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1. 发明申请

WO2012129344A1 FUSED TRICYCLIC DUAL INHIBITORS OF CDK 4/6 AND FLT3 审中-公开
标题翻译： CDK 4/6和FLT3的熔融TRICYCLIC双重抑制剂
公开(公告)号：WO2012129344A1
公开(公告)日：2012-09-27
申请号：PCT/US2012/030007
申请日：2012-03-21
申请人： AMGEN INC. , CHEN, Xiaoqi , DAI, Kang , DUQUETTE, Jason , GRIBBLE, Michael W., Jr. , HUARD, Justin N. , KEEGAN, Kathleen S. , LI, Zhihong , LIVELY, Sarah E. , MCGEE, Lawrence R. , RAGAINS, Mark L. , WANG, Xianghong , WEIDNER, Margaret F. , ZHANG, Jian
发明人： CHEN, Xiaoqi , DAI, Kang , DUQUETTE, Jason , GRIBBLE, Michael W., Jr. , HUARD, Justin N. , KEEGAN, Kathleen S. , LI, Zhihong , LIVELY, Sarah E. , MCGEE, Lawrence R. , RAGAINS, Mark L. , WANG, Xianghong , WEIDNER, Margaret F. , ZHANG, Jian
IPC分类号： C07D471/14 , C07D519/00 , A61K31/519 , A61P35/00 , A61P35/02
CPC分类号： C07D519/00 , C07D471/14
摘要： Compounds of Formula (I) are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula (I) have the following structure: where R 1 is a group of Formula (IA), Formula (IB), Formula (IC), or Formula (ID) and the definitions of the other variables are provided herein.
摘要翻译：式（I）化合物是CDK4，CDK6和FLT3的有用抑制剂。这些化合物可用于治疗癌症和各种其他疾病状况。式（I）化合物具有以下结构：其中R1是式（IA），式（IB），式（IC）或式（ID）的基团，其他变量的定义在本文中提供。

2. 发明申请

WO2005027907A1 USE OF CHK1 INHIBITORS TO CONTROL CELL PROLIFERATION 审中-公开
标题翻译：使用CHK1抑制剂控制细胞增殖
公开(公告)号：WO2005027907A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/030806
申请日：2004-09-17
申请人： ICOS CORPORATION , CLARK, Darcey , KEEGAN, Kathleen, S. , PETERSON, Scott , WEIDNER, Margaret
发明人： CLARK, Darcey , KEEGAN, Kathleen, S. , PETERSON, Scott , WEIDNER, Margaret
IPC分类号： A61K31/4745
CPC分类号： A61K31/7068 , A61K31/13 , A61K31/15 , A61K31/19 , A61K31/4745 , A61K31/513 , A61K31/522 , A61K31/525 , A61K31/53 , A61K31/66 , A61K31/7048 , A61K31/7072 , A61K31/7076 , A61K33/24 , A61K38/14 , A61K45/06 , A61K2300/00
摘要： The present invention relates to improved methods for inhibiting aberrant cell proliferation involving the scheduling of administration of Chk1 activators (e.g., chemotherapeutic agents) and Chk1 inhibitors. At least one Chk1 activator is administered at a dose and for a time sufficient to induce substantial synchronization of cell cycle arrest in proliferating cells. Upon achieving substantial phase synchronization, at least one Chk1 inhibitor is administered to abrogate the cell cycle arrest and induce therapeutic cell death. The invention is useful with any Chk1 activator and any Chk1 inhibitor, and finds application in treating or preventing cancerous and non-cancerous aberrant cell proliferation.
摘要翻译：本发明涉及用于抑制异常细胞增殖的改进方法，其涉及调节施用Chk1激活剂（例如化学治疗剂）和Chk1抑制剂。至少一种Chk1激活剂以足以诱导增殖细胞中细胞周期阻滞的实质同步的剂量施用。在实现大量相位同步时，施用至少一种Chk1抑制剂以消除细胞周期停滞并诱导治疗性细胞死亡。本发明适用于任何Chk1活化剂和任何Chk1抑制剂，可用于治疗或预防癌性和非癌性异常细胞增殖。

3. 发明申请

WO1997018323A2 CELL CYCLE CHECKPOINT PIK-RELATED KINASE MATERIALS AND METHODS 审中-公开
标题翻译：细胞周期检测点PIK相关激素材料和方法
公开(公告)号：WO1997018323A2
公开(公告)日：1997-05-22
申请号：PCT/US1996019337
申请日：1996-11-18
申请人： ICOS CORPORATION , HOEKSTRA, Merl, F. , HOLTZMAN, Doug, A. , KEEGAN, Kathleen, S.
发明人： ICOS CORPORATION
IPC分类号： C12Q00/00
CPC分类号： C12N9/1205
摘要： The present invention generally relates to genes encoding cell cycle checkpoint phosphatidylinositol kinase (PIK)-related proteins essential to DNA damage responses in cells. These PIK-related kinases are required in regulatory pathways that arrest the cell cycle following DNA damage to allow DNA repair prior to mitosis or initiation of DNA replication. More particularly, the invention provides a novel human cell cycle checkpoint PIK-related kinase, MCCS1, and polynucleotide sequences encoding the MCSS1. Assays for identifying modulators of MCCS1 useful as, for example, chemotherapy and radiation adjuvants, are also provided by the invention. Further, assays for identifying modulators of the cell cycle checkpoint phosphatidylinositol kinase (PIK)-related protein identified as ATM are provided.
摘要翻译：本发明一般涉及编码细胞中DNA损伤反应所必需的细胞周期检查点磷脂酰肌醇激酶（PIK）相关蛋白的基因。这些PIK相关的激酶是在DNA损伤后阻止细胞周期的调节途径中需要的，以便在有丝分裂或启动DNA复制之前进行DNA修复。更具体地，本发明提供了新的人细胞周期检查点PIK相关激酶，MCCS1和编码MCSS1的多核苷酸序列。用于鉴定可用作例如化疗和放射辅助剂的MCCS1调节剂的测定也由本发明提供。此外，提供用于鉴定作为ATM鉴定的细胞周期检查点磷脂酰肌醇激酶（PIK）相关蛋白的调节剂的测定。

4. 发明申请

WO9718323A3 CELL CYCLE CHECKPOINT PIK-RELATED KINASE MATERIALS AND METHODS 审中-公开
标题翻译：细胞周期检测点PIK相关激素材料和方法
公开(公告)号：WO9718323A3
公开(公告)日：1997-10-09
申请号：PCT/US9619337
申请日：1996-11-18
申请人： ICOS CORP , HOEKSTRA MERL F , HOLTZMAN DOUG A , KEEGAN KATHLEEN S
发明人： HOEKSTRA MERL F , HOLTZMAN DOUG A , KEEGAN KATHLEEN S
IPC分类号： C12N9/12 , C12Q
CPC分类号： C12N9/1205
摘要： The present invention generally relates to genes encoding cell cycle checkpoint phosphatidylinositol kinase (PIK)-related proteins essential to DNA damage responses in cells. These PIK-related kinases are required in regulatory pathways that arrest the cell cycle following DNA damage to allow DNA repair prior to mitosis or initiation of DNA replication. More particularly, the invention provides a novel human cell cycle checkpoint PIK-related kinase, MCCS1, and polynucleotide sequences encoding the MCSS1. Assays for identifying modulators of MCCS1 useful as, for example, chemotherapy and radiation adjuvants, are also provided by the invention. Further, assays for identifying modulators of the cell cycle checkpoint phosphatidylinositol kinase (PIK)-related protein identified as ATM are provided.

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