申请人:FUJIWARA Hideyasu
公开号:US20130116430A1
公开(公告)日:2013-05-09
An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R
1
represents a halogen atom; R
2
represents a C
1-12
alkyl group, a C
2-12
alkenyl group, a C
2-12
alkynyl group, a C
3-8
cycloalkyl group, an aryl group, an ar-C
1-6
alkyl group or a heterocyclic group, each optionally having at least one substituent; R
3
represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R
4
and R
5
each independently represent a hydrogen atom; and R
2
and R
4
may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
本发明的目的是提供一种具有优异的Syk抑制活性的化合物和制药组合物。本发明提供了一种由以下式(I)表示的烟酰胺衍生物(其中R1表示卤素原子;R2表示C1-12烷基、C2-12烯基、C2-12炔基、C3-8环烷基、芳基、芳基-C1-6烷基或杂环基,每种均可选地具有至少一个取代基;R3表示芳基或杂环基,每种均可选地具有至少一个取代基;R4和R5各自独立地表示氢原子;且R2和R4可以与它们结合的氮原子一起形成具有至少一个取代基的环状氨基团)或其盐,并且用于治疗Syk相关疾病的制药组合物包括该烟酰胺衍生物或其盐。