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101. 发明申请

US20110105437A1 Mitochondrially Delivered Anti-Cancer Compounds 有权
标题翻译：线粒体交付抗癌化合物
公开(公告)号：US20110105437A1
公开(公告)日：2011-05-05
申请号：US12922525
申请日：2009-03-16
申请人： Stephen John Ralph , Jiri Neuzil
发明人： Stephen John Ralph , Jiri Neuzil
IPC分类号： A61K31/665 , C07F9/655 , C12N5/09 , A61P35/00
CPC分类号： C07F9/65522 , A61K31/355 , A61K47/54 , A61K47/551 , C07D311/72
摘要： This invention relates to anti-cancer compounds and to methods for treating or preventing cancer. In one aspect the invention concerns mitochondrially delivered pro-oxidant anti-cancer compounds that generate reactive oxygen species and induce apoptosis of cancerous cells. The delivery moiety can be a lipophilic cation and the pro-oxidant vitamin E analogue, such as α-tocopheryl succinate, α-tocopheryl maleate, α-tocopheryl maleyl amide, or 2,5,7,8-tetramethyl-2R-(4R,8R,12-trimethyltridecyl)-chroman-6-yloxyacetic acid (α-tocopheryloxyacetic acid).
摘要翻译：本发明涉及抗癌化合物以及治疗或预防癌症的方法。一方面，本发明涉及产生活性氧物质并诱导癌细胞凋亡的线粒体递送的促氧化剂抗癌化合物。递送部分可以是亲脂性阳离子和促氧化维生素E类似物，例如琥珀酸α-生育酚酯，马来酸α-生育酚酯，α-生育酚基马来酰胺酰胺或2,5,7,8-四甲基-2R-（4R ，8R，12-三甲基十三烷基） - 苯并二氢吡喃-6-基氧基乙酸（α-生育酚乙酸）。

102. 发明申请

US20100204183A1 Substituted Phosphonates and Their Use In Decreasing Amyloid Aggregates 失效
标题翻译：取代的膦酸酯及其在降低淀粉样蛋白聚集体中的应用
公开(公告)号：US20100204183A1
公开(公告)日：2010-08-12
申请号：US12598510
申请日：2008-05-02
申请人： Alice Sullivan , Adina Michael-Titus , Lesley Robson
发明人： Alice Sullivan , Adina Michael-Titus , Lesley Robson
IPC分类号： A61K31/662 , C07F9/655 , C07F9/6506 , C07F9/60 , C07F9/40 , A61K31/665 , A61K31/675 , A61P25/28
CPC分类号： C07F9/65522 , A61K31/662 , A61K31/665 , A61K31/675 , C07F9/4006 , C07F9/4056 , C07F9/5728 , C07F9/60 , C07F9/64 , C07F9/65068 , C07F9/65324 , C07F9/6561
摘要： The invention relates to novel and known substituted phosphonates for use in ameliorating amyloid aggregates, particularly for use in the treatment of Alzheimer's disease.
摘要翻译：本发明涉及用于改善淀粉样蛋白聚集体的新型和已知的取代膦酸盐，特别是用于治疗阿尔茨海默氏病。

103. 发明申请

US20100168422A1 METHODS AND INTERMEDIATES USEFUL IN THE SYNTHESIS OF HEXAHYDROFURO [2,3-B]FURAN-3-OL 审中-公开
标题翻译：合成十六氢呋喃[2,3-B] FURAN-3-OL的方法和中间体
公开(公告)号：US20100168422A1
公开(公告)日：2010-07-01
申请号：US12345838
申请日：2008-12-30
申请人： Weiping Chen
发明人： Weiping Chen
IPC分类号： C07D413/14 , C07D493/04 , C07D307/32 , C07D265/30 , C07C291/04 , C07D417/14 , C07F9/655
CPC分类号： C07D295/088 , C07C239/12 , C07D307/33 , C07D493/04 , C07F9/4006 , C07F9/6561
摘要： Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.
摘要翻译：本文提供了可用于制备六氢呋喃并[2,3-b]呋喃-3-醇的化合物和方法。六氢呋喃并[2,3-b]呋喃-3-醇可以从容易获得的起始原料四步高效地合成。

