283 results about "Alpha amino acid" patented technology

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and / or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided. Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer, methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer.

Alpha-amino acid containing chemical mechanical polishing compositions and slurries that are useful for polishing substrates including multiple layers of metals, or metals and dielectrics.

Metal L-seleno-alpha-amino acids salts and their use as a bioavailable feed and water ration supplement for domesticated animals such as cattle, pigs and poultry.

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N-O-P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N-O-P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and / or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

The invention belongs to the field of drug synthesis and in particular relates to a series of novel peptide boric acids as well as an ester compound or pharmaceutical salt thereof, and a preparation method and application of the peptide boric acids as well as the ester compound or pharmaceutical salt thereof in pharmacodynamics. A structure of the peptide boric acid and the ester compound or pharmaceutical salt thereof is shown in a formula I (described in the specification). The compound provided by the invention can be used for preparing a proteasome inhibitor and can further be used for treating solid tumours and blood tumours, wherein the solid tumours are selected from non-small cell lung cancer, small cell lung cancer, lung adenocarcinoma, lung squamous carcinoma, pancreatic cancer, breast cancer, prostate cancer, liver cancer, skin cancer, epithelial cell cancer, gastrointestinal stromal tumor, nasopharynx cancer and leukemia; and the blood tumours are selected from multiple myeloma, mantle cell lymphoma and histiocytic lymphoma.

A process for preparing enantiomerically enriched amines by reacting a ketone with ammonia or an ammonium salt and a reducing agent in the presence of a catalytic system comprising the components:a) an amino acid transaminase,b) an alpha-amino acid which is a substrate of the amino acid transaminase,c) an amino acid dehydrogenase suitable for preparing the alpha-amino acid,d) NAD(P)+ ande) an NAD(P)+-reducing enzyme, which reacts NAD(P)+ with the reducing agent to give NAD(P)H.The process can be carried out with catalytic amounts of alpha-amino acid and NAD(P)+, and enables an enantioselective reductive amination of ketones.

The invention discloses a lignin-based foam concrete foaming agent, and a preparation method and application thereof. The preparation method comprises the following steps: adding lignin solid powder to water, preparing into a water solution of which the mass fraction is 30-50%; adjusting the pH value to 9-11 by using an alkaline regulator; heating to 60-70 DEG C; adding an alpha-amino acids compound and aldehyde substances and reacting for 1-3 hours, so as to obtain amination carboxyl alkali lignin; heating to 70-90 DEG C, adding a sulfonic acid monomer and an initiator and reacting for 3-4 hours; then adding a surfactant and a foam stabilizer to the product, evenly stirring and cooling, so as to obtain a liquid product. The foaming agent prepared by the method has strong foaming capability and high stability, generates fine and uniform foams, and is low in price. Furthermore, the path of resource utilization of papermaking black liquor is also expanded by the foaming agent; the pollution of the black liquor to the environment is reduced; and therefore the lignin-based foam concrete foaming agent has significant economic and social value.

A process for preparing an oligomeric phenolic detergent composition comprising contacting an oil soluble alkylphenol with an alkaline earth metal base, an alpha amino acid, and a C1 to C6 aldehyde, in the in the presence of a C2 to C6 alkylene glycol and a C2 to C4 carboxylic acid; and reacting under reactive conditions at a temperature of from 150° C. to 225° C. The oligomeric phenolic detergent product can be employed in a lubricating oil.

The invention provides gene transfer compositions using as the gene carrier a biodegradable polymer that contains one or more cationic alpha amino acids, such as arginine or agmatine. The compositions form a tight soluble complex with a poly nucleic acid suitable for transfecting target cells to effect translation of the cargo poly nucleic acid by the target cell. Thus, such compounds are useful both in vitro and in vivo.

