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    Thyroid receptor ligands and method II
    3.
    发明授权
    Thyroid receptor ligands and method II 失效
    甲状腺受体配体及方法二

    公开(公告)号：US07288571B2

    公开(公告)日：2007-10-30

    申请号：US11189654

    申请日：2005-07-26

    Applicant: Jon Hangeland ,  Minsheng Zhang ,  Yolanda Caringal ,  Denis Ryono ,  Yi-Lin Li ,  Johan Malm ,  Ye Liu ,  Neeraj Garg ,  Chris Litten ,  Ana Maria Garcia Collazo ,  Konrad Koehler

    Inventor： Jon Hangeland ,  Minsheng Zhang ,  Yolanda Caringal ,  Denis Ryono ,  Yi-Lin Li ,  Johan Malm ,  Ye Liu ,  Neeraj Garg ,  Chris Litten ,  Ana Maria Garcia Collazo ,  Konrad Koehler

    IPC: A61K31/18 ,  C07C311/50

    CPC classification number: C07D207/27 ,  C07C235/32 ,  C07C235/52 ,  C07C307/06 ,  C07C311/51 ,  C07C323/41 ,  C07C323/60 ,  C07D207/09 ,  C07D211/24 ,  C07D211/34 ,  C07D211/58 ,  C07D211/96 ,  C07D213/40 ,  C07D223/12 ,  C07D231/38 ,  C07D233/64 ,  C07D257/04 ,  C07D285/06 ,  C07D285/135 ,  C07D295/13 ,  C07D295/185 ,  C07D333/20

    Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; 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 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR′R″) or an acylsulphonamide (CONHSO2R′) derivative, or a pharmaceutically acceptable salt thereof, and all stereolsom thereof; or when n is equal to or greater than one, R4 may be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5—H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependant 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.

    Abstract translation: 提供了具有通式（I）的新甲状腺受体配体，其中：n为0至4的整数; 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5个碳的环烷基，R 1， SUB 2和R 3不是氢; R 4是羧酸酰胺（CONR'R“）或酰基磺酰胺（CONHSO 2 R'）衍生物或其药学上可接受的盐及其所有立体异构体; 或当n等于或大于1时，R 4可以是可被取代或未取代的杂芳族部分，或胺（NR'R“）。 R 5是氢或酰基（如乙酰基或苯甲酰基）或能够生物转化以产生游离酚结构的其它基团（其中R 5 -H）。 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。

    Thyroid receptor ligands and method II
    4.
    发明授权
    Thyroid receptor ligands and method II 失效
    甲状腺受体配体及方法二

    公开(公告)号：US06989402B1

    公开(公告)日：2006-01-24

    申请号：US09868889

    申请日：1999-12-23

    Applicant: Jon Hangeland ,  Minsheng Zhang ,  Yolanda Caringal ,  Denis Ryono ,  Yi-Lin Li ,  Johan Malm ,  Ye Liu ,  Neeraj Garg ,  Chris Litten ,  Ana Maria Garcia Collazo ,  Konrad Koehler

    Inventor： Jon Hangeland ,  Minsheng Zhang ,  Yolanda Caringal ,  Denis Ryono ,  Yi-Lin Li ,  Johan Malm ,  Ye Liu ,  Neeraj Garg ,  Chris Litten ,  Ana Maria Garcia Collazo ,  Konrad Koehler

    IPC: A61K31/44 ,  A61K31/192 ,  A61K31/40 ,  A61K31/4174 ,  C07D211/56 ,  C07D213/72 ,  C07D229/38 ,  C07D265/30 ,  C07D241/04 ,  C07D207/14

    CPC classification number: C07D207/27 ,  C07C235/32 ,  C07C235/52 ,  C07C307/06 ,  C07C311/51 ,  C07C323/41 ,  C07C323/60 ,  C07D207/09 ,  C07D211/24 ,  C07D211/34 ,  C07D211/58 ,  C07D211/96 ,  C07D213/40 ,  C07D223/12 ,  C07D231/38 ,  C07D233/64 ,  C07D257/04 ,  C07D285/06 ,  C07D285/135 ,  C07D295/13 ,  C07D295/185 ,  C07D333/20

    Abstract: New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; 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 5 carbons, at least one of R2 and R3 being other than hydrogen; R4 is a carboxylic acid amide (CONR′R″) or an acylsulphonamide (CONHSO2R′) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, R4 may be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR′R″). R5 is hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R5=H). 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.

    Abstract translation: 提供了具有通式（I）的新甲状腺受体配体，其中：n为0至4的整数; 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5个碳的环烷基，R 1， SUB 2和R 3不是氢; R 4是羧酸酰胺（CONR'R“）或酰基磺酰胺（CONHSO 2 R'）衍生物或其药学上可接受的盐及其所有立体异构体; 或当n等于或大于1时，R 4可以是可被取代或未取代的杂芳族部分，或胺（NR'R“）。 R 5是氢或酰基（例如乙酰基或苯甲酰基）或能够生物转化以产生游离酚结构（其中R 5 = H）的其它基团。 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。

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