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41. 发明授权

US07399884B2 Histone deacetylase inhibitors 失效
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US07399884B2
公开(公告)日：2008-07-15
申请号：US11557402
申请日：2006-11-07
申请人： Jerome C. Bressi , Sheldon X. Cao , Jeffrey A. Stafford , Phong H. Vu
发明人： Jerome C. Bressi , Sheldon X. Cao , Jeffrey A. Stafford , Phong H. Vu
IPC分类号： C07C259/04 , C07C229/34 , C07D231/16 , C07D239/22 , C07D241/36
CPC分类号： C07C259/06 , C07D231/16 , C07D239/38 , C07D241/44
摘要： Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen;R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl;M is a substituent capable of complexing with a protein metal ion; andL is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.
摘要翻译：提供组蛋白脱乙酰酶抑制剂及其用途，其具有以下通式：其中R 1，R 2，R 3和R 4， / SUB>各自独立地选自氢，取代或未取代的直链C 1-12烷基，C 2-12-12氨基烷基或C 1 -C 12烷基， 2-12个氧杂烷基，以及取代和未取代的3,4,5,6,7或8元环，条件是R 3和R 4 不是氢; R 5选自羰基，取代或未取代的C 1-3烷基，取代或未取代的C 1-3烷基，烷基-C（O），取代或未取代的-C（O）-C 1-3烷基和取代或未取代的-C（O）C（O）C 1-3烷基; M是能与蛋白质金属离子络合的取代基; L是包含连接M取代基与L取代基的α原子的3-12个原子的链的取代基。

42. 发明申请

US20110053873A1 HSP90 INHIBITORS 审中-公开
标题翻译： HSP90抑制剂
公开(公告)号：US20110053873A1
公开(公告)日：2011-03-03
申请号：US12865713
申请日：2009-01-30
申请人： Young K. Chen , Eric Wang Co , Prasuna Guntupalli , John David Lawson , Wolfgang Reinhard Ludwig Notz , Jeffrey A. Stafford , Huong-Thu Ton-Nu
发明人： Young K. Chen , Eric Wang Co , Prasuna Guntupalli , John David Lawson , Wolfgang Reinhard Ludwig Notz , Jeffrey A. Stafford , Huong-Thu Ton-Nu
IPC分类号： C07D471/04 , A61K31/497 , A61K31/4985 , A61K31/519 , A61K31/5377 , C07H17/02 , A61K31/706 , A61P35/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P19/02 , A61P9/00
CPC分类号： C07D401/10 , C07D239/84 , C07D401/14 , C07D487/04
摘要： The invention relates to HSP90 inhibiting compounds consisting of the formula: (I) wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
摘要翻译：本发明涉及由下式（I）组成的HSP90抑制化合物，其中变量如本文所定义。本发明还涉及包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

43. 发明申请

US20100216765A1 KINASE INHIBITORS 失效
标题翻译：激酶抑制剂
公开(公告)号：US20100216765A1
公开(公告)日：2010-08-26
申请号：US12755301
申请日：2010-04-06
申请人： Qing Dong , David J. Hosfield , Bheema R. Paraselli , Nicholas Scorah , Jeffrey A. Stafford , Michael B. Wallace , Zhiyuan Zhang
发明人： Qing Dong , David J. Hosfield , Bheema R. Paraselli , Nicholas Scorah , Jeffrey A. Stafford , Michael B. Wallace , Zhiyuan Zhang
IPC分类号： A61K31/519 , C07D487/04 , A61K31/5377 , A61K31/53 , C07D471/04 , A61P35/00 , A61P25/00 , A61P37/02 , A61P25/28 , A61P3/10
CPC分类号： C07D487/04
摘要： Compounds, pharmaceutical compositions and kits are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
摘要翻译：化合物，药物组合物和试剂盒提供用于包含选自以下的化合物的激酶：其中变量如本文所定义。

44. 发明申请

US20100190816A1 KINASE INHIBITORS 失效
标题翻译：激酶抑制剂
公开(公告)号：US20100190816A1
公开(公告)日：2010-07-29
申请号：US12708304
申请日：2010-02-18
申请人： Qing Dong , Bheema R. Paraselli , Nicholas Scorah , Michael B. Wallace , Jeffrey A. Stafford
发明人： Qing Dong , Bheema R. Paraselli , Nicholas Scorah , Michael B. Wallace , Jeffrey A. Stafford
IPC分类号： A61K31/4745 , C07D491/02
CPC分类号： C07D471/04 , C07D471/12 , C07D487/04 , C07D487/14
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
摘要翻译：提供化合物，药物组合物，试剂盒和方法用于包含选自以下的化合物的激酶：其中变量如本文所定义。

45. 发明申请

US20100120717A1 KINASE INHIBITORS 审中-公开
标题翻译：激酶抑制剂
公开(公告)号：US20100120717A1
公开(公告)日：2010-05-13
申请号：US12444957
申请日：2007-10-08
申请人： Jason W. Brown , Qing Dong , Bheema R. Paraselli , Jeffrey A. Stafford , Michael B. Wallace , Hasanthi Wijesekera
发明人： Jason W. Brown , Qing Dong , Bheema R. Paraselli , Jeffrey A. Stafford , Michael B. Wallace , Hasanthi Wijesekera
IPC分类号： A61K31/675 , C07D471/02 , A61K31/437 , C07D471/12 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/496 , A61K31/397 , C07F9/06 , A61P35/00 , A61P29/00 , A61P25/00
CPC分类号： C07D471/14 , C07D241/18 , C07D401/12 , C07D471/04 , C07D487/04
摘要： Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture in comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
摘要翻译：化合物被提供用于包含选自式（I）的化合物的激酶，其中变量如本文所定义。还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

