(5-Methyl-2-Oxo-1,3-Dioxol-4-yl)Methyl 4-(1-Hydroxy-1-Methylethyl)-1-({2'-[1-(4-Methoxybenzyl)-1H-Tetrazol-5-Yl]Biphenyl-4-Yl}Methyl)-2-Propyl-1H-Imidazole-5-Carboxylate置于三氟乙酸体系中,化学反应 72.0H,以83%的收率获得奥美沙坦酯 参考文献:2,4-Dimethoxybenzyl Group For The Protection Of Tetrazole: An Efficient Synthesis Of Olmesartan Medoxomil Through C-h Arylation 标题:2,4-Dimethoxybenzyl Group For The Protection Of Tetrazole: An Efficient Synthesis Of Olmesartan Medoxomil Through C-h Arylation 摘要:The 2,4-Dimethoxybenzyl (Dmb) Group Was Found To Be Effective For Protecting Tetrazoles. The Dmb Group Is Inert To Various Conditions,Including Those For Ruthenium-Catalyzed C-H Arylation,But Is Readily Cleaved Under Mild Conditions. The Use Of A Dmb Protecting Group Permitted A Synthesis Of Highly Functionalized Olmesartan Medoxomil In A Few Steps. Doi:10.1055/s-0034-1378848
专利号:US-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-2008214637-A1 优先权日:2004-11-11 标题 :Process for the Synthesis of Tetrazoles 发明人:ANTONCIC LJUBOMIR; LUDESCHER JOHANNES 权利人:LEK PHARMACEUTICALS 摘要:A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-8431712-B2 优先权日:2004-02-09 标 题 :Methods for the synthesis of pyridoxamine 发明人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT 权利人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT; NEPHROGENEX INC 摘要:The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): n nand salts thereof.n nThe invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.
专利号:US-9981949-B2 优先权日:2008-12-01 标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:OYSTER POINT PHARMA INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
1: Choi EY, McKenna BJ. Olmesartan-Associated Enteropathy: A Review of Clinical and Histologic Findings. Arch Pathol Lab Med. 2015 Oct;139(10):1242-7. doi: 10.5858/arpa.2015-0204-RA. Review. Review. Russian. doi: 10.1111/apt.12780. Epub 2014 May 7. Review. doi: 10.1007/s40292-013-0037-9. Epub 2014 Jan 17. Review. doi: 10.3109/10641963.2013.846363. Epub 2013 Oct 28. Review. doi: 10.1007/s40266-013-0130-8. Review. doi: 10.1586/14779072.2013.827449. Review. doi: 10.2165/11636080-000000000-00000. Review. doi: 10.1517/14656566.2012.745510. Epub 2012 Nov 21. Review. doi: 10.2165/11597390-000000000-00000. Review. doi: 10.1586/erc.12.100. Review. doi: 10.1177/1753944711432902. Epub 2012 Jan 5. Review. doi: 10.1177/1753944711420464. Epub 2011 Sep 5. Review. Epub 2011 Sep 1. Review. 15: Tocci G, Volpe M. Fixed-combination therapy to improve blood pressure control: experience with olmesartan-based therapy. Expert Rev Cardiovasc Ther. 2011 Jul;9(7):829-40. doi: 10.1586/erc.11.59. Review. doi: 10.1358/dot.2011.47.3.1587028. Review. doi: 10.2147/VHRM.S20737. Epub 2011 Jun 24. Review. 18: Tocci G, Volpe M. Olmesartan medoxomil for the treatment of hypertension in children and adolescents. Vasc Health Risk Manag. 2011;7:177-81. doi: 10.2147/VHRM.S11672. Epub 2011 Mar 31. Review.
合成参考文献
参考文献:10.1253/circj.cj-09-0862 摘要:Hosoya M, Ohashi J, Sawada A, Takaki A, Shimokawa H. Combination therapy with olmesartan and azelnidipine improves EDHF-mediated responses in diabetic apolipoprotein E-deficient mice. Circ J. 2010 Apr;74(4):798–806. doi: 10.1253/circj.cj-09-0862. 参考文献:10.1038/hr.2011.74 摘要:Hayashi K. L-/T-type Ca channel blockers for kidney protection: ready for sophisticated use of Ca channel blockers. Hypertens Res. 2011 Aug;34(8):910–2. doi: 10.1038/hr.2011.74. 参考文献:10.4061/2011/284823 摘要:Kinouchi K, Ichihara A, Bokuda K, Kurosawa H, Itoh H. Differential Effects in Cardiovascular Markers between High-Dose Angiotensin II Receptor Blocker Monotherapy and Combination Therapy of ARB with Calcium Channel Blocker in Hypertension (DEAR Trial). International Journal of Hypertension. 2011;2011():1–11. doi: 10.4061/2011/284823. 参考文献:10.1016/j.clpt.2005.08.001 摘要:Hasler C, Nussberger J, Maillard M, Forclaz A, Brunner HR, Burnier M. Sustained 24‐hour blockade of the renin‐angiotensin system: A high dose of a long‐acting blocker is as effective as a lower dose combined with an angiotensin‐converting enzyme inhibitor. Clinical Pharmacology & Therapeutics. 2005 Sep 26;78(5):501–7. doi: 10.1016/j.clpt.2005.08.001. 参考文献:10.1185/03007995.2011.589434 摘要:Swindle JP, Buzinec P, Iorga ŞR, Ramaswamy K, Panjabi S. Long-term clinical and economic outcomes associated with angiotensin II receptor blocker use in hypertensive patients. Current Medical Research and Opinion. 2011 Jul 18;27(9):1719–31. doi: 10.1185/03007995.2011.589434.