CAS: 23651-95-8; Droxidopa

该化合物是能够跨越血压屏障,使其在治疗因自动功能障碍导致的低血压条件下有效发挥作用.Droxidopa通常通过口服方式进行,并因其相对有利的安全特征而为人所知,尽管它可能会造成副作用,如头痛,恶心和高血压.其致癌性肿瘤涉及快速吸收和代谢,最高等离子浓度在经管后的几小时内发生.

结构式图片

欧盟法规

C&L通报

上下游产品

D,L-threo-3-(3,4-Dibenzyloxyphenyl)serine 3,4-dibenzyloxybenzaldehyde 3,4-bis(ethoxycarboxy)-benzaldehyde RS.3RS)-2-amino-3-(3,4-bis-benzyloxy-phenyl)-3-hydroxy-propionic acid(2RS.3RS)-2-amino-3-(3,4-bis-benzyloxy-phenyl)-3-hydroxy-propionic acid

合成工艺路线路线简述

    (2S,3R)-2-Amino-3-[3,4-Bis(Benzyloxy)Phenyl]-3-Hydroxypropionic Acid置于盐酸,Palladium 10% On Activated Carbon,氢气体系中,用 乙醇,水 用作溶剂,以85%的收率获得屈西多巴
    参考文献:Compositions And Methods For The Treatment Of Autonomic And Other Neurological Disorders
    标题:Compositions And Methods For The Treatment Of Autonomic And Other Neurological Disorders
    摘要:该发明涉及公式i的化合物或其药用可接受的盐,以及其多晶型,溶剂合物,对映体,立体异构体和水合物.包括公式i化合物的有效量的药物组合物,以及用于治疗自主神经和其他神经系统疾病的方法可以制成口服,颊下,直肠,局部,经皮,经粘膜,静脉,肠道给药,糖浆或注射剂形式.这些组合物可用于治疗神经源性直立性低血压(noh),以及与多系统萎缩(msa),家族性淀粉样多神经病(fap),纯自主神经功能衰竭(paf)和帕金森病(pd),透析期低血压(idh)或血液透析诱发的低血压,与纤维肌痛综合症(fms)和慢性疲劳综合症(cfs)相关的低血压.

    海关参考信息

    专利信息


    专利号:US-9353057-B2
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
    发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
    权利人:XENOPORT INC
    摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

    专利号:US-6603070-B2
    优先权日:2000-07-21
    标题 :Convergent synthesis of multiporphyrin light-harvesting rods
    发明人:LINDSEY JONATHAN S; LOEWE ROBERT S
    权利人:UNIV NORTH CAROLINA STATE
    摘要:The present invention provides a convergent method for the synthesis of light harvesting rods. The rods are oligomers of the formula A 1 (A b+1 ) b , wherein b is at least 1, A 1 through A b+1 are covalently coupled rod segments, and each rod segment A 1 through A 1+b comprises a compound of the formula X 1 (X m+1 ) m wherein m is at least 1 and X 1 through X m+1 are covalently coupled porphyrinic macrocycles. Light harvesting arrays and solar cells containing such light harvesting rods are also described, along with intermediates useful in such methods and rods produced by such methods.

    专利号:US-7576211-B2
    优先权日:2004-09-30
    标题 :Synthesis of thienopyridinone compounds and related intermediates
    发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
    权利人:EPIX DELAWARE INC
    摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

    专利号:US-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:US-12348700-B2
    优先权日:2022-05-09
    标题:Real-time novel view synthesis with forward warping and depth
    发明人:JOHNSON JUSTIN; Cao ang; ROCKWELL CHRIS
    权利人:UNIV MICHIGAN REGENTS
    摘要:A fast and generalizable novel view synthesis method with sparse inputs is disclosed. The method may comprise: accessing at least a first input image with a first view of a subject in the first input image, and a second input image with a second view of the subject in the second input image using a computer system; estimating depths for pixels in the at least first and second input images; constructing a point cloud of image features from the estimated depths; and synthesizing a novel view by forward warping by using a point cloud rendering of the constructed point cloud.

    专利号:US-6093805-A
    优先权日:1991-01-22
    标 题:Glycoside compounds and methods of synthesis
    发明人:SHULL BRIAN K; TUINMAN ROELAND J; HOUSTON TODD A; KLEMKE R ERICH; KOREEDA MASATO
    权利人:UNIV MICHIGAN
    摘要:Novel glycosides, especially steroidal and non-steroidal glycosides are provided. The steroidal and non-steroidal glycosides preferably are prepared from aglycons which possess valuable properties such as pharmacological properties. The glycosides are prepared from useful aglycons and possess useful properties which are the same as those of their respective unglycosylated aglycons. The glycosides are provided in acylated and deacylated form. The acylated glycosides after hydrolysis of the acyl groups possess enhanced water solubility properties, as illustrated in the case where the aglycon is acetominophen.
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    主要参考文献


    1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Droxidopa. 2017 Apr 17. 34(10):1933-41. doi: 10.1097/HJH.0000000000001043. 15(5):e38907. doi: 10.7759/cureus.38907.
    4: Keating GM. Droxidopa: a review of its use in symptomatic neurogenic orthostatic hypotension. Drugs. 2015 Feb;75(2):197-206. doi: 10.1007/s40265-014-0342-1. 62(6):1904-1911. doi: 10.1016/j.japh.2022.06.002. Epub 2022 Jun 13. 20(6):635-645. doi: 10.1080/14656566.2019.1574746. Epub 2019 Feb 7. 26(3):171-80. doi: 10.1007/s10286-016-0349-7. Epub 2016 Mar 7. 26(1):154-177. doi: 10.1212/CON.0000000000000816.
    9: White WB, Hauser RA, Rowse GJ, Ziemann A, Hewitt LA. Cardiovascular Safety of Droxidopa in Patients With Symptomatic Neurogenic Orthostatic Hypotension. Am J Cardiol. 2017 Apr 1;119(7):1111-1115. doi: 10.1016/j.amjcard.2016.11.066. Epub 2017 Jan 6. 36(1):53-67. doi: 10.1016/j.cger.2019.09.002. Epub 2019 Sep 6.

    合成参考文献


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