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    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：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。

    Substituted pyrazolylamides useful as glucokinase activators
    7.
    发明授权
    Substituted pyrazolylamides useful as glucokinase activators 有权
    用作葡糖激酶活化剂的取代的吡唑基酰胺

    公开(公告)号：US08614332B2

    公开(公告)日：2013-12-24

    申请号：US13397123

    申请日：2012-02-15

    申请人： Denis E. Ryono ,  Peter T. W. Cheng ,  Scott A. Bolton ,  Sean Chen ,  Yan Shi ,  Wei Meng ,  Joseph A. Tino ,  Richard B. Sulsky

    发明人： Denis E. Ryono ,  Peter T. W. Cheng ,  Scott A. Bolton ,  Sean Chen ,  Yan Shi ,  Wei Meng ,  Joseph A. Tino ,  Richard B. Sulsky

    IPC分类号： C07D231/00

    CPC分类号： C07F9/6539 ,  C07F9/58 ,  C07F9/65031 ,  C07F9/650952 ,  C07F9/6518

    摘要： Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure is a heteroaryl ring; R4 is —(CH2)n—Z—(CH2)m—PO(OR7)(OR8), —(CH2)nZ—(CH2)m—PO(OR7)R9, —(CH2)n—Z—(CH2)m—OPO(OR7)R9, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from H, alkyl and halogen; Y is R7(CH2)s or is absent; and X, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

    摘要翻译： 提供了膦酸酯和次膦酸酯活化剂的化合物，因此可用于治疗糖尿病和相关疾病，并且其结构是杂芳基环; R4是 - （CH2）nZ-（CH2）m-PO（OR7）（OR8）， - （CH2）nZ-（CH2）m-PO（OR7）R9， - （CH2）nZ-（CH2） （OR7）R9， - （CH2）nZ-（CH2）m-OPO（R9）（R10）或 - （CH2）nZ-（CH2）m-PO（R9）（R10） R5和R6独立地选自H，烷基和卤素; Y为R 7（CH 2）s或不存在; 并且X，n，Z，m，R 4，R 5，R 6，R 7和s如本文所定义; 或其药学上可接受的盐。 还提供了使用上述化合物治疗糖尿病和相关疾病的方法。

    Substituted pyrazolylamide compounds useful as glucokinase activators
    9.
    发明授权
    Substituted pyrazolylamide compounds useful as glucokinase activators 有权
    用作葡糖激酶活化剂的取代的吡唑基酰胺化合物

    公开(公告)号：US08153677B2

    公开(公告)日：2012-04-10

    申请号：US13012351

    申请日：2011-01-24

    申请人： Denis E. Ryono ,  Peter T. W. Cheng ,  Scott A. Bolton ,  Sean Chen ,  Yan Shi ,  Wei Meng ,  Joseph A. Tino ,  Richard B. Sulsky

    发明人： Denis E. Ryono ,  Peter T. W. Cheng ,  Scott A. Bolton ,  Sean Chen ,  Yan Shi ,  Wei Meng ,  Joseph A. Tino ,  Richard B. Sulsky

    IPC分类号： A61K31/415

    CPC分类号： C07F9/6539 ,  C07F9/58 ,  C07F9/65031 ,  C07F9/650952 ,  C07F9/6518

    摘要： Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n—Z—(CH2)m—PO(OR7)(OR8), —(CH2)nZ—(CH2)m—OPO(OR7)R9, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10); R5 and R6 are independently selected from hydrogen, alkyl and halogen; Y is R7(CH2)s or is absent; and X, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

    摘要翻译： 提供了膦酸酯和次膦酸酯活化剂的化合物，因此可用于治疗糖尿病和相关疾病，并且其结构是杂芳基环; R4是 - （CH2）n-Z-（CH2）m-PO（OR7）（OR8）， - （CH2）nZ-（CH2）m-OPO（OR7）R9， - （CH2）nZ-（CH2） -OPO（R9）（R10）或 - （CH2）nZ-（CH2）m-PO（R9）（R10）; R5和R6独立地选自氢，烷基和卤素; Y为R 7（CH 2）s或不存在; 并且X，n，Z，m，R 4，R 5，R 6，R 7和s如本文所定义; 或其药学上可接受的盐。 还提供了使用上述化合物治疗糖尿病和相关疾病的方法。

    Benzamide ligands for the thyroid receptor
    10.
    发明授权
    Benzamide ligands for the thyroid receptor 失效
    苯甲酰胺配体甲状腺受体

    公开(公告)号：US06395784B1

    公开(公告)日：2002-05-28

    申请号：US09871347

    申请日：2001-05-31

    申请人： Denis E. Ryono

    发明人： Denis E. Ryono

    IPC分类号： A01N3712

    CPC分类号： A61K31/166 ,  C07C235/52 ,  C07C2601/02

    摘要： New thyroid receptor ligands are provided which have the general formula in which: X is —O—, —S—, —CH2—, —CO—, or —NH—; 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 methyl, ethyl, n-propyl or trifluoromethyl; 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-; R 1是卤素，三氟甲基或1-6个碳原子的烷基或 3至7个碳原子的环烷基; R2和R3相同或不同，为氢，卤素，1至4个碳原子的烷基或3至6个碳原子的环烷基，R2和R3中的至少一个不是氢; R4是甲基 乙基，正丙基或三氟甲基; 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。另外，提供了一种预防，抑制或治疗 与代谢功能障碍相关的疾病或其依赖于T3调节基因的表达，其中如上所述的化合物以治疗有效量施用。 与代谢功能障碍相关或依赖于T3调节基因的表达的这些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，甲状腺癌以及青光眼，充血性心力衰竭和皮肤病 。