申请人:Kalindjian Sarkis Barret
公开号:US06878736B1
公开(公告)日:2005-04-12
Compounds of formula (I) (and pharmaceutically acceptable salts thereof) are histamine H
3
receptor ligands. A in the formula represents (CH
2
)
m
, m being from 1 to 3; B is (CH
2
)
n
, n being from 1 to 3; x is from 0 to 2; R
1
is C
1
to C
10
hydrocarbyl, in which up to 2 carbon atoms may be replaced by O, S or N; and up to 2 hydrogen atoms may be replaced by halogen; R
2
is H or C
1
to C
15
hydrocarbyl, in which up to 3 carbon atoms may be replaced by O, S or N, and up to 3 hydrogen atoms may be replaced by halogen; R
3
is absent when —Y—Z—R
2
is attached to W, or is H or C
1
to C
7
hydrocarbyl when —Y—Z—R
2
is not attached to W; W is nitrogen; X is —CH
2
—, —O— or —NR
4
—, R
4
being H or C
1
to C
3
alkyl; Y replaces a hydrogen atom on any of A, B, W and X, and is C
2
to C
10
alkylene, in which one non-terminal carbon atom may be replaced by O; and Z is (II), (III), (IV), (V), (VI), or (VII) wherein R
5
, R
6
and R
7
are independently H or C
1
to C
15
hydrocarbyl, in which up to 3 carbon atoms may be replaced by O or N, and up to 3 hydrogen atoms may be replaced by halogen, and Q is H or methyl, or Q is linked to R
5
or R
7
to form a five-membered ring or Q is linked to R
2
to form a six-membered ring
公式(I)的化合物(及其药学上可接受的盐)是组胺H3受体配体。 公式中的A代表(CH2)m,其中m为1至3; B为(CH2)n,其中n为1至3; x为0至2; R1为C1至C10烃基,其中最多可有2个碳原子被O,S或N取代; 最多可将2个氢原子替换为卤素; R2为H或C1至C15烃基,其中最多可有3个碳原子被O,S或N取代,最多可将3个氢原子替换为卤素; 当-Y-Z-R2连接到W时,R3不存在,或当-Y-Z-R2未连接到W时,R3为H或C1至C7烃基; W为氮; X为—CH2—,—O—或—NR4—,其中R4为H或C1至C3烷基; Y替换A,B,W和X中的任何一个氢原子,为C2至C10的烷基,其中一个非端碳原子可被O取代; Z为(II),(III),(IV),(V),(VI)或(VII),其中R5,R6和R7独立地为H或C1至C15烃基,其中最多可有3个碳原子被O或N取代,最多可将3个氢原子替换为卤素,Q为H或甲基,或Q与R5或R7连接形成五元环,或Q与R2连接形成六元环。