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    Heterocyclic and carbonate derivatives of NDGA and their use as new anti-HIV and anti-cancer agents
    1.
    发明授权
    Heterocyclic and carbonate derivatives of NDGA and their use as new anti-HIV and anti-cancer agents 有权
    NDGA的杂环和碳酸酯衍生物及其作为新型抗HIV和抗癌剂的用途

    公开(公告)号：US08420692B1

    公开(公告)日：2013-04-16

    申请号：US12755077

    申请日：2010-04-06

    申请人： Ru Chih C. Huang ,  Apostolos Gittis ,  Evangelos Moudrianakis ,  Julie A. Dohm ,  Jih Ru Hwu ,  Ming-Hua Hsu

    发明人： Ru Chih C. Huang ,  Apostolos Gittis ,  Evangelos Moudrianakis ,  Julie A. Dohm ,  Jih Ru Hwu ,  Ming-Hua Hsu

    IPC分类号： A01N43/36 ,  A61K31/40

    CPC分类号： C07C69/96 ,  A61K31/09

    摘要： Reaction of nordihydroguaiaretic acid with various alkyl chlorides, 1-piperidinecarbonyl chloride, methyl chloroformate, or 1,1′-carbonyldiimidazole under alkaline conditions produced the corresponding phenol ethers, carbamates and carbonates, respectively, in 67-83% yields (Scheme 1 and Scheme 2). Among these derivatives, the nitrogen-containing compounds were converted to the corresponding hydrochloride salts. Having good solubility, these NDGA derivatives were found to be stable in aqueous solution. These new compounds exerted potent activities against HIV Tat-regulated transactivation in cos-7 cells. The most active transcription inhibitor compound of this series 5b (P4N, Tetrapiperidino NDGA, meso-2,3-dimethyl-1,4-bis(3,4-[2-(piperidino)ethoxypehnyl])butane tetrakishydrochloride salt) has an IC50 of 0.88 μM.

    摘要翻译： 在碱性条件下，二氢愈创木酸与各种烷基氯，1-哌啶羰基氯，氯甲酸甲酯或1,1'-羰基二咪唑的反应分别产生相应的酚醚，氨基甲酸酯和碳酸酯，产率为67-83％（方案1和方案 2）。 在这些衍生物中，将含氮化合物转化为相应的盐酸盐。 发现这些NDGA衍生物具有良好的溶解性，在水溶液中是稳定的。 这些新化合物对cos-7细胞中的HIV Tat调节的反式激活起到了有效的作用。 该系列5b（P4N，四哌啶基-NOGA，内消旋-2,3-二甲基-1,4-双（3,4- [2-（哌啶子基）乙氧基]苯基]）丁烷四盐酸盐的最活跃的转录抑制剂化合物具有IC 50 为0.88μM。

    PHOSPHATE-CONTAINING NANOPARTICLE DELIVERY VEHICLE
    2.
    发明申请
    PHOSPHATE-CONTAINING NANOPARTICLE DELIVERY VEHICLE 审中-公开
    含磷酸盐的纳米粒子交付车辆

    公开(公告)号：US20110077414A1

    公开(公告)日：2011-03-31

    申请号：US12686996

    申请日：2010-01-13

    申请人： Jih-Ru Hwu ,  Yu-Sern Lin ,  Chen-Sheng Yeh ,  Dar-Bin Shieh

    发明人： Jih-Ru Hwu ,  Yu-Sern Lin ,  Chen-Sheng Yeh ,  Dar-Bin Shieh

    IPC分类号： C07D305/14

    CPC分类号： C07F9/65512 ,  A61K47/6923

    摘要： A phosphate-containing nanoparticle delivery vehicle includes a nanoparticle, an active ingredient, and a phosphodiester moiety connecting the nanoparticle and the active ingredient and forms a prodrug. The nanoparticle delivery vehicle achieves the function of increasing hydrophilicity of the active ingredient and specificity against tumor cells. Advantages of the nanoparticle material include biocompatibility, magnetism and/or controllable drug release.

