[EN] ESTROGEN RECEPTOR MODULATORS AND USES THEREOF<br/>[FR] MODULATEURS DE RÉCEPTEURS D'OESTROGÈNES ET LEURS UTILISATIONS
申请人:SERAGON PHARMACEUTICALS INC
公开号:WO2013142266A1
公开(公告)日:2013-09-26
Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure:
or a pharmaceutically acceptable salt thereof,
wherein R
1
is structure (a), (b), (c) or (d):
and R
a
, R
b
, R
c
, R
2
, R
3
, R
4
, R
5
, R
6
and R
7
are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed, as well as uses of the same to treat a condition or disorder mediated by a Syk and/or JAK kinase.
化合物,特别是具有脾酪氨酸激酶(Syk)抑制活性的化合物,具有以下结构:
或其药学上可接受的盐,
其中R
1
为结构(a)、(b)、(c)或(d):
而R
a
,R
b
,R
c
,R
2
,R
3
,R
4
,R
5
,R
6
和R
7
如本文所定义。涉及其制备和使用的方法,以及含有其的药物组合物,也被揭示,以及使用其来治疗由Syk和/或JAK激酶介导的疾病或疾病。
BICYCLIC HETEROCYCLIC DERIVATIVES AS MNK1 AND MNK2 MODULATORS AND USES THEREOF
申请人:Agency for Science, Technology and Research
公开号:US20140371199A1
公开(公告)日:2014-12-18
The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.