CAS: 115956-12-2; Rel-(5S,6R,8R,9As)-3-Oxooctahydro-1H-2,6-Methanoquinolizin-8-Yl 1H-Indole-3-Carboxylate

该化合物是5-HT5-HT3(Ki = 20 nM) 5-HT3 受体子型5-HT3受体的敌国(5-HT 1A,5-HT 1B,5-HT 2, dopamiine D 2, 1 -, 2 -, -, --肾上腺素2, 1 -, 2 -, M-1-5 muscarinic aceptylcholine, 和...

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1H-indole-3-carboxylic acid endo-hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one endo-hexahydro-8-hydroxy-2.6-methano-2H-quinolizin-3(4H)-one 3,8]-undecan-10-oneendo-5-hydroxy-8-azatricyclo[5.3.1.03,8]-undecan-10-one dolasetron mesylate dolasetron mesylate 4O3S*C19H20N2O3CH4O3S*C19H20N2O3 endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one mesylate

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    专利号:US-12383499-B2
    优先权日:2018-01-01
    标题:Scale up synthesis of silicasome nanocarriers
    发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
    权利人:UNIV CALIFORNIA
    摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

    专利号:US-9518034-B2
    优先权日:2013-10-14
    标题 :Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof
    发明人:STOLTZ BRIAN M; DOUGHERTY DENNIS A; DUQUETTE DOUGLAS; DUFFY NOAH
    权利人:CALIFORNIA INST OF TECHN
    摘要:This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): n ncomprising treating a compound of formula (II):n n nwith a transition metal catalyst under alkylation conditions.

    专利号:US-8734846-B2
    优先权日:2008-06-16
    标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
    发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
    权利人:BIND BIOSCIENCES INC
    摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

    专利号:US-2013035307-A1
    优先权日:2010-01-26
    标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
    发明人:PRESTWICH GLENN D; KENNEDY THOMAS P
    权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
    摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    专利号:WO-9964032-A1
    优先权日:1998-06-08
    标题 :Combinatorial synthesis of multibinding libraries
    发明人:CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
    权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
    摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.

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    主要参考文献


    1: Long-term Use of Ondansetron, Dolasetron and Granisetron for the Prevention of Nausea and Vomiting: A Review of the Clinical Effectiveness and Safety [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2014 Apr 23. Available from http://www.ncbi.nlm.nih.gov/books/NBK269203/ Review. Review.
    4: Ogilvie GK. Dolasetron: a new option for nausea and vomiting. J Am Anim Hosp Assoc. 2000 Nov-Dec;36(6):481-3. Review. Review. Review. doi: 10.1186/s12916-015-0379-3. Review.
    8: Rojas C, Raje M, Tsukamoto T, Slusher BS. Molecular mechanisms of 5-HT(3) and NK(1) receptor antagonists in prevention of emesis. Eur J Pharmacol. 2014 Jan 5;722:26-37. doi: 10.1016/j.ejphar.2013.08.049. Epub 2013 Oct 31. Review. Review.

    合成参考文献


    参考文献:10.3350/kjhep.2011.17.2.120
    摘要:Kim JS, Park YM, Kim NY, Yun HK, Lee KJ, Kim BH, Park SJ, Yeon JW, Jung G. Combination treatment with intrahepatic arterial infusion and intratumoral injection chemotherapy in patients with far-advanced hepatocellular carcinoma and arterioportal or arteriovenous shunts: preliminary results. Korean J Hepatol. 2011 Jun;17(2):120–9.
    参考文献:10.4103/0974-2700.82200
    摘要:Bhattarai B, Shrestha S, Singh J. Comparison of ondansetron and combination of ondansetron and dexamethasone as a prophylaxis for postoperative nausea and vomiting in adults undergoing elective laparoscopic surgery. J Emerg Trauma Shock. 2011 Apr;4(2):168–72.
    参考文献:10.1155/2011/426813
    摘要:Pergolizzi JV, Raffa R, Taylor R. Prophylaxis of Postoperative Nausea and Vomiting in Adolescent Patients: A Review with Emphasis on Combination of Fixed-Dose Ondansetron and Transdermal Scopolamine. Journal of Drug Delivery. 2011 Jul 02;2011():1–7. doi: 10.1155/2011/426813.
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