    摘要翻译： 含磷酸盐的纳米颗粒递送载体包括连接纳米颗粒和活性成分并形成前药的纳米颗粒，活性成分和磷酸二酯部分。 纳米颗粒递送载体实现增加活性成分的亲水性和对肿瘤细胞的特异性的功能。 纳米颗粒材料的优点包括生物相容性，磁性和/或可控制的药物释放。

    ANTI-BACTERIAL, ANTI-VIRUS, AND ANTI-FUNGUS COMPOSITION, ITS PREPARATION AND USE
    3.
    发明申请
    ANTI-BACTERIAL, ANTI-VIRUS, AND ANTI-FUNGUS COMPOSITION, ITS PREPARATION AND USE 有权
    抗菌，抗病毒和抗真菌组合物，其制备和使用

    公开(公告)号：US20090098098A1

    公开(公告)日：2009-04-16

    申请号：US12240755

    申请日：2008-09-29

    申请人： Jih-Ru Hwu ,  Shwu-Chen Tsay

    发明人： Jih-Ru Hwu ,  Shwu-Chen Tsay

    IPC分类号： A01N59/20 ,  A01N59/16 ,  A01N55/02 ,  A01N43/14 ,  A01P1/00 ,  A01P3/00

    CPC分类号： A61L2/22 ,  A61K31/28 ,  A61K33/24 ,  A61K45/06 ,  A61L2/186 ,  A61K2300/00

    摘要： The present invention relates to an anti-bacterial, anti-virus, and anti-fungus composition, its preparation and use. The composition of the present invention mainly includes the following three ingredients in an adequate ratio: (A) a metal compound having a catalytic function; (B) a mixture of a coenzyme having reducing ability and quinones, and (C) an additive. The anti-bacterial, anti-virus, and anti-fungus composition of the present invention is capable of destroying viruses as well as killing bacterial and fungi. Therefore, the composition can be formulated as an aerosol and a film for applying to protection devices such as respirators, masks, gloves, filters, condoms, etc. The present composition can also be used in household, vehicle, hospital, school, restaurant, hotel, internet coffee shop for applying to filter of air-conditioner, tap, stool, interior of elevator and its keyboard. Additionally, the present composition can be applied to human being such as applying to hand, foot, genital organs, oral cavity, and the like in a lower dose to attain the effect of destroying of bacteria, viruses, and fungi.

    摘要翻译： 本发明涉及抗菌，抗病毒和抗真菌组合物，其制备和应用。 本发明的组合物主要包括足够比例的以下三种成分：（A）具有催化功能的金属化合物; （B）具有还原能力的辅酶和醌类的混合物，和（C）添加剂。 本发明的抗细菌，抗病毒和抗真菌组合物能够破坏病毒以及杀死细菌和真菌。 因此，该组合物可以配制成用于应用于诸如呼吸器，面罩，手套，过滤器，避孕套等保护装置的气雾剂和膜。本发明组合物还可以用于家庭，车辆，医院，学校，餐厅， 酒店，互联网咖啡店，适用于空调，水龙头，凳子，电梯内部及其键盘。 此外，本发明的组合物可以以较低剂量施用于人，例如施用于手，脚，生殖器，口腔等，以达到破坏细菌，病毒和真菌的效果。

    Compositions counteracting pesticides and malodorants
    4.
    发明申请
    Compositions counteracting pesticides and malodorants 有权
    防止农药和恶臭的组合物

    公开(公告)号：US20080234158A1

    公开(公告)日：2008-09-25

    申请号：US11726703

    申请日：2007-03-22

    申请人： Jih Ru Hwu ,  Shwu-Chen Tsay

    发明人： Jih Ru Hwu ,  Shwu-Chen Tsay

    IPC分类号： A62D3/30 ,  A62D101/04

    CPC分类号： A62D3/38 ,  A61L9/01 ,  A62D2101/04 ,  Y10S71/903

    摘要： This invention relates to compositions that counteract chemicals such as pesticides and malodorants. Also disclosed are a method for preparing such compositions and a method for applying such compositions to counteract pesticides or malordorants.

