TRICYCLIC PYRIDINE DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION
申请人:WAGNER Holger
公开号:US20120046304A1
公开(公告)日:2012-02-23
The present invention relates to compounds defined by formula I
wherein the variables R
1
-R
8
are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation
申请人:Wagner Holger
公开号:US20130053404A1
公开(公告)日:2013-02-28
The present invention relates to compounds defined by formula I
wherein the variables R
1
-R
8
are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.
There is disclosed a method for producing a biaryl compound of formula (I):
1
wherein R
1
is the same or different and independently denotes a substituted or unsubstituted hydrocarbon group or the like, A and B denote an aromatic hydrocarbon ring having from 6 to 14 carbon atoms or the like, k and m independently denote an integer of from 0 to 5, and 1 denotes an integer of 1 or 2, which method is characterized by reacting an aromatic compound of formula (II):
2
wherein R
1
, k and l denote the same as defined above, and X
1
denotes a leaving group, with a Grignard reagent of formula (III):
3
(R
2
). 9MgX
2
(IIIg)
wherein R
2
, B, and m denote the same as defined above and X
2
denotes chlorine or the like, in the presence of a cyclic ether, or an acyclic ether having two or more ether oxygens in the molecule and a nickel catalyst.