60-32-2 = 79778-41-9 反应条件:1.1 Reagents: Methanesulfonic Acid,Phosphorus Trichloride,Phosphonic Acid; 65 °C; 16 - 20 H,65 - 70 °C1.2 Solvents: Water; Cooled; 5 H,Reflux 标题:Systematic Study Of The Physicochemical Properties Of A Homologous Series Of Aminobisphosphonates 作者:Alanne,Aino-Liisa; Et Al 参考文献:Molecules 日期:2012 卷标:17 页码:10928-10945]
60-32-2 = 79778-41-9 反应条件:1.1 Reagents: Methanesulfonic Acid,Phosphorus Trichloride; 15 Min,Rt; 4 - 6 H,80 - 85 °C; 85 °C -> Rt1.2 Reagents: Water; 4 H,105 °C; Cooled1.3 Reagents: Sodium Hydroxide Solvents: Water; Ph 6 - 7,Cooled 标题:Biocompatible Organic Coatings Based On Bisphosphonic Acid Rgd-Derivatives For Peo-Modified Titanium Implants 作者:Parfenova,Lyudmila V.; Et Al 参考文献:Molecules 日期:2020 卷标:25(1)]
60-32-2 = 79778-41-9 反应条件:1.1 Reagents: Methanesulfonic Acid,Phosphorus Trichloride,Phosphonic Acid; Overnight,65 °C1.2 Reagents: Water; 5 H,Reflux1.3 Reagents: Sodium Hydroxide Solvents: Water; Rt 标题:Synthesis And Biological Evaluation Of New Bisphosphonate-Dextran Conjugates Targeting Breast Primary Tumor 作者:Migianu-Griffoni,Evelyne; Et Al 参考文献:Bioconjugate Chemistry 日期:2014 卷标:25(2) 页码:224-230]
948317-80-4 = 79778-41-9 反应条件:1.1 Reagents: Hydrazine Hydrate (1:1) Solvents: Water; 0 °C; 0.5 H,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 标题:Syntheses Of Phosphonic Esters Of Alendronate,Pamidronate And Neridronate 作者:Guenin,Erwann; Et Al 参考文献:European Journal Of Organic Chemistry 日期:2007 卷标:(20) 页码:3380-3391]
31968-60-2 = 79778-41-9 反应条件:1.1 Reagents: Silanol,1,1,1-Trimethyl-,1,1′,1′′-Phosphite; -5 °C; 4 H,Rt1.2 Reagents: Methanol2.1 Reagents: Hydrazine Hydrate (1:1) Solvents: Water; 0 °C; 0.5 H,Rt2.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 标题:Syntheses Of Phosphonic Esters Of Alendronate,Pamidronate And Neridronate 作者:Guenin,Erwann; Et Al 参考文献:European Journal Of Organic Chemistry 日期:2007 卷标:(20) 页码:3380-3391]
4443-26-9 = 79778-41-9 反应条件:1.1 Reagents: Oxalyl Chloride Solvents: Dichloromethane; 6 H,Reflux2.1 Reagents: Silanol,1,1,1-Trimethyl-,1,1′,1′′-Phosphite; -5 °C; 4 H,Rt2.2 Reagents: Methanol3.1 Reagents: Hydrazine Hydrate (1:1) Solvents: Water; 0 °C; 0.5 H,Rt3.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 标题:Syntheses Of Phosphonic Esters Of Alendronate,Pamidronate And Neridronate 作者:Guenin,Erwann; Et Al 参考文献:European Journal Of Organic Chemistry 日期:2007 卷标:(20) 页码:3380-3391]
60-32-2 = 79778-41-9 反应条件:1.1 6 H,170 °C2.1 Reagents: Oxalyl Chloride Solvents: Dichloromethane; 6 H,Reflux3.1 Reagents: Silanol,1,1,1-Trimethyl-,1,1′,1′′-Phosphite; -5 °C; 4 H,Rt3.2 Reagents: Methanol4.1 Reagents: Hydrazine Hydrate (1:1) Solvents: Water; 0 °C; 0.5 H,Rt4.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 1 标题:Syntheses Of Phosphonic Esters Of Alendronate,Pamidronate And Neridronate 作者:Guenin,Erwann; Et Al 参考文献:European Journal Of Organic Chemistry 日期:2007 卷标:(20) 页码:3380-3391
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:EP-1566177-A1 优先权日:2004-02-23 标 题:The use of bisphosphonates for treating skin by stimulating of collagen synthesis 发明人:KIM JIN; YOOK JONG IN; KIM NAM HEE; RYU JU KYOUNG 权利人:TIGEN BIOTECH CO LTD 摘要:The present invention relates to a novel use of bisphosphonate, and morenparticularly to a composition for increasing collagen synthesis comprisingnbisphosphonate as an active ingredient, as well as the use thereof. The inventivencomposition comprising the bisphosphonate promotes collagen synthesis, and thus, whennit is applied to the skin, it reduces wrinkles of the skin and makes the skin elastic. Fornthis reason, the inventive composition will be useful as cosmetics for the prevention ornimprovement of skin aging or a wound-healing agent. Furthermore, the inventivencomposition can remarkably increase the collagen synthesis of fibroblasts in vitro , andnthus, can be effectively used in the production of products containing collagen.
