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    • 61. 发明授权
    • Improvement in the method of NMR imaging employing a manganese II
chelates of N,N'-bis[pyridoxal-alkylene (or cycloalkylene) (or
arylene)]-N,N'-diacetic acid derivatives
    • 使用N,N'-双[吡哆醛 - 亚烷基(或亚环烷基)(或亚芳基)] -N,N'-二乙酸衍生物的锰II螯合物的NMR成像方法的改进
    • US4994259A
    • 1991-02-19
    • US380185
    • 1989-07-14
    • Scott M. RocklageSteven C. Quay
    • Scott M. RocklageSteven C. Quay
    • A61K49/06C07D213/66C07F13/00
    • C07D213/66A61K49/06C07F13/005Y10T436/145555Y10T436/24
    • Manganese(II) chelates of N,N'-bis-(pyridoxal)-alkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-alkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N-acetic acids, and their salts are highly stable, superior NMRI contrast agents. They maintain the manganese(II) ion in the +2 valence state. Preferred contrast agents are manganese(II) ion chelates of N,N'-bis-(pyridoxal)ethylenediamine-N,N'-diacetic acid, N,N'-bis-(pyridoxal)trans-1,2-cyclohexylenediamine-N,N'-diacetic acid, and the salts and esters thereof.Novel chelate forming compounds are the N,N'-bis-(pyridoxal)-1,2-cycloalkylenediamine-N,N'-diacetic acids and N,N'-bis-(pyridoxal)1,2-arylene-diamine-N,N'-diacetic acids, N,N'-bis-(pyridoxal)-alkylenediamine-N-acetic acids, N,N'-bis(pyridoxal)-1,2-cycloalkylenediamine-N-acetic acids, N,N'-bis-(pyridoxal)-1,2-arylenediamine-N-acetic acids, and their salts and esters.
    • N,N'-双 - (吡哆醛) - 亚烷基二胺-N,N'-二乙酸,N,N'-双 - (吡哆醛)-1,2-环烷二胺-N,N'-二乙酸的锰(II)螯合物 酸,N,N'-双 - (吡哆醛)-1,2-芳基二胺-N,N'-二乙酸,N,N'-双 - (吡哆醛) - 亚烷基二胺-N-乙酸,N, 双(吡哆醛)-1,2-环亚烷基二胺-N-乙酸N,N'-双 - (吡哆醛)-1,2-芳基二胺-N-乙酸及其盐是高度稳定的,优良的NMRI造影剂 。 它们保持+2价态的锰(II)离子。 优选的造影剂是N,N'-双 - (吡哆醛)乙二胺-N,N'-二乙酸,N,N'-双 - (吡哆醛)反-1,2-环己二胺-N ,N'-二乙酸及其盐和酯。 新型螯合形成化合物是N,N'-双 - (吡哆醛)-1,2-环烷二胺-N,N'-二乙酸和N,N'-双(吡哆醛)1,2-亚芳基二胺-N N,N'-二 - (吡哆醛) - 亚烷基二胺-N-乙酸,N,N'-双(吡哆醛)-1,2-环烷二胺-N-乙酸,N,N' 双 - (吡哆醛)-1,2-芳基二胺-N-乙酸及其盐和酯。
    • 66. 发明申请
    • Second Generation Fatty Acid Compositions, Formulations, and Methods of Use and Synthesis Thereof
    • 第二代脂肪酸组合物,制剂及其使用和合成方法
    • US20130149378A1
    • 2013-06-13
    • US13761243
    • 2013-02-07
    • Steven C. Quay
    • Steven C. Quay
    • A61K31/164A61K31/353
    • A61K31/202A23L33/12A61K9/0053A61K9/145A61K9/146A61K9/4858A61K9/4866A61K31/16A61K31/164A61K31/353A61K31/355
    • An orally administered fatty acid composition for the treatment of cardiovascular diseases, and a method of treating same, are provided. The compound includes 5Z,8Z,11Z,14Z,17Z-eicosapentaenoic ethanolamide (EPA ethanolamide), 4Z,7Z,10Z,13Z,16Z,19Z-docosahexaenoic ethanolamide (DHA ethanolamide), and at least one tocotrienol. The EPA ethanolamide and the DHA ethanolamide are preferably each substantially in a range of 100-900 mg per dosage form. The at least one tocotrienol is substantially in a range of 10-500 mg per dosage form. The at least one tocotrienol includes at least one of α-tocotrienol, β-tocotrienol, γ-tocotrienol, or δ-tocotrienol and is preferably substantially tocopherol-free. The composition may take the form of a medical food or a pharmaceutical preparation. A preferred formulation of the composition includes approximately 525 mg EPA ethanolamide, approximately 315 mg DHA ethanolamide, and approximately 50 mg δ-tocotrienol. The EPA and DHA ethanolamides may be synthesized from fatty acid triglycerides.
