Modified forms of pharmacologically active agents and uses therefor
    1.
    发明授权
    Modified forms of pharmacologically active agents and uses therefor 失效
    药理活性剂的修饰形式及其用途

    公开(公告)号:US06429223B1

    公开(公告)日:2002-08-06

    申请号:US09715767

    申请日:2000-11-17

    IPC分类号: A61K3148

    摘要: In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflammatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

    摘要翻译: 根据本发明,提供非甾体抗炎药(NSAID)的修饰形式。 根据本发明的修饰的NSAID提供了一类新的抗炎剂,其提供NSAIDs的治疗益处,同时引起副作用的发生率低得多,然后通常用这些药剂观察到。

    Conjugates of dithiocarbamates with pharmacologically active agents and uses therefor
    2.
    发明授权
    Conjugates of dithiocarbamates with pharmacologically active agents and uses therefor 失效
    二硫代氨基甲酸酯与药理活性剂的结合物及其用途

    公开(公告)号:US06407135B1

    公开(公告)日:2002-06-18

    申请号:US09453608

    申请日:1999-12-03

    IPC分类号: C07D20704

    CPC分类号: C07C333/16

    摘要: In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e.g., dithiocarbamates, or “DC”) and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.

    摘要翻译: 根据本发明,提供了一氧化氮清除剂(例如二硫代氨基甲酸盐或“DC”)和药理活性剂(例如NSAID)的缀合物。 本发明共轭物提供了一类新的药理活性剂(例如抗炎剂),其由于通过改变如本文所述的药理学活性剂而赋予的保护作用,导致副作用的低得多的发生率。 此外,发明共轭物比未改性的药理活性剂更有效,因为与药理活性剂接触的细胞和组织被保护免受由于一氧化氮的共同产生而导致的一氧化氮过量产生的潜在的破坏性作用 除了游离的药理学活性剂之外,当发明结合物被切割时,清除剂(例如,二硫代氨基甲酸盐)。

    Protected forms of a combination of pharmacologically active agents and uses therefor
    3.
    发明授权
    Protected forms of a combination of pharmacologically active agents and uses therefor 失效
    药理活性剂的组合的保护形式及其用途

    公开(公告)号:US06306842B1

    公开(公告)日:2001-10-23

    申请号:US09586344

    申请日:2000-06-02

    IPC分类号: A01N3736

    CPC分类号: C07D261/08 A61K47/55

    摘要: In accordance with the present invention, there are provided conjugates of a combination of pharmacologically active agents (e.g., NSAIDs and selective COX-2 inhibitors). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which provide the therapeutic benefits of both NSAIDs and selective COX-2 inhibitors, while causing a much lower incidence of side-effects then are typically observed with such agents due to the protective effects imparted by modifying the pharmacologically active agents as described herein.

    摘要翻译: 根据本发明,提供了药理活性剂(例如NSAID和选择性COX-2抑制剂)的组合的缀合物。 本发明共轭物提供了一类新的药理学活性剂(例如抗炎剂),其提供了NSAID和选择性COX-2抑制剂的治疗益处,同时引起副作用的发生率低得多,然后通常用这些药剂观察到 由于通过改变本文所述的药理活性剂而赋予的保护作用。

    Protected forms of pharmacologically active agents and uses therefor
    4.
    发明授权
    Protected forms of pharmacologically active agents and uses therefor 有权
    保护形式的药理活性剂及其用途

    公开(公告)号:US06355666B1

    公开(公告)日:2002-03-12

    申请号:US09602688

    申请日:2000-06-23

    IPC分类号: A61K3148

    CPC分类号: A61K47/555 A61K47/54

    摘要: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

    摘要翻译: 根据本发明,提供了非甾体抗炎药的正常修饰形式。 根据本发明的修饰的NSAID提供了一类新的抗炎剂,其提供NSAIDs的治疗益处,同时引起副作用的发生率低得多,然后通常用这些药剂观察到。

    Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor
    5.
    发明授权
    Conjugates of dithiocarbamate disulfides with pharmacologically active agents and uses therefor 失效
    二硫代氨基甲酸二硫化物与药理活性剂的结合物及其用途

    公开(公告)号:US06274627B1

    公开(公告)日:2001-08-14

    申请号:US09416619

    申请日:1999-10-12

    IPC分类号: A61K3116

    CPC分类号: A61K47/55

    摘要: In accordance with the present invention, there are provided conjugates of physiologically compatible free radical scavengers (e.g., dithiocarbamate disulfides (DD)) and pharmacologically active agents (e.g., NSAIDS). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of free radical overproduction induced thereby as a result of the co-production of free radical scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.

