专利号:US-11603382-B2 优先权日:2015-12-11 标题 :Diastereoselective synthesis of phosphate derivatives 发明人:KOTALA MANI BUSHAN; DAMMALAPATI VENKATA LAKSHMI NARASIMHA RAO 权利人:NuCana plc 摘要:The present invention provides a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. It also provides a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate.
专利号:US-7101854-B2 优先权日:2000-10-09 标题:Tetrapeptide stimulating the functional activity of hepatocytes, pharmacological substance on its basis and the method of its application 发明人:KHAVINSON VLADIMIR KHATSKELEVI 权利人:SANKT PETERBURGSKAYA OBSCHESTV 摘要:The invention refers to the field of medicine and may be applied as a substance stimulating the functional activity of hepatocytes, restoring the synthesis of non-specific proteins, normalising metabolism activating the processes of proliferation and differentiation of the liver cells. There is proposed a new compound -tetrapeptide lysyl-glutamyl-aspartyl-alanine of the general formula Lys-Glu-Asp-Ala [SEQ ID NO:1]. There is proposed a pharmaceutical composition capable of stimulating the functional activity of hepatocytes and a pharmaceutical peptide substance containing as its active base a therapeutically effective quantity of tetrapeptide of the formula Lys-Glu-Asp-Ala [SEQ ID NO:1] or one of its salts intended for parenteral administration. There is proposed a method of stimulating the functional activity of hepatocytes including therapeutic administration to a patient of the pharmaceutical peptide substance in doses 0.01–100 μg/kg of the body weight at least once a day during a period required for attaining a therapeutic effect.
专利号:US-12054511-B2 优先权日:2017-06-14 标题 :Synthesis of phosphate derivatives 发明人:GRIFFITH HUGH; KENNOVIN GORDON; DAMMALAPATI VENKATA LAKSHMI NARASIMHA RAO; KOTALA MANI BUSHAN 权利人:NuCana plc 摘要:The present invention is a process for the preparation of certain 5′-phosphoramidate nucleotide diastereoisomers. The phosphoramidates include those useful in the treatment of cancer such as NUC-3373 (5-fluoro-2′-deoxyuridine-5′-O-[1-naphthyl(benzyloxy-L-alaninyl)]phosphate].
专利号:US-8703747-B2 优先权日:2008-07-23 标题 :Aminophosphinic derivatives that can be used in the treatment of pain 发明人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE 权利人:ROQUES BERNARD; PORAS HERVÉ; FOURNIE-ZALUSKI MARIE-CLAUDE; PHARMALEADS 摘要:The present invention relates to a compound of the following general formula (I): R 1 —NH—CH(R 2 )—P(â• O)(OR 3 )—CH 2 —C(R 4 )(R 5 )—CONH—CH(R 6 )—COOR 7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R 1 represents a —C(â• O)—O—C(R 8 )(R 9 )—OC(â• O)—R 10 group; R 2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R 3 represents a hydrogen atom or a —C(R 12 )(R 13 )—OC(â• O)—R 14 group; R 4 and R 5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R 4 represents a hydrogen atom and R 5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R 6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R 7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, —CHMe—COOR 18 , —CHR 19 —OC(â• O)OR 20 and —CHR 19 —OC(â• O)OR 20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more avantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
专利号:US-2018362571-A1 优先权日:2015-12-11 标题:Diastereoselective synthesis of phosphate derivatives
专利号:US-11897913-B2 优先权日:2017-06-14 标 题:Synthesis of 3′-deoxyadenosine-5′-O-[phenyl(benzyloxy-L-alaninyl)]phosphate (NUC-738)
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合成参考文献
参考文献:10.1007/s00726-024-03424-3 摘要:Jakobsen S, Pedersen M, Nielsen CU. Structure-activity relationship of amino acid analogs to probe the binding pocket of sodium-coupled neutral amino acid transporter SNAT2. Amino Acids. 2024 Oct 19;56(1):64.