申请人：——
公开号：US20020025965A1
公开（公告）日：2002-02-28
1
wherein:
R
1
, R
2
, R
3
and R
4
independently represent hydrogen, halogen, or alkyl, alkoxy, hydroxy, cyano, optionally substituted amino, nitro, carboxy, alkoxycarbonyl, optionally substituted aminocarbonyl or carbamoyl,
L
1
and L
2
each represents hydrogen or together form —CH
2
—CH
2
—,
X
1
, attached at the 2 or 3 position of the aromatic ring, represents a bond, and in that case X
2
represents hydrogen, halogen, or alkyl, alkoxy, hydroxy, nitro, cyano or optionally substituted amino, or X
1
and X
2
, together with two adjacent carbon to which they are bonded in the 2, 3 or 4 position of the aromatic ring, form a (C
4
-C
7
)cycloalkyl group, wherein one or two —CH
2
— of the cycloalkyl ring are optionally replaced by oxygen or NH,
X
3
represents hydrogen, halogen, or alkyl, alkoxy, hydroxy, nitro, cyano or optionally substituted amino,
G represents a group selected from:
2
wherein:
the broken lines indicate the optional presence of a double bond,
Alk represents linear or branched (C
1
-C
6
)alkylene,
n is 0 or 1,
T
3
represents alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl,
T
4
represents alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl,
and medicinal products containing the same are useful as dual &agr;
2
/5-HT
2c
antagonist receptors.
其中：R1、R2、R3 和 R4 分别代表氢、卤素或烷基、烷氧基、羟基、氰基、可选择地取代的氨基、硝基、羧基、烷氧羰基、可选择地取代的氨基羰基或氨基甲酰基，L1 和 L2 分别代表氢或共同形成 -CH2-CH2-，X1，连接在芳香环的2或3位，代表键，此时X2代表氢、卤素、烷基、烷氧基、羟基、硝基、氰基或可选择地取代的氨基，或X1 和 X2，与它们连接在芳香环的2、3或4位的两个相邻碳原子一起，形成一个(C4-C7)环烷基团，其中环烷基环的一个或两个-CH2-可选择地被氧或NH取代，X3 代表氢、卤素、烷基、烷氧基、羟基、硝基、氰基或可选择地取代的氨基，G 代表从中选择的一个基团：其中：虚线表示双键的可选存在，Alk 代表直链或支链(C1-C6)烷基，n 为0或1，T3 代表烷基、可选择地取代的芳基、可选择地取代的芳基烷基、可选择地取代的杂环芳基或可选择地取代的杂环芳基烷基，T4 代表烷基、可选择地取代的芳基、可选择地取代的芳基烷基、可选择地取代的杂环芳基或可选择地取代的杂环芳基烷基，以及含有这些化合物的药物制品作为双α2/5-HT2C拮抗受体是有用的。
