申请人:——
公开号:US20040132738A1
公开(公告)日:2004-07-08
This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula:
1
In the above formula, each of
and
, independently, is a single bond or a double bond; A is H or CH(R
a
R
b
) when
is a single bond, or C(R
a
R
b
) when
is a double bond; Z is CH(R
c
R
d
) when
is a single bond, or C(R
c
R
d
) when
is a double bond; each of R
1
and R
2
, independently, is H, C(O)R
e
, C(O)OR
e
, C(O)NR
e
R
f
, or SO
2
R
e
; and each of R
a
, R
b
, R
c
, R
d
, R
e
, and R
f
, independently, is H, C
1
-C
6
alkyl, aryl, heteroaryl, C
3
-C
8
cycloalkyl, or C
3
-C
8
heterocycloalkyl; or R
a
and R
b
taken together are C
3
-C
8
cycloalkyl, C
3
-C
8
heterocycloalkyl, aryl, or heteroaryl; or R
1
and R
a
or R
1
and R
b
taken together are C
3
-C
8
cycloalkyl, C
3
-C
8
heterocycloalkyl, aryl, or heteroaryl; provided that one of R
c
and R
d
is aryl or heteroaryl.
本发明涉及一种治疗血管生成相关疾病的方法。该方法包括向需要治疗的受体内投入具有以下式子的哌嗪二酮化合物的有效量:1
在上述式子中,每个单独的和是单键或双键;当是单键时,A为H或CH(RaRb),当是双键时,A为C(RaRb);当是单键时,Z为CH(RcRd),当是双键时,Z为C(RcRd);每个单独的R1和R2为H、C(O)Re、C(O)ORe、C(O)NReRf或SO2Re;每个单独的Ra、Rb、Rc、Rd、Re和Rf为H、C1-C6烷基、芳基、杂环芳基、C3-C8环烷基或C3-C8杂环烷基;或Ra和Rb一起为C3-C8环烷基、C3-C8杂环烷基、芳基或杂环芳基;或R1和Ra或R1和Rb一起为C3-C8环烷基、C3-C8杂环烷基、芳基或杂环芳基;前提是Rc和Rd中的一个为芳基或杂环芳基。