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74 条记录 (耗时 0.047 秒)

    Glucocorticoid receptor modulators
    65.
    发明授权
    Glucocorticoid receptor modulators 有权
    糖皮质激素受体调节剂

    公开(公告)号：US07713989B2

    公开(公告)日：2010-05-11

    申请号：US11580996

    申请日：2006-10-13

    申请人： Robert L. Dow ,  Kevin K. Liu ,  Bradley P. Morgan ,  Andrew G. Swick

    发明人： Robert L. Dow ,  Kevin K. Liu ,  Bradley P. Morgan ,  Andrew G. Swick

    IPC分类号： A61K31/44 ,  C07D471/12

    CPC分类号： C07D213/40 ,  C07D213/30 ,  C07D233/64 ,  C07D241/12 ,  C07D295/13 ,  C07D295/205 ,  C07D455/06

    摘要： The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to the diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides intermediates and processes for preparing these compounds.

    摘要翻译： 本发明提供了类固醇受体的选择性调节剂（即激动剂和拮抗剂），特别是糖皮质激素受体的式I的非类固醇化合物。 本发明还提供含有这些化合物的药物组合物和使用这些化合物治疗需要糖皮质激素受体激动剂或拮抗剂治疗的动物的方法。 糖皮质激素受体调节剂可用于如下所述的疾病，例如肥胖，糖尿病，炎症等。 本发明还提供了制备这些化合物的中间体和方法。

    Certain Chemical Entities, Compositions and Methods
    66.
    发明申请
    Certain Chemical Entities, Compositions and Methods 失效
    某些化学实体，组成和方法

    公开(公告)号：US20090247571A1

    公开(公告)日：2009-10-01

    申请号：US12359186

    申请日：2009-01-23

    申请人： Alex T. Muci ,  Gustave Bergnes ,  Bradley P. Morgan

    发明人： Alex T. Muci ,  Gustave Bergnes ,  Bradley P. Morgan

    IPC分类号： A61K31/437 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： Provided are certain chemical entities, and methods of use to modulate skeletal myosin, skeletal actin, skeletal tropomyosin, skeletal troponin C, skeletal troponin I, skeletal troponin T, and skeletal muscle, including fragments and isoforms thereof, as well as the skeletal sarcomere, and methods of use in the treatment of obesity, sarcopenia, wasting syndrome, frailty, cachexia, muscle spasm, post-surgical and post-traumatic muscle weakness, neuromuscular disease, and other indications.

    摘要翻译： 提供某些化学实体以及用于调节骨骼肌球蛋白，骨骼肌动蛋白，骨骼原肌球蛋白，骨骼肌钙蛋白C，骨骼肌钙蛋白I，骨骼肌钙蛋白T和骨骼肌（包括其片段和同种型）以及骨骼肌节的使用方法， 以及用于治疗肥胖，肌肉减少症，消瘦综合征，虚弱，恶病质，肌肉痉挛，手术后和创伤后肌肉无力，神经肌肉疾病等症状的治疗方法。

    Thyromimetic antiobesity agents
    67.
    发明授权
    Thyromimetic antiobesity agents 失效
    甲状腺功能亢进剂

    公开(公告)号：US06555578B2

    公开(公告)日：2003-04-29

    申请号：US09978980

    申请日：2001-10-16

    申请人： Peter Cornelius ,  Diane Hargrove ,  Bradley P. Morgan ,  Andrew G. Swick

    发明人： Peter Cornelius ,  Diane Hargrove ,  Bradley P. Morgan ,  Andrew G. Swick

    IPC分类号： A61K3124

    CPC分类号： A61K31/216 ,  A61K31/195 ,  A61K31/198 ,  A61K31/215 ,  A61K2300/00 ,  A61K31/00

    摘要： The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or R3 is the radical  wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R9 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group; R4 is hydrogen, halogen, trifluoromethyl or lower alkyl; R5 and R6 are, independently, hydrogen or lower alkyl or R5 and R6, taken together with the carbon atom to which they are attached, form a carbonyl group; X is O, S or —NR7; R7 is hydrogen or lower alkyl; W is O or S; and Z is carboxyl or carboxyl derivatized as a pharmaceutically acceptable ester or amide. The invention further provides for pharmaceutical compositions and methods of using the compounds of structural formula (I), or the pharmaceutically acceptable salts, racemates and enantiomers thereof, in combination with an anorectic agent, in treating obesity.

