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    Aniline-derived ligands for the thyroid receptor
    2.
    发明授权
    Aniline-derived ligands for the thyroid receptor 有权
    苯胺衍生的甲状腺受体配体

    公开(公告)号：US07109164B2

    公开(公告)日：2006-09-19

    申请号：US10930360

    申请日：2004-08-30

    申请人： Todd J. Friends ,  Denis E. Ryono ,  Minsheng Zhang

    发明人： Todd J. Friends ,  Denis E. Ryono ,  Minsheng Zhang

    IPC分类号： C07C37/00

    CPC分类号： C07C233/27 ,  A61K31/167 ,  A61K45/06 ,  C07C233/25 ,  A61K2300/00

    摘要： New thyroid receptor ligands are provided which have the general formula in which: X is —O—, —S—, —CH2—, —CO—, or —NH—; Y is —(CH2)n— where n is an integer from 1 to 5, or cis- or trans-ethylene; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.

    摘要翻译： 提供了新的甲状腺受体配体，其具有以下通式：其中：X是-O - ， - S - ， - CH 2 - ， - CO-或-NH-; Y是 - （CH 2 CH 2）n - 其中n是1至5的整数，或顺式或反式 - 亚乙基; R 1是卤素，三氟甲基或1至6个碳的烷基或3至7个碳的环烷基; R 2和R 3相同或不同，为氢，卤素，1至4个碳的烷基或3至6个碳的环烷基，R 1， SUB 2和R 3不是氢; R 4是氢或低级烷基; R 5是氢或低级烷基; R 6是羧酸，或酯或前药; R 7是氢或烷酰基或芳酰基。 此外，提供了一种用于预防，抑制或治疗与代谢功能障碍相关的疾病或依赖于T 3 N调节基因的表达的方法，其中如上所述的化合物以 治疗有效量。 与代谢功能障碍相关或依赖于T 3受体基因表达的这种疾病的实例包括肥胖症，高胆固醇血症，动脉粥样硬化，心律失常，抑郁症，骨质疏松症，甲状腺机能减退，甲状腺肿，甲状腺癌以及 青光眼，充血性心力衰竭和皮肤疾病。

    Aniline-derived ligands for the thyroid receptor
    5.
    发明授权
    Aniline-derived ligands for the thyroid receptor 有权
    苯胺衍生的甲状腺受体配体

    公开(公告)号：US06800605B1

    公开(公告)日：2004-10-05

    申请号：US09761050

    申请日：2001-01-16

    申请人： Todd J. Friends ,  Denis E. Ryono ,  Minsheng Zhang

    发明人： Todd J. Friends ,  Denis E. Ryono ,  Minsheng Zhang

    IPC分类号： C07C3700

    CPC分类号： C07C233/27 ,  A61K31/167 ,  A61K45/06 ,  C07C233/25 ,  A61K2300/00

    摘要： New thyroid receptor ligands are provided which have the general formula in which: X is —O—, —S—, —CH2—, —CO—, or —NH—; Y is —(CH2)n— where n is an integer from 1 to 5, or cis- or trans-ethylene; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a T3 regulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.

    摘要翻译： 提供了新的甲状腺受体配体，其具有以下通式：X是-O-，-S-，-CH 2 - ， - CO-或-NH-; Y是 - （CH 2）n - ，其中n是 1至5，或顺式或反式 - 亚乙基; R 1为卤素，三氟甲基，或1至6个碳原子的烷基或3至7个碳的环烷基; R 2和R 3相同或不同，为氢，卤素， 至4个碳或3至6个碳的环烷基，R2和R3中的至少一个不是氢; R4是氢或低级烷基; R5是氢或低级烷基; R6是羧酸或酯或前药; R7是氢 或烷酰基或芳酰基。此外，提供了用于预防，抑制或治疗与代谢功能障碍相关的疾病或取决于T3调节基因的表达的方法，其中如上所述的化合物以治疗 有效量。 与代谢功能障碍相关或依赖于T3调节基因的表达的这种疾病的实例包括肥胖症，高胆固醇血症，动脉粥样硬化，心律失常，抑郁症，骨质疏松症，甲状腺功能减退，甲状腺癌，青光眼，充血性心力衰竭和皮肤病 。