    • 提供了用于治疗心血管疾病的口服给药脂肪酸组合物及其治疗方法。 该化合物包括5Z,8Z,11Z,14Z,17Z-二十碳五烯酸乙醇酰胺(EPA乙醇酰胺),4Z,7Z,10Z,13Z,16Z,19Z-二十二碳六烯酸乙醇酰胺(DHA乙醇酰胺)和至少一种生育三烯酚。 EPA乙醇酰胺和DHA乙醇酰胺优选地每个剂型基本上在100-900mg的范围内。 至少一种生育三烯酚基本上在每种剂型10-500mg的范围内。 至少一种生育三烯酚包括α-生育三烯酚,β-生育三烯酚,γ-生育三烯酚或δ-生育三烯酚中的至少一种,并且优选基本上不含生育酚。 组合物可以采取医疗食品或药物制剂的形式。 组合物的优选制剂包括约525mg EPA乙醇酰胺,约315mg DHA乙醇酰胺和约50mgδ-生育三烯酚。 EPA和DHA乙醇酰胺可以由脂肪酸甘油三酯合成。
    • 68. 发明申请
    • Second Generation Fatty Acid Compositions, Formulations, and Methods of Use and Synthesis Thereof
    • 第二代脂肪酸组合物,制剂及其使用和合成方法
    • US20110033531A1
    • 2011-02-10
    • US12852620
    • 2010-08-09
    • Steven C. Quay
    • Steven C. Quay
    • A61K9/48A61K31/355A61P9/00A61P9/10A61P9/12A61P3/06
    • A61K31/202A23L33/12A61K9/0053A61K9/145A61K9/146A61K9/4858A61K9/4866A61K31/16A61K31/164A61K31/353A61K31/355
    • An orally administered fatty acid composition for the treatment of cardiovascular diseases, and a method of treating same, are provided. The compound includes 5Z,8Z,11Z,14Z,17Z-eicosapentaenoic ethanolamide (EPA ethanolamide), 4Z,7Z,10Z,13Z,16Z,19Z-docosahexaenoic ethanolamide (DHA ethanolamide), and at least one tocotrienol. The EPA ethanolamide and the DHA ethanolamide are preferably each substantially in a range of 100-900 mg per dosage form. The at least one tocotrienol is substantially in a range of 10-500 mg per dosage form. The at least one tocotrienol includes at least one of α-tocotrienol, β-tocotrienol, γ-tocotrienol, or δ-tocotrienol and is preferably substantially tocopherol-free. The composition may take the form of a medical food or a pharmaceutical preparation. A preferred formulation of the composition includes approximately 525 mg EPA ethanolamide, approximately 315 mg DHA ethanolamide, and approximately 50 mg δ-tocotrienol. The EPA and DHA ethanolamides may be synthesized from fatty acid triglycerides.
    • 提供了用于治疗心血管疾病的口服给药脂肪酸组合物及其治疗方法。 该化合物包括5Z,8Z,11Z,14Z,17Z-二十碳五烯酸乙醇酰胺(EPA乙醇酰胺),4Z,7Z,10Z,13Z,16Z,19Z-二十二碳六烯酸乙醇酰胺(DHA乙醇酰胺)和至少一种生育三烯酚。 EPA乙醇酰胺和DHA乙醇酰胺优选地每个剂型基本上在100-900mg的范围内。 至少一种生育三烯酚基本上在每种剂型10-500mg的范围内。 至少一种生育三烯酚包括α-生育三烯酚,生育三烯酚,γ-生育三烯酚或δ-生育三烯酚中的至少一种,优选基本上不含生育酚。 组合物可以采取医疗食品或药物制剂的形式。 组合物的优选制剂包括约525mg EPA乙醇酰胺,约315mg DHA乙醇酰胺和约50mgδ-生育三烯酚。 EPA和DHA乙醇酰胺可以由脂肪酸甘油三酯合成。
    • 69. 发明授权
    • Cyanocobalamin low viscosity aqueous formulations for intranasal delivery
    • 用于鼻内给药的氰钴胺素低粘度含水制剂
    • US07879349B2
    • 2011-02-01
    • US12079875
    • 2008-03-27
    • Steven C. QuayPeter C. AprileZenaida O. GoAnthony P. Sileno
    • Steven C. QuayPeter C. AprileZenaida O. GoAnthony P. Sileno
    • A61F13/00C07H23/00A61K31/70
    • A61K9/0043A61K9/08A61K31/7056A61K31/714A61K47/10A61K47/12A61K47/186
    • A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.
    • 一种由氰钴胺素和水组成的稳定的药用无汞水溶液,其中所述氰钴胺溶液适合于鼻内给药,其粘度小于约1000cPs,其中所述氰钴胺溶液在鼻内给药时具有氰钴胺素的生物利用度 相对于肌内注射氰钴胺素至少约7%,条件是溶液基本上不含汞和含汞化合物。 本发明还涉及提高脑脊髓液(CSF)中维生素B12水平的方法,其包括向鼻内施用足够量的无汞氰钴胺溶液,以增加CSF中维生素B12的平均比例 在血清(B12 CSF / B12血清×100)中至少约1.1,其包括鼻内施用氰钴胺水溶液,其中所述氰钴胺溶液相对于肌内注射氰钴胺素具有至少7%的生物利用度 。