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28 条记录 (耗时 0.029 秒)

    Sulfonylpyrrolidine modulators of androgen receptor function and method
    3.
    发明申请
    Sulfonylpyrrolidine modulators of androgen receptor function and method 有权

    公开(公告)号：US20050187267A1

    公开(公告)日：2005-08-25

    申请号：US11048439

    申请日：2005-02-01

    申请人： Lawrence Hamann ,  Yingzhi Bi ,  Mark Manfredi ,  Alexandra Nirschl ,  James Sutton

    发明人： Lawrence Hamann ,  Yingzhi Bi ,  Mark Manfredi ,  Alexandra Nirschl ,  James Sutton

    IPC分类号： A61K31/4015 ,  A61K31/433 ,  C07D207/48 ,  C07D285/06 ,  C07D285/14 ,  C07D498/04

    CPC分类号： C07D285/14 ,  C07D207/48

    摘要： Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure wherein R1 is hydrogen (H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, arylalkyl or substituted arylalkyl, CO2R4a, CONR4aR4b, and CH2OR4a; R2 is hydrogen (H), OR3, SR3, halo, NHR3, NHCOR4c1, NHCO2R4c1, NHCONR4cR4d and NHSO2R4c; R3 in each functional group is hydrogen (H), alkyl or substituted alkyl, CHF2, CF3 and CON4e; R4, R4a, R4b, R4c, R4c1, R4d, R4e, R4f, R4g, or R4h in each functional group are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R5 and R5′ are the same or different and are hydrogen(H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl, wherein at least one of R5 and R5′ is hydrogen, or R5 and R5′ taken together form a double bond with oxygen (O), sulfur (S), NR7 or CR7R7′; where R7 and R7′ are as defined herein; G is an aryl, heterocyclo or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; and n is an integer of 1 or 2, m is an integer of 1 or 2, Z is oxygen (—O—) or NR4h, a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.

    Method of using 3-cyano-4-arylpyridine derivatives as modulators of androgen receptor function
    7.
    发明申请
    Method of using 3-cyano-4-arylpyridine derivatives as modulators of androgen receptor function 审中-公开
    使用3-氰基-4-芳基吡啶衍生物作为雄激素受体功能的调节剂的方法

    公开(公告)号：US20050182105A1

    公开(公告)日：2005-08-18

    申请号：US11048437

    申请日：2005-02-01

    申请人： Alexandra Nirschl ,  Lawrence Hamann

    发明人： Alexandra Nirschl ,  Lawrence Hamann

    IPC分类号： A61K31/44 ,  A61K31/4439 ,  A61K45/06

    CPC分类号： A61K45/06 ,  A61K31/44 ,  A61K31/4439 ,  A61K2300/00

    摘要： A method is provided for treating androgen receptor-associated conditions such as age-related diseases, for example sarcopenia, employing a compound of the structure wherein R1 is CN or H; X is O or S; R2 is alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R3 and R4 are the same or different and are independently selected from H, C(O)R2a, alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; R2a is alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl or substituted heteroaryl; G is aryl or heteroaryl, or aryl or heteroaryl substituted with one, two, three, four or five, where possible, of the substituents selected from the group consisting of hydrogen (H), halo, NO2, CN, OR2b, OH, CF3, NR3aR4a; wherein R3a and R4a, and R2b are the same or different and are independently selected from alkyl or substituted alkyl, cycloalkyl or substituted cycloalkyl, arylalkyl or substituted arylalkyl, aryl or substituted aryl, or heteroaryl and substituted heteroaryl; or a pharmaceutically acceptable salt thereof and a prodrug ester thereof.

    摘要翻译： 提供了一种用于治疗雄激素受体相关病症例如年龄相关疾病，例如肌钙蛋白减少症的方法，使用其中R 1为CN或H的结构的化合物; X是O或S; R 2是烷基或取代的烷基，环烷基或取代的环烷基，芳基烷基或取代的芳基烷基，芳基或取代的芳基或杂芳基或取代的杂芳基; R 3和R 4相同或不同，独立地选自H，C（O）R 2a，烷基或取代的烷基， 环烷基或取代的环烷基，芳基烷基或取代的芳基烷基，芳基或取代的芳基，或杂芳基或取代的杂芳基; R 2a是烷基或取代的烷基，环烷基或取代的环烷基，芳烷基或取代的芳基烷基，芳基或取代的芳基或杂芳基或取代的杂芳基; G是芳基或杂芳基，或在可能的情况下用一个，两个，三个，四个或五个取代基取代的芳基或杂芳基，所述取代基选自氢（H），卤素， ，CN，OR 2b，OH，CF 3，NR 3a，R 4a， 其中R 3a和R 4a和R 2b相同或不同，并且独立地选自烷基或取代的烷基，环烷基或取代的环烷基 ，芳基烷基或取代的芳基烷基，芳基或取代的芳基，或杂芳基和取代的杂芳基; 或其药学上可接受的盐和其前药酯。