1399 results about "Amide bonds" patented technology

PCT No. PCT/SE97/01968 Sec. 371 Date Aug. 2, 1999 Sec. 102(e) Date Aug. 2, 1999 PCT Filed Nov. 21, 1997 PCT Pub. No. WO98/23636 PCT Pub. Date Jun. 4, 1998Heptapeptide analogues or pharmaceutically acceptable salts thereof consist of a hexapeptide moiety S and a C-terminal beta -aminoalcohol residue Z bound to the moiety S by an amide bond, wherein the beta -aminoalcohol Z is -NR-CH(Q)-CH2OH, Q is (CH2)n-NH-A is H or -C(=NH)NH2, and R is CH3 or C2H5, and the moiety S wherein H is a D-aromatic alpha -aminoacid and Y is an aliphatic alpha -aminoacid and have oxytocin antagonist activity. Also disclosed is: a method of their synthesis; pharmaceutical compositions containing these analogues; the synthesis of such compositions; a method of control of uterine contractions.

Fumaric acid amides of the general formula (I)

wherein R¹ represents OR³ or a D- or L-amino acid radical —NH—CHR⁴—COOH bonded via an amide bond, wherein R³ is hydrogen, a straight-chained or branched, optionally substituted C_1-24 alkyl radical, a phenyl radical or C_6-10 aralkyl radical and R⁴ is a side chain of a natural or synthetic amino acid and R² represents a D- or L-amino acid radical —NH—CHR⁵—COOH bonded via an amide bond or a peptide radical comprising 2 to 100 amino acids bonded via an amide bond, wherein R⁵ is a side chain of a natural or synthetic amino acid, are used for preparing a drug (1) for the therapy of an autoimmune disease; (2) for use in transplantation medicine; (3) for the therapy of mitochondrial diseases; or (4) for the therapy of NF-kappaB mediated diseases.

There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).

The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Novel chemical compounds, with application in fluorometric analytical methods, for qualitative and quantitative determination of biomolecules. The aim of the invention is to identify and prove the suitability of such compounds. Said aim is achieved with compounds of formula (1) where R′ is an antenna function, R² is a chelate forming agent, containing a coordinated lanthanide(III)ion, X is —OH or a group with affinity for the biomolecule, bonded to a carboxylate group of the chelate forming agent by means of an amide bond and Y is —H or a group with affinity for the biomolecule, coupled to the antenna function.

Abstract of Disclosure The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain;B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.

Improved integrally skinned asymmetric membranes for organic solvent nanofiltration, and their methods of preparation and use are disclosed. Membranes are formed from polyimides by phase inversion and are then crosslinked by addition of amine crosslinking agents that react with the imide groups of the polyimide, creating amide bonds. These stabilise the membranes and allow solvent nanofiltration to be maintained even in the solvents from which the membranes were formed by phase phase inversion.

The invention relates to the technical field of nano materials and specifically relates to amino-modified silica with dual drug-loading effects. According to the technical scheme, firstly, mesoporous silica nanoparticles are prepared by a template method; secondly, surface amino modification is carried out onto the mesoporous silica nanoparticles by 3-aminopropyltriethoxy silane; thirdly, ursolic acid is chemically coupled to the spherical mesoporous silica nanoparticles by amido bonds; and fourthly, the coupled nanoparticles are dispersed in DMF (dimethyl formamide) solution; a proper amount of ursolic acid is added, mixed and stirred; and finally vacuum drying is carried out to obtain the amino-modified silica with dual drug-loading effects. The mesoporous nano material with dual drug-loading effects prepared by the mesoporous silica disclosed by the invention is high in loading rate, can achieve controlled release effect for the loading drug ursolic acid, so that drug effect lasts for a long period time, and therefore, bioavailability of the ursolic acid is greatly improved.

The present invention refers to conjugates of erythropoietin with poly(ethylene glycol) comprising an erythropoietin glycoprotein having an N-terminal α-amino group and having the in vivo biological activity of causing bone marrow cells to increase production of reticulocytes and red blood cells and selected from the group consisting of human erythropoietin and analogs thereof which have the sequence of human erythropoietin modified by the addition of from 1 to 6 glycosylation sites or a rearrangement of at least one glycosylation site; said glycoprotein being covalently linked to one poly(ethylene glycol) group of the formula

—CO—(CH₂)_x—(OCH₂CH₂)_m—OR

wherein the —CO of the poly(ethylene glycol) group forms an amide bond with said N-terminal α-amino group; and wherein R is lower alkyl; x is 2 or 3; and m is from about 450 to about 1350.

