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    Glucocorticoid and thyroid hormone receptor ligands for the treatment of metabolic disorders
    1.
    发明授权
    Glucocorticoid and thyroid hormone receptor ligands for the treatment of metabolic disorders 失效
    糖皮质激素和甲状腺激素受体配体用于治疗代谢紊乱

    公开(公告)号：US06492424B1

    公开(公告)日：2002-12-10

    申请号：US09744865

    申请日：2001-04-09

    申请人： Theresa Apelqvist ,  Patrick Goede ,  Erik Holmgren

    发明人： Theresa Apelqvist ,  Patrick Goede ,  Erik Holmgren

    IPC分类号： A61K3119

    CPC分类号： C07D295/192 ,  C07C59/68 ,  C07C59/90 ,  C07C65/40 ,  C07C69/736 ,  C07C69/92 ,  C07C217/90 ,  C07C233/56 ,  C07C235/34

    摘要： Novel glucocorticoid and thyroid receptor ligands as provided which have the general formula (I): in which R1 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano, or a pharmaceutically acceptable salt thereof. R2 and R3 are the same or different, and are hydrogen, halogen, alkyl of 1 to 4 carbons, or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen. X is carbonyl or methylene. R4 is an aliphatic, aromatic or heteroaromatic. Y is hydroxyl, methoxy, amino, or alkyl amino. n is an integer from 0 to 4. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid or thyroid receptor gene such as diabetes, hypercholesterolemia, or obesity using these compounds is also disclosed.

    摘要翻译： 提供具有通式（I）的新型糖皮质激素和甲状腺受体配体：其中R 1是脂族烃，芳族烃，羧酸或其酯，链烯基羧酸或其酯，羟基，卤素或氰基，或 其药学上可接受的盐。 R2和R3相同或不同，为氢，卤素，1至4个碳的烷基或3至5个碳的环烷基，R2和R3中的至少一个不是氢。 X是羰基或亚甲基。 R 4是脂族，芳族或杂芳族。 Y是羟基，甲氧基，氨基或烷基氨基。 n是0至4的整数。还公开了用于治疗与代谢功能障碍相关的疾病或依赖于使用这些化合物的糖皮质激素或甲状腺受体基因如糖尿病，高胆固醇血症或肥胖症的表达的方法。

    Estrogen receptor ligands
    8.
    发明授权
    Estrogen receptor ligands 有权
    雌激素受体配体

    公开(公告)号：US08710243B2

    公开(公告)日：2014-04-29

    申请号：US13500471

    申请日：2010-10-06

    申请人： Lars Hagberg ,  Sandra Gordon ,  Aiping Cheng ,  Theresa Apelqvist ,  Patrik Rhönnstad ,  Mattias Wennerstål

    发明人： Lars Hagberg ,  Sandra Gordon ,  Aiping Cheng ,  Theresa Apelqvist ,  Patrik Rhönnstad ,  Mattias Wennerstål

    IPC分类号： C07D209/12

    CPC分类号： C07D207/32 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

    摘要： The invention provides a compound of formula(I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula(I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification.

    摘要翻译： 本发明提供式（I）化合物或其药学上可接受的酯，酰胺，溶剂化物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物。 本发明还提供了这样的化合物在治疗或预防与与雌激素受体活性相关的疾病或病症相关的病症中的用途。 式（I）其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10如说明书中所定义。