43 results about "Diamino acid" patented technology

Compositions and methods for preventing and treating pneumococcal infections are provided. Compositions include novel polypeptides comprising an amino acid sequence corresponding to the R2i or R22 domain of CbpA or a consensus sequence of one of these domains, and variants and fragments thereof, wherein the polypeptide is stabilized in a desired conformation, particularly a loop conformation. The polypeptides of the invention may be engineered to comprise a first and a second cysteine residue, thereby resulting in the formation of a disulfide bond that stabilizes the polypeptide in the desired conformation. Alternatively, a polypeptide of the invention may be modified to create a synthetic linkage between a first and second amino acid residue present within the polypeptide, wherein the synthetic linkage stabilizes the polypeptide in the desired conformation. The polypeptides of the invention may further comprise an amino acid sequence for a T cell epitope. Compositions further include isolated nucleic acid molecules that encode the polypeptides of the invention, immunogenic compositions and vaccines comprising the disclosed polypeptides, and antibodies specific for these polypeptides.

The present invention provides synthetic immunogenic lipopeptide molecules comprising co-linear T-helper and B cell epitopes, and methods for their production and use in the generation of primary and secondary immune responses, and for the vaccination of animal subjects against particular antigens. More particularly, the present invention provides highly soluble lipopeptides wherein the lipid moiety is attached to the terminal side-chain group of an internal lysine or lysine analog, preferably to the terminal side-chain group of an internal diamino acid residue. Preferably the internal lysine or lysine analog is positioned between the T-helper epitope and the B cell epitope or within the T-helper epitope.

The invention relates to an alpha,beta-diamino acid derivative, and a synthetic method and application thereof. The alpha,beta-diamino acid derivative is shown as a structural formula (A). The synthetic method comprises the following steps of: dissolving imide, amide, a catalyst and a molecular sieve in solvent, dripping a diazo compound into the mixture, and after reacting with stirring, and removing the solvent by reduced pressure distillation to obtain a coarse product; and purifying by column chromatography to obtain the alpha,beta-diamino acid derivative. The synthetic method has the advantages of high atom economy, selectivity and yield, mild reaction conditions and simplicity and safety of operation. The alpha,beta-diamino acid derivative is an important intermediate of chemical engineering and medicines, is widely applied to the field of pharmaceutical chemical engineering; and due to a certain of anticancer activity, the alpha,beta-diamino acid derivative has the wide application prospect in the field of the pharmaceutical chemical engineering.

The invention relates to a novel cationic gemini surfactant used for the petroleum industry and a composition method thereof, which is provided in order to satisfy the requirements of the cationic gemini surfactant, proposed by different application conditions. The technical scheme is as follows: the cationic gemini surfactant is toluene-2, 4-diamino acid-N-dimethyl alkyl amidocyanogen ethyl ester; a drying reactor is firstly added with proper amount of acetone as a solvent, then is added with N, N-deanol and is dripped with 2, 4-TDI of a mol ratio of 2:1, all of which are stirred well and sealed for a rest at the room temperature and for a reaction for 6 hours; the solution is added with bromoalkane of the same molar weight as the 2, 4-TDI and is stirred, sealed and kept at a constant temperature of 45 DEG C for a water bath reaction for 12 hours; at last a solid product is acquired by drying at 80 DEG C. The surfactant has higher surface activity, excellent concertedness, simple composition method, mild reaction condition, high productive rate and good stability; besides, the surfactant can be used for producing household chemicals and for tertiary oil recovery.

The invention discloses a synthetic method of an alpha, beta-diamino acid derivative. In the method, a one-step reaction is undergone by taking a diazo compound, aniline and aldehyde acid ester as raw materials, taking metal Lewis acid and chiral phosphoric acid as catalysts, taking an organic solvent as a solvent and taking a 4 Angtrom molecular sieve as a water absorbing agent, so that the alpha, beta-diamino acid derivative is obtained. The synthetic method disclosed by the invention has the advantages of high atom economy, high selectivity and high yield, the reaction conditions are mild, and operation is easy and safe. The alpha, beta-diamino acid derivative has anticancer activity and structural diversity, and is suitable for preparing and applying antitumor, antibiotic and antifungal medicaments.

