专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
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.
专利号:US-8716507-B2 优先权日:2008-10-31 标题 :Iron(II) catalysts containing diimino-diphosphine tetradentate ligands and their synthesis 发明人:MIKHAILINE ALEXANDRE; FREUTEL FRIEDERIKE; SUI-SENG CHRISTINE; MEYER NILS; MORRIS ROBERT H; LAGADITIS PARASKEVI OLYMPIA 权利人:MIKHAILINE ALEXANDRE; FREUTEL FRIEDERIKE; SUI-SENG CHRISTINE; MEYER NILS; MORRIS ROBERT H; LAGADITIS PARASKEVI OLYMPIA; GOVERNING COUNCIL OF UNIVERSITY OF TORONTO 摘要:New hexa-coordinate iron (II) complexes comprising compounds of formula (I) are described. These compounds comprise a tetradentate ligand with donor atoms comprising nitrogen and phosphorus. These complexes are shown for the first time to be useful catalysts for the hydrogenation of ketones, aldehydes, or imines to produce alcohols or amines, and the asymmetric hydrogenation of prochiral ketones or imines to produce non-racemic alcohols or amines. The source of the hydrogen can be hydrogen gas or a hydrogen-donating molecule such as isopropanol or hydrogen-donating mixture such as formic acid and an amine depending on the structure of the catalyst. In certain embodiments, the axial ligands on the catalyst comprise organonitrile ligands, carbonyl ligands, isonitrile ligands, or combinations thereof. The catalysts and the preparation thereof are disclosed. A reaction using phosphine and diamine precursors that is templated by the iron ion is the preferred route to the catalysts.
专利号:US-7671208-B2 优先权日:2007-03-30 标题 :Acetone solvate of phthaloyl amlodipine 发明人:BERENGUER MAIMO RAMON; MEDRANO RUPEREZ JORGE; MERODIO CABANILLAS JUAN FRANCISCO 权利人:ESTEVE QUIMICA SA 摘要:An acetone solvate of phthaloyl amlodipine, as well as a process for its preparation including dissolving phthaloyl amlodipine in acetone and cooling the mixture. The present invention also comprises a method for the synthesis of amlodipine, its salts or solvates, which comprises the use of an acetone solvate of phthaloyl amlodipine.
专利号:WO-2004058711-A1 优先权日:2002-12-30 标 题 :Isolation of dihydropyridine derivative and preparation salts thereof 发明人:ASLAN TUNCER; ADIYAMAN MUSTAFA; YURDAKUL AYCIL; SAHPAZ FILIZ; OZARSLAN EVREN A; GUNER DIDEM; RIDVANOGLU NURTEN 权利人:EOS ECZACIBASI OZGUN KIMYASAL; ASLAN TUNCER; ADIYAMAN MUSTAFA; YURDAKUL AYCIL; SAHPAZ FILIZ; OZARSLAN EVREN A; GUNER DIDEM; RIDVANOGLU NURTEN 摘要:The title compound is isolated in pure form by using a crystallization process and converted to its pharmaceutically acceptable salts. The crystallization process affects stability and purity of the amlodipine salts. All known impurities and one unknown impurity, which forms during the synthesis of the amlodipine salts, were isolated, characterized, and synthesized. A new method allowing the quantitative HPLC analysis of all related impurities of amlodipine salts in a single chromatogram was developed.
专利号:US-7558732-B2 优先权日:2002-09-23 标题 :Method and system for computer-aided speech synthesis 发明人:KUSTNER MICHAEL; SCHNELL MARKUS 权利人:INFINEON TECHNOLOGIES AG 摘要:Method and system for computer-aided speed synthesis for synthesizing electronic text by performing a predefined series of rules-based analyses in a predefined order, each of the analyses operating in a graduated manner to convert respective electronic text into electronic lexicons, and announcing analog speech based on the results of the performing step.
1: Sievers P, Uhlmann L, Korkmaz-Icöz S, Fastner C, Bea F, Blessing E, Katus HA, Preusch MR. Combined treatment with olmesartan medoxomil and amlodipine besylate attenuates atherosclerotic lesion progression in a model of advanced atherosclerosis. Drug Des Devel Ther. 2015 Jul 29;9:3935-42. doi: 10.2147/DDDT.S85203. eCollection 2015. 2: Nam JH, Oh M, Kim HJ, Han SK, Kim EJ, Song GS, Kim EY, Shin JG, Ghim JL, Kim HS. Pharmacokinetic comparison of amlodipine adipate/valsartan fixed-dose combination with amlodipine besylate/valsartan fixed-dose combination in healthy volunteers. Int J Clin Pharmacol Ther. 2015 Jan;53(1):66-74. doi: 10.5414/CP202045. doi: 10.2147/DDDT.S82820. eCollection 2015. 4: Kaur M, Ita KB, Popova IE, Parikh SJ, Bair DA. Microneedle-assisted delivery of verapamil hydrochloride and amlodipine besylate. Eur J Pharm Biopharm. 2014 Feb;86(2):284-91. doi: 10.1016/j.ejpb.2013.10.007. Epub 2013 Oct 28. doi: 10.1016/j.jpba.2015.01.059. Epub 2015 Feb 18. doi: 10.1007/s40256-015-0144-1. Review. Chinese. doi: 10.3109/10837450.2013.840847. Epub 2013 Oct 7. doi: 10.1186/1471-2415-14-124.
合成参考文献
摘要:Gekkan Yakuji. Pharmaceuticals Monthly., 36(1169), 1994 摘要:Drugs in Japan, -(71), 1995 参考文献:10.1007/s13346-017-0361-z 摘要:Nalluri BN, Uppuluri C, Devineni J, Nayak A, Nair KJ, Whiteside BR, Das DB. Effect of microneedles on transdermal permeation enhancement of amlodipine. Drug Delivery and Translational Research. 2017 Feb 03;7(3):383–94. doi: 10.1007/s13346-017-0361-z. 参考文献:10.1038/s41371-018-0066-x 摘要:Wang G, Chen Y, Li L, Tang W, Wright JM. First-line renin–angiotensin system inhibitors vs. other first-line antihypertensive drug classes in hypertensive patients with type 2 diabetes mellitus. Journal of Human Hypertension. 2018 May 01;32(7):494–506. doi: 10.1038/s41371-018-0066-x.