CAS: 104-31-4; 2,5,8,11,14,17,20,23,26-Nonaoxaoctacosan-28-Yl 4-(Butylamino)Benzoate

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    专利号:US-12295961-B2
    优先权日:2009-12-31
    标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
    发明人:DHINGRA OM
    权利人:MARIUS PHARMACEUTICALS INC
    摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

    专利号:US-11617758-B2
    优先权日:2009-12-31
    标 题 :Emulsion formulations
    发明人:DHINGRA OM; BERNSTEIN JAMES S
    权利人:MARIUS PHARMACEUTICALS LLC
    摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

    专利号:US-2006035327-A1
    优先权日:2001-02-28
    标题:Recombinant super-compound interferon and uses thereof
    发明人:WEI GUANGWEN
    权利人:WEI GUANGWEN
    摘要:This invention provides a recombinant super-compound interferon (rSIFN-co) and its equivalent with changed spatial configuration, high efficacy and low side effects. Therefore, high dose of rSIFN-co may be used. One characteristic of rSIFN-co is its ability to inhibit the HBV DNA duplication and secretion of HBsAg and HBeAg in in vitro pharmacological studies. The cytotoxic effect of rSIFN-co is only one-eighth (â…›) of currently clinically available interferons but its anti-viral effect is approximately five to twenty (5-20) times higher, and when used in vivo it has a broader spectrum of clinical applications and longer biofeedback response. This invention further provides super-compound interferon or its equivalent, synthesis of artificial gene with codon preference which codes for said rSIFN-co and its equivalent, vector comprising said gene and appropriate expression system for expression of said rSIFN-co. Finally this invention provides the super-compound interferon (rSIFN-co) and its equivalent, a process to produce same and uses thereof.

    专利号:US-2013303495-A1
    优先权日:2009-12-31
    标题:Emulsion formulations
    发明人:DHINGRA OM; BERNSTEIN JAMES S
    权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES LLC
    摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

    专利号:US-7935686-B2
    优先权日:2004-11-03
    标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis, and use
    发明人:GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of making prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof, methods of using prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphonous acid, 3-aminopropylphosphinic acid, and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.

    专利号:US-7566738-B2
    优先权日:2004-11-03
    标题 :Acyloxyalkyl carbamate prodrugs of sulfinic acids, methods of synthesis, and use
    发明人:GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions of 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, methods of using prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.
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    主要参考文献


    1: Evans MS, Maglinger GB, Fletcher AM, Johnson SR. Benzonatate inhibition of voltage-gated sodium currents. Neuropharmacology. 2016 Feb;101:179-87. doi: 10.1016/j.neuropharm.2015.09.020. doi: 10.1002/phar.1153. doi: 10.5863/1551-6776-17.3.270.
    4: Winter ML, Spiller HA, Griffith JR. Benzonatate Ingestion Reported to the National Poison Center Database System (NPDS). J Med Toxicol. 2010 Dec;6(4):398-402. doi: 10.1007/s13181-010-0086-6.
    5: Cohen V, Jellinek SP, Stansfield L, Truong H, Baseluos C, Marshall JP. Cardiac arrest with residual blindness after overdose of Tessalon® (benzonatate) perles. J Emerg Med. 2011 Aug;41(2):166-71. doi: 10.1016/j.jemermed.2009.08.027. doi: 10.1097/ICO.0b013e318207f229. doi: 10.1097/PEC.0000000000000733. doi: 10.1016/j.rmed.2008.12.008. Review. doi: 10.1016/j.jaad.2015.02.1102. English, Italian.

    合成参考文献


    摘要:Schweizerische Medizinische Wochenschrift., 86(94), 1956 []
    摘要:Helvetica Physiologia et Pharmacologica Acta., 15(55), 1957 []
    摘要:National Library of Medicine's Medical Subject Headings online file (MeSH, 2011)
    摘要:US Natl Inst Health; DailyMed. Benzonatate. Available from, as of Dec 9, 2011:
    摘要:HANSCH,C ET AL. (1995)
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