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-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
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-RE41998-E 优先权日:1990-02-26 标题 :Compositions and methods of treatment of sympathetically maintained pain 发明人:CAMPBELL JAMES N 权利人:ARCLON THERAPEUTICS INC 摘要:Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an α-1-adrenergic antagonist, α-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.
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.
1: Opitz K. The effect of clonidine and related substances on voluntary ethanol consumption in rats. Drug Alcohol Depend. 1990 Feb;25(1):43-8. doi: 10.1016/0376-8716(90)90139-6. 341(1-2):128-36. doi: 10.1007/BF00195069. 43(6):648-54. doi: 10.1038/clpt.1988.90. 332(2):113-23. doi: 10.1007/BF00511400. 28 Suppl:3-11. doi: 10.1007/BF00543703. 36(5):628-33. doi: 10.1038/clpt.1984.232. 6(5 Pt 2):II71-5. doi: 10.1161/01.hyp.6.5_pt_2.ii71. 227(2):421-8. 1(2):157-69. doi: 10.1111/j.1474-8673.1981.tb00508.x. 31(3):419-24. 11(1):73-7. doi: 10.1111/j.1365-2125.1981.tb01105.x. 12: Summers RJ, Jarrott B, Louis WJ. Selectivity of a series of clonidine-like drugs for alpha 1 and alpha 2 adrenoceptors in rat brain. Neurosci Lett. 1980 Dec;20(3):347-50. doi: 10.1016/0304-3940(80)90172-x. 18(6):449-54. doi: 10.1007/BF00874654. 66(2-3):233-41. doi: 10.1016/0014-2999(80)90147-8. 32(4):272-7. doi: 10.1111/j.2042-7158.1980.tb12911.x. 2(6):408-11. 8(4):390P. 54(1-2):185-9. doi: 10.1016/0014-2999(79)90423-0. 21(1):71-8. 6(1):27-30. doi: 10.1002/bms.1200060107.
合成参考文献
参考文献:10.1007/bf00511400 摘要:Kobinger W. Rudolf Buchheim lecture. Drugs as tools in research on adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol. 1986 Feb;332(2):113–23. doi: 10.1007/bf00511400. 参考文献:10.1007/bf00167236 摘要:Barrios M, Robles I, Baeyens JM. Role of L-type calcium channels on yohimbine-precipitated clonidine withdrawal in vivo and in vitro. Naunyn Schmiedebergs Arch Pharmacol. 1993 Dec;348(6):601–7. doi: 10.1007/bf00167236.