    摘要翻译： 本发明涉及可用于治疗肥胖症的药物组合物和方法，该方法包括向需要这种治疗的动物，包括人或伴侣动物施用有效量的结构式化合物或其药学上可接受的盐，外消旋体或 其中R是羟基，酯化的羟基或醚化羟基; R 1和R 2独立地是卤素，三氟甲基或低级烷基; R 3是卤素，三氟甲基，低级烷基，芳基，芳基 - 低级烷基，环烷基或环烷基 - 低级烷基， 碳环芳基甲基，碳环芳酰基，碳环芳基羟甲基; 或R 3是其中R 8是氢，低级烷基，芳基，环烷基，芳基 - 低级烷基或环烷基 - 低级烷基的基团; R 9是羟基或酰氧基; R 10是氢或低级烷基; 或R 9和R 10与它们所连接的碳原子一起形成羰基; R 4是氢，卤素，三氟甲基或低级烷基; R 5和R 6独立地是氢或低级烷基或R 5和R 6，取代 与它们所连接的碳原子一起形成羰基; X是O，S或-NR 7; R 7是氢或低级烷基; W是O或S; 并且Z是作为药学上可接受的酯或酰胺衍生的羧基或羧基。本发明还提供了药物组合物和使用结构式（I）化合物或其药学上可接受的盐，外消旋体和对映异构体与厌食症 代理，治疗肥胖。

    Thyromimetic antiobesity agents
    68.
    发明授权
    Thyromimetic antiobesity agents 失效
    甲状腺功能亢进剂

    公开(公告)号：US06344481B1

    公开(公告)日：2002-02-05

    申请号：US09488110

    申请日：2000-01-20

    申请人： Peter Cornelius ,  Diane M. Hargrove ,  Bradley P. Morgan ,  Andrew G. Swick

    发明人： Peter Cornelius ,  Diane M. Hargrove ,  Bradley P. Morgan ,  Andrew G. Swick

    IPC分类号： A61K3124

    CPC分类号： A61K31/216 ,  A61K31/195 ,  A61K31/198 ,  A61K31/215 ,  A61K2300/00 ,  A61K31/00

    摘要： The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or R3 is the radical wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R6 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group; R4 is hydrogen, halogen, trifluoromethyl or lower alkyl; R5 and R6 are, independently, hydrogen or lower alkyl or R5 and R6, taken together with the carbon atom to which they are attached, form a carbonyl group; X is O, S or —NR7; R7 is hydrogen or lower alkyl; W is O or S; and Z is carboxyl or carboxyl derivatized as a pharmaceutically acceptable ester or amide. The invention further provides for pharmaceutical compositions and methods of using the compounds of structural formula (I), or the pharmaceutically acceptable salts, racemates and enantiomers thereof, in combination with an anorectic agent, in treating obesity.

    摘要翻译： 本发明涉及可用于治疗肥胖症的药物组合物和方法，该方法包括向需要这种治疗的动物，包括人或伴侣动物施用有效量的结构式化合物或其药学上可接受的盐，外消旋体或 其中R是羟基，酯化的羟基或醚化羟基; R 1和R 2独立地是卤素，三氟甲基或低级烷基; R 3是卤素，三氟甲基，低级烷基，芳基，芳基 - 低级烷基，环烷基或环烷基 - 低级烷基， 碳环芳基甲基，碳环芳酰基，碳环芳基羟甲基; 或R 3是其中R 8是氢，低级烷基，芳基，环烷基，芳基 - 低级烷基或环烷基 - 低级烷基的基团; R 6是羟基或酰氧基; R 10是氢或低级烷基; 或R 9和R 10与它们所连接的碳原子一起形成羰基; R 4是氢，卤素，三氟甲基或低级烷基; R 5和R 6独立地是氢或低级烷基或R 5和R 6，取代 与它们所连接的碳原子一起形成羰基; X是O，S或-NR 7; R 7是氢或低级烷基; W是O或S; 并且Z是作为药学上可接受的酯或酰胺衍生的羧基或羧基。本发明还提供了药物组合物和使用结构式（I）化合物或其药学上可接受的盐，外消旋体和对映异构体与厌食症 代理，治疗肥胖。

    Glucocorticoid receptor modulators
    70.
    发明授权
    Glucocorticoid receptor modulators 失效
    糖皮质激素受体调节剂

    公开(公告)号：US06852719B2

    公开(公告)日：2005-02-08

    申请号：US10012274

    申请日：2001-10-26

    申请人： Kevin K. Liu ,  Bradley P. Morgan ,  Ralph P. Robinson

    发明人： Kevin K. Liu ,  Bradley P. Morgan ,  Ralph P. Robinson

    IPC分类号： A61K31/4245 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  A61P3/04 ,  A61P3/10 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P29/00 ,  C07D271/06 ,  C07D413/04 ,  C07D413/06

    CPC分类号： C07D271/06 ,  C07D413/04 ,  C07D413/06

    摘要： The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds

    摘要翻译： 本发明提供式I的非类固醇化合物，包括其前体药物和药学上可接受的盐，其是类固醇受体的特异性调节剂（例如激动剂，部分激动剂和拮抗剂），特别是糖皮质激素受体。 本发明还提供含有这些化合物的药物组合物和使用这些化合物治疗需要糖皮质激素受体激动剂或拮抗剂治疗的动物的方法。 糖皮质激素受体调节剂可用于治疗如下所述的疾病，例如肥胖，糖尿病，炎症等。 本发明还提供了制备这些化合物的方法