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1. 发明申请

WO2015124941A1 PYRAZOLO[1,5-A]PYRIMIDINE-5,7-DIAMINE COMPOUNDS AS CDK INHIBITORS AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：吡咯并[1,5-A]嘧啶-5,7-二胺化合物作为CDK抑制剂及其治疗用途
公开(公告)号：WO2015124941A1
公开(公告)日：2015-08-27
申请号：PCT/GB2015/050494
申请日：2015-02-20
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , IMPERIAL INNOVATIONS LIMITED
发明人： BONDKE, Alexander , KROLL, Sebastian , BARRETT, Anthony , FUCHTER, Matthew , SLAFER, Brian , ALI, Simak , COOMBES, Charles , SNYDER, James Patrick
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyrazolo[1,5-a]pyrimidine-5,7- diamine compounds (referred to herein as "PPDA compounds") that, inter alia , inhibit (e.g., selectively inhibit) CDK (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CDK; and to treat disorders including: disorders that are associated with CDK; disorders that result from an inappropriate activity of a cyclin-dependent kinase (CDK); disorders that are associated with CDK mutation; disorders that are associated with CDK overexpression; disorders that are associated with upstream pathway activation of CDK; disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections (including HIV); neurodegenerative disorders (including Alzheimer's disease and Parkinson's disease); ischaemia; renal diseases; and cardiovascular disorders (including atherosclerosis). Optionally, the treatment further comprises treatment (e.g., simultaneous or sequential treatment) with a further active agent which is, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地，本发明涉及特别是抑制（例如，选择性抑制）CDK的某些吡唑并[1,5-a]嘧啶-5,7-二胺化合物（本文称为“PPDA化合物”）， CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8，CDK9，CDK10，CDK11，CDK12，CDK13等）。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制CDK的用途; 并治疗疾病，包括：与CDK相关的疾病; 由细胞周期蛋白依赖性激酶（CDK）的不适当活动引起的疾病; 与CDK突变有关的疾病; 与CDK过表达有关的疾病; 与CDK的上游途径激活相关的疾病; 通过抑制CDK改善的疾病; 增生性疾病; 癌症; 病毒感染（包括艾滋病）; 神经变性疾病（包括阿尔茨海默病和帕金森病）; 缺血; 肾脏疾病; 和心血管疾病（包括动脉粥样硬化）。任选地，治疗还包括用另外的活性剂（例如芳香酶抑制剂，抗雌激素，Her2阻断剂，细胞毒性化学治疗剂等）治疗（例如，同时或顺序治疗）

2. 发明授权

EP3107914B1 PYRAZOLO[1,5-A]PYRIMIDINE-5,7-DIAMINE COMPOUNDS AS CDK INHIBITORS AND THEIR THERAPEUTIC USE 有权转让
公开(公告)号：EP3107914B1
公开(公告)日：2019-01-30
申请号：EP15706282.9
申请日：2015-02-20
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , IMPERIAL INNOVATIONS LIMITED , Emory University
发明人： BONDKE, Alexander , KROLL, Sebastian , BARRETT, Anthony , FUCHTER, Matthew , SLAFER, Brian , ALI, Simak , COOMBES, Charles , SNYDER, James Patrick
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K31/519 , A61P35/04
摘要： Certain pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds that inhibit cycline dependent kinase (CDK) (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.) are disclosed. Pharmaceutical compositions comprising these compounds, and the use of these compounds and compositions to inhibit CDK; to treat disorders associated with CDK such as those arising from an inappropriate activity, mutation, overexpression, or upstream pathway activation of CDK; or disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections; neurodegenerative disorders; ischaemia; renal diseases; and cardiovascular disorders are also disclosed. Optionally, the treatment further comprises simultaneous or sequential treatment with a further active agent, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.

3. 发明公开

EP3107914A1 PYRAZOLO[1,5-A]PYRIMIDINE-5,7-DIAMINE COMPOUNDS AS CDK INHIBITORS AND THEIR THERAPEUTIC USE 有权转让
标题翻译： - 吡唑并[1,5-a]嘧啶-5,7-二胺化合物作为CDK抑制剂的及其用途THERAPEUTIC
公开(公告)号：EP3107914A1
公开(公告)日：2016-12-28
申请号：EP15706282.9
申请日：2015-02-20
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , IMPERIAL INNOVATIONS LIMITED , Emory University
发明人： BONDKE, Alexander , KROLL, Sebastian , BARRETT, Anthony , FUCHTER, Matthew , SLAFER, Brian , ALI, Simak , COOMBES, Charles , SNYDER, James Patrick
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K31/519 , A61P35/04
摘要： Certain pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds that inhibit cycline dependent kinase (CDK) (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.) are disclosed. Pharmaceutical compositions comprising these compounds, and the use of these compounds and compositions to inhibit CDK; to treat disorders associated with CDK such as those arising from an inappropriate activity, mutation, overexpression, or upstream pathway activation of CDK; or disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections; neurodegenerative disorders; ischaemia; renal diseases; and cardiovascular disorders are also disclosed. Optionally, the treatment further comprises simultaneous or sequential treatment with a further active agent, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.

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