利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

87 条记录 (耗时 0.033 秒)

    LIVER SPECIFIC BILE ACID DERIVATIVES OF THE GLUCOCORTICOID ANTAGONIST RU486
    2.
    发明授权
    LIVER SPECIFIC BILE ACID DERIVATIVES OF THE GLUCOCORTICOID ANTAGONIST RU486 有权
    糖皮质激素拮抗剂RU486的肝特异性胆汁酸衍生物

    公开(公告)号：EP1165595B1

    公开(公告)日：2003-05-14

    申请号：EP00922530.1

    申请日：2000-03-18

    申请人： KARO BIO AB

    发明人： APELQVIST, Theresa ,  WU, Jinchang ,  KOEHLER, Konrad, F.

    IPC分类号： C07J41/00 ,  A61K31/575 ,  A61P5/46

    CPC分类号： C07J41/0061 ,  C07J41/0083

    摘要： Novel glucocorticoid receptor ligands as provided which have general formula (I) in which: R is a hydrogen atom, an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano halogen, or cyano, or a pharmaceutically acceptable salt thereof. W is a methine carbon atom (CH) having the R, S, or racemic stereochemistry. X and Z are the same or are different and are a bond, an amide (-CONR'- or -NR'CO-), an amine (-NR'-), and ether (-O-), or a thioether (-S-) and R' is a hydrogen atom, an aliphatic hydrocarbon, or an aromatic hydrocarbon. The subscripts n, o are the same or are different and are integers from one (1) to six (6). m is an integer from zero to 6. Y is hydroxyl group, carboxylic acid or ester thereof, a tetrazole, an acylsulfonamide (-CONHSO2R" or -SO2NHCOR" where R" is an aliphatic or aromatic hydrocarbon), or a pharmaceutically acceptable salt thereof. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid such as diabetes.

    摘要翻译： 具有通式（I）的新型糖皮质激素受体配体，其中：R为氢原子，脂族烃，芳族烃，羧酸或其酯，烯基羧酸或其酯，羟基，卤素或氰基卤素 或氰基，或其药学上可接受的盐。 W是具有R，S或外消旋立体化学的次甲基碳原子（CH）。 X和Z相同或不同，并且是键，酰胺（-CONR'-或-NR'CO-），胺（-NR'-）和醚（-O-），或硫醚 -S-），R'为氢原子，脂肪族烃或芳香族烃。 下标n，o相同或不同，并且是从一（1）到六（6）的整数。 m为0至6的整数.Y为羟基，羧酸或其酯，四唑，酰基磺酰胺（-CONHSO2R“或-SO 2 NHCOR”，其中R“为脂族或芳族烃）或其药学上可接受的盐 。治疗与代谢功能障碍有关的疾病或依赖于糖皮质激素例如糖尿病的表达的方法。

    LIVER SPECIFIC BILE ACID DERIVATIVES OF THE GLUCOCORTICOID ANTAGONIST RU486
    4.
    发明公开
    LIVER SPECIFIC BILE ACID DERIVATIVES OF THE GLUCOCORTICOID ANTAGONIST RU486 有权
    糖皮质激素拮抗剂RU486的肝特异性胆汁酸衍生物

    公开(公告)号：EP1165595A1

    公开(公告)日：2002-01-02

    申请号：EP00922530.1

    申请日：2000-03-18

    申请人： KARO BIO AB

    发明人： APELQVIST, Theresa ,  WU, Jinchang ,  KOEHLER, Konrad, F.

    IPC分类号： C07J41/00 ,  A61K31/575 ,  A61P5/46

    CPC分类号： C07J41/0061 ,  C07J41/0083

    摘要： Novel glucocorticoid receptor ligands as provided which have general formula (I) in which: R is a hydrogen atom, an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano halogen, or cyano, or a pharmaceutically acceptable salt thereof. W is a methine carbon atom (CH) having the R, S, or racemic stereochemistry. X and Z are the same or are different and are a bond, an amide (-CONR'- or -NR'CO-), an amine (-NR'-), and ether (-O-), or a thioether (-S-) and R' is a hydrogen atom, an aliphatic hydrocarbon, or an aromatic hydrocarbon. The subscripts n, o are the same or are different and are integers from one (1) to six (6). m is an integer from zero to 6. Y is hydroxyl group, carboxylic acid or ester thereof, a tetrazole, an acylsulfonamide (-CONHSO2R' or -SO2NHCOR' where R' is an aliphatic or aromatic hydrocarbon), or a pharmaceutically acceptable salt thereof. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid such as diabetes.

