moiety and a peptide moiety, the nucleic acid moiety contains a barcode sequence and a nucleic acid sequence encoding the peptide, and the plurality of nucleic acid display libraries are nucleic acid display libraries, each of which is independently produced by translation using a cell-free translation system; (2) mixing the plurality of nucleic acid display libraries to prepare a mixed nucleic acid display library; (3) bringing the mixed nucleic acid display library into contact with the target molecule; and (4) amplifying a nucleic acid corresponding to the nucleic acid moiety of the barcoded peptide-nucleic acid complex bound to the target molecule, using a barcode primer.

The present invention provides a composition suitable for use in switchable mirror devices, said composition comprising, dissolved in a solvent, a reducing compound E, a metal cation Mn+, and an organic ligand L able to form a coordination complex with Mn+, wherein E does not spontaneously reduce oxidized metal present in the composition, and wherein L comprises the following moiety I: Wherein X and X' are independently selected from O, and.

Disclosed herein are novel bifunctional compounds formed by conjugating an EGFR inhibitor moiety with an E3 ligase ligand moiety, methods for preparing the same, and uses thereof.

The present invention relates to an antifungal prodrug comprising an antifungal moiety linked to a trigger moiety by means of a self-immolative spacer. The trigger moiety is selected from a glycosyl residue and an oligosaccharide, stabilizing the self-immolative spacer and enabling cleavage by a pathogen hydrolase, preferably an extracellular glycosidase (EC 3.2.1). Upon cleavage of the trigger moiety by the pathogen hydrolase, the self-immolative spacer undergoes spontaneous degradation in order to release the antifungal moiety. The present invention further relates to pharmaceutical compositions comprising the prodrug and to the use thereof in the treatment of infectious diseases.

The present invention provides a pharmaceutical composition comprising a radiolabeled complex comprising a radionuclide and a targeting moiety linked to a chelating moiety, and a stabilizer against radiolytic degradation of a radiolabeled complex comprising para-aminohippuric acid or a pharmaceutically acceptable salt or carboxylic derivative thereof. The pharmaceutical composition of the present invention is characterized by high stability of its radiolabeled complex against radiolytic degradation. The present invention also provides a method for preparing such a pharmaceutical composition, and use of para-aminohippuric acid or a pharmaceutically acceptable salt or carboxylic derivative thereof for the stabilization of the radiolabeled complex of such a pharmaceutical composition.

Provided is a compound represented by general formula (1). In formula (1), X1 and X2 are each independently selected from the group consisting of a methine group and a nitrogen atom, n is an integer of 0-3, R1 and R2 are each independently a hydrogen atom, a halogen atom, or a monovalent organic group, R1 and / or R2 is a monovalent organic group having a Hammett substituent constant σp of 0.50 or greater, and the adjacent R1 and R2 moieties may be a part of a fused ring, the fused ring optionally including one or more atoms other than carbon.

The invention allows for the upgrade recovery of chemical products and relates to a method for generating synthesis instructions for producing one or more target products associated with one or more target product properties, the method comprising: providing one or more target product properties; providing a digital representation of a chemical structure of one or more reactants; determining a digital representation of a chemical structure of one or more products from at least a portion of the digital representation of the chemical structure of the one or more reactants by determining that the one or more products are formed in one or more chemical reactions of at least a portion of the one or more reactants associated with one or more formation scores; determining whether the one or more products are the one or more target products based on the one or more formation scores and determining whether one or more product properties associated with the one or more products correspond to the one or more target product properties; responsive to determining that the one or more product properties correspond to the one or more target products, providing the digital representation of the chemical structure of the one or more products and optionally providing a digital representation of the one or more reactants associated with the one or more target products.

The present invention provides a cyclic peptide compound optionally linked to a nucleic acid, the cyclic peptide compound having a cyclic moiety wherein: (1) the cyclic moiety is composed of 13 or 14 amino acid residues; (2) among the amino acid residues constituting the cyclic moiety, the number of N-substituted amino acid residues is 7 or more, the number of amino acid residues in a single side chain is 3 or fewer, and the number of native amino acid residues is 4 or fewer; and (3) the ClogP / total amide bond (ClogP / total AB) is 1.0 to 1.8.

