CAS: 33178-86-8; Alinidine

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    参考文献:Staehle H.; Daniel H.; Koebinger W.; Lillie C.; Pichler L.,J. Med. Chem.,1980,23,No 11,1217-1222
    标题:Staehle H.; Daniel H.; Koebinger W.; Lillie C.; Pichler L.,J. Med. Chem.,1980,23,No 11,1217-1222

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    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-8017776-B2
    优先权日:2003-07-15
    标题 :Methods for synthesis of acyloxyalkyl compounds
    发明人:BHAT LAXMINARAYAN; GALLOP MARK A
    权利人:XENOPORT INC
    摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

    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-8143437-B2
    优先权日:2002-02-19
    标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
    发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
    权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
    摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

    专利号:WO-2009094569-A2
    优先权日:2008-01-25
    标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

    专利号:US-2005222431-A1
    优先权日:2003-12-30
    标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

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    主要参考文献


    1: Meinertz T, Kasper W, Meier R, Wiegand U, Bechtold H, Förster I, Pop T, Jähnchen E. Alinidine in angina. Clin Pharmacol Ther. 1983 Dec;34(6):770-6. doi: 10.1038/clpt.1983.248. 13(6):821-7. doi: 10.1111/j.1365-2125.1982.tb01873.x.
    3: Harron DW, Shanks RG. Pharmacology, clinical pharmacology and potential therapeutic uses of the specific bradycardiac agent alinidine. Eur Heart J. 1985 Sep;6(9):722-9. doi: 10.1093/oxfordjournals.eurheartj.a061932. 16(4):451-5. doi: 10.1111/j.1365-2125.1983.tb02196.x.
    5: Hageman GR, Neely BH, Urthaler F, James TN. Negative chronotropic and parasympatholytic effects of alinidine on canine sinus node and AV junction. Am J Physiol. 1985 Mar;248(3 Pt 2):H324-30. doi: 10.1152/ajpheart.1985.248.3.H324. 15(1):21-9. doi: 10.1111/j.1365-2125.1983.tb01458.x.

    合成参考文献


    参考文献:10.1007/s003920050360
    摘要:Mitrovic V, Miskovic A, Straub M, Beckmann K, Thormann J, Pitschner H. [Effects of the K(+) channel blocker tedisamil on hemodynamics, myocardial ischemia and neurohumoral systems in patients with stable angina pectoris. A comparison with the beta blocker atenolol]. Z Kardiol. 1999 Oct;88(10):838–49. doi: 10.1007/s003920050360.
    参考文献:10.1161/01.cir.0000138933.85923.36
    摘要:Lei L, Zhou R, Zheng W, Christensen LP, Weiss RM, Tomanek RJ. Bradycardia induces angiogenesis, increases coronary reserve, and preserves function of the postinfarcted heart. Circulation. 2004 Aug 17;110(7):796–802. doi: 10.1161/01.cir.0000138933.85923.36.
    参考文献:10.1007/s10456-005-9012-y
    摘要:Brown MD, Davies MK, Hudlicka O. Angiogenesis in ischaemic and hypertrophic hearts induced by long-term bradycardia. Angiogenesis. 2005;8(3):253–62. doi: 10.1007/s10456-005-9012-y.
    参考文献:10.1111/j.1476-5381.2009.00588.x
    摘要:Szollosi A, Nenquin M, Henquin J. Pharmacological stimulation and inhibition of insulin secretion in mouse islets lacking ATP‐sensitive K+channels. British J Pharmacology. 2010 Feb;159(3):669–77. doi: 10.1111/j.1476-5381.2009.00588.x.
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