Identification of amide bioisosteres of triazole Oxytocin antagonists
摘要:
A series of amides were investigated as potential bioisosteres of previously reported triazole Oxytocin antagonists. A range of potent analogues were identified, although SAR for potency and selectivity over the related V(1A) and V(2) receptors was found to be somewhat divergent from that observed for the corresponding triazole series. The high synthetic accessibility of this new amide series also facilitated the identification of a range of alternative left hand side (biaryl replacement) substituents which gave good levels of Oxytocin antagonism. (C) 2010 Elsevier Ltd. All rights reserved.
Identification of a urea bioisostere of a triazole oxytocin antagonist
摘要:
A series of azetidine ureas were investigated as potential bioisosteres of previously reported azetidinyltriazole oxytocin antagonists. Although potency was somewhat reduced in several close-in analogues, one compound, 9, was both a potent oxytocin antagonist and demonstrated significant selectivity over the closely related vasopressin V(1A) receptor. (C) 2010 Elsevier Ltd. All rights reserved.
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
1
The present invention provides compounds of formula I
and pharmaceutically acceptable salts thereof.
The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
Disclosed are compounds and pharmaceutically acceptable salts of Formula I
wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
, n, Q
1
, Q
2
, Q
3
, Y, and X
1
-X
4
are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
Derivatives of 3-aminocarbonylquinoline, pharmaceutical compositions containing them and processes and intermediates for their preparation
申请人:Edlin Christopher
公开号:US20070191426A1
公开(公告)日:2007-08-16
Compounds of formula (I)
or pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.