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    METHOD FOR TREATING LIVER DISEASES OF VARIOUS ORIGINS
    1.
    发明申请
    METHOD FOR TREATING LIVER DISEASES OF VARIOUS ORIGINS 审中-公开
    用于治疗各种原始肝脏疾病的方法

    公开(公告)号：US20150158825A1

    公开(公告)日：2015-06-11

    申请号：US14611539

    申请日：2015-02-02

    Applicant: Viktor Veniaminovich Tets ,  Georgy Viktorovich Tets

    Inventor： Georgy Viktorovich TETS ,  Viktor Veniaminovich TETS ,  Konstantin Andreevich KRASNOV

    IPC: C07D239/66

    CPC classification number: A61K31/515 ,  C07D239/66

    Abstract: The invention relates to medicine, in particular to gastroenterology, and lies in the field of treatment of liver diseases of various origins. For this purpose, the hepatoprotective agent that is introduced to the patient is embodied as derivatives of bis(2-thio-4,6-dioxo-1,2,3,4,5,6-hexahydropyrimidine-5-yl) arylmethanes. The method provides reduction of the manifestations of cytolysis under the influence of damaging agents and a statistically significant reduction of dysproteinemia, it accelerates restoration of detoxifying processes of the liver, increases induction of endogenic interferon alfa and, consequently, makes the protection of liver cells during hepatitides of various origins more effective.

    Abstract translation: 本发明涉及药物，特别涉及胃肠病学，并且在于各种来源的肝脏疾病的治疗领域。 为此，引入患者的肝脏保护剂被实施为双（2-硫代-4,6-二氧代-1,2,3,4,5,6-六氢嘧啶-5-基）芳基甲烷的衍生物。 该方法在损伤剂​​的影响下减少细胞溶解的表现，统计学上显着降低血清蛋白血症，加速肝脏解毒过程的恢复，增加内源性干扰素α的诱导，从而使肝细胞保护 各种来源的肝细胞更有效。

    Ultrashort acting hypnotic barbiturates
    3.
    再颁专利
    Ultrashort acting hypnotic barbiturates 失效
    超短效催眠巴比妥类

    公开(公告)号：USRE41289E1

    公开(公告)日：2010-04-27

    申请号：US12009446

    申请日：2007-12-20

    Applicant: Pascal Druzgala ,  Peter G. Milner

    Inventor： Pascal Druzgala ,  Peter G. Milner

    IPC: C07D239/42 ,  C07D239/62 ,  A61K31/505 ,  A61K31/515 ,  A61P25/20

    CPC classification number: C07D239/62 ,  C07D239/66

    Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.

    Abstract translation: 本发明涉及可用作超短效催眠巴比妥酸盐的新型化合物。 具体举例说明的是巴比妥酸和硫代巴比妥酸的衍生物。 它们被血液和组织酶快速代谢，以形成无催眠活性的极性代谢物，并迅速消除。

    Detection of transmembrane potentials by optical methods
    4.
    发明授权
    Detection of transmembrane potentials by optical methods 有权
    通过光学方法检测跨膜电位

    公开(公告)号：US07173130B2

    公开(公告)日：2007-02-06

    申请号：US09967772

    申请日：2001-09-28

    Applicant: Roger Y. Tsien ,  Jesus E. Gonzalez, III

    Inventor： Roger Y. Tsien ,  Jesus E. Gonzalez, III

    IPC: C07D403/06

    CPC classification number: G01N33/502 ,  C07D209/08 ,  C07D215/227 ,  C07D239/60 ,  C07D239/62 ,  C07D239/66 ,  C07D239/80 ,  C07D241/44 ,  C07D265/36 ,  C07D279/16 ,  C07D311/16 ,  C07D487/04 ,  C07F5/003 ,  C07F5/02 ,  C07F5/027 ,  C07F9/10 ,  C07F9/5728 ,  C07K2319/033 ,  C09B23/02 ,  G01N33/5005 ,  G01N33/5008 ,  G01N33/5044 ,  G01N33/5058 ,  G01N33/5061 ,  G01N33/5076 ,  G01N33/52 ,  G01N33/542 ,  G01N33/582 ,  G01N33/6872 ,  G01N33/92 ,  G01N2405/04 ,  G01N2500/10 ,  Y10S436/80 ,  Y10S436/805