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-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.
1: Varenna M, Zucchi F, Failoni S, Becciolini A, Berruto M. Intravenous neridronate in the treatment of acute painful knee osteoarthritis: a randomized controlled study. Rheumatology (Oxford). 2015 Oct;54(10):1826-32. doi: 10.1093/rheumatology/kev123. Epub 2015 May 20. doi: 10.1038/pr.2014.20. Epub 2014 Feb 11. doi: 10.1093/rheumatology/ket321. Epub 2013 Sep 24. doi: 10.1093/rheumatology/kes312. Epub 2012 Nov 30. doi: 10.3390/molecules170910928. doi: 10.1111/j.1365-2141.2012.09152.x. Epub 2012 May 10. doi: 10.1016/j.bone.2011.11.028. Epub 2011 Dec 10. doi: 10.1007/s00774-011-0331-3. Epub 2011 Nov 8. doi: 10.1159/000331128. Epub 2011 Sep 27. doi: 10.1007/s00223-011-9489-x. Epub 2011 May 13. doi: 10.1002/jbmr.237. doi: 10.1016/j.ejpb.2010.05.013. Epub 2010 Jun 8. doi: 10.3899/jrheum.091016. doi: 10.1016/j.biopha.2009.06.014. Epub 2009 Oct 23. doi: 10.1007/s10637-009-9325-6. Epub 2009 Oct 2. doi: 10.1517/17425250903029190. Review. doi: 10.1016/j.ijpharm.2009.09.011. Epub 2009 Sep 11. Review.
合成参考文献
参考文献:10.1023/a:1006271332400 摘要:Ingram GC, Magnard JL, Vergne P, Dumas C, Rogowsky PM. ZmOCL1, an HDGL2 family homeobox gene, is expressed in the outer cell layer throughout maize development. Plant Mol Biol. 1999 May;40(2):343–54. doi: 10.1023/a:1006271332400. 参考文献:10.1007/s12519-020-00378-w 摘要:Sydlik C, Dürr HR, Pozza SB, Weißenbacher C, Roeb J, Schmidt H. Hypercalcaemia after treatment with denosumab in children: bisphosphonates as an option for therapy and prevention World Journal of Pediatrics. 2020 Aug 10;16(5):520–7. doi: 10.1007/s12519-020-00378-w. 参考文献:10.1186/s40348-020-00101-9 摘要:Etich J, Leßmeier L, Rehberg M, Sill H, Zaucke F, Netzer C, Semler O. Osteogenesis imperfecta—pathophysiology and therapeutic options. Molecular and Cellular Pediatrics. 2020 Aug 14;7(1):9. doi: 10.1186/s40348-020-00101-9. 参考文献:10.1021/jm0303709 摘要:Sanders JM, Ghosh S, Chan JM, Meints G, Wang H, Raker AM, Song Y, Colantino A, Burzynska A, Kafarski P, Morita CT, Oldfield E. Quantitative structure-activity relationships for gammadelta T cell activation by bisphosphonates. J Med Chem. 2004 Jan 15;47(2):375–84. doi: 10.1021/jm0303709.