公开(公告)号：US20050043396A1

公开(公告)日：2005-02-24

申请号：US10674148

申请日：2003-09-29

Applicant: Hayley Zen ,  Shiqi Peng ,  Lanrong Bi ,  Ming Zhao ,  Chao Wang

Inventor： Hayley Zen ,  Shiqi Peng ,  Lanrong Bi ,  Ming Zhao ,  Chao Wang

IPC: C07D273/06 ,  C07D319/06 ,  C07D321/12 ,  A61K31/335

CPC classification number: C07D319/06 ,  C07D273/06 ,  C07D321/12

Abstract: The present invention discloses a series of benzoylamino-1,3-dioxacyclane compounds, of which compounds 1-21 were prepared via transacetalisation reaction between N-benzoylaminoglycol and 1,1,3,3-tetramethoxypropane; while compounds 22-48 were prepared via stereospecific acetalisation reaction between N-benzoylamino glycol and aromatic aldehyde, and if necessary, the nitro groups were reduced and further be salified with propane diacid and L-Arg or L-Lys. These compounds possess the structural type of PKC inhibitor and positive anti-inflammatory effect, and can be applied in medical fields as PKC inhibitor for corresponding therapy.

Abstract translation: 本发明公开了一系列苯甲酰基氨基-1,3-二氧杂环烷化合物，其中化合物1-21是通过N-苯甲酰氨基甘氨酸与1,1,3,3-四甲氧基丙烷之间的转化反应制备的; 而化合物22-48通过N-苯甲酰氨基二醇和芳族醛之间的立体特异性缩醛化反应制备，并且如果需要，硝基还原，并进一步用丙烷二酸和L-Arg或L-Lys进行成盐。 这些化合物具有PKC抑制剂的结构型和阳性消炎作用，可作为PKC抑制剂用于医学领域，用于相应的治疗。