发明名称 LOW MOLECULAR WEIGHT THYROID STIMULATING HORMONE RECEPTOR (TSHR) AGONISTS
摘要 Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
申请公布号 US2014301944(A1) 申请公布日期 2014.10.09
申请号 US201414243821 申请日期 2014.04.02
申请人 Forschungsverbund Berlin E.V. ;The United States of America, as represented by the Secretary, Department of Health and Human Serv 发明人 Gershengorn Marvin C.;Neumann Susanne;Raaka Bruce M.;Thomas Craig J.;Inglese James;Southall Noel T.;Titus Steven;Huang Wenwei;Krause Gerd;Kleinau Gunnar;Zheng Wei
分类号 C07D405/06;C07D239/91;A61K31/517;A61K49/00;A61K51/00 主分类号 C07D405/06
代理机构 代理人
主权项 1. A method for detecting thyroid cancer in a subject, comprising administering to the subject in need thereof a diagnostically effective amount of at least one compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1-R4 are each independently H, hydroxyl, alkyl, alkoxy, aminocarbonyl, or halogen; R5 is H, alkyl, aryl, aralkyl, or aminocarbonyl; A represents —N═C(R15)— (wherein a bond at the left end bonds to the benzene ring of formula I above and a bond at the right end bonds to the nitrogen heteroatom of formula I above) or —NH—CH(R15)— (wherein a bond at the left end bonds to the benzene ring of formula I above and a bond at the right end bonds to the nitrogen heteroatom of formula I above); R15 is represented by formula II: wherein: R6-R9 are each independently H, hydroxyl, alkyl, or alkoxy; R10-R14 are each independently H, hydroxyl, alkyl, alkoxy, or aminocarbonyl; and X is O, S or N(H).
地址 Berlin-Adlershof DE