A (S or R)-2(or 3)-tert-butyloxy-(3+n)-(9-fluorenyl methoxy) carbonylamino fatty-chain carboxylic acid with protected hydroxy and amino is prepared from (S or R)-2(or 3)-hydroxy-(3+n)-amino fatty-chain carboxylic acid through reaction on dichlorosulfoxide in solvent to generate the hydrochloride of relative methylester, reacting on FmocONSu in solvent to generate (S or R)-2(or 3)-hydroxy-(3+n)-(9- fluorenylmethoxy) carbonylamino fatty-chain methyl carboxylate, reacting on isobutene in solvent to generate (S or R)-2(or 3)-tert-butyloxy-(3+n)-(9-fluorenyl methoxy) carbonylamino fatty-chain methyl carboxylate, hydrolyzing, acidifying to generate (S or R)-2(or 3)-tert-butyloxy-(3+n)-amino fatty-chain carboxylic acid, and reacting of FmocONSu in solvent.

The present invention provides a compound of the following formula (I) below. This compound (I) can be produced by reacting a 2,2′-dimethylene bromide-1,1′-binaphthyl derivative, which can be produced by a relatively small number of processes, with an easily available secondary amine. This compound (I) is useful as a chiral phase-transfer catalyst.

The present invention relates to feed rations, processes for formulating feed rations, and methods for improving weight gain in growing ruminants. The feed rations comprise a forage or other feed ingredient that meets daily nutritional requirements, other than methionine, and exceeds daily maintenance energy requirements of a growing ruminant. The feed rations further comprise an alpha-amino acid supplement, wherein the alpha-amino acid supplement is an analog of an alpha-amino acid.

The invention provides sequential poly(ester amide)s derived from Proline and that are synthesized by a two-step method, involving a final thermal polyesterification reaction. Molecular weights of polymers prepared by this method are from 14,000 Da to about 77,000 Da.1 When invention proline-based PEAs were thermally characterized, their glass transition temperatures were lower than other alpha-amino acid based poly(ester amides) due to lack of internal hydrogen bonding. These Proline-based PEAs assemble as nano-particles in aqueous solutions and form complexes with various cations and biologies, including hydrophobic small molecule drugs and biologies. Therefore the invention Proline-based PEAs are useful for drug delivery applications requiring a polymer with a molecular weight in the range from 14,000 Da to about 77,000 Da and for fabrication of nanoparticles for delivery of hydrophobic drugs.

New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure:wherein R1-R5 and FG are define herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and / or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided.

The invention relates to a manufacture method for amino acid and lactic acid copolymer used for medicine slow release that uses alpha-amino acid and lactic acid as raw material. It adopts the method of fusion copolymerization condensation to shorten compounding time. And is easy to operate and is benefit to decrease the compound cost of the biology degradation.

The invention discloses an L-alpha-amino acid ester contained Z-configuration anabasine pesticide and a preparation method thereof. The structure is shown by a general formula (I). The prior anabasine pesticide only has a function of disinsection and has no function of promoting the growth of crops. The preparation method comprises the following steps: preparing a hydrochlorate of an L-alpha-amino acid methyl ester or ethyl ester; adding the prepared hydrochlorate of the L-alpha-amino acid methyl ester or the ethyl ester, nitenpyram, 37 percent formaldehyde and triethylamine into a round-bottom three-necked flask; and placing the round-bottom three-necked flask containing the solution in a microwave reactor, controlling the reaction temperature not more than 75 DEG C, and carrying out microwave reaction for 30 minutes to prepare the L-alpha-amino acid ester contained Z-configuration anabasine pesticide shown by the general formula (I). The L-alpha-amino acid ester contained Z-configuration anabasine pesticide has the advantages of high efficient insecticidal activity, good insecticidal effect, low toxicity, safety of human beings and livestock, crop growth promotion, simple using method, simple preparation method, and short reaction time.

