公开(公告)号：US20110159019A1

公开(公告)日：2011-06-30

申请号：US13061311

申请日：2009-08-31

申请人： Akira Tanaka ,  Koichiro Mukoyoshi ,  Shigeki Kunikawa ,  Yuji Takasuna ,  Jun Maeda ,  Noboru Chida ,  Shinya Nagashima

发明人： Akira Tanaka ,  Koichiro Mukoyoshi ,  Shigeki Kunikawa ,  Yuji Takasuna ,  Jun Maeda ,  Noboru Chida ,  Shinya Nagashima

IPC分类号： A61K31/551 ,  C07D403/12 ,  C07D401/12 ,  C07D239/48 ,  C07D413/12 ,  C07D405/12 ,  C07D409/12 ,  C07D405/14 ,  C07D413/14 ,  A61K31/506 ,  A61K31/505 ,  A61K31/5377 ,  A61P37/06

CPC分类号： C07D239/48

摘要： Provided is a compound which is useful as an active ingredient for a pharmaceutical having a PKCθ inhibition activity, particularly a pharmaceutical composition for inhibiting acute rejection occurring in transplantation. The present inventors have conducted extensive studies on a compound having a PKCθ inhibition activity, and as a result, they have found that a compound having a structure such as aralkyl and the like on an amino group at the 2-position and also having a structure such as an adamantylalkyl group and the like on an amino group at the 4-position of 2,4-diaminopyrimidine, or a salt thereof has an excellent PKCθ inhibition activity, thereby completing the present invention. The 2,4-diaminopyrimidine compound of the present invention can be used as a PKCθ inhibitor or an inhibitor of acute rejection occurring in transplantation.

摘要翻译： 提供可用作具有PKC和药物的药物的活性成分的化合物; 特别是用于抑制移植中发生急性排斥反应的药物组合物。 本发明人对具有PKC的化合物进行了广泛的研究; 抑制活性，结果发现，在2-位的氨基上具有芳烷基等结构的化合物，还具有金刚烷基烷基等的结构，氨基上的氨基上 2,4-二氨基嘧啶的4位或其盐具有优异的PKC和重量; 从而完成了本发明。 本发明的2,4-二氨基嘧啶化合物可以用作PKC＆amp; 抑制剂或移植中发生的急性排斥抑制剂。