The invention discloses a synthetic method of an alpha-quaternary carbon-contained alpha, beta-diamino acid derivative. The alpha-quaternary carbon-contained alpha, beta-diamino acid derivative is obtained by treating a diazo compound, an imine and a phosphoramidate as raw materials, chiral phosphoric acid and rhodium acetate as catalysts, an organic solvent as a solvent and a molecular sieve as a water absorbent, and carrying out a catalytic reaction. The synthetic method of the invention has the advantages of simple and easily available raw materials, simple and safe operation, high atom economy, high yield and high selectivity. The alpha-quaternary carbon-contained alpha, beta-diamino acid derivative obtained through the method of the invention, which has a diverse compound skeleton, has a very important meaning to a new medicine screening and preparing technology.

The present invention is drawn to an ephedra- and artificial stimulant-free energy promoting composition, comprising effective amounts of a magnesium amino acid chelate, a B vitamin, a pyruvate salt, and rhodiola. These ingredients work synergistically together to provide energy, without the use of artificial stimulants, caffeine, or ephedrine. Additional amino acid chelates can also be present, such as iron amino acid chelate, zinc amino acid chelate, copper amino acid chelate, manganese amino acid chelate, chromium amino acid chelate, and mixtures of second amino acid chelates.

The invention relates to a novel biaryl-structured chiral N-methyl pyridoxal catalyst and synthesis and application thereof. The general structural formula is as shown in the specification, wherein R1is hydrogen or C1-C24 alkyl, and R2 and R3 are independently hydrogen or C1-C24 alkyl. In comparison with the prior art, the prepared pyridoxal catalyst can be used in a bionic Mannich reaction process, and fast and effective synthesis of a chiral alpha-beta-diamino acid derivative is realized.

The present invention provides synthetic immunogenic lipopeptide molecules comprising co-linear T-helper and CTL epitopes, and methods for their production and use in the generation of primary and secondary immune responses, and for the vaccination of animal subjects against particular CTL epitopes. More particularly, the present invention provides highly soluble lipopeptides wherein the lipid moiety is attached to the terminal side-chain group of an internal lysine or lysine analog, preferably to the terminal side-chain group of an internal diamino acid residue. Preferably the internal lysine or lysine analog is positioned between the T-helper epitope and the CTL epitope.

The invention discloses a derivative containing alpha-aryl-alpha, beta-diamino acid ester and a synthesis method thereof. The derivative containing the alpha-aryl-alpha, beta-diamino acid ester is prepared through one-step reaction of a diazo compound, amide and imine as raw materials in an organic solvent under the catalysis of a metal catalyst. The synthesis method has the advantages of high atom economy, high selectivity, mild reaction conditions and simple and safe operation. The prepared derivative containing the alpha-aryl-alpha, beta-diamino acid ester can be used as an important chemical and medical intermediate, has biological activity and is suitable for preparation of drugs for resisting colon cancer and liver cancer.

The present invention provides soluble CTLA4 mutant molecules that bind CD80 and/or CD86 antigens with higher affinity than wild-type CTLA4 or non-mutated CTLA4Ig. The soluble CTLA4 molecule has a first amino acid sequence comprising the extracellular domain of CTLA4, wherein certain amino acid residues in the S25-R33 region and the M97-G107 region are mutated. A mutant molecule of the invention may also comprise a second amino acid sequence that enhances the solubility of said mutant molecule.

The invention discloses a preparation method of an alpha, beta-diamino acid derivative with optically active alpha-quaternary carbon. The preparation method comprises the following steps: dissolving aromatic aldehyde, arylamine, chiral phosphoric acid, p-cymene ruthenium dichloride dimer and a 4A molecular sieve in an organic solvent, adding an organic solvent of a diazo-compound, reacting at the temperature of minus 10 DEG C- minus 20 DEG C, and carrying out rotary evaporateion to obtain the alpha, beta-diamino acid derivative of alpha-quaternary carbon. Raw materials of the derivative are simple and easily available. The preparation method is simple and safe to operate, has advantages of high atom economy, high yield and high selectivity, and is of great significance for the screening and pharmaceutical preparation technology of a new drug.