    摘要翻译： 具有通式（I）的新型糖皮质激素受体配体，其中：R为氢原子，脂族烃，芳族烃，羧酸或其酯，烯基羧酸或其酯，羟基，卤素或氰基卤素 或氰基，或其药学上可接受的盐。 W是具有R，S或外消旋立体化学的次甲基碳原子（CH）。 X和Z相同或不同，并且是键，酰胺（-CONR'-或-NR'CO-），胺（-NR'-）和醚（-O-），或硫醚 -S-），R'为氢原子，脂肪族烃或芳香族烃。 下标n，o相同或不同，并且是从一（1）到六（6）的整数。 m是0至6的整数.Y是羟基，羧酸或其酯，四唑，酰基磺酰胺（-CONHSO2R'或-SO 2 NHCOR'，其中R'是脂族或芳族烃），或其药学上可接受的盐 。 一种治疗与代谢功能障碍有关的疾病或依赖于糖皮质激素例如糖尿病的表达的方法。

    AN IN VITRO METHOD OF EVALUATING THE EFFECTS OF A SUBSTANCE
    6.
    发明授权
    AN IN VITRO METHOD OF EVALUATING THE EFFECTS OF A SUBSTANCE 无效
    体外方法进行评估的物质影响的

    公开(公告)号：EP0607268B1

    公开(公告)日：1997-08-13

    申请号：EP92921468.2

    申请日：1992-10-06

    申请人： KARO BIO AB

    发明人： NILSSON, Stefan ,  ÖSTERLUND, Marten ,  HEEROMA, Karin

    IPC分类号： C12Q1/00 ,  G01N33/74 ,  G01N33/76 ,  G01N33/78

    CPC分类号： G01N33/6872 ,  G01N33/5008 ,  G01N33/5011 ,  G01N33/502 ,  G01N33/5044 ,  G01N33/74

    摘要： An in vitro method of evaluating the antagonistic versus agonistic effects of a receptor-binding test substance on a selected type of cells containing endogenous intra-cellular hormone receptors, is disclosed. Said test substance, and separately a reference substance, known to be either an antagonist or an agonist, are incubated with said selected type of cells, and the magnitude of the selected cellular response resulting from hormone/receptor interaction, is analyzed. In case the method is performed on at least two selected types of cells which derive from different kinds of tissues, it is possible to evaluate the pattern of antagonistic versus agonistic effects of the selected test substance on said kinds of tissues.

    RECEPTOR LIGANDS
    7.
    发明授权
    RECEPTOR LIGANDS 失效
    受体配体

    公开(公告)号：EP0584186B1

    公开(公告)日：1996-08-21

    申请号：EP92910804.1

    申请日：1992-05-12

    申请人： KARO BIO AB

    发明人： NORINDER, Ulf ,  BAJORATH, Jürgen ,  STEARNS, Jay F.

    IPC分类号： A61K31/055 ,  A61K31/135 ,  A61K31/14 ,  A61K31/34 ,  C07D307/78 ,  C07D307/80 ,  C07C225/16 ,  C07C33/20 ,  C07C33/46

    CPC分类号： C07C217/22 ,  C07C39/367 ,  C07D307/80 ,  C07D307/81

    摘要： Use of a compound selected from the group consisting of 3,5-diiodo-4-(2-N,N-diethylaminoethoxy)phenyl-(2-butylbenzofur-3-yl)methanol hydrochloride (001), 2-methyl-3-(3,5-diiodo-4-(2-N,N-diethylaminoethoxy)-benzoyl)benzofuran hydrochloride (003), 2-n-butyl-3-(3,5-diiodo-4-carboxymethoxybenzoyl)benzofuran (005), 2-methyl-3-(3,5-diiodo-4-hydroxy-benzoyl)benzofuran (011), 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (015), 4'-hydroxy-3'-iodo-3,5-diiodo-4-(2-N,N-dimethylaminoethoxy)benzophenon hydrochloride (024), 2-butyl-3-(3-iodo-4-hydroxybenzoyl)benzofuran (029), 4',4-dihydroxy-3'3,5-triiodo-diphenylmethan (032), which compound is a 3,5,3'-triiodothyronine (T-3) receptor ligand, for the preparation of a medicament for the therapeutic or prophylactic treatment of a disorder which depends on the expression of T-3 regulated genes, and pharmaceutical preparations comprising said compounds, are disclosed. Further, a method of prophylactically or therapeutically treating a patient having a disorder which depends on the expression of 3,5,3'-triiodo-thyronine (T-3) regulated genes is also disclosed. The invention additionally comprises product protection for all the above listed compounds, except the compound (011).