The invention relates to a common carrier material based on graphene oxide for a targeting anticancer drug and a gene and application and application. Folic acid, lactobionic acid and other tumor cell targeting or liver targeting molecules and part of amino groups of soluble chitosan are connected by amide bonds to prepare a conjugate, the conjugate is then connected with graphene oxide, quaternization is performed by using an epoxy compound with a quaternary ammonium group, and gene molecules are loaded by the quaternizationquaternized part of the chitosan through electrostatic attraction; and then the anticancer drug is loaded by pi-pi conjugates, hydrogen bonds and hydrophobic effects in a non-covalent bond method. By adopting the targeting performance of targeting molecules and effects of graphene oxide of a particular size to enhance penetration and retention in tumor tissues and combining the performance of the graphene oxide for pH response control release of the loaded drug, the drug can be realized released in a tumor cell, an intelligent delivery system for the common carrier of the tumor targeting or liver targeting anticancer drug and the gene is synthesized from the perspective of synergetic medication, and a theoretical basis and a method basis are provided for combined therapy of tumor.

The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAPalpha), said prodrug having a cleavage site which is recognized by FAPalpha, and said drug being cytotoxic or cytostatic under physiological conditions, wherein said prodrug comprises an oligomeric part comprising at least two amino carboxylic residues, and a cytotoxic or cytostatic part, wherein the C-terminal amino carboxylic residue of the oligomeric part is an acyclic amino acid, the nitrogen atom of the amino function thereof is attached to a substituent being different from a hydrogen atom, and the C-terminal carboxy function thereof is linked to the cytotoxic or cytostatic part by an amide bond.

A method of decomposing wastes containing target compounds having one or more of hydrolyzable bonds of ether bond, ester bond, amide bond and isocyanate bond wherein the method comprises continuously supplying the wastes in a molten state or liquid state to a reactor, continuously supplying super-critical water or high pressure/high temperature water to the reactor, bringing the water into contact with the wastes, thereby decomposing the target compounds and then recovering them as raw material compounds or derivatives thereof for the target compounds. Target compounds contained in wastes in chemical plants which could not be utilized but merely incinerated or discarded so far are continuously decomposed into raw material compounds or derivatives thereof for the aimed compound and can be reutilized effectively.

The invention provides reagents and methods for conjugating polymers specifically to the α-amine of polypeptides in high yield. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a thioester moiety capable of specifically conjugating to the α-amine of a polypeptide having a cysteine or histidine at the N-terminus. The invention provides active thioester derivatives of PEG that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG and polypeptide. Use of these active esters to prepare PEG-proteins and PEG-peptides is described.

A precursor for the construction of chelated metal conjugates which demonstrate improved assay performance and utility in minimizing non-specific binding while maintaining specificity for target molecules is disclosed. The precursor has tridentate functionality towards multivalent ions such as iron and nickel and contains a diacetyl glycine group covalently linked via an amide to a molecule such as a proteinaceous molecule providing a primary amide group for amide bond formation. The precursor is preferably prepared in monomeric form by reacting nitrilotriacetic acid or a salt thereof in an aqueous medium at an alkaline pH of at least 8 with a proteinaceous molecule containing a primary amine group in the presence of a carbodiimide. The proteinaceous molecule may be bovine serum albumin or an enzyme such as alkaline phosphatase or horseradish peroxidase.

To provide a lactic acid polymer composition excellent in transparency, heat resistance and productivity, a molded article, a sheet and a multilayer sheet each of which comprises the composition, a thermoformed article obtained by secondary-forming the sheet or the multilayer sheet, and a process for producing the thermoformed article with excellent productivity. The lactic acid polymer composition of the invention comprises 100 parts by weight of a lactic acid polymer (A), 0.1 to 3 parts by weight of an organic crystal nucleating agent (B) comprising an aliphatic carboxylic acid amide having an amide bond, and 0.1 to 7 parts by weight of a crystallization accelerator (C). The thermoformed article of the invention is obtained with excellent production efficiency by thermoforming the sheet comprising the composition of the invention at a temperature of 60 to 130° C.