    Abstract: Methods and compositions are provided for detecting changes in membrane potential in membranes biological systems. In one aspect, the method comprises; a) providing a living cell with a first reagent comprising a charged hydrophobic molecule which is typically a fluorescence resonance energy transfer (FRET) acceptor or donor, or is a quencher and is capable of redistributing within the membrane of a biological membrane in response to changes in the potential across the membrane; b) providing the cell with a second reagent that can label the first face or the second face of a biological membrane within the cell; c) detecting light emission from the first reagent or the second reagent. One aspect of this method involves monitoring membrane potential changes in subcellular organelle membranes in a living cells.Another aspect of the invention is the use of certain embodiments of the method for the screening of test chemicals for activity to modulate the activity of a target ion channel.Another aspect of the present invention is a transgenic organism comprising a first reagent that comprises a charged hydrophobic fluorescent molecule, and a second reagent comprising a bioluminescent or naturally fluorescent protein.

    Abstract translation: 提供了用于检测膜生物系统中膜电位变化的方法和组合物。 一方面，该方法包括： a）向活细胞提供包含通常为荧光共振能量转移（FRET）受体或供体的带电荷的疏水性分子的第一试剂，或者是猝灭剂，并且能够响应于变化而重新分布在生物膜的膜内 在膜的潜力; b）向细胞提供可以标记细胞内生物膜的第一面或第二面的第二试剂; c）检测来自第一试剂或第二试剂的发光。 该方法的一个方面涉及监测活细胞中亚细胞细胞器膜中的膜电位变化。 本发明的另一方面是该方法的某些实施方案用于筛选测试化学品以调节靶离子通道的活性的活性。 本发明的另一方面是转基因生物，其包含含有带电荷的疏水荧光分子的第一试剂和包含生物发光或天然荧光蛋白的第二试剂。

    N-substituted derivatives of 5-oxyiminobarbituric acid
    5.
    发明授权
    N-substituted derivatives of 5-oxyiminobarbituric acid 失效
    5-氧亚氨基巴比妥酸的N-取代衍生物

    公开(公告)号：US07074925B1

    公开(公告)日：2006-07-11

    申请号：US09701204

    申请日：1998-05-26

    Applicant: Rimma Lliinichna Ashkinazi

    Inventor： Rimma Lliinichna Ashkinazi

    IPC: C07D239/52 ,  A01K31/505 ,  A01P31/22

    CPC classification number: C07D239/66 ,  C07D239/60

    Abstract: N-substituted derivatives of 5-oximinobarbituric add of the general formula where X is sulfur; R1 is selected from the group consisting of saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl; and R2 is selected from the group consisting of hydrogen, saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl possessing a biological activity.

    Abstract translation: 其中X为硫的通式为5-氧亚氨基巴比妥酸的N-取代衍生物; R 1选自饱和或不饱和的烷基，环烷基，芳基和芳基烷基; R 2选自具有生物活性的氢，饱和或不饱和的烷基，环烷基，芳基和芳基烷基。

    Purification of 5-pyrimidinecarboxamides
    7.
    发明授权
    Purification of 5-pyrimidinecarboxamides 失效
    5-嘧啶甲酰胺的纯化

    公开(公告)号：US4845217A

    公开(公告)日：1989-07-04

    申请号：US939373

    申请日：1986-12-08

    Applicant: Arthur D. Brewer

    Inventor： Arthur D. Brewer

    IPC: C07D239/66 ,  C07D239/68

    CPC classification number: C07D239/66 ,  C07D239/68

    Abstract: A process is provided for the purification to highly purified states of 5-pyrimidinecarboxamides which are essentially insoluble in both organic and inorganic solvents. The 5-pyrimidinecarboxamide to be purified is contacted with an organic base having a pKa value in excess of 6.95 to form an adduct. The adduct is purified through recrystallization and the desired 5-pyrimidinecarboxamide is regenerated from the adduct in highly purified form with acid. Additionally, an adduct resulting from the combination of a 5-pyrimidinecarboxamide with such an organic base is provided, which adduct is capable of being purified using recrystallization techniques, where the 5-pyrimidinecarboxamide is not itself capable of being so purified due to its relative insolubility in organic and inorganic solvents.