Compounds of formula (I) are inhibitors of P13 kinase activity, and useful in treatment of, inter alia, autoimmune, inflammatory and proliferative diseases: wherein: s is 0 or 1; U is hydrogen or halogen; X is —(C═O), an optionally substituted divalent phenylene, pyridinylene, pyrimidinylene, or pyrazinylene radical, or a bond; P is optionally substituted C1-C6 alkyl and Z is —(CH2)Z—X1-L1-NHCHR1R2; or Z is optionally substituted C1-C6 alkyl and P is —(CH2)Z—X1-L1-NHCHR1R2; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; X1 is (i) a bond; —NR4C(═O)NR5— or —NR4S(═O)2—; or except when X is —(C═O)— (ii) —C(═O)—, —S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z and L1 are as defined in the specification.

The invention provides a rubiaceae-type cyclopeptide taken as a novel Hedgehog signal channel inhibitor as well as a preparation method and an application of the rubiaceae-type cyclopeptide in preparation of a medicine for treating and preventing relevant cancers activated by the abnormity of Hedgehog signal channels. The rubiaceae-type cyclopeptide is prepared by the condensation of one D-alpha-alanine, one L-alpha-alanine, three substituted N-methyl-L-alpha-tyrosines and one L-alpha-amino acid of another type via peptide bonds, wherein six amino acids are condensed into an eighteen-membered rings; and benzene rings between two adjacent tyrosines are connected via an oxygen bridge so as to form a fourteen-membered ring.

The invention provides construction of leucine dehydrogenase mutants and application thereof and belongs to the field of genetic engineering. The invention provides three leucine dehydrogenase mutantsof SEQ ID NO.4, SEQ ID NO.6 and SEQ ID NO.8, and application of the mutants and genetically engineered bacteria producing the mutants in preparation of optical pure chiral L-alpha-amino acid throughammoniation reduction of alpha-ketoacid. The invention has the advantages that the L-alpha-amino acid prepared by ammoniation reduction from the leucine dehydrogenase mutants or the genetically engineered bacteria has high catalytic activity and stability, high-optical purity L-alpha-amino acids can be synthesized (ee is greater than 99%), the conversion rate of L-phenylglycine catalyzed by mutantenzymes is improved by 2.62 times, and a practical and effective strategy is provided for industrial production.

The invention relates to a method for preparing alpha-amino alcohol by taking alpha-amino acid as raw material and a catalyst used in the method and a preparation method for the catalyst. The catalyst consists of three components; a first component is selected from the elements of Ru and Pd and one or more salts and oxides thereof; a second component is selected from the elements of cuprum, nickel, iron, bismuth, stannum, cadmium, magnesium, aluminum, cobalt, lead, titanium, selenium, zinc, zirconium, germanium, rhodium and cerium and one or more of oxides and salts thereof; a third component is a carrier. The alpha-amino acid is deoxidized by hydrogen in a water solution or the mixed solution of water and a water-miscible dissolvent in the effect of the catalyst and synthesized into the alpha-amino alcohol with one-step method. The method is characterized by simple steps, short production period, little pollution, and low production cost, etc.

The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an α-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an α-alkyl-α-amino acid and a derivative thereof as well as an α,α-dialkyl-α-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.

Compounds of the formula: are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

The invention discloses dual-network poly(N-acryloyl-L-alpha-amino acid) / hyaluronic acid composite hydrogel and a preparation method thereof. Hydrazide hyaluronic acid and N-acryloyl-L-alpha-amino acid are used as main raw materials and are radiated by ultraviolet after being uniformly mixed with a crosslinking agent, and hydrazone bond crosslinking and photochemical crosslinking are realized to form the dual-network poly(N-acryloyl-L-alpha-amino acid) / hyaluronic acid composite hydrogel containing disulfide bonds in a crosslinking network chain. The disulfide bond in the hydrogel can be broken by responding to a reducing substance, so that the rapid dissociation of the hydrogel can be realized. The method has advantages of easiness in obtaining of raw materials, moderate reaction conditions, simple and rapid process and the like. The prepared hydrogel has characteristics of adjustability in strength, degradation speed, microhole structure, charge state and the like and is good in biological compatibility and cell adhesion property and wide in application prospect on the aspects of tissue engineering, three-dimensional cell culture, in-vitro tumor models and the like.