104. 发明申请

US20090227805A1 Axially Asymmetric Phosphorus Compound and Production Method Thereof 审中-公开
标题翻译：轴向不对称磷化合物及其制备方法
公开(公告)号：US20090227805A1
公开(公告)日：2009-09-10
申请号：US12396751
申请日：2009-03-03
申请人： Ken Tanaka , Goushi Nishida , Tohru Yokozawa , Yukinori Yusa
发明人： Ken Tanaka , Goushi Nishida , Tohru Yokozawa , Yukinori Yusa
IPC分类号： C07F9/655
CPC分类号： C07F9/5027 , C07F9/5059 , C07F9/65517
摘要： Problem to be Solved: To provide an axially asymmetric optically active biarylphosphorus compound that can easily produced without the step of optical resolution which was almost indispensable in conventional methods. Solution: A method for producing an axially asymmetric phosphorus compound represented by the general formula (1), comprising a cycloaddition reaction of a compound having a triple bond with the use of a catalyst containing rhodium metal and an optically active bisphosphine. (In the formula, J is an oxygen atom, a sulfur atom or BH3; R1 and R2 independently are an alkyl, cycloalkyl, aryl, alkoxy and aryloxy group; a1 and a2 independently are 0 or 1; R3 to R10 independently are an alkyl, cycloalkyl, aryl, alkoxy and aryloxy group; two among R3 to R10 may form a ring; and * is axial asymmetry.)
摘要翻译：要解决的问题：提供一种轴向不对称光学活性联芳基磷化合物，其可以容易地在没有光学拆分步骤的情况下产生，这在常规方法中几乎不可缺少。溶液：用于制备由通式（1）表示的轴向不对称磷化合物的方法，其包括使用含铑金属和光学活性双膦的催化剂的具有三重键的化合物的环加成反应。（式中，J为氧原子，硫原子或BH 3; R1和R2分别独立地为烷基，环烷基，芳基，烷氧基和芳氧基; a1和a2独立地为0或1; R3至R10独立地为烷基，环烷基，芳基，烷氧基和芳氧基; R3至R10中的两个可以形成环; *是轴不对称的）

105. 发明申请

US20090163725A1 PHOSPHONIC ACID DIESTER DERIVATIVE AND METHOD FOR PRODUCING THEREOF 有权
标题翻译：磷酸二氢钙衍生物及其生产方法
公开(公告)号：US20090163725A1
公开(公告)日：2009-06-25
申请号：US12096321
申请日：2006-11-30
申请人： Jun Hiratake , Kanzo Sakata , Liyou Han
发明人： Jun Hiratake , Kanzo Sakata , Liyou Han
IPC分类号： C07F9/40 , C07F9/655
CPC分类号： C07F9/3808 , C07F9/4046 , C07F9/405 , C07F9/4084 , C07F9/5765 , C07F9/65522
摘要： A phosphonic acid diester derivative represented by the following general formula (1): wherein at least one of R1 and R2 denotes a leaving group.
摘要翻译：由以下通式（1）表示的膦酸二酯衍生物：其中R1和R2中的至少一个表示离去基团。

106. 发明申请

US20080318901A1 Novel Lysophosphatidic Acid Receptor Selective Antagonists 有权
标题翻译：新型溶血磷脂酸受体选择性拮抗剂
公开(公告)号：US20080318901A1
公开(公告)日：2008-12-25
申请号：US11579658
申请日：2005-05-06
申请人： Kevin R. Lynch , Timothy L. Macdonald , Brian H. Heasley
发明人： Kevin R. Lynch , Timothy L. Macdonald , Brian H. Heasley
IPC分类号： A61K31/661 , C07F9/08 , C07F9/572 , A61K31/665 , A61P17/02 , A61K31/675 , C07F9/6506 , C07F9/655
CPC分类号： C07F9/65515 , C07F9/091 , C07F9/094 , C07F9/3891 , C07F9/404 , C07F9/5728 , C07F9/58 , C07F9/6506
摘要： The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
摘要翻译：本发明涉及包含溶血磷脂酸类似物的组合物和使用此类类似物作为LPA受体活性的激动剂或拮抗剂的方法。此外，本发明涉及LPA受体激动剂，其在各个LPA受体（即LPA1，LPA2和LPA3）上的选择度变化。更具体地说，本发明涉及LPA类似物，其中甘油被乙醇胺替代，并且多种取代已经在第二个碳原子连接。

107. 发明申请

US20080249067A1 Organophosphorous Compounds for the Activation of Gamma/Delta T Cells 失效
标题翻译：用于激活γ/ T细胞的有机磷化合物
公开(公告)号：US20080249067A1
公开(公告)日：2008-10-09
申请号：US12137241
申请日：2008-06-11
申请人： Hassan Jomaa , Matthias Eberl , Boran Altincicek , Martin Hintz , Oliver Wolf , Ann-Kristin Kollas , Armin Reichenberg , Jochen Wiesner
发明人： Hassan Jomaa , Matthias Eberl , Boran Altincicek , Martin Hintz , Oliver Wolf , Ann-Kristin Kollas , Armin Reichenberg , Jochen Wiesner
IPC分类号： A61K31/665 , C07F9/655 , C07F9/06 , A61K31/663 , C12N5/06 , A01N57/16 , A61P33/00 , A01P13/00 , A61P31/04 , A61P31/12
CPC分类号： C07F9/65746 , A61K31/661 , C07F9/098 , C07F9/3821 , C07F9/3826 , C07F9/4025
摘要： The present invention describes organophosphorus compounds of general formula (I) their preparation and their uses in the activation of gamma/delta T-cells, in the screening of GcpE and LytB enzyme inhibitors and in the prophylaxis and treatment of diseases in humans and animals.
摘要翻译：本发明描述了在筛选GcpE和LytB酶抑制剂以及预防和治疗人和动物疾病中通式（I）的有机磷化合物及其制备方法及其在γ/δT细胞活化中的用途。

