[EN] NICOTINIC RECEPTOR NON-COMPETITIVE ANTAGONISTS<br/>[FR] ANTAGONISTES NON COMPÉTITIFS DU RÉCEPTEUR NICOTINIQUE
申请人:TARGACEPT INC
公开号:WO2014004417A1
公开(公告)日:2014-01-03
The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for their use, and their pharmaceutical compositions.
本发明涉及调节尼古丁受体的化合物,作为非竞争性拮抗剂,其合成方法,使用方法以及它们的药物组合物。
Reactions of halonorbornane and oxo-substituted derivatives with different anions by the electron transfer mechanism; redox catalysis in stabilized radicals
作者:Jorge G. Uranga、Ana N. Santiago
DOI:10.1039/b9nj00503j
日期:——
3-chloronorbornan-2-one and 3-bromocamphor with Me3Sn−, Ph2P− or PhS− ions were studied by an SRN1 mechanism in liquid ammonia or DMSO. The results show that substrates having a carbonyl group facilitate electrontransfer reactions, which are impeded in the absence of such a group. However, when the free radical formed is stabilized by conjugation, the coupling reaction decreases, causing a concomitant increase
Compounds of the formula (I), (II), and wherein R
1
, R
2
, R′
2
and R′″
2
for example are C
1
-C
20
alkyl; R
3
, R
4
, and R
5
for example independently of one another are hydrogen or a defined substituent provided that at least one of R
3
, R
4
or R
5
is other than hydrogen or C
1
-C
20
alkyl; R
6
, R
7
, R
8
, R′
6
, R′
7
, R′
8
, R″
6
, R″
7
, R′″6 and R′″7 for example independently of one another have one of the meanings as given for R
3
, R
4
, and R
5
; and R
9
for example is C
1
-C
20
alkyl; exhibit an unexpectedly good performance in photopolymerization reactions.
Compounds of the formula (I), wherein A
1
is formula (II); A
2
is formula (III); A
3
is formula (IV); A
4
is formula (V); w, x, y and z independently of each other are an integer from 0-4, provided that the sum of x+y+z is an integer from 2-4, corresponding to the valency of Q; M
1
, M
2
, M
3
and M
4
for example are a direct bond, CO or O; Y for example is a direct bond or S; Q is a (x+y)-valent linking group; R
1
is for example hydrogen, C
1
-C
20
alkyl or phenyl or naphthyl; R
2
and R″
2
for example are is hydrogen or C
1
-C
20
alkyl; R
3
, R
4
, R′
3
, R′
4
, R″
3
and R″
4
for example are hydrogen, halogen, phenyl, or C
1
-C
20
alkyl; and R
24
is for example a direct bond; exhibit an unexpectedly good performance in photopolymerization reactions.