公开(公告)号：US20060014708A1

公开(公告)日：2006-01-19

申请号：US11165912

申请日：2005-06-24

申请人： David Bartkovitz ,  Xin-Jie Chu ,  Allen Lovey ,  Peter Wovkulich

发明人： David Bartkovitz ,  Xin-Jie Chu ,  Allen Lovey ,  Peter Wovkulich

IPC分类号： A61K31/44 ,  A61K31/4439 ,  C07D401/02

CPC分类号： C07D213/73

摘要： Novel 2,6-diaminopyridine derivatives of formula wherein R1 and R2 are as defined below, are disclosed. These compounds inhibit cyclin-dependent kinases. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 2,6-diaminopyridine derivatives.

摘要翻译： 公开了下述新的2,6-二氨基吡啶衍生物，其中R 1和R 2定义如下。 这些化合物抑制细胞周期蛋白依赖性激酶。 这些化合物及其药学上可接受的盐和酯具有抗增殖活性，并且可用于治疗或控制癌症，特别是实体瘤。 本发明还涉及含有这些化合物的药物组合物以及治疗或控制癌症的方法，特别是乳腺癌，肺癌，结肠癌和前列腺肿瘤的治疗或控制。 还公开了可用于制备这些新型2,6-二氨基吡啶衍生物的中间体。

公开(公告)号：US20060229330A1

公开(公告)日：2006-10-12

申请号：US11471001

申请日：2006-06-20

申请人： David Bartkovitz ,  Xin Chu ,  Qingjie Ding ,  Nan Jiang ,  Allen Lovey ,  John Moliterni ,  John Mullin ,  Binh Vu ,  Peter Wovkulich

发明人： David Bartkovitz ,  Xin Chu ,  Qingjie Ding ,  Nan Jiang ,  Allen Lovey ,  John Moliterni ,  John Mullin ,  Binh Vu ,  Peter Wovkulich

IPC分类号： A61K31/506 ,  A61K31/505 ,  C07D409/02 ,  C07D239/46

CPC分类号： C07D239/47 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

摘要： Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.

公开(公告)号：US20070060607A1

公开(公告)日：2007-03-15

申请号：US11516905

申请日：2006-09-07

申请人： David Bartkovitz ,  Yi Chen ,  Xin-Jie Chu ,  Kin-Chun Luk ,  Pamela Rossman ,  Sung-Sau So

发明人： David Bartkovitz ,  Yi Chen ,  Xin-Jie Chu ,  Kin-Chun Luk ,  Pamela Rossman ,  Sung-Sau So

IPC分类号： A61K31/4743 ,  C07D498/02

CPC分类号： C07D495/04 ,  Y02P20/582

摘要： The present invention relates to compounds of the formula medicaments containing them and the use of these compounds as pharmaceutically active agents. The compounds exhibit activity as Raf kinase inhibitors and therefore may be useful for the treatment of diseases mediated by said kinases, especially as anticancer agents.

摘要翻译： 本发明涉及含有它们的式药物的化合物以及这些化合物作为药物活性剂的用途。 该化合物表现出作为Raf激酶抑制剂的活性，因此可用于治疗由所述激酶介导的疾病，特别是作为抗癌剂。