An efficient one pot transfer hydrogenation and N-alkylation of quinolines with alcohols mediated by Pd/C/Zn
作者:Belén Abarca、Rosa Adam、Rafael Ballesteros
DOI:10.1039/c1ob05888f
日期:——
A Pd/C/Zn mixture with alcohols has been revealed to be an efficient transfer hydrogenation system to quinolines. Furthermore, the metals mixture is able to activate alcohols as N-alkylating agents in a hydrogen autotransfer process. 1,2,3,4-Tetrahydroquinolines and N-alkylated tetrahydroquinolines from quinolines have been obtained with excellent yields in one step.
[EN] INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS<br/>[FR] NOUVEAUX COMPOSÉS
申请人:GLAXO GROUP LTD
公开号:WO2009050244A1
公开(公告)日:2009-04-23
The present invention provides compounds of formula (I), a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation and/or allergic conditions.
Compounds of formula I:
(wherein variables A
1
, A
2
, A
3
, A
4
, A
5
, A
6
, A
7
, B, E
1
, E
2
, E
3
, E
4
, E
5
, G
1
, G
2
, J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
PYRIDAZINONE COMPOUNDS AND P2X7 RECEPTOR INHIBITORS
申请人:Shigeta Yukihiro
公开号:US20100286390A1
公开(公告)日:2010-11-11
Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.
Compounds of formula I:
(wherein variables A
1
, A
2
, A
3
, A
4
, A
5
, A
6
, A
7
, B, E
1
, E
2
, E
3
, E
4
, E
5
, G
1
, G
2
and R
6
are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.