    摘要翻译： 本发明涉及抵抗诸如杀虫剂和恶臭剂的化学物质的组合物。 还公开了制备这种组合物的方法以及用于施用这样的组合物以抵抗农药或恶臭剂的方法。

    Anti-bacterial, anti-viral, and anti-fungus composition, its preparation and use
    5.
    发明授权
    Anti-bacterial, anti-viral, and anti-fungus composition, its preparation and use 有权
    抗菌，抗病毒和抗真菌组成，其制备和使用

    公开(公告)号：US07387799B2

    公开(公告)日：2008-06-17

    申请号：US10628259

    申请日：2003-07-29

    申请人： Jih-Ru Hwu ,  Shwu-Chen Tsay

    发明人： Jih-Ru Hwu ,  Shwu-Chen Tsay

    IPC分类号： A01N59/00 ,  A01N59/08 ,  A01N59/16 ,  A01N55/02 ,  A61K33/26 ,  A61K33/30 ,  A61K33/00 ,  A61K31/295 ,  A61K31/315 ,  A61K33/24

    CPC分类号： A61L2/22 ,  A61K31/28 ,  A61K33/24 ,  A61K45/06 ,  A61L2/186 ,  A61K2300/00

    摘要： The present invention relates to an anti-bacterial, anti-viral, and anti-fungus composition, its preparation and use. The composition of the present invention mainly includes the following three ingredients in an adequate ratio: (A) a metal compound having catalytic function; (B) ionic compound, and (C) an additive. The anti-bacterial, anti-virus, and anti-fungus composition of the present invention is capable of destroying viruses as well as killing bacterial and fungi. Therefore, the composition can be formulated as an aerosol and a film for applying to protection devices such as respirators, masks, gloves, filters, condoms, etc. The present composition can also be used in household, vehicle, hospital, school, restaurant, hotel, internet coffee shop for applying to filter of air-conditioner, tap, stool, interior of elevator and its keyboard. Additionally, the present composition can be applied to human being such as applying to hand, foot, genital organs, oral cavity, and the like in a lower dose to attain the effect of destroying bacteria, viruses, and fungi.

    摘要翻译： 本发明涉及抗细菌，抗病毒和抗真菌组合物，其制备和应用。 本发明的组合物主要包括以下三种成分：（A）具有催化功能的金属化合物; （B）离子化合物，（C）添加剂。 本发明的抗细菌，抗病毒和抗真菌组合物能够破坏病毒以及杀死细菌和真菌。 因此，该组合物可以配制成用于应用于诸如呼吸器，面罩，手套，过滤器，避孕套等保护装置的气雾剂和膜。本发明组合物还可以用于家庭，车辆，医院，学校，餐厅， 酒店，互联网咖啡店，适用于空调，水龙头，凳子，电梯内部及其键盘。 此外，本发明的组合物可以以较低剂量施用于人体，例如施用于手，脚，生殖器，口腔等，以达到破坏细菌，病毒和真菌的效果。

    Anti-bacterial, anti-virus, and anti-fungus composition, its preparation and use
    6.
    发明申请
    Anti-bacterial, anti-virus, and anti-fungus composition, its preparation and use 审中-公开
    抗菌，抗病毒，抗真菌组成，其制备及用途

    公开(公告)号：US20060246148A1

    公开(公告)日：2006-11-02

    申请号：US11344235

    申请日：2006-02-01

    申请人： Jih-Ru Hwu ,  Shwu-Chen Tsay

    发明人： Jih-Ru Hwu ,  Shwu-Chen Tsay

    IPC分类号： A61K38/43 ,  A61K31/28 ,  A61K31/315 ,  A61K33/42 ,  A61K33/40 ,  A61K33/24 ,  A61K33/26 ,  A61K31/12

    CPC分类号： A61K31/12 ,  A01N59/16 ,  A01N59/20 ,  A61K31/28 ,  A61K31/315 ,  A61K31/7084 ,  A61K33/00 ,  A61K33/24 ,  A61K33/40 ,  A61K45/06 ,  C11D3/38654 ,  C11D3/3947 ,  C11D3/48 ,  C11D7/10 ,  A01N57/16 ,  A01N59/00 ,  A01N59/02 ,  A01N59/04 ,  A01N59/06 ,  A01N59/08 ,  A01N59/26 ,  A01N61/00 ,  A01N2300/00

