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1. 发明申请

US20080070916A1 Dihydropyrancarboxamides and uses thereof 审中-公开
标题翻译：二氢吡喃甲酰胺及其用途
公开(公告)号：US20080070916A1
公开(公告)日：2008-03-20
申请号：US11714689
申请日：2007-03-06
申请人： Stuart Schreiber , Robert Stavenger , Timothy Mitchison , Zoltan Maliga
发明人： Stuart Schreiber , Robert Stavenger , Timothy Mitchison , Zoltan Maliga
IPC分类号： A61K31/438 , A61K31/435 , A61K31/5377 , A61P35/00 , C07D413/14 , C07D455/04 , C07D471/10 , C40B40/04
CPC分类号： C07D471/04 , C07D309/30 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10
摘要： The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1-R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
摘要翻译：本发明提供新的式（I）二氢吡喃甲酰胺化合物：这些化合物的收集，并提供这些化合物的合成方法; 其中R 1〜R 6如本文所定义。此外，本发明提供了用于治疗诸如增殖性疾病和癌症等疾病的药物组合物和方法。

2. 发明申请

US20100152206A1 Bicyclic Dihydropyrimidines and Uses Thereof 审中-公开
标题翻译：双环二嘧啶及其用途
公开(公告)号：US20100152206A1
公开(公告)日：2010-06-17
申请号：US11794586
申请日：2006-01-06
申请人： Ralph Mazitschek , John A. Tallarico , Zoltan Maliga , Timothy J. Mitchison
发明人： Ralph Mazitschek , John A. Tallarico , Zoltan Maliga , Timothy J. Mitchison
IPC分类号： A61K31/519 , C07D491/052 , C07D491/048 , C07D487/04 , C07D471/04 , A61P35/00 , C12N5/00
CPC分类号： C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention provides compounds having formula (I): (I) and pharmaceutically acceptable derivatives thereof; as described generally and in subclasses herein, which compounds are useful as kinesin inhibitors (e.g., Eg5 inhibitors), and thus are useful, for example, for the treatment of proliferative disorders e.g., cancer. The invention additionally provides methods for preparing compounds of the invention, compositions comprising them, and methods for the use thereof in the treatment of various disorders where Eg5 is involved. In certain embodiments, the present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.
摘要翻译：本发明提供具有式（I）的化合物：（I）及其药学上可接受的衍生物; 如本文中通常和在本文中所述的那样，哪些化合物可用作驱动蛋白抑制剂（例如Eg5抑制剂），因此可用于例如治疗增殖性疾病例如癌症。本发明另外提供了制备本发明化合物的方法，包含它们的组合物，以及用于治疗其中涉及Eg5的各种疾病的方法。在某些实施方案中，本发明提供了用于抑制细胞生长的化合物，组合物，方法和系统。更具体地，本发明提供能够抑制代谢活性细胞中有丝分裂的方法，化合物和组合物。本发明的化合物，组合物和方法抑制参与有丝分裂纺锤体的组装和维持的蛋白质的活性。作用于有丝分裂纺锤体的一类蛋白质是有丝分裂驱动蛋白家族，是驱动蛋白超家族的一个子集。

3. 发明授权

US07186709B2 Dihydropyrancarboxamides and uses thereof 有权
标题翻译：二氢吡喃甲酰胺及其用途
公开(公告)号：US07186709B2
公开(公告)日：2007-03-06
申请号：US10649532
申请日：2003-08-27
申请人： Stuart L. Schreiber , Robert A. Stavenger , Timothy J. Mitchison , Zoltan Maliga
发明人： Stuart L. Schreiber , Robert A. Stavenger , Timothy J. Mitchison , Zoltan Maliga
IPC分类号： A61K31/351 , A61K31/436 , A61K31/4375 , C07D405/06 , C07D405/08
CPC分类号： C07D471/04 , C07D309/30 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10
摘要： The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
摘要翻译：本发明提供新的式（I）二氢吡喃甲酰胺化合物：这些化合物的收集，并提供这些化合物的合成方法; 其中R 1〜R 6如本文所定义。此外，本发明提供了用于治疗诸如增殖性疾病和癌症等疾病的药物组合物和方法。

4. 发明授权

US06890933B1 Kinesin inhibitors 失效
公开(公告)号：US06890933B1
公开(公告)日：2005-05-10
申请号：US09791339
申请日：2001-02-23
申请人： Yan Feng , Tarun M. Kapoor , Thomas Mayer , Zoltan Maliga , Timothy J. Mitchison , Justin Yarrow
发明人： Yan Feng , Tarun M. Kapoor , Thomas Mayer , Zoltan Maliga , Timothy J. Mitchison , Justin Yarrow
IPC分类号： C07D471/14 , A61K31/437 , C02D471/04
CPC分类号： C07D471/14
摘要： The present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.

5. 发明申请

US20050004156A1 Kinesin inhibitors 审中-公开
标题翻译：驱动蛋白抑制剂
公开(公告)号：US20050004156A1
公开(公告)日：2005-01-06
申请号：US10899495
申请日：2004-07-26
申请人： Yan Feng , Tarun Kapoor , Thomas Mayer , Zoltan Maliga , Timothy Mitchison , Justin Yarrow
发明人： Yan Feng , Tarun Kapoor , Thomas Mayer , Zoltan Maliga , Timothy Mitchison , Justin Yarrow
IPC分类号： C07D471/14 , A61K31/4745
CPC分类号： C07D471/14
摘要： The present invention provides for compounds, compositions, methods and systems for inhibiting cell growth. More specifically, the present invention provides for methods, compounds and compositions which are capable of inhibiting mitosis in metabolically active cells. Compounds, compositions and methods of the present invention inhibit the activity of a protein involved in the assembly and maintenance of the mitotic spindle. One class of proteins which acts on the mitotic spindle is the family of mitotic kinesins, a subset of the kinesin superfamily.
摘要翻译：本发明提供了抑制细胞生长的化合物，组合物，方法和系统。更具体地，本发明提供能够抑制代谢活性细胞中有丝分裂的方法，化合物和组合物。本发明的化合物，组合物和方法抑制参与有丝分裂纺锤体的组装和维持的蛋白质的活性。作用于有丝分裂纺锤体的一类蛋白质是有丝分裂驱动蛋白家族，是驱动蛋白超家族的一个子集。

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