公开(公告)号：EP1567487A2

公开(公告)日：2005-08-31

申请号：EP03808410.9

申请日：2003-11-13

申请人： Bristol-Myers Squibb Company

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

IPC分类号： C07D207/04 ,  C07D211/06 ,  A61K31/445 ,  A61K31/401 ,  A61P3/04 ,  A61P3/10 ,  A61P9/12 ,  A61P25/22 ,  A61P25/24

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 R1, R2, R3, 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雄激素受体的药物组合物，其包含式（I）的化合物，其中R 1，R 2，R 3，X，Y，Z和G如本文所述。 进一步提供了使用这种化合物治疗核激素受体相关病症如年龄相关疾病例如肌肉减少症的方法，并且还提供了含有这些化合物的药物组合物。

公开(公告)号：EP1718626A1

公开(公告)日：2006-11-08

申请号：EP05712320.0

申请日：2005-02-02

申请人： Bristol-Myers Squibb Company

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

IPC分类号： C07D285/06 ,  A61K31/433

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); whereinR1 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 COR4e; 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.