3-Aryloxy/thio-3-substituted propanamines and their use in inhibiting serotonin and norephinephrine reuptake
申请人:Boulet Louis Serge
公开号:US20060014779A1
公开(公告)日:2006-01-19
There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C
2
-C
8
alkyl, C
2
-C
8
alkenyl, C
3
-C
8
cycloalkyl and C
4
-C
8
cycloalkylalkyl, each of which may be optionally substituted with up to
3
substituents each independently selected from halo, C
1
-C
4
alkyl, C
1
-C
4
alkoxy, C
1
-C
4
alkyl-S(O)
n
— where n is
0, 1
or
2
, —CF
3
, —CN and —CONH
2
; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl,
1,3
-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to
4
or, where possible,
5
substituents each independently selected from halo, C
1
-C
4
alkyl, C
1
-C
4
alkoxy, C
1
-C
4
alkyl-S(O)
n
— where n is
0, 1
or
2
, nitro, acetyl, —CF
3
, —SCF
3
and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C
1
-C
4
alkyl; Z is selected from H, OR
3
or F, wherein R
3
is selected from H, C
1
-C
6
alkyl and phenyl C
1
-C
6
alkyl; R
1
and R
2
are each independently H or C
1
-C
4
alkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl.
提供了一种化合物,其化学式为(I),其中A从—O—和—S—中选择;X从C2-C8烷基,C2-C8烯基,C3-C8环烷基和C4-C8环烷基烷基中选择,每种基团均可选用最多3个取代基,每个取代基可独立地从氯,C1-C4烷基,C1-C4烷氧基,C1-C4烷基-S(O)n-其中n为0,1或2,—CF3,—CN和—CONH2中选择;Y从苯基,萘基,二氢苯并噻吩基,苯并噻唑基,苯并异噻唑基,喹啉基,异喹啉基,萘啉基,噻吩基,茚基,1,3-苯并二氧杂环基,苯并噻吩基,吲哚基和苯并呋喃基中选择,每种基团均可选用最多4个或在可能的情况下最多5个取代基,每个取代基可独立地从氯,C1-C4烷基,C1-C4烷氧基,C1-C4烷基-S(O)n-其中n为0,1或2,硝基,乙酰基,—CF3,—SCF3和氰基中选择;当Y为吲哚基时,它可以被一个N-取代基所取代,所述取代基从C1-C4烷基中选择;Z从H,OR3或F中选择,其中R3从H,C1-C6烷基和苯基C1-C6烷基中选择;R1和R2各自独立地为H或C1-C4烷基;但是,当Z为H时,Y可能不是可选取代的苯基或可选取代的萘基。