Fusion proteins that contain the fusion of (i) a peptide of less than 100 amino acids comprising a first amino acid sequence comprising AASSG (SEQ ID NO: 1) and a second amino acid sequence comprising XAGXDXXTEXPXS (SEQ ID NO: 2), wherein X designates any amino acid, and (ii) a protein transduction domain (PTD) are provided, along with pharmaceutical compositions containing the fusion protein. The proteins can be used to treat Huntington's disease.

The present invention relates to a peptide-resin conjugate of Formula (2), wherein: Pr₁ is selected from H, alkyl, aryl, aralkyl, acyl, aroyl and a protecting group; Y is a direct bond; or an optionally protected natural or unnatural amino acid residue; or a peptide comprising 2 to 200 natural or unnatural amino acid residues, each of which is optionally protected; Dia is a natural or unnatural diamino acid; A is a polymer resin conjugated to the side chain amino function of the diamino acid; X is an optionally protected natural or unnatural amino acid residue; or a peptide comprising 2 to 15 natural or unnatural amino acid residues, each of which is optionally protected; R₁, and R₂ are each independently selected from H, alkyl, aryl, aralkyl, NH₂, NH—CO—NH₂. Further aspects of the invention relate to a process of preparing peptide-resin conjugates of Formula (2), and their use in the preparation of peptides.

The invention discloses a synthesis method of (2S, 3S, 4S)-5-(3, 4-diamino-thiophane-2-group) valeric acid, while prior method has long reaction and partial decomposition of product in reaction caused by concentrated halogen acid, to affect the quality of d-biotin. The invention processes reflux reaction on diethyl malonate condensate, cyano compound or bis-benzyl biotin in halogen acid, adds glacial acetic acid later, refluxes until no single-benzyl biotin and d-biotin exist in product, concentrates to remove unreacted halogen acid and glacial acetic acid, adds absolute ethyl alcohol, freezes to 0-5DEG C, adds lithium hydrate to neutralize and precipitate white solid crystals, filters, poaches filter cake via absolute ethyl alcohol, and dries to obtain target product. The invention has short reaction and controllable reaction end, which leads glacial acetic acid in later reaction to effectively avoid diamino acid being decomposed in concentrated halogen acid, to improve product yield and content.

The present invention is drawn to an ephedra- and artificial stimulant-free energy promoting composition, comprising effective amounts of a magnesium amino acid chelate, a B vitamin, a pyruvate salt, and rhodiola. These ingredients work synergistically together to provide energy, without the use of artificial stimulants, caffeine, or ephedrine. Additional amino acid chelates can also be present, such as iron amino acid chelate, zinc amino acid chelate, copper amino acid chelate, manganese amino acid chelate, chromium amino acid chelate, and mixtures of second amino acid chelates.

Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate or carrying a Hofmann degradation of the primary amide of the 3^rd amino acid asparagines with phenyl-bis-trifluoroacetate to give the primary amine. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

The invention provides a method for auxiliary synthesis of 4,4'-diphenyl methane diamino acid methyl ester by microwave, and relates to an ester synthesis method. The invention aims to solve the problems of long process reaction time and single intermittent operation production mode in the conventional method for preparing the 4,4'-diphenyl methane diamino acid methyl ester by using methyl carbonate. The method of the invention comprises the following steps of: mixing 4,4'-diaminodiphenyl methane and methyl carbonate in a microwave reactor, adding a ZS-6 catalyst, performing a reaction of theraw materials under a power of the microwave reactor of 60 to 250W and at the temperature of between 150 and 200 DEG C, cooling the product of the reaction to room temperature, and then performing filtration, separation and recrystallization to obtain the 4,4'-diphenyl methane diamino acid methyl ester. The method has the advantages of short reaction time and the suitability for continuous industrialized production; and the conversion rate of the 4,4'-diaminodiphenyl methane reaches 99.6 percent, and the 4,4'-diphenyl methane diamino acid methyl ester yield reaches 98.1 percent.