The invention relates to a multi-arm polyamino acid (ester) grafted polyethyleneimine copolymer, a preparation method and application in gene delivery. The method includes the steps of: dissolving polyamine initiator in organic solvent and initiating the ring opening polymerization of alpha-amino acid-N-carboxylic acid anhydride protected by phenmethyl under anhydrous and oxygen free conditions to obtain the multi-arm polyamino acid (ester); and then causing the full or partial aminolysis reaction to occur between benzyl ester at the lateral chain of the multi-arm polyamino acid (ester) and amino group of polyethyleneimine to form the grafted copolymer. The polymer is a novel high-efficiency polycation gene vector, integrates the properties of polyethyleneimine and polyamino acid and is high in transfection efficiency, and the highest transfection efficiency to the mediate luciferase plasmid of Chinese Hamster Ovary epithelial cell is ten times than that of the Lipofectamine2000 of the commercial transfection reagent in US Invitrogen biomax under the same conditions; cytotoxicity is small; and cell survival rate is over 80% within the best transfection rate range, thus having broad application prospect.

The invention discloses genetic engineering bacteria and belongs to the technical field of bioengineering. With the introduction of L-alpha-amino acid transaminase, L-glutamic acid gene, alpha-keto acid decarboxylase gene and alcohol dehydrogenase, the genetic engineering bacteria can be applied to biosynthesis of hydroxytyrosol. The invention also discloses a construction method and application of the recombinant Escherichia coli genetic engineering bacteria. And further, substrate transport is promoted and decomposition of the product is reduced by knocking out or enhancing the expression ofrelated genes on the Escherichia coli genome, and the production efficiency of recombinant bacteria is improved. The method for production of hydroxytyrosol by conversion of the recombinant bacteriahas characteristics of simple operation, low cost and high synthesis efficiency of the product, and has a good industrial prospect.

The present invention provides a compound of the following formula (I) below. This compound (I) can be produced by reacting a 2,2′-dimethylene bromide-1,1′-binaphthyl derivative, which can be produced by a relatively small number of processes, with an easily available secondary amine. This compound (I) is useful as a chiral phase-transfer catalyst.

The present invention provides a process for the preparation of a nonracemic a-amino acid derivative from an optically active N-acyl lactam using an organometallic reagent to effect the opening of the ring followed by reduction of the ketone carbonyl to an alcohol or a methylene, or by a reductive amination to an amine, or by a ketalization reaction.

The invention discloses a method for efficiently synthesizing alpha-amino-acid ester, which comprises the following steps: by using alpha-eleostearates and benzyl amine as raw materials and triethylamine as a catalyst, ammonifying alpha-eleostearates in different structures by a one-pot method under the action of the catalyst; and carrying out after-treatments, including hydrolysis, extraction, column chromatography and the like, to obtain the alpha-amino-acid ester. The maximum reaction yield is up to 95%. In view of the advantages of wide substrate applicability, mild reaction conditions, simple operation and high yield in the method disclosed by the invention, the invention has certain potential industrial application value.

Compounds of formula (I) or (II) are dihydrofolate reductase inhibitors, useful for the treatment of, for example, cell proliferative diseases:wherein A and D are independently —CHR7— or —NR7—; E and G are independently ═CR7— or ═N—; each R6 independently represents hydrogen or —OR7; R7 is hydrogen or C1-C6 alkyl; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid which does not contain a carboxyl, or carboxyl ester group; Y is a bond, —C(═O)—, —S(═O)2—, —C(═O)NR3—, —C(═S)—NR3, —C(═NH)NR3 or —S(═O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, and Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(═O)NR4—, —NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z is 0 or 1.