    摘要翻译: 根据本发明,提供了生理上相容的自由基清除剂(例如二硫代氨基甲酸酯二硫化物(DD))和药理活性剂(例如NSAIDS)的缀合物。 本发明共轭物提供了一类新的药理活性剂(例如抗炎剂),其由于通过改变如本文所述的药理学活性剂而赋予的保护作用,导致副作用的低得多的发生率。 此外,发明共轭物比未改性的药理学活性剂更有效,因为与药理活性剂接触的细胞和组织被保护免受由此引起的自由基过度产生的潜在的破坏性作用,这是由于自由基的共同产生 除了游离的药理学活性剂之外,当发明结合物被切割时,清除剂(例如,二硫代氨基甲酸盐)。

    Protected forms of pharmacologically active agents and uses therefor
    7.
    发明授权
    Protected forms of pharmacologically active agents and uses therefor 失效
    保护形式的药理活性剂及其用途

    公开(公告)号:US06710086B1

    公开(公告)日:2004-03-23

    申请号:US09515043

    申请日:2000-02-25

    IPC分类号: A61K3116

    CPC分类号: A61K47/555 A61K47/54

    摘要: In accordance with the present invention, there are provided conjugates of dithiocarbamates “DC”) and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein.

    摘要翻译: 根据本发明,提供二硫代氨基甲酸酯“DC”的缀合物和药理学活性剂(例如NSAID)。 本发明共轭物提供了一类新的药理活性剂(例如抗炎剂),其由于通过改变如本文所述的药理学活性剂而赋予的保护作用,导致副作用的低得多的发生率。

    Hydroxamate derivatives of non-steroidal anti-inflammatory drugs
    8.
    发明授权
    Hydroxamate derivatives of non-steroidal anti-inflammatory drugs 失效
    非甾体抗炎药的羟肟酸衍生物

    公开(公告)号:US06620813B1

    公开(公告)日:2003-09-16

    申请号:US10177683

    申请日:2002-06-21

    IPC分类号: A61K3153

    摘要: In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs)), and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compounds are useful for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; and the like.

    摘要翻译: 根据本发明,提供了具有多种用途的新型化学实体,例如作为NSAID的前药; 作为环氧合酶(COX)和5-脂氧合酶(5-LO)的双重抑制剂; 作为抗癌剂(通过促进细胞凋亡和/或抑制基质金属蛋白酶(MMPs))等。 本发明化合物包含与羟肟酸共价连接的非甾体抗炎剂(NSAID)。 本发明化合物可用于各种应用,例如治疗炎症和炎症相关病症; 减少与抗炎剂的施用相关的副作用; 促进凋亡; 抑制基质金属蛋白酶; 等等。

    Substituted cyclic compounds and mixtures comprising same
    10.
    发明授权
    Substituted cyclic compounds and mixtures comprising same 失效
    取代的环状化合物和包含它们的混合物

    公开(公告)号:US06191273B1

    公开(公告)日:2001-02-20

    申请号:US09148762

    申请日:1998-09-04

    IPC分类号: C07D48702

    摘要: Novel chemical compounds and mixtures of same are provided having antibacterial and other utilities. The mixtures preferably are formed by reacting a cyclic scaffold moiety with a set of chemical substituients. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.

    摘要翻译: 提供新的化合物及其混合物具有抗菌和其他效用。 混合物优选通过使环状支架部分与一组化学取代基反应而形成。 根据本发明形成的图书馆本身具有效用,并且是商品。 它们可用于筛选农药,药物和其他生物活性化合物。