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公开(公告)号:US08697685B2
公开(公告)日:2014-04-15
申请号:US13130368
申请日:2009-11-18
申请人: Jeffrey Michael Axten , Charles William Blackledge, Jr. , Gerald Patrick Brady, Jr. , Yanhong Feng , Seth W. Grant , Jesus Raul Medina , William H. Miller , Stuart P. Romeril
发明人: Jeffrey Michael Axten , Charles William Blackledge, Jr. , Gerald Patrick Brady, Jr. , Yanhong Feng , Seth W. Grant , Jesus Raul Medina , William H. Miller , Stuart P. Romeril
IPC分类号: A61K31/33 , A61K31/54 , A61K31/505 , A61K31/55 , C07D401/08 , C07D417/02 , C07D413/06 , C07D239/02
CPC分类号: C07D403/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
摘要: The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译: 本发明涉及6-(4-嘧啶基)-1H-吲唑衍生物。 具体地,本发明涉及式(I)的化合物,其中R 1 -R 4在本文中定义。 本发明的化合物可以用于治疗由组成型激活的ACG激酶(例如癌症,更特别是乳腺癌,结肠癌和肺癌)特征的免疫和代谢疾病和病症的治疗。 因此,本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制PDK1活性的方法和使用本发明化合物或与本发明化合物组合的药物组合物治疗与之相关的病症的方法。