Drug efflux pump inhibitor
    3.
    发明授权
    Drug efflux pump inhibitor 失效
    药物外排泵抑制剂

    公开(公告)号:US07056917B2

    公开(公告)日:2006-06-06

    申请号:US09842234

    申请日:2001-04-26

    摘要: A medicament for preventive and/or therapeutic treatment of a microbial infection which comprises as an active ingredient a compound represented by the following general formula (I): wherein, R1 and R2 represent hydrogen atom, a halogen atom, hydroxyl group or the like, W1 represents —CH═CH—, —CH2O—, —CH2CH2— or the like; R3 represents hydrogen atom, a halogen atom, hydroxyl group or an amino group; R4 represents hydrogen atom, a group of —OZ0-4R5 (Z0-4 represents an alkylene group, a fluorine-substituted alkylene group or a single bond, and R5 represents a cyclic alkyl group, an aryl group or the like); W2 represents a single bond or —C(R8)═C(R9)— (R8 and R9 represent hydrogen atom, a halogen atom, a lower alkyl group or the like, Q represents an acidic group, but W2 and Q may together form vinylidenethiazolidinedione or an equivalent heterocyclic ring; m and n represent an integer of 0 to 2, and q represents an integer of 0 to 3.

    摘要翻译: 一种用于预防和/或治疗微生物感染的药物,其包含作为活性成分的由以下通式(I)表示的化合物:其中R 1和R 2, SUP>表示氢原子,卤素原子,羟基等,W 1表示-CH-CH - , - CH 2 O - , - CH- 2 CH 2 - 或类似物; R 3表示氢原子,卤素原子,羟基或氨基; R 4表示氢原子,-OZ 0-4R 5(Z 0-4)的基团表示 亚烷基,氟取代的亚烷基或单键,R 5表示环状烷基,芳基等)。 -C(R 9) - (R 9) - (R 9) - (R 8) >和R 9表示氢原子,卤素原子,低级烷基等,Q表示酸性基团,但W 2和Q可以一起形成亚乙烯基乙二胺二酮或 等价杂环; m和n表示0〜2的整数,q表示0〜3的整数。

    Drug efflux pump inhibitor
    4.
    发明申请
    Drug efflux pump inhibitor 审中-公开
    药物外排泵抑制剂

    公开(公告)号:US20060106034A1

    公开(公告)日:2006-05-18

    申请号:US11320229

    申请日:2005-12-29

    IPC分类号: A61K31/519

    摘要: A medicament for preventive and/or therapeutic treatment of a microbial infection which comprises as an active ingredient a compound represented by the following general formula (I): wherein, R1 and R2 represent hydrogen atom, a halogen atom, hydroxyl group or the like, W1 represents —CH═CH—, —CH2O—, —CH2CH2— or the like; R3 represents hydrogen atom, a halogen atom, hydroxyl group or an amino group; R4 represents hydrogen atom, a group of —OZ0-4R5 (Z0-4 represents an alkylene group, a fluorine-substituted alkylene group or a single bond, and R5 represents a cyclic alkyl group, an aryl group or the like); W2 represents a single bond or —C(R8)═C(R9)−(R8 and R9 represent hydrogen atom, a halogen atom, a lower alkyl group or the like, Q represents an acidic group, but W2 and Q may together form vinylidenethiazolidinedione or an equivalent heterocyclic ring; m and n represent an integer of 0 to 2, and q represents an integer of 0 to 3.

    摘要翻译: 一种用于预防和/或治疗微生物感染的药物,其包含作为活性成分的由以下通式(I)表示的化合物:其中R 1和R 2, SUP>表示氢原子,卤素原子,羟基等,W 1表示-CH-CH-,-CH 2 O - , - CH- 2 CH 2 - 或类似物; R 3表示氢原子,卤素原子,羟基或氨基; R 4表示氢原子,-OZ 0-4R 5(Z 0-4)的基团表示 亚烷基,氟取代的亚烷基或单键,R 5表示环状烷基,芳基等)。 -C(R 9) - (R 9) - (R 9) - (R 8) >和R 9表示氢原子,卤素原子,低级烷基等,Q表示酸性基团,但W 2和Q可以一起形成亚乙烯基乙二胺二酮或 等价杂环; m和n表示0〜2的整数,q表示0〜3的整数。