46. 发明申请

US20090156557A1 KINASE INHIBITORS 审中-公开
公开(公告)号：US20090156557A1
公开(公告)日：2009-06-18
申请号：US12103625
申请日：2008-04-15
申请人： Jason W. Brown , Qing Dong , Bheema R. Paraselli , Jeffrey A. Stafford , Xianchang Gong , Yan Liu , Nicholas Scorah , Michael B. Wallace
发明人： Jason W. Brown , Qing Dong , Bheema R. Paraselli , Jeffrey A. Stafford , Xianchang Gong , Yan Liu , Nicholas Scorah , Michael B. Wallace
IPC分类号： C07D487/04 , A61K31/437 , A61K31/496 , A61K31/5377 , A61K31/675 , C07F9/576 , C12N9/99 , A61P25/28 , A61P29/00 , A61P25/00 , A61P35/00
CPC分类号： C07F9/6561 , C07D471/04
摘要： Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

47. 发明授权

US07381825B2 Histone deacetylase inhibitors 失效
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US07381825B2
公开(公告)日：2008-06-03
申请号：US10803575
申请日：2004-03-17
申请人： Jerome C. Bressi , Jason W. Brown , Sheldon X. Cao , Anthony R. Gangloff , Andrew J. Jennings , Jeffrey A. Stafford , Phong H. Vu , Xiao-Yi Xiao
发明人： Jerome C. Bressi , Jason W. Brown , Sheldon X. Cao , Anthony R. Gangloff , Andrew J. Jennings , Jeffrey A. Stafford , Phong H. Vu , Xiao-Yi Xiao
IPC分类号： C07D401/04
CPC分类号： C07D235/18 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/10
摘要： Compounds that may be used to inhibit histone deacetylase having the formula Z-Q-L-M or Z-L-M wherein M is a substituent capable of complexing with a deacetylase catalytic site and/or a metal ion; L is a substituent providing between 0-10 atoms separation between the M substituent and the remainder of the compound; and Z and Q are as defined herein.
摘要翻译：可用于抑制组氨酸脱乙酰酶的化合物，其具有式<？in-line-formula description =“In-line Formulas”end =“lead”？> ZQLM或ZLM <？in-line-formula description =“In-line 式“end =”tail“？>其中M是能够与脱乙酰酶催化部位和/或金属离子络合的取代基; L是在M取代基和化合物的其余部分之间分离0-10个原子之间的取代基; Z和Q如本文所定义。

48. 发明申请

US20120095233A1 KINASE INHIBITORS 失效
标题翻译：激酶抑制剂
公开(公告)号：US20120095233A1
公开(公告)日：2012-04-19
申请号：US12103882
申请日：2008-04-16
申请人： Jason W. Brown , Qing Dong , Bheema R. Paraselli , Jeffrey A. Stafford , Michael B. Wallace , Hasanthi Wijesekera , Nicholas Scorah
发明人： Jason W. Brown , Qing Dong , Bheema R. Paraselli , Jeffrey A. Stafford , Michael B. Wallace , Hasanthi Wijesekera , Nicholas Scorah
IPC分类号： C07D471/04 , C07D209/88
CPC分类号： C07D471/14 , C07D241/18 , C07D401/12 , C07D471/04 , C07D487/04
摘要： Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
摘要翻译：提供化合物用于与包含选自以下的化合物的激酶一起使用：其中变量如本文所定义。还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。

49. 发明授权

US08119655B2 Kinase inhibitors 失效
公开(公告)号：US08119655B2
公开(公告)日：2012-02-21
申请号：US11539857
申请日：2006-10-09
申请人： Qing Dong , Bheema R. Paraselli , Nicholas Scorah , Jeffrey A. Stafford , Michael B. Wallace
发明人： Qing Dong , Bheema R. Paraselli , Nicholas Scorah , Jeffrey A. Stafford , Michael B. Wallace
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04 , C07D471/12 , C07D487/04 , C07D487/14
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.

50. 发明申请

US20100075973A1 POLO-LIKE KINASE INHIBITORS 审中-公开
标题翻译： POLO-like激素抑制剂
公开(公告)号：US20100075973A1
公开(公告)日：2010-03-25
申请号：US12544419
申请日：2009-08-20
申请人： Sheldon X. Cao , Takashi Ichikawa , Andre A. Kiryanov , Christopher McBride , Srinivasa Reddy Natala , Stephen W. Kaldor , Jeffrey A. Stafford
发明人： Sheldon X. Cao , Takashi Ichikawa , Andre A. Kiryanov , Christopher McBride , Srinivasa Reddy Natala , Stephen W. Kaldor , Jeffrey A. Stafford
IPC分类号： A61K31/5025 , C07D471/14 , A61P35/00
CPC分类号： C07D487/14
摘要： The present invention provides PLK inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using the compounds.
摘要翻译：本发明提供下式的PLK抑制剂，其中变量如本文所定义。还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 和使用该化合物的方法。

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