ERβ Ligands. Part 2: Synthesis and structure–activity relationships of a series of 4-hydroxy-biphenyl-carbaldehyde oxime derivatives
摘要:
A series of biphenyl carbaldehyde oximes (6) was prepared and shown to have significant selectivity for the estrogen receptor-beta (ERbeta). The exploitation of the oxime moiety as a hydrogen bond donating group, which mimicked the C-ring of genistein makes these compounds unique. Molecular modeling studies showed the oxime moiety hydrogen bonding to the histidine residue, which was supported by the structure-activity relationships. The most potent compounds in this study had IC50 values in a radio-liaand binding assay of between 8-35 nM. Among the most selective compounds were 6i and 6s (49- and 31-fold ERbeta selective, respectively). (C) 2004 Elsevier Ltd. All rights reserved.
Quinolines useful in treating cardiovascular disease
申请人:Collini D. Michael
公开号:US20050131014A1
公开(公告)日:2005-06-16
This invention provides compounds of formula I
that are useful in the treatment or inhibition of LXR mediated diseases.
本发明提供了式I化合物的用途,它们在治疗或抑制LXR介导的疾病中是有用的。
Benzo[ b ]thiophene-2-carboxamide derivatives as potent urotensin-II receptor antagonists
作者:Chae Jo Lim、Seong Eun Woo、Su Ik Ko、Byung Ho Lee、Kwang-Seok Oh、Kyu Yang Yi
DOI:10.1016/j.bmcl.2016.08.049
日期:2016.10
Members of a series of benzo[b]thiophene-2-carboxamide derivatives, possessing an N-(1-(3-bromo-4-(piperidin-4-yloxy)benzyl)piperidin-4-yl) group, were synthesized and evaluated as urotensin-II receptor antagonists. The results show that these substances have potent UT binding affinities. Observations made in a systematic SAR investigation of the effects of a variety of substituents (R(1) and R(2))
Hydroxy-biphenyl-carbaldehyde oxime derivatives and their use as estrogenic agents
申请人:Mewshaw Eric Richard
公开号:US20050020676A1
公开(公告)日:2005-01-27
This invention provides estrogen receptor modulators having the structure:
wherein R
1
to R
6
and R
8
are as defined in the specification; or a pharmaceutically acceptable salt thereof.
Hydroxy-Biphenyl-Carbaldehyde Oxime Derivatives and Their Use As Estrogenic Agents
申请人:Mewshaw Eric Richard
公开号:US20080033049A1
公开(公告)日:2008-02-07
This invention provides estrogen receptor modulators having the structure:
wherein R
1
to R
6
and R
8
are as defined in the specification; or a pharmaceutically acceptable salt thereof.
该发明提供了具有以下结构的雌激素受体调节剂:其中R1至R6和R8如规范中定义;或其药用盐。
Quinolines and pharmaceutical compositions thereof
申请人:Wyeth
公开号:US07576215B2
公开(公告)日:2009-08-18
This invention provides compounds of formula I
that are useful in the treatment or inhibition of LXR mediated diseases.