申请人:——
公开号:US20020091131A1
公开(公告)日:2002-07-11
Novel epoxysuccinamide derivatives represented by the general formula (1) or physiologically acceptable salts thereof, which are useful particularly as remedies for bone diseases and arthritis, wherein R
1
and R
3
are each hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; R
2
is alkyl, alkenyl, alkynyl, aryl, aralkyl, a heterocyclic group, or a hetericyclic-alkyl group; X is —O— or —NR
4
— (wherein R
4
is hydrogen, alkyl, aryl, aralkyl, a heterocyclic group, or a heterocyclic-alkyl group; Y
1
is OR
5
, SR
6
, or NR
7
R
8
(wherein each of R
5
, R
6
and R
7
is hydrogen, alkyl, aryl, aralkyl, acyl, a heterocyclic group, or a heterocyclic-alkyl group, and R
8
is the same as defined for R
4
); and Y
2
is hydrogen or alkyl, or alternatively Y
1
and Y
2
can be combined to form ═O, ═S, ═N—R
9
, or ═N—OR
10
(wherein each of R
9
and R
10
is the same as defined for R
4
), provided that each of the alkyl, aryl and heterocyclic groups defined for R
5
to R
10
can have one or more specific substituents and that each of the group defined for R
1
to R
10
and Y
2
is specificed in the number of carbon atoms.
1
一种新型环氧琥珀酰亚胺衍生物,其通式表示为(1),或其生理上可接受的盐,特别适用于治疗骨疾病和关节炎。其中,R1和R3分别为氢、烷基、烯基、炔基、芳基、芳基烷基、杂环基或杂环烷基;R2为烷基、烯基、炔基、芳基、芳基烷基、杂环基或杂环烷基;X为—O—或—NR4—(其中R4为氢、烷基、芳基、芳基烷基、杂环基或杂环烷基);Y1为OR5、SR6或NR7R8(其中R5、R6和R7各自为氢、烷基、芳基、芳基烷基、酰基、杂环基或杂环烷基,R8与R4定义相同);Y2为氢或烷基,或者Y1和Y2可以结合形成═O、═S、═N—R9或═N—OR10(其中R9和R10各自为与R4定义相同),但是需要注意,R5到R10定义的烷基、芳基和杂环基可以有一个或多个特定的取代基,而R1到R10和Y2定义的每个基团的碳原子数是特定的。