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    THIENOPYRIMIDINONE DERIVATIVES AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
    1.
    发明申请
    THIENOPYRIMIDINONE DERIVATIVES AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
    作为MELANIN浓缩激素受体-1拮抗剂的三烯酰基嘧啶衍生物

    公开(公告)号：WO2007050726A3

    公开(公告)日：2007-08-30

    申请号：PCT/US2006041725

    申请日：2006-10-26

    申请人： SQUIBB BRISTOL MYERS CO ,  WASHBURN WILLIAM N ,  HERNANDEZ ANDRES S ,  MANFREDI MARK C ,  ROBL JEFFREY A

    发明人： WASHBURN WILLIAM N ,  HERNANDEZ ANDRES S ,  MANFREDI MARK C ,  ROBL JEFFREY A

    IPC分类号： C07D495/04 ,  A61K31/522 ,  A61P5/00 ,  A61P25/00

    CPC分类号： C07D495/04

    摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

    摘要翻译： 本申请提供化合物，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。 最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法。

    OPEN CHAIN PROLYL UREA-RELATED MODULATORS OF ANDROGEN RECEPTOR FUNCTION
    2.
    发明申请
    OPEN CHAIN PROLYL UREA-RELATED MODULATORS OF ANDROGEN RECEPTOR FUNCTION 审中-公开
    OPEN链与尿素相关的调节器的雄激素受体功能

    公开(公告)号：WO2004045518A2

    公开(公告)日：2004-06-03

    申请号：PCT/US2003/036331

    申请日：2003-11-13

    申请人： BRISTOL-MYERS SQUIBB COMPANY ,  HAMANN, Lawrence, G. ,  AUGERI, David, J. ,  MANFREDI, Mark, C.

    发明人： HAMANN, Lawrence, G. ,  AUGERI, David, J. ,  MANFREDI, Mark, C.

    IPC分类号： A61K

    CPC分类号： C07D207/16 ,  C07D401/12

    摘要： The invention provides for a pharmaceutical composition capable of modulating the androgen receptor comprising a compound of formula (I), wherein R 1 , R 2 , R 3 , X, Y, Z and G are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.

    摘要翻译： 本发明提供能够调节包含式（I）化合物的雄激素受体的药物组合物，其中R 1，R 2，R 3，X，Y，Z和G如本文所述。 还提供了使用这些化合物治疗核激素受体相关病症（如与年龄有关的疾病，例如肌肉减少症）的方法，并且还提供含有这些化合物的药物组合物。

    NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
    4.
    发明申请
    NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
    非基础麦芽宁浓缩激素受体-1拮抗剂

    公开(公告)号：WO2007050726A2

    公开(公告)日：2007-05-03

    申请号：PCT/US2006/041725

    申请日：2006-10-26

    申请人： BRISTOL-MYERS SQUIBB COMPANY ,  WASHBURN, William N. ,  HERNANDEZ, Andres S. ,  MANFREDI, Mark C. ,  ROBL, Jeffrey, A.

    发明人： WASHBURN, William N. ,  HERNANDEZ, Andres S. ,  MANFREDI, Mark C. ,  ROBL, Jeffrey, A.

    IPC分类号： C07D495/04 ,  A61K31/522 ,  A61P5/00 ,  A61P25/00

    CPC分类号： C07D495/04

    摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

    摘要翻译： 本申请提供化合物，包括根据式I的所有立体异构体，溶剂合物，前药和药学上可接受的形式。另外，本申请提供含有至少一种根据式I的化合物和任选的至少一种另外的治疗剂的药物组合物。 最后，本申请提供了通过施用治疗有效剂量的根据式I的化合物治疗患有MCHR-1调节的疾病或病症例如肥胖，糖尿病，抑郁或焦虑的患者的方法。

    SULFONYLPYRROLODINE MODULATORS OF ANDROGEN RECEPTOR FUCTION AND METHOD
    5.
    发明申请
    SULFONYLPYRROLODINE MODULATORS OF ANDROGEN RECEPTOR FUCTION AND METHOD 审中-公开
    雄激素受体拮抗剂和方法的磺酰吡咯烷酮调节剂

    公开(公告)号：WO2005077925A1

    公开(公告)日：2005-08-25

    申请号：PCT/US2005/002834

    申请日：2005-02-02

    申请人： BRISTOL-MYERS SQUIBB COMPANY ,  HAMANN, Lawrence, H. ,  BI, Yingzhi ,  MANFREDI, Mark, C. ,  NIRSCHL, Alexandra, A. ,  SUTTON, James, C.

    发明人： HAMANN, Lawrence, H. ,  BI, Yingzhi ,  MANFREDI, Mark, C. ,  NIRSCHL, Alexandra, A. ,  SUTTON, James, C.

    IPC分类号： C07D285/06

    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 of formulae (I) or (II); whereinR 1 is hydrogen (H), alkyl or substituted alkyl, alkenyl or substituted alkenyl, arylalkyl or substituted arylalkyl, CO 2 R 4a , CONR 4a R 4b , and CH 2 OR 4a ; R 2 is hydrogen (H), OR 3 , SR 3 , halo, NHR 3 , NHCOR 4c1 , NHCO 2 R 4c1 , NHCONR 4c R 4d and NHSO 2 R 4c ; R 3 in each functional group is hydrogen (H), alkyl or substituted alkyl, CHF 2 , CF 3 and COR 4e ; R 4 , R 4a , R 4b , R 4c , R 4c1 , R 4d , R 4e , R 4f , R 4g , or R 4h 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; R 5 and R 5 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 R 5 and R 5 is hydrogen, or R 5 and R 5 taken together form a double bond with oxygen (O), sulfur (S), NR 7 or CR 7 R 7 ; where R 7 and R 7 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 NR 4h , 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.

    摘要翻译： 提供了可用于治疗雄激素受体相关病症例如年龄相关疾病的化合物，该化合物具有式（I）或（II）结构; 其中R 1是氢（H），烷基或取代的烷基，烯基或取代的烯基，芳基烷基或取代的芳基烷基，CO 2 R 4 a，CONR 4 a R 4 b和CH 2 OR 4 a; R2是氢（H），OR3，SR3，卤素，NHR3，NHCOR4c1，NHCO2R4c1，NHCONR4cR4d和NHSO2R4c; 每个官能团中的R 3是氢（H），烷基或取代的烷基，CHF 2，CF 3和COR 4e; 每个官能团中的R 4，R 4a，R 4b，R 4c，R 4c 1，R 4d，R 4c，R 4c，R 4，R 4，R 4e或R 4h相同或不同，为氢（H），烷基或取代的烷基，烯基或取代的烯基，炔基或取代的炔基 芳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 5和R 5相同或不同，为氢（H），烷基或取代的烷基，烯基或取代的烯基，炔基或取代的炔基，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 其中R 5和R 5中的至少一个是氢，或者R 5和R 5一起与氧（O），硫（S），NR 7或CR 7 R 7形成双键; 其中R7和R7如本文所定义; G是芳基，杂环或杂芳基，其中所述基团是单环或多环，并且其任选被取代; n为1或2的整数，m为1或2的整数，Z为氧（-O-）或NR4h，前药酯，其全部立体异构体和药学上可接受的盐。 还提供了治疗雄激素受体相关病症如年龄相关疾病的方法。