申请人:——
公开号:US20020161000A1
公开(公告)日:2002-10-31
Selective MMP-13 inhibitors are pyridine derivatives of the formula
1
or a pharmaceutically acceptable salt thereof,
wherein:
R
1
and R
2
independently are hydrogen, halo, hydroxy, C
1
-C
6
alkyl, C
1
-C
6
alkoxy, C
2
-C
6
alkenyl, C
2
-C
6
alkynyl, NO
2
, NR
4
R
5
, CN, or CF
3
,
E is independently O or S;
A and B independently are OR
4
or NR
4
R
5
;
R
4
and R
5
independently are H. C
1
-C
6
alkyl, C
2
-C
6
alkenyl, C
2
-C
6
alkynyl, (CH
2
)
n
aryl, (CH
2
)
n
cycloalkyl, (CH
2
)
n
heteroaryl, or R
4
and R
5
when taken together with the nitrogen to which they are attached complete a 3 to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted,
n is an integer of from 0 to 6.
选择性MMP-13抑制剂是符合以下结构式1的吡啶衍生物或其药用盐,其中:
R1和R2独立地是氢、卤素、羟基、C1-C6烷基、C1-C6烷氧基、C2-C6烯基、C2-C6炔基、NO2、NR4R5、CN或CF3;
E独立地是O或S;
A和B独立地是OR4或NR4R5;
R4和R5独立地是H、C1-C6烷基、C2-C6烯基、C2-C6炔基、(CH2)n芳基、(CH2)n环烷基、(CH2)n杂环芳基,或者R4和R5当与它们连接的氮一起形成含碳原子的3至8元环,可选地含有O、S或NH等杂原子,并可选择性地取代或未取代;
n是0到6的整数。