Propanolaminomethyltetralines, their preparation and pharmaceutical composition comprising same
申请人:Barzaghi Laura
公开号:US20050054641A1
公开(公告)日:2005-03-10
The invention concerns compounds of formula (1), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a —S(O)
z
(C
1
-C
4
)Alk wherein z is 0, 1 or 2, a —NHSO
2
(C
1
-C
4
)Alk, —SO
2
NH(C
1
-C
4
)Alk, —NHSO
2
—(C
1
-C
4
)Alk-phenyl or —NHSO
2
-phenyl group, said phenyl capable of bearing a halogen atom, a (C
1
-C
4
)Alk group or a (C
1
-C
6
)alkoxy group; R
1
represents a hydrogen atom or a —(C
1
-C
4
)Alk, —CO(C
1
-C
4
)Alk, —(C
1
-C
4
)Alk-phenyl or —CO-phenyl group, said phenyl capable of bearing a halogen atom or a —(C
1
-C
4
)Alk or (C
1
-C
6
)alkoxy group; R
2
is a hydrogen atom, a —SO
2
(C
1
-C
4
)Alk, —SO
2
—(C
1
-C
4
)Alk-phenyl, —SO
2
-phenyl group, or a —(C
1
-C
4
)Alk group; X completes a saturated or unsaturated cycle of 5 to 8 atoms, capable of bearing one or two —(C
1
-C
4
)Alk groups and/or two carbonyl groups; R
3
and R′
3
represent each independently a hydrogen or halogen atom, a —(C
1
-C
6
)Alk, hydroxy, —CN, —(C
1
-C
6
)alkoxy, —COR
4
or Y—CR
8
R
9
—COR
4
group; Y represents O or CH
2
; R
4
represents a hydroxy, (C
1
-C
6
)alkoxy or —NR
5
R
6
group; R
5
and R
6
independently represent a hydrogen atom, a —(C
1
-C
4
)Alk, group, aryl or heteroaryl optionally substituted by a R
7
group, aralkyl or heteroaralkyl optionally substituted by a R
7
group; or R
5
and R
6
, with the nitrogen atom which bears them, form a saturated or unsaturated cycle of 5 to 7 atoms optionally substituted by a R
7
group; and R
7
represents a hydrogen or halogen atom, a hydroxy, —(C
1
-C
4
)Alk, —(C
1
-C
6
)alkoxy, —NH(C
1
-C
4
)Alk, —N(C
1
-C
4
)Alk
2
, —COO(C
1
-C
4
)Alk, aralkyl or heteroaryl group; R
8
and R
9
independently represent a hydrogen atom or a —(C
1
-C
4
)Alk group; their salts or solvates, the pharmaceutical compositions containing them, a method for preparing them and synthesis intermediates.
本发明涉及公式(1)的化合物,其中A是公式(a)或(b)的基团,其中:R代表氢或卤素原子,-S(O)z(C1-C4)Alk,其中z为0,1或2,-NHSO2(C1-C4)Alk,-SO2NH(C1-C4)Alk,-NHSO2-(C1-C4)Alk-苯基或-NHSO2-苯基,所述苯基能够承载卤素原子,(C1-C4)Alk基团或(C1-C6)alkoxy基团;R1代表氢原子或-(C1-C4)Alk,-CO(C1-C4)Alk,-(C1-C4)Alk-苯基或-CO-苯基,所述苯基能够承载卤素原子或-(C1-C4)Alk或(C1-C6)alkoxy基团;R2是氢原子,-SO2(C1-C4)Alk,-SO2-(C1-C4)Alk-苯基,-SO2-苯基或-(C1-C4)Alk基团;X完成一个饱和或不饱和的5至8个原子环,能够承载一个或两个-(C1-C4)Alk基团和/或两个羰基基团;R3和R′3各自独立地代表氢或卤素原子,-(C1-C6)Alk,羟基,-CN,-(C1-C6)alkoxy,-COR4或Y-CR8R9-COR4基团;Y代表O或CH2;R4代表羟基,(C1-C6)alkoxy或-NR5R6基团;R5和R6独立地代表氢原子,-(C1-C4)Alk基团,芳基或杂环芳基,可选地被R7基团取代,芳基烷基或杂环芳基烷基,可选地被R7基团取代;或R5和R6与它们所承载的氮原子形成一个饱和或不饱和的5到7个原子环,可选地被R7基团取代;R7代表氢或卤素原子,羟基,-(C1-C4)Alk,-(C1-C6)alkoxy,-NH(C1-C4)Alk,-N(C1-C4)Alk2,-COO(C1-C4)Alk,芳基烷基或杂环芳基;R8和R9独立地代表氢原子或-(C1-C4)Alk基团;它们的盐或溶剂,含有它们的制药组合物,制备它们的方法和合成中间体。