| 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 | US9187457(B2) | 申请公布日期 | 2015.11.17 |
| 申请号 | US201313897330 | 申请日期 | 2013.05.17 |
| 申请人 | The United States of America as represented by the Secretary of the Department of Health and Human Services;Forschungsverbund Berlin E.V. | 发明人 | Gershengorn Marvin C.;Neumann Susanne;Raaka Bruce M.;Thomas Craig J.;Inglese James;Southall Noel T.;Titus Steven;Zheng Wei;Huang Wenwei;Krause Gerd;Kleinau Gunnar |
| 分类号 | A61K51/00;C07D239/88;C07D217/24;A61K31/47;A61P35/00;A61K31/167;A61K31/517;C07C233/01;C07D405/06;C07D239/91;C07D401/06;C07D405/14;C07D487/04;A61K49/00 | 主分类号 | A61K51/00 |
| 代理机构 | Klarquist Sparkman, LLP | 代理人 | Klarquist Sparkman, LLP |
| 主权项 | 1. A compound having formula I: or a pharmaceutically acceptable salt thereof, wherein: R1-R4 are each independently H, hydroxyl, alkyl, alkoxy, aminocarbonyl, or halogen; R5 is —CH2-Ph, wherein Ph is a substituted phenyl; 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, R11, R13 and R14 are each independently H; R12 is acetamido; and X is O, S or N(H). | ||
| 地址 | Washington DC US | ||