The present invention relates to a process for stereoselective polyene cyclization to produce tricyclic compounds of formula (I), wherein X is CH2or C=O, comprising reacting a compound of formula (II), wherein X is CH2or C=O and wherein the curved line indicates the E- or Z-configuration, in the presence of a catalytic amount of a Bronsted acid having an acidic sulfonamide moiety.(I)(II)

The present invention describes a multispecific antigen-binding polypeptide comprising at least three antigen-binding moietyes, each of which is paired with a universal light chain polypeptide. Additionally, the present invention describes a multispecific antigen-binding polypeptide comprising a first antigen-binding moiety and a second antigen-binding moiety, wherein the C-terminus of CH1 of the first antigen-binding moiety is coupled to the N-terminus of the heavy chain variable region of the second antigen-binding moiety.

A drug-polymer conjugate, which is a copolymer of at least one monomer of formula (I) where: X may be the same or different at each occurrence and represents a terminal functional group comprising an alkyne or an azide; Q is independently selected at each occurrence and may be present or absent and when present, represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon, optionally substituted aryl and optionally substituted heteroaryl; D is a releasable bicyclic prostaglandin; L is a linker group; and at least one co-monomer of Formula III J-(Y1-A)n, J represents a linking functional group, n is 2 to 8 preferably 3 to 8; Y1 comprises a polyether of formula (ORa)m wherein Ra is independently ethylene, propylene and butylene and m is from 1 to 300 (preferably 2 to 300) and the polyether is in chain with one or more groups which are preferably selected from one or more of optionally substituted straight or branched C1 to C10 alkylene, amino, ether, ester, amide, carbonate and carbamate; A may be the same or different at each occurrence and represents a group comprising a terminal functional group comprising an alkyne or an azide functionality, wherein said terminal functional group is complementary to the terminal functional group X of formula (I) providing triazole moieties from reaction of X and A.

A conjugate compound comprises a payload unit, a targeting moiety, a linker, and an albumin binder. In some embodiments, a compound provided herein demonstrates improved stability under physiological conditions, e.g., in human serum.

Adhesive articles are described that include a substrate; a release layer disposed on the substrate, the release layer comprising a release compound; wherein the release compound has the formula wherein X is -CH2-; L is a divalent linking group comprising a moiety selected from a urea, an amide, or an ester; and R1and R2independently comprise a C4-C30 hydrocarbon group; and an adhesive bonded to the release layer. The release layer typically further comprises an organic polymer. Compositions comprising an organic polymer and a compound of Formula 1, as well as methods of making the compositions and release layers are also described.

A method of producing an oligofuran moiety-containing polycarbosilane, the method including a polymerization step of reacting a dihydrosilyloligofuran compound with a diene compound and / or diyne compound in the presence of ahydrosilylation catalyst in which method the dihydrosilyloligofuran compound being a compound having a 2- to 256-mer of a furan ring and a hydrosilyl group at the α-position of each of both terminal furan rings of the 2- to 256-mer of the furan ring.

The present invention relates among other aspects to a conjugate or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising said conjugate or its pharmaceutically acceptable salt for use in a method of preventing or treating an infection, wherein said conjugate is water-insoluble and comprises a polymeric moiety —Z to which a plurality of moieties -L2-X0D-L1-D are covalently conjugated, wherein each -D is independently an antibiotic moiety; each -L1- is independently a linker moiety to which -D is covalently and reversibly conjugated; each —X0D— is independently absent or a linkage and each -L2- is independently either a chemical bond or a spacer moiety.

Disclosed are compositions and methods for the treatment of disease (e.g., cancer) using conjugates comprising a protein-binding moiety (e.g., an antibody or an antigen-binding fragment thereof) and one or more radiolabeled metalloporphyrin complexes. Also disclosed are conjugates that further include one or more chemotherapeutic agents.

A first aspect of the invention relates to a conjugate comprising an immunoglobulin Fc polypeptide, and an oligothiophene moiety. The invention further relates to the use of a conjugate according to the invention as set forth above in treatment and / or prevention of a disease, particularly in treatment and / or prevention of a neurodegenerative disease.

The disclosure concerns methods of high throughput sequencing that utilize labeled moieties comprising a fluorophore having a Stokes Shift of at least 90nm.

The present invention relates to a nucleic acid molecule encoding a chimeric polypeptide comprising a peptide of interest fused to one or more heterologous moieties, wherein at least one of the heterologous moieties is a ligand of the Sortilin receptor. The invention also relates to a chimeric polypeptide encoded by said nucleic acid molecule and uses thereof.

