Butyrophenone transdermal compositions
    2.
    发明公开
    Butyrophenone transdermal compositions 失效
    透皮米特米丁丁香精。

    公开(公告)号:EP0622074A1

    公开(公告)日:1994-11-02

    申请号:EP94106236.6

    申请日:1994-04-21

    IPC分类号: A61K9/70 A61K31/445

    摘要: A butyrophenone transdermal composition which comprises the following components (a) to (f):

    (a) a water-soluble polymer which is constituted by a monomer containing, partly or wholly, aliphatic carboxylic acid having a polymerizable double bond or a salt of the carboxylic acid,
    (b) a cross linking agent,
    (c) a cross linking promoter,
    (d) water,
    (e) a butyrophenone drug, and
    (f) a solvent for the butyrophenone drug (e),
    as essential components. The pH of the composition is adjusted to fall in the range of 5.5 to 8.0.
    With the composition of the invention, the concentration of the active component butyrophenone in blood can be controlled. The composition is capable of exhibiting its primary action, antiemetic action, without causing rash in the skin and with less adverse side effects.

    摘要翻译: 一种丁酰苯酚透皮组合物,其包含以下组分(a)至(f):(a)水溶性聚合物,其由含有部分或全部具有可聚合双键的脂肪族羧酸的单体或 羧酸,(b)交联剂,(c)交联促进剂,(d)水,(e)丁酰苯酮药物和(f)丁酰苯胺药物(e)的溶剂作为必需组分。 将组合物的pH调节至5.5〜8.0的范围。 利用本发明的组合物,可以控制血液中活性成分丁酰苯的浓度。 该组合物能够表现出其主要作用,止吐作用,而不会在皮肤中引起皮疹并且具有较少的副作用。

    USE OF TCF-II FOR PREVENTING OR TREATING SEPSIS
    5.
    发明授权
    USE OF TCF-II FOR PREVENTING OR TREATING SEPSIS 有权
    TCF-II对于脓毒病的治疗或预防

    公开(公告)号:EP0982037B1

    公开(公告)日:2007-06-06

    申请号:EP99909244.8

    申请日:1999-03-19

    IPC分类号: A61K38/17 A61K38/18 A61P43/00

    CPC分类号: A61K38/1833

    摘要: Novel preventives and/or remedies for sepsis. The above preventives and/or remedies contain as the active ingredient tumor cytotoxic factor-II (TCF-II) and exert particularly excellent effects on sepsis caused by at least one factor selected from the group consisting of infectious disease, burn, operation, cancer, acquired immunological deficiency syndrome (AIDS), radiation therapy, chemotherapy and total parenteral nutrition (TPN).

    PYRAZOLE DERIVATIVES
    7.
    发明公开
    PYRAZOLE DERIVATIVES 审中-公开
    吡唑衍生物

    公开(公告)号:EP1762568A1

    公开(公告)日:2007-03-14

    申请号:EP05755841.3

    申请日:2005-07-01

    CPC分类号: C07D401/14 C07D417/14

    摘要: A compound represented by formula (I):

    (wherein Ar 1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar 2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II):

    (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.

    摘要翻译: 式(I)所示的化合物:(式中,Ar 1表示可具有1〜3个取代基的苯基或未取代的5或6元芳香族杂环基,Ar 2表示(i)未取代的苯基 ,(ii)被选自氨基甲酰基,氨基,羟基,低级烷氧基和卤素原子的具有1〜3个基团或原子的低级烷基取代的苯基或( iii)被1至3个选自低级烷基,低级炔基,低级链烷酰基,氨基甲酰基,氰基的基团或原子取代的5或6元含氮芳族杂环基 基团,氨基,羟基,低级烷氧基和卤原子; X表示由式(II)表示的基团:(其中环结构表示可以具有的4-7元杂环基 除式(II)中所示的氮原子外,还选择一个杂原子 可以被选自低级烷基,氨基甲酰基,氨基,羟基,低级烷氧基,氧代基,氨基甲酰基,氨基甲酰基,氨基甲酰基等的1〜4个基团或原子取代, 低级烷酰基,低级烷基磺酰基和卤素原子)),其盐,该化合物或盐的溶剂化物和药物。

    sFRP EXPRESSION POTENTIATING AGENT
    10.
    发明公开
    sFRP EXPRESSION POTENTIATING AGENT 审中-公开
    MITTEL ZURVERSTÄRKUNGDER SFRP-EXPRESSION

    公开(公告)号:EP1733739A1

    公开(公告)日:2006-12-20

    申请号:EP05727369.0

    申请日:2005-03-30

    摘要: Tumor formation and reduced transcription of both sFRP1 gene and sFRP2 gene were found in Dlg gene knock-out mice, and thereby the following has been provided: an agent for enhancing the expression and/or function of sFRP, containing a compound having an effect of enhancing the expression and/or function of Dlg; an agent for inhibiting tumor formation or an agent for preventing and/or treating a tumor disease, containing the agent for enhancing the expression and/or function of sFRP; a method of enhancing the expression and/or function of sFRP, comprising enhancing the expression and/or function of Dlg; a method of inhibiting tumor formation or a method of preventing and/or treating a tumor disease, comprising using the aforementioned enhancing agent or the aforementioned enhancing method; a non-human mammal that is deficient in one or both of Dlg alleles; a cell originating in the mammal; a method of identifying a compound, comprising using the mammal or the cell; and a method of examining a tumor tissue or a tumor cell, comprising measuring the expression and/or function of Dlg.

    摘要翻译: 在Dlg基因敲除小鼠中发现了sFRP1基因和sFRP2基因的肿瘤形成和降低的转录,从而提供了以下:用于增强sFRP的表达和/或功能的试剂,其含有具有 增强Dlg的表达和/或功能; 用于抑制肿瘤形成的药剂或用于预防和/或治疗肿瘤疾病的药剂,其含有增强sFRP的表达和/或功能的药剂; 增强sFRP的表达和/或功能的方法,包括增强Dlg的表达和/或功能; 包括使用上述增强剂或上述增强方法的抑制肿瘤形成的方法或预防和/或治疗肿瘤疾病的方法; 缺乏一种或两种Dlg等位基因的非人类哺乳动物; 起源于哺乳动物的细胞; 鉴定化合物的方法,包括使用哺乳动物或细胞; 以及检查肿瘤组织或肿瘤细胞的方法,包括测量Dlg的表达和/或功能。