申请人:Mikoshiba Katsuhiko
公开号:US20120277423A1
公开(公告)日:2012-11-01
The present invention relates to: a ketone compound having transglutaminase-inhibiting activity, which is represented by the following Formula 1, 2, or 3:
wherein R
1
is a substituted or unsubstituted aryl or heterocyclyl group, R
2
, R
3
, and R
4
are hydrogen atoms, n is 2, X is halogen, R
5
and R
6
independently represent a hydrogen atom or a substituted or unsubstituted C1-C10 alkyl, aryl, or aralkyl group, wherein R
5
and R
6
are not hydrogen atoms at the same time, or R
5
and R
6
may be taken together to form a saturated or unsaturated and substituted or unsubstituted heterocyclyl group containing a nitrogen atom (N); an inhibitor of protein crosslinking comprising the compound; and a composition for preventing or treating a protein-crosslinking causative disease, which comprises the compound or the protein crosslinking inhibitor.
本发明涉及:一种具有转谷氨酰胺酶抑制活性的酮化合物,由下式1、2或3表示:
其中R1是取代或未取代的芳基或杂环基团,R2、R3和R4是氢原子,n是2,X是卤素,R5和R6独立地表示氢原子或取代或未取代的C1-C10烷基、芳基或芳烷基团,其中R5和R6不同时为氢原子,或者R5和R6可以共同形成含氮原子(N)的饱和或未饱和的、取代或未取代的杂环基团;包含该化合物的蛋白质交联抑制剂;以及包含该化合物或蛋白质交联抑制剂的用于预防或治疗由蛋白质交联引起的疾病的组合物。