A device may receive, by the computer system, a digital chemical structure for each of a plurality of ligand-drug conjugate compounds. A device may calculate by said one or more processors, an aggregation number for each of said plurality of ligand-drug conjugate compounds. A device may rank, by the computer system, at least a portion of said plurality of ligand-drug conjugate compounds based on said aggregation number. A device may identify, by the computer system, a plurality of low aggregation ligand-drug conjugate compounds based on said ranking, wherein said plurality of low aggregation ligand-drug conjugate compounds is a portion of said plurality of ligand-drug conjugate compounds having an aggregation number indicative of a predicted molecular aggregation lower than the predicted molecular aggregation of a remaining ligand-drug conjugate compounds within said plurality of ligand-drug conjugate compounds.

Provided is a fluorine-containing ether compound represented by the following formula: R1–CH2–R2[–CH2–R3–CH2–R2]x–CH2–R4. (In the formula, x is 0-2. R2 represents a perfluoropolyether chain. R3 represents a divalent linking group having 1-4 polar groups. R1 and R4 each represent a terminal group having 1-4 polar groups and 1-50 carbon atoms. At least one of R1 and R4 is a group represented by formula (2). In formula (2), a is 0-2. b of a moieties and c of a moieties are 1-6. One of d and e is 0 and the other is 1-6. Ra, Rb, Rc, and Rd of a moieties each represent an alkyl group having 1-8 carbon atoms or a hydrogen atom.)

Provided herein are compositions and methods for treating an autoimmune disease or disorder in a subject. In some cases, the compositions and methods use chemical inducers of proximity (CIPs). In some cases, the CIPs include a first moiety having specific binding for a BTB domain-containing protein or a transcriptional repressor expressed in B cell subpopulations and a second moiety having specific binding for a modulator of gene regulation. In some cases, the BTB domain-containing protein comprises BCL6. In some cases, the transcriptional repressor expressed in B cell subpopulations is PRDM1 or IRF4. In some cases the modulator of gene regulation comprises BRD4, CDK9, and / or p300.

This article describes multispecific antigen-binding peptides comprising at least three antigen-binding moieties, each of which pairs with a universal light chain peptide. This article also describes multispecific antigen-binding peptides comprising a first antigen-binding moieties and a second antigen-binding moieties, wherein the C-terminus of the CH1 region of the first antigen-binding moieties is coupled to the N-terminus of the heavy chain variable region of the second antigen-binding moieties.

The disclosure provides conjugates comprising a targeting moiety, e.g., an antibody or functional fragment thereof, and a lipid nanoparticle (LNP) encapsulating a therapeutic agent, wherein the targeting moiety is conjugated to the LNP through a linker comprising a thiol moiety and a click product formed via a click reaction between a first click handle and a second click handle.

Disclosed herein are detectable moieties and detectable conjugates comprising one or more detectable moieties. In some embodiments, the disclosed detectable moieties have a narrow wavelength and are suitable for multiplexing. Also disclosed are methods of labeling one or more targets within a biological specimen using any of the detectable conjugates and / or detectable moieties described herein.

MULTISPECIFIC MOLECULES BINDING TO TCR AND USES THEREOF ABSTRACT Provides herein are multifunctional molecules comprising T cell receptor variable beta-binding moieties, and methods of treating conditions or diseases in a subject using the same.

The present invention provides an oligonucleotide, wherein the oligonucleotide has at least 15 nucleotides sufficiently complementary to the target mRNA, wherein one or more sites of the oligonucleotide are conjugated to a lipophilic moiety.

A method for determining nitric oxide concentration in biological samples. The method includes for determining nitric oxide concentration in a sample including: (i) providing a nucleic acid complex comprising a first single-stranded nucleic acid molecule comprising a fluorophore crosslinked to the first strand, the fluorophore comprising diaminorhodamine-4-methylamine (DAR-4M) conjugated, to dibenzocyclooctyne-polyethylene glycol (DBCO-PEGn) linker, wherein n equals 4-12 and a second single-stranded nucleic acid molecule that is partially or fully complementary to the first single-stranded molecule, wherein the nucleic acid complex further comprises a first label and a targeting moiety conjugated to the first single-stranded nucleic acid molecule or the second single-stranded nucleic acid molecule, the first label is capable of producing a signal, wherein the intensity of the signal is dependent at least on concentration of the nucleic acid complex in the sample; (ii) contacting the sample with the nucleic acid complex; (iii) measuring the intensity of the signal: and (iii) determining the nitric oxide concentration from the measured signal. Compositions for determining nitric oxide concentrations in biological samples are also included.