Modulators of Preripheral 5-Ht Receptors
    91.
    发明申请
    Modulators of Preripheral 5-Ht Receptors 有权
    Preripheral 5-Ht受体的调节剂

    公开(公告)号:US20070254874A1

    公开(公告)日:2007-11-01

    申请号:US10583829

    申请日:2004-12-23

    摘要: Novel modulators of 5-HT4 receptors have been developed which have a selectivity for peripheral receptors rather than those of the central nervous systems. Theses include novel derivatives of known modulators as well as entirely novel entities. Surprisingly, the derivatised compounds of the known modulators maintain a high binding affinity to 5-HT4 receptors, despite the presence of an acidic moiety at the end of an optional chain. The entirely novel entities also exhibit good binding affinity to 5-HT4 receptors. All of the compounds of the invention have a common motif which includes a basic nitrogen moiety and an acidic moiety. The compounds of the invention, due at least in part to their high ionisation potential at physiological pH, have the unique properties of selectively for peripheral 5HT4 receptors over those of the CNS, good binding affinity, and selectively of 5HT4 receptors over other serotonin receptors.

    摘要翻译: 已经开发了具有对外周受体而不是中枢神经系统的选择性的5-HT 4受体的新型调节剂。 论文包括已知调制剂的新型衍生物以及完全新颖的实体。 令人惊奇的是,尽管已知调节剂的衍生化合物在任选链的末端存在酸性部分,但仍保持与5-HT 4受体的高结合亲和力。 完全新颖的实体也表现出对5-HT4受体的良好的结合亲和力。 本发明的所有化合物都具有共同的基序,其包括碱性氮部分和酸性部分。 本发明的化合物至少部分地由于其在生理pH下的高电离电位具有对于周围5HT4受体的选择性优于CNS的那些的独特性质,良好的结合亲和力以及5HT4受体的选择性超过其他5-羟色胺受体。

    Pyrazolidinol compounds
    92.
    发明申请
    Pyrazolidinol compounds 审中-公开
    吡唑啉醇化合物

    公开(公告)号:US20070037772A1

    公开(公告)日:2007-02-15

    申请号:US11371226

    申请日:2006-03-09

    摘要: The invention provides the use of an optionally hydroxyl-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in drug therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient.

    摘要翻译: 本发明提供任选羟基保护的4-羟基或氢过氧-3,5-二氧杂吡唑烷或其等价物,其中连接有吡唑烷环的氧被硫或其生理上可接受的盐替代,用于制备药物 用于药物治疗或预防。 另外,本发明提供了一种抗艾滋病毒感染的方法,其包括以足以抑制所述患者的T淋巴细胞生长的量向HIV感染的患者施用T淋巴细胞生长抑制剂,优选吡唑烷醇,时间足以 降低患者淋巴结中的T淋巴细胞浓度。

    Peroxide compositions
    94.
    发明申请
    Peroxide compositions 审中-公开
    过氧化物组成

    公开(公告)号:US20060161121A1

    公开(公告)日:2006-07-20

    申请号:US10544362

    申请日:2004-02-06

    IPC分类号: A61M35/00

    CPC分类号: A61Q19/02 A61K8/22

    摘要: A kit comprising: a sealed container containing a ready-to-use skin bleaching composition including an emulsion containing 2 to 6% wt of a peroxide bleaching agent selected from hydrogen peroxide, organic peracids and salts thereof, hydrogen peroxide adducts, and metal peroxides, percarbonates and perborates; and instructions for the use of the composition to bleach chemically tanned skin.

