专利号:WO-2024165450-A1 优先权日:2023-02-09 标题:Method of chemical synthesis of single-chain antibody fragments and products thereby obtained 发明人:FIGINI MARIANGELA; LUISON ELENA 权利人:GLYTECH INC; FIGINI MARIANGELA 摘要:A new method is disclosed for the protein full-chemical synthesis of single-chain antibody fragments (scFv); the obtained products are structurally close and functionally equivalent to their biological counterpart, being however, advantageously free of impurities and more reproducible in properties. The method includes the general steps of: (a) separately synthetizing sub-sequences (peptide fragments) (b) sequentially assembling the sub-sequences obtained in step (a) in the order as they appear in the target scFv amino acid sequence, and (c) performing oxidative folding of the assembled whole peptide molecule obtained in step (b) and dialyzing the resulting product in a buffer.
专利号:US-5962737-A 优先权日:1997-01-08 标 题 :2-amino-1-phenylpropanols, stereospecific synthesis thereof, and method of optically resolving the same 发明人:WEST DANIEL DAVID 摘要:Stereospecific synthesis of the racemic threo isomers of 2-nitro-1-phenylpropanols by reacting a benzaldehyde derivative with nitroalkane in the presence of a tertiary amine and reducing 2-nitro-1-phenylpropanols with, for example, lithium aluminum hydride to 2-amino-1-phenylpropanols is described. Also described are phase transfer resolution of racemic mixtures of 2-amino-1-phenylpropanol and its derivatives into their optically pure isomers by reacting a racemic mixture with the mono alkali metal salt of a tartaric acid ester in a two phase system of a hydrocarbon and water. The specification further describes therapeutically useful optically pure isomers of threo-2-amino-1-(dialkoxy or alkoxy) phenylpropanols and acid addition salts thereof.
专利号:US-7176332-B2 优先权日:2001-08-28 标题:Methods for the synthesis of amines such as ephedrine and intermediates 发明人:SMALLRIDGE ANDREW JOHN; TREWHELLA MAURICE ARTHUR; WILKINSON KYLIE ANNE 权利人:POLYCHIP PHARMACEUTICALS PTY 摘要:A method for the preparation of a compound of formula (VI): in which R 2 is an optionally substituted C1–C6 alkyl; R 4 is H, OH, an optionally substituted C1–C6 alkyl or an optionally substituted C1–C6 alkoxy; R 5 is an optionally substituted aryl, an optionally substituted aralkyl, or an optionally substituted alkyl; and R 6 is H or an optionally substituted C1–C6 alkyl; the method including the step of subjecting a ketone of formula (V) in which R 2 , R 4 and R 5 are as defined above, to reductive amination with an amine of formula R 3 NH 2 in which R 3 is an optionally substituted alkyl, and a reductant to form the compound of formula (VI), wherein the reaction is conducted in the presence of a supercritical fluid or a liquefied gas.
专利号:US-6153615-A 优先权日:1991-12-26 标 题 :Blocking induction of tetrahydrobioterin to block induction of nitric oxide synthesis 发明人:GROSS STEVEN S 权利人:CORNELL RES FOUNDATION INC 摘要:Guanosine triphosphate pathway tetrahydrobiopterin synthesis antagonist and/or pterin salvage pathway tetrahydrobiopterin synthesis antagonists are administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylactic or curative effect for endotoxin- or cytokine-induced hypotension or for restoration of vascular contractile sensitivity to pressor agents in the treatment of such hypotension). The tetrahydrobiopterin synthesis antagonist may be administered with α 1 -adrenergic agonist or with nitric oxide synthase inhibitor. The tetrahydrobiopterin synthesis antagonists are also administered to attenuate inflammation caused by induced nitric oxide production in immune cells. Unwanted counterproductive or side effects can be eliminated or ameliorated by administration additionally of levodopa with or without carbidopa and L-5-hydroxytryptophane.
专利号:US-5874433-A 优先权日:1993-11-29 标题 :Blocking utilization of tetrahydrobiopterin to block induction of nitric oxide synthesis 发明人:GROSS STEVEN S 权利人:CORNELL RES FOUNDATION INC 摘要:Inhibitor of the use of tetrahydrobiopterin as a cofactor for nitric oxide synthase, e.g., substituted 4-phenyl(hydropyridines) such as 1-methyl-4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine or, 4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine) or tetrahydropterin analog which does not replace tetrahydrobiopterin as a substrate for nitric oxide synthase such as (6R,S)-6,7-dimethyl-tetrahydropterin or (6R,S)-tetrahydrofolic acid or 2,4-diamino-, 2,6-diamino, or 4,6-diamino mono- or disubstituted pyrimidines or the corresponding pyrimidine-3-oxides such as 2,4-diamino-6-(diethylamino)pyrimidine, 2,4-diamino-6-piperidino-pyrimidine-3-oxide, 2,4-diamino-6-hydroxypyrimidine, 4,6-diamino-2-hydroxypyrimidine or 2,5-diamino-4,6-dihydroxypyrimidine is administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylaxis or treatment of cytokine- or endotoxin-induced hypotension (e.g., septic shock). The latter two types are advantageously administered with nitric oxide synthase inhibitors (concurrent therapy) or to potentiate the effect of α 1 -adrenergic agonists in the prophylaxis or treatment of induced hypotension.
专利号:CN-107200717-A 优先权日:2017-06-07 标题:A novel prosthetic linking arm for the synthesis of diubiquitin and its synthesis method
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