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公开(公告)号:US08669249B2
公开(公告)日:2014-03-11
申请号:US13260680
申请日:2010-03-26
IPC分类号: C07D265/36 , C07D413/06 , A61K31/538
CPC分类号: C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D473/12
摘要: Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are 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: 提供下式的化合物用于抑制聚(ADP-核糖)聚合酶(PARP):其中变量在本文中定义。 还提供了包含这种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,以及使用该化合物的方法。
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公开(公告)号:US07399884B2
公开(公告)日:2008-07-15
申请号:US11557402
申请日:2006-11-07
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 SUB >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。
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公开(公告)号:US07642253B2
公开(公告)日:2010-01-05
申请号:US11382659
申请日:2006-05-10
IPC分类号: C07D403/02 , A61K31/513
CPC分类号: C07D513/04 , C07D239/80 , C07D285/24 , C07D417/04 , C07D417/06 , C07D417/12
摘要: Compounds, pharmaceutical compositions, kits and methods useful for inhibiting HDAC, thereby treating a disease state for which HDAC possess activity that contributes to the pathology and/or symptomology of the disease state. The compound is selected from the group consisting of: wherein the variables are as defined herein.
摘要翻译: 用于抑制HDAC的化合物,药物组合物,试剂盒和方法,从而治疗HDAC具有促进疾病状态和/或症状的活性的疾病状态。 该化合物选自:其中变量如本文所定义。
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公开(公告)号:US07375228B2
公开(公告)日:2008-05-20
申请号:US10803580
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.
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公开(公告)号:US07169801B2
公开(公告)日:2007-01-30
申请号:US10803344
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: A61K31/415 , A61K31/44 , C07D401/02 , C07D403/02
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。
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公开(公告)号:US07154002B1
公开(公告)日:2006-12-26
申请号:US10681049
申请日:2003-10-07
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; and L 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 SUB >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。
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公开(公告)号:US07642275B2
公开(公告)日:2010-01-05
申请号:US11303455
申请日:2005-12-16
申请人: Jerome C. Bressi , Jason W. Brown , Robert J. Skene , Jeffrey A. Stafford , Phong H. Vu , Anthony R. Gangloff , Andrew J. Jennings , Stephen W. Kaldor
发明人: Jerome C. Bressi , Jason W. Brown , Robert J. Skene , Jeffrey A. Stafford , Phong H. Vu , Anthony R. Gangloff , Andrew J. Jennings , Stephen W. Kaldor
IPC分类号: A61K31/423 , A61K31/428 , A61K31/416 , C07D265/12 , C07D277/68 , C07D235/26
CPC分类号: C07D235/06 , C07D235/26 , C07D263/38 , C07D263/58 , C07D277/68 , C07D277/72 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D471/04 , C07D495/04 , C07D513/04
摘要: Compounds, pharmaceutical compositions, kits and methods are provided for use with histone deacetylases (HDACs) that comprise a compound of the formulae: wherein the variables are as defined herein.
摘要翻译: 提供化合物,药物组合物,试剂盒和方法用于组蛋白脱乙酰酶(HDAC),组蛋白脱乙酰酶包含下式化合物:其中变量如本文所定义。
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公开(公告)号:US20120094992A1
公开(公告)日:2012-04-19
申请号:US13260680
申请日:2010-03-26
IPC分类号: A61K31/538 , A61P3/00 , A61P25/28 , A61P9/00 , A61P9/10 , C07D265/36 , A61P35/00
CPC分类号: C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D473/12
摘要: Compounds of the following formula are provided for use in inhibiting Poly (ADP-ribose) Polymerase (PARP): wherein the variables are 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: 提供下式的化合物用于抑制聚(ADP-核糖)聚合酶(PARP):其中变量在本文中定义。 还提供了包含这种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,以及使用该化合物的方法。
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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。
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