    Abstract translation: 提供了一种纯化至高度纯化的5-嘧啶甲酰胺的状态的方法，其基本上不溶于有机溶剂和无机溶剂。 待纯化的5-嘧啶甲酰胺与pKa值超过6.95的有机碱接触以形成加合物。 加合物通过重结晶纯化，所需的5-嘧啶甲酰胺由加合物以酸的高纯度形式再生。 另外，提供了由5-嘧啶甲酰胺与这种有机碱的组合产生的加合物，该加合物能够使用重结晶技术纯化，其中5-嘧啶甲酰胺本身不能如此纯化，因为其相对不溶性 在有机和无机溶剂中。

    Thiobarbituric acid derivatives and their use as anthelminthics
    9.
    发明授权
    Thiobarbituric acid derivatives and their use as anthelminthics 失效
    硫代巴比妥酸衍生物及其作为抗凝药物的用途

    公开(公告)号：US4670441A

    公开(公告)日：1987-06-02

    申请号：US751715

    申请日：1985-07-05

    Applicant: Manfred Kuhne ,  Jean J. Gallay

    Inventor： Manfred Kuhne ,  Jean J. Gallay

    IPC: C07D213/64 ,  A61K31/505 ,  A61K31/515 ,  A61P33/10 ,  C07C65/24 ,  C07C265/12 ,  C07D213/643 ,  C07D239/66 ,  C07D401/12 ,  C07D239/68

    CPC classification number: C07D213/643 ,  C07C265/12 ,  C07C65/24 ,  C07D239/66 ,  C07D401/12

    Abstract: The invention relates to novel 5-phenylcarbamoylthiobarbituric acid derivatives of the general formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently C.sub.1 -C.sub.5 alkyl or methoxy,R.sub.3 is unsubstituted phenyl, unsubstituted pyridyl, or phenyl which is substituted by 1 to 3 identical or different members selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 cyanoalkyl, halogen, nitro and C.sub.1 -C.sub.5 haloalkyl containing 1 to 5 halogen atoms, or is pyridyl which is substituted by 1 to 3 identical or different members selected from the group consisting of C.sub.1 -C.sub.5 alkyl, halogen, nitro and C.sub.1 -C.sub.5 haloalkyl containing 1 to 5 halogen atoms andR.sub.4 and R.sub.5 are each independently hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.2 haloalkyl containing 1 to 3 halogen atoms, or are C.sub.1 -C.sub.3 -alkoxy or nitro,and to the tautomers and salts thereof, as anthelmintics.The compounds may be used by themselves or together with suitable carriers and further adjuvants for controlling helminths which are parasites of animals.

    Abstract translation: 本发明涉及通式为：其中R 1和R 2各自独立地为C 1 -C 5烷基或甲氧基，R 3为未取代的苯基，未被取代的吡啶基或被1位取代的苯基的新的5-苯基氨基甲酰硫代巴比妥酸衍生物 至3个选自C 1 -C 5烷基，C 1 -C 4氰基烷基，卤素，硝基和含有1至5个卤原子的C 1 -C 5卤代烷基的相同或不同的成员，或者是被1至3个相同或不同的成员所取代的吡啶基， 由C1-C5烷基，卤素，硝基和含有1-5个卤素原子的C1-C5卤代烷基组成的组，R4和R5各自独立地为氢，卤素，C1-C5烷基，含1-3个卤素原子的C1-C2卤代烷基，或C1- C3-烷氧基或硝基，以及其互变异构体和盐，作为驱肠虫剂。 这些化合物本身或与合适的载体一起使用，以及用于控制作为动物寄生虫的蠕虫的另外的辅助剂。

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