    NOVEL PROSTAGLANDIN E1 DERIVATIVE AND NANOPARTICLE HAVING THE SAME ENCAPSULATED THEREIN
    5.
    发明申请
    NOVEL PROSTAGLANDIN E1 DERIVATIVE AND NANOPARTICLE HAVING THE SAME ENCAPSULATED THEREIN 审中-公开
    新型PROSTAGLANDIN E1衍生物和具有其相同性质的纳米颗粒

    公开(公告)号:US20110262548A1

    公开(公告)日:2011-10-27

    申请号:US13129729

    申请日:2009-10-16

    摘要: A PGE1 derivative is provided which has an excellent sustained, slow-release PGE1 action. In addition, a PGE1-derivative-containing nanoparticle produced using this PGE1 derivative is provided, which effectively targets an affected site, has excellent drug slow-release properties, and has reduced side effects. This PGE1-derivative-containing nanoparticle is a nanoparticle containing a prostaglandin E1 derivative represented by the following formula (1) (wherein n denotes an integer of 1 to 12), obtained by hydrophobicizing the prostaglandin E1 derivative with a metal ion, and reacting the hydrophobicized prostaglandin E1 derivative with poly L-lactic acid or a poly(L-lactic acid/glycolic acid) copolymer and a poly DL- or L-lactic acid-polyethylene glycol block copolymer or a poly(DL- or L-lactic acid/glycolic acid)-polyethylene glycol block copolymer.

    摘要翻译: 提供PGE1衍生物,其具有优异的持续缓释PGE1作用。 此外,提供了使用该PGE1衍生物制备的含PGE1衍生物的纳米粒子,其有效靶向受影响部位,具有优异的药物缓释性能,并且具有降低的副作用。 该含有PGE1衍生物的纳米粒子是含有前述的前列腺素E1衍生物的下述式(1)表示的纳米粒子,其中n表示1〜12的整数,通过用金属离子对前列腺素E1衍生物进行疏水化, 具有聚L-乳酸或聚(L-乳酸/乙醇酸)共聚物的疏水化前列腺素E1衍生物和聚DL-或L-乳酸 - 聚乙二醇嵌段共聚物或聚(DL-或L-乳酸/ 乙醇酸) - 聚乙二醇嵌段共聚物。

    Loxoprofen derivative and pharmaceutical preparation containing the same
    6.
    发明授权
    Loxoprofen derivative and pharmaceutical preparation containing the same 有权
    洛索丙芬衍生物和含有它的药物制剂

    公开(公告)号:US08431614B2

    公开(公告)日:2013-04-30

    申请号:US13148566

    申请日:2010-02-18

    摘要: There is provided a novel loxoprofen derivative that has no side effect such as a gastrointestinal disorder and also has excellent anti-inflammatory and analgesic effects and is represented by the following formula (I) or (II): (wherein R1 and R2 each represent a halogen atom or a substituted or unsubstituted phenyl group) or a pharmacologically acceptable salt thereof. In the derivative, the halogen atom is selected from a chlorine atom, a bromine atom, a fluorine atom, and an iodine atom, and a substituent of the substituted phenyl group is a halogen atom, a hydroxyl group, a substituted or unsubstituted lower alkyl group, a lower alkylthio group, a lower alkoxy group, a nitro group, an amino group, or a carboxyl group.

    摘要翻译: 本发明提供一种新颖的洛索洛芬衍生物,其不具有胃肠功能紊乱等副作用,具有优异的抗炎镇痛效果,并且由下式(I)或(II)表示:(其中R1和R2各自表示 卤素原子或取代或未取代的苯基)或其药理学上可接受的盐。 在衍生物中,卤素原子选自氯原子,溴原子,氟原子和碘原子,取代苯基的取代基为卤素原子,羟基,取代或未取代的低级烷基 低级烷硫基,低级烷氧基,硝基,氨基或羧基。