Novel aminotriazolone compounds, method for preparing same and pharmaceutical compositions containing same
申请人:——
公开号:US20040029875A1
公开(公告)日:2004-02-12
A compound of formula (I):
1
wherein:
R
1
and R
2
represent hydrogen or a group as defined in the description,
R
3
represents hydrogen or alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl,
R
4
represents a group of formula (II):
2
wherein W and B are as defined in the description,
R
5
represents hydrogen or alkyl,
A represents a group selected from -A
2
-, -A
1
-A
2
-, -A
2
-A
1
- and -A
1
-A
2
-A
1
-,
V is as defined in the description.
NOVEL INDOLE DERIVATIVES AND THEIR USE IN NEURODEGENERATIVE DISEASES
申请人:Merck Patent GmbH
公开号:US20160168090A1
公开(公告)日:2016-06-16
The present invention relates to indole compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.
本发明涉及吲哚化合物及其药用可接受的组合物,用作P2X7拮抗剂,用于治疗与P2X7相关的疾病。
SUBSTITUTED IMIDAZOPYRIDAZINES AND BENZIMIDAZOLES AS INHIBITORS OF FGFR3
申请人:YAO Wenqing
公开号:US20120165305A1
公开(公告)日:2012-06-28
The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.
Disclosed herein are modulators of TRPV3 of formula (I)
wherein X
1
, X
2
, R
1
, R
2
, R
x
, and n are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
作者:Susanne Berglund、Bryan J. Egner、Henrik Gradén、Joakim Gradén、David G.A. Morgan、Tord Inghardt、Fabrizio Giordanetto
DOI:10.1016/j.bmcl.2009.05.066
日期:2009.8
The discovery and optimization of piperidin-4-yl-urea derivatives as MCH-R1 antagonists is herein described. Previous work around the piperidin-4-yl-amides led to the discovery of potent MCH-R1 antagonists. However, high affinity towards the hERG potassium channel proved to be an issue. Different strategies to increase hERG selectivity were implemented and resulted in the identification of piperidin-4-yl-urea