CAS: 13404-22-3; H-Ala-Otbu.Hcl

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21691-50-9 59531-86-1 69320-88-3

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CAS号50300-96-4 cis,trans-1-phe... | CAS号540-88-5 醋酸叔丁酯 | CAS号56-41-7 L-丙氨酸 | CAS号58177-77-8 B°C-Ala-Otbu | CAS号82717-96-2 N-[1-(S)-乙氧羰基-3... | CAS号58177-77-8 B°C-Ala-Otbu

2-甲基-2-丙基n-{[(2-甲基-2-丙基)氧基]羰基}-L-丙氨酸酯置于盐酸,水体系中,用 1,4-二氧六环 用作溶剂,化学反应生成L-丙氨酸叔丁酯盐酸盐
参考文献:Cyclic Phosphoramidates As Prodrugs Of 2'-C-Methylcytidine
标题:Cyclic Phosphoramidates As Prodrugs Of 2'-C-Methylcytidine
摘要:The Currently Approved Treatment For Hepatitis C Virus Infections Is A Combination Of Ribavirin And Pegylated Interferon. It Leads To A Sustained Virologic Response In Approximately Only Half Of The Patients Treated. For This Reason There Is An Urgent Need Of New Therapeutic Agents. 2'-C-Methylcytidine Is The First Nucleoside Inhibitor Of The Hcv Ns5B Polymerase That Was Efficacious In Reducing The Viral Load In Patients Infected With Hcv. The Application Of A Monophosphate Prodrug Approach Based On Unprecedented Cyclic Phosphoramidates Is Reported. Our Sar Studies Led To Compounds That Are Efficiently Converted To The Active Triphosphate In Human Hepatocytes. (C) 2009 Elsevier Masson Sas. All Rights Reserved.
Doi:10.1016/j.Ejmech.2009.04.043

专利信息

专利号:US-9453037-B2
优先权日:2011-07-28
标 题 :Methylphenidate-prodrugs, processes of making and using the same
发明人：GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB
权利人:KEMPHARM INC; KEMPHARM INC
摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.

专利号:US-8044173-B2
优先权日:2005-09-13
标 题 :Asymmetric synthesis of peptides
发明人：HARWOOD LAURENCE M; YAN RAN
权利人:UNIV READING
摘要:A process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S, or NR 8 , where R 8 is C 1-6 alkyl, C 6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC(O)— occurs without racemisation, is provided. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.

专利号:US-8399612-B2
优先权日:2005-09-13
标 题 :Asymmetric synthesis of peptides
发明人：HARWOOD LAURENCE M; YAN RAN
权利人:HARWOOD LAURENCE M; YAN RAN; UNIV READING
摘要:A process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S, or NR 8 , where R 8 is C 1-6 alkyl, C 6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC(O)— occurs without racemization, is provided. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerization.

专利号:WO-2005033127-A1
优先权日:2003-09-30
标 题:Method for the synthesis of n-[(s)-1-carbethoxybutyl]-(s)-alanine and use thereof for the synthesis of perindopril

专利号:US-2006275768-A1
优先权日:2002-12-30
标 题 :Multiplex polymer ligation
发明人：KOCHENDOERFER GERD G; SHAO HAIYAN; CRESSMAN SONYA
权利人:KOCHENDOERFER GERD G; SHAO HAIYAN; CRESSMAN SONYA
摘要:The invention concerns a multiplex polymer ligation method involving water-soluble polymeric protecting groups, compositions and methods of use. The method involves synthesis of a first compound bearing one or more water-soluble polymeric protecting groups followed by replacing one or more of the water-soluble protecting groups with a chemical adduct of interest. Multiple different compounds derived from the first compound can be readily prepared by splitting the first compound into first and second reaction systems, followed by replacing one or more of the water-soluble polymeric protecting groups of the first reaction system with a first chemical adduct, and replacing one or more of the water-soluble polymeric protecting groups of the second reaction system with a second chemical adduct of interest, where the first and second chemical adducts are different. Also provided are kits useful for carrying out the multiplex polymer ligation methods of the invention.

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.