CAS: 2922-83-0; (S)-2-Amino-4-(2-Aminophenyl)-4-Oxobutanoic Acid

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Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于臭氧,溶剂黄146体系中,化学反应生成L-犬尿氨酸
参考文献:The Preparation Of L-,D-And Dl-Kynurenine1
标题:The Preparation Of L-,D-And Dl-Kynurenine1
摘要:
Doi:10.1021/ja01635A084

专利信息

专利号:US-2016031800-A1
优先权日:2013-03-14
标 题:Synthesis of chiral kynurenine compounds and intermediates
发明人：TRETYAKOV ALEXANDER; DROUET KEITH E; SANDERS WILLIAM
权利人:VISTAGEN THERAPEUTICS INC
摘要:Provided are methods for the synthesis of compounds including chiral kynurenine compounds, intermediates useful for the synthesis thereof, and related compounds. For example, methods are provided for the synthesis of L-4-chlorokynurenine.

专利号:US-11427530-B2
优先权日:2018-02-09
标 题 :Synthesis of 4-chlorokynurenines and intermediates
发明人：LEVIN DANIEL; LEEMING PETER; EISENREICH EMERICH; LIU XUEJUN KARL
权利人:VISTAGEN THERAPEUTICS INC
摘要:The invention relates to an overall enantio-specific synthesis of 4-chlorokynurenine compounds, in particular L-4-chlorokynurenine, with improved yields. Large-scale syntheses are disclosed. The invention also relates to novel intermediates in the synthesis of L-4-chlorokynurenine.

专利号:US-9873688-B2
优先权日:2013-11-08
标 题:Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor
发明人：TAO MING; FRIETZE WILLIAM; MELONI DAVID J; WENG LINGKAI; ZHOU JIACHENG; PAN YONGCHUN
权利人:INCYTE CORP; INCYTE HOLDINGS CORP
摘要:The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

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-2022160788-A1
优先权日:2019-03-22
标题 :Bifunctional vectors allowing bcl11a silencing and expression of an anti-sickling hbb and uses thereof for gene therapy of b-hemoglobinopathies
发明人：MICCIO ANNARITA; AMENDOLA MARIO; BRUSSON MÉGANE; CAVAZZANA MARINA; MAVILIO FULVIO
权利人:INST NAT SANTE RECH MED; UNIV DEVRY VAL DESSONNE; ASSIST PUBLIQUE HOPITAUX PARIS APHP; UNIV PARIS; FOND IMAGINE
摘要:The #β-hemoglobinopathies #β-thalassemia (BT) and sickle cell disease (SCD) are the most frequent genetic disorders worldwide. These diseases are caused by mutations causing reduced or abnormal synthesis of the β-globin chain of the adult hemoglobin (Hb) tetramer. Here, the inventors intend to improve HSC-based gene therapy for β-thalassemia and SCD by developing an innovative, highly infectious LV vector expressing a potent anti-sickling β-globin transgene and a second biological function either increasing fetal γ-globin expression (for β-thalassemia and SCD). More particularly, the inventors have designed a novel lentivirus (LV), which carry two different functions: βAS3 gene addition and gene silencing. This last strategy allows the re-expression of the fetal γ-globin genes (HBG1 and HBG2) and production of the endogenous fetal hemoglobin (HbF). Elevated levels of HbF and HbAS3 (Hb tetramer containing βAS3-globin) will benefit the β-hemoglobinopathy phenotype by increasing the total amount of β-like globin that will: (i) reduce the alpha precipitates and improve the alpha/non alpha ratio in β-thalassemia, and (ii) reduce the sickling in SCD. This combined strategy will improve the β-hemoglobinopathy phenotype at a lower vector copy number (VCN) per cell compared to a LV expressing the βAS3 alone.