    摘要翻译: 一种试剂盒,其包括:含有即用型皮肤漂白组合物的密封容器,其包含含有2至6重量%选自过氧化氢,有机过酸及其盐,过氧化氢加合物和金属过氧化物的过氧化物漂白剂的乳液, 过碳酸盐和过硼酸盐; 以及使用组合物漂白化学鞣制皮肤的说明。

    Functional acylglycerides
    96.
    发明授权
    Functional acylglycerides 失效
    功能酰基甘油酯

    公开(公告)号:US06677470B2

    公开(公告)日:2004-01-13

    申请号:US09989835

    申请日:2001-11-20

    IPC分类号: C07C5700

    摘要: The present invention relates to the field of human and animal nutrition, and in particular to certain novel compositions of conjugated linoleic acids (CLA). In particular, the present invention relates certain isomers of conjugated linoleic acids at either the SN1 and SN3 or SN2 positions of the acylglyceride molecule and another fatty acyl residue at the other of the SN1 and SN3 or SN2 positions of the acylglyceride molecule. These novel acylglyceride compositions containing conjugated linoleic acyl residues, medium chain fatty acyl residues, long chain fatty acyl residues, and &ohgr;3, &ohgr;6, and &ohgr;9 fatty acyl residues are efficacious as pharmaceutical compositions, animal feed additives, and human dietary supplements.

    摘要翻译: 本发明涉及人和动物营养领域,特别涉及某些共轭亚油酸(CLA)的新型组合物。 特别地,本发明涉及在酰基甘油酯分子的SN1和SN3或SN2位置和酰基甘油酯分子的SN1和SN3或SN2位置的另一个脂肪酰基残基上的共轭亚油酸的某些异构体。 含有共轭亚油酰基残基,中链脂肪酰基残基,长链脂肪酰基残基和ω-3,ω6和ω9脂肪酰基残基的这些新型酰基甘油酯组合物作为药物组合物,动物饲料添加剂和人类膳食补充剂是有效的。

    Contrast agents
    97.
    发明授权
    Contrast agents 失效
    对比剂

    公开(公告)号:US06610269B1

    公开(公告)日:2003-08-26

    申请号:US09422977

    申请日:1999-10-22

    IPC分类号: A61K4900

    摘要: The invention provides a composition of matter of the formula (I): V—L—R, where V is a vector moiety having affinity for an angiogenesis-related endothelias cell receptor, L is a linker moiety or a bond and R is a detectable moiety, characterized in that V is a non-peptidic organic group, or V is peptidic and R is a macromolecular or particulate species providing a multiplicity of labels detectable in in vivo imaging.

    摘要翻译: 本发明提供式(I)的物质组合物:VLR,其中V是对血管生成相关内皮细胞受体具有亲和性的载体部分,L是连接体部分或键,R是可检测部分,其特征在于 V是非肽类有机基团,或V是肽类,R是提供在体内成像中可检测到的多种标记物的大分子或微粒物质。

    Polymeric surfactant-encapsulated microbubbles and their use in
ultrasound imaging
    100.
    发明授权
    Polymeric surfactant-encapsulated microbubbles and their use in ultrasound imaging 失效
    聚合物表面活性剂包封的微泡及其在超声成像中的应用

    公开(公告)号:US5919434A

    公开(公告)日:1999-07-06

    申请号:US602797

    申请日:1997-03-14

    摘要: The present invention relates to polymer-based gas-containing contrast agents in which microbubbles of gas are encapsulated by non-polymerizable wall-forming block or graft copolymer surfactants. The polymer surfactants are preferably biodegradable and include block and graft copolymers containing linkages of formula (I):--(O).sub.m --CO--O--C(R.sup.1 R.sup.2)--O--CO--(O).sub.n --(I)where R.sup.1 and R.sup.2 each represent a hydrogen atom or a carbon-attached monovalent organic group, or R.sup.1 and R.sup.2 together form a carbon-attached divalent organic group and m and n are each zero or 1.

    摘要翻译: PCT No.PCT / GB94 / 01923 Sec。 371日期1997年3月14日 102(e)1997年3月14日PCT PCT 1994年9月5日PCT公布。 第WO95 / 06518号公报 日期:1995年3月9日本发明涉及气体微气泡被不可聚合的壁形成嵌段或接枝共聚物表面活性剂包封的基于聚合物的含气体造影剂。 聚合物表面活性剂优选是可生物降解的,并且包括含有式(I)的键的嵌段和接枝共聚物: - (O)m -CO-OC(R 1 R 2)-O-CO-(O)n - (I),其中R 1和R 2各自 表示氢原子或碳键的一价有机基团,或者R 1和R 2一起形成碳键的二价有机基团,m和n各自为0或1。