申请人:Allelix Biopharmaceuticals, Inc.
公开号:US20010049441A1
公开(公告)日:2001-12-06
Described herein are compounds with affinity for the 5-HT
6
receptor, which have the general formula I:
1
wherein:
R represents a group of Formula II or Formula III;
one of A, B D or E is a N atom, the remainder being CH groups;
R
1
is selected from the group consisting of SO
2
Ar, C(O)Ar, CH
2
Ar and Ar;
R
2
, R
3
and R
4
are independently selected from the group consisting of H and alkyl;
----- represents a single or double bond, with the proviso that there is only one double bond in the ring at a time;
n is an integer of from 1-3;
Z is selected from the group consisting of C, CH and N, provided that when ----- is a double bond, Z is C and when ----- is a single bond, Z is selected from CH and N;
Ar is an optionally substituted aryl group;
with the proviso that when R is a group of Formula II, R
1
is SO
2
Ar.
Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT
6
receptor is implicated, such as schizophrenia.
本文描述了具有对5-HT6受体亲和力的化合物,其具有通式I:其中:R表示式II或式III的基团;A、B、D或E中的一个是N原子,其余为CH基团;R1选自SO2Ar、C(O)Ar、CH2Ar和Ar组成的群;R2、R3和R4独立地选自H和烷基组成的群;-----表示单键或双键,但环中只有一个双键;n为1-3的整数;Z选自C、CH和N组成的群,但当-----为双键时,Z为C,当-----为单键时,Z选自CH和N;Ar是可选取代的芳基基团;但当R是式II的基团时,R1为SO2Ar。还描述了将这些化合物用作药物治疗5-HT6受体抑制相关的疾病,例如精神分裂症。