Compounds Comprising an Oxazoline or Thiazoline Moiety, Processes for Making Them, and Their Uses
申请人:Leurs Regorius
公开号:US20080161331A1
公开(公告)日:2008-07-03
The present invention relates to compounds comprising an oxazoline or thiazoline moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H
3
-receptor ligands, (I), wherein A
1
is CH C(CH
3
) or N; R
1
is hydrogen or halogen; R
2
is (II); A
2
is O or S; R
3
is hydrogen, halogen, C
1-4
alkyl or C
1-4
alkoxy; R
4
is hydrogen, halogen, C
1-4
alkyl, C
1-4
alkoxy, trifluoromethyl or —O—(CH
2
)n-NR
12a
R
each CH
2
in —O—(CH
2
)n-NR
12a
R
12b being optionally substituted by one or two C
1-4
alkyl; R
5
is hydrogen or —O—(CH
2
)
m
—NR
13a
R
13b
, each CH
2
in —O—(CH
2
)
m
—NR
13a
R
13b
being optionally substituted by one or two C
1-4
alkyl, and at least one of R
4
and R
5
should be a —O—(CH
2
)n-NR
12/13a
R
12/13b
group.
本发明涉及包含氧唑啉或噻唑啉基团的化合物,制备它们的方法,包含所述化合物的制药组合物以及它们作为H3受体配体的用途,其中A1为CH、C(CH3)或N;R1为氢或卤素;R2为(II);A2为O或S;R3为氢、卤素、C1-4烷基或C1-4烷氧基;R4为氢、卤素、C1-4烷基、C1-4烷氧基、三氟甲基或-O-(CH2)n-NR12aR12b,其中-O-(CH2)n-NR12aR12b可以选择地被一个或两个C1-4烷基取代;R5为氢或-O-(CH2)m-NR13aR13b,每个-O-(CH2)m-NR13aR13b中的CH2可以选择地被一个或两个C1-4烷基取代,并且R4和R5中至少有一个应为-O-(CH2)n-NR12/13aR12/13b基团。