108. 发明申请

US20080207887A1 PHOSPHONYLATED FLUORESCENT DYES AND CONJUGATES 审中-公开
标题翻译：磷酸荧光染色和结合
公开(公告)号：US20080207887A1
公开(公告)日：2008-08-28
申请号：US11937448
申请日：2007-11-08
申请人： Eugeny Lukhtanov , Alexei Vorobiev
发明人： Eugeny Lukhtanov , Alexei Vorobiev
IPC分类号： C07H21/04 , C07F9/655 , C07F9/6533 , C07F9/572
CPC分类号： C07F9/1411 , C07F9/5728 , C07F9/5765 , C07F9/58 , C07F9/6533 , C07F9/65335 , C07F9/6541 , C07F9/6547 , C07F9/65522 , C07F9/65583 , C07F9/65586 , C07F9/6561 , C07F9/65842 , C09B11/24 , C09B15/00 , C09B57/00
摘要： Reagents are provided for the introduction of phosphonate groups into fluorescent dyes. Methods are also provided for preparing dye conjugates.
摘要翻译：提供试剂以将膦酸酯基团引入荧光染料中。还提供了制备染料缀合物的方法。

109. 发明申请

US20080132713A1 Probe for measuring phytase activity 有权
公开(公告)号：US20080132713A1
公开(公告)日：2008-06-05
申请号：US11982811
申请日：2007-11-05
申请人： David A. Berry
发明人： David A. Berry
IPC分类号： C07F9/28 , C07F9/655
CPC分类号： C07F9/117 , C12Q1/42 , Y02P20/55
摘要： A myo-inositol derivative: R1, R2, R3 and R4 are identical, being selected from PO3H2, PO3Na2, PO3K2, PO3Li2, PO3Ca, PO3Mg, PO3(NH4)2, PO3(RNH3)2, PO3(R2NH2)2, PO3(R4N)2, PO(OR)2, H, COZ and BHPP, where R is benzyl or alkyl of 1 to 6 carbon atoms and Z is an alkyl or arylalky group providing a cleavable protecting group; R5 is one of H, benzyl, 4-methoxybenzyl, COZ, PO3H2, PO3Na2, PO3K2, PO3Li2, PO3Ca, PO3Mg, PO3(NH4)2, PO3(RNH3)2, PO3(R2NH2)2, PO3(R4N)2, PO(OR)2, and BHPP, where R is benzyl or alkyl of 1 to 6 carbon atoms and Z is an alkyl or arylalky group providing a cleavable protecting group; X is one of CH2, CH2CH2O, and CH2CH2CH2O; n is an integer from 1 to 8; L1 is a single bond or CH2; L2 is one of a single bond, CONH, CH2CONH, CH2CH2CONH, CH2CH2NHCO, CH2CH2NHCONH, CH2CH2NHCSNH, CH2CH2NHSO2, CH2CH2CH2NHCO, CH2CH2CH2NHCONH, CH2CH2CH2NHCSNH, CH2CH2CH2NHSO2, NHCO, NHCONH, NHCSNH, OCONH, CH2, CH2CH2, CH2CH2O, CH2CH2S, CH2CH2NH, CH2CH2CH2, CH2CH2CH2O, CH2CH2CH2S, CH2CH2CH2NH, and NH—SO2; and R6 is a UV-visible chromophore, a UV-chromophore, a fluorescent moiety, or a radiolabeled moiety.

110. 发明申请

US20070027116A1 Therapeutic phosphonate derivatives 审中-公开
标题翻译：治疗性膦酸酯衍生物
公开(公告)号：US20070027116A1
公开(公告)日：2007-02-01
申请号：US11406750
申请日：2006-04-19
申请人： Aesop Cho , Thorsten Kirschberg , William Watkins , Maria Fardis , Lee Chong
发明人： Aesop Cho , Thorsten Kirschberg , William Watkins , Maria Fardis , Lee Chong
IPC分类号： A61K31/665 , C07F9/655
CPC分类号： C07D307/88 , A61K47/548 , C07F9/65517 , C07F9/65586
摘要： Phosphorus substituted mycophenolate derivatives with anti-cancer, anti-viral, anti-inflammatory and anti-tissue/organ transplant rejection properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit tumor growth, viral growth, inflammation, and tissue/organ transplant rejection and/or are useful therapeutically for the treatment or prevention of cancer, viral infection, inflammation and tissue/organ transplant rejection, as well as in assays for the detection of cancer, viral infection, inflammation and tissue/organ transplant rejection.
摘要翻译：公开了具有用作治疗剂和用于其它工业目的的抗癌，抗病毒，抗炎和抗组织/器官移植排斥物质的磷取代的霉酚酸衍生物。组合物抑制肿瘤生长，病毒生长，炎症和组织/器官移植排斥和/或治疗用于治疗或预防癌症，病毒感染，炎症和组织/器官移植排斥以及用于检测的检测癌症，病毒感染，炎症和组织/器官移植排斥。

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