    摘要： The present invention relates to an anti-bacterial, anti-virus, and anti-fungus composition, its preparation and use. The composition of the present invention mainly includes the following three ingredients in an adequate ratio: (A) a metal compound having a catalytic function; (B) a mixture of a coenzyme having reducing ability and an agent having oxidizing ability; and (C) an additive. The anti-bacterial, anti-virus, and anti-fungus composition of the present invention is capable of destroying viruses as well as killing bacterial and fungi. Therefore, the composition can be formulated as an aerosol and a film for applying to protection devices such as respirators, masks, gloves, filters, condoms, etc. The present composition can also be used in household, vehicle, hospital, school, restaurant, hotel, internet coffee shop for applying to filter of air-conditioner, tap, stool, interior of elevator and its keyboard. Additionally, the present composition can be applied to human being such as applying to hand, foot, genital organs, oral cavity, and the like in a lower dose to attain the effect of destroying of bacteria, viruses, and fungi.

    摘要翻译： 本发明涉及抗菌，抗病毒和抗真菌组合物，其制备和应用。 本发明的组合物主要包括足够比例的以下三种成分：（A）具有催化功能的金属化合物; （B）具有还原能力的辅酶和具有氧化能力的试剂的混合物; 和（C）添加剂。 本发明的抗细菌，抗病毒和抗真菌组合物能够破坏病毒以及杀死细菌和真菌。 因此，该组合物可以配制成用于应用于诸如呼吸器，面罩，手套，过滤器，避孕套等保护装置的气雾剂和膜。本发明组合物还可以用于家庭，车辆，医院，学校，餐厅， 酒店，互联网咖啡店，适用于空调，水龙头，凳子，电梯内部及其键盘。 此外，本发明的组合物可以以较低剂量施用于人，例如施用于手，脚，生殖器，口腔等，以达到破坏细菌，病毒和真菌的效果。

    Thymidylate analogs and the use thereof
    9.
    发明授权
    Thymidylate analogs and the use thereof 失效
    胸苷酸类似物及其应用

    公开(公告)号：US5760013A

    公开(公告)日：1998-06-02

    申请号：US700795

    申请日：1996-08-21

    申请人： Jih Ru Hwu ,  Gholam H. Hakimelahi ,  Shwu-Chen Tsay

    发明人： Jih Ru Hwu ,  Gholam H. Hakimelahi ,  Shwu-Chen Tsay

    IPC分类号： C07H19/10 ,  C07H21/00 ,  A61K31/70

    CPC分类号： C07H19/10 ,  C07H21/00 ,  Y10S514/885

    摘要： Novel thymidylate analogs having the following formula are synthesized in the present invention, which are found active against human immunodeficiency virus type 1 (HIV-1): ##STR1## wherein R.sup.1 is hydrogen, cyano (--CN), halogen or azido (--N.sub.3); R.sup.2 is hydroxyl or an amino ester radical having a formula of --NHR.sup.4 COOR.sup.5, wherein R.sup.4 is a bivalent C.sub.1 -C.sub.4 saturated hydrocarbon and R.sup.5 is C.sub.1 -C.sub.4 alkyl; Me is methyl; and R.sup.3 is hydroxyl or thymidinyl having a formula as follows: ##STR2##

    摘要翻译： 具有下式的新型胸苷酸类似物在本发明中合成，其被发现对人类免疫缺陷病毒1型（HIV-1）具有活性：其中R 1是氢，氰基（-CN），卤素或叠氮基（-N 3 ）; R2是羟基或具有式-NHR4COOR5的氨基酯基，其中R4是二价C1-C4饱和烃，R5是C1-C4烷基; 我是甲基; 并且R3是具有如下公式的羟基或胸腺嘧啶：