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公开(公告)号:US20060106025A1
公开(公告)日:2006-05-18
申请号:US11231041
申请日:2005-09-20
申请人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Laurent Rigoreau , Roger Griffin , Bernard Golding , David Newell , Hilary Calvert , Nicola Curtin , Ian Hardcastle , Kappusamy Saravanan
发明人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Laurent Rigoreau , Roger Griffin , Bernard Golding , David Newell , Hilary Calvert , Nicola Curtin , Ian Hardcastle , Kappusamy Saravanan
IPC分类号: A61K31/496 , C07D409/14
CPC分类号: C07D413/14 , C07D409/04 , C07D409/14
摘要: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(═O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3, or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(═O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R6 and R7 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and if Q is —NH—C(═O)—, —Y—X may additionally be selected from C1-7 alkyl.
摘要翻译: 式I化合物及其异构体,盐,溶剂合物,化学保护形式及其前药,其中:R 1和R 2独立地选自氢,任选地 取代的C 1-7烷基,C 3-20杂环基或C 5-20-20芳基,或者可以一起形成 与它们所连接的氮原子一起形成具有4至8个环原子的任选取代的杂环; Q是-NH-C(-O) - 或-O-; Y是任选取代的C 1-5亚烷基; X选自SR 3或NR 4 R 5,其中R 3,R 3,R 3, 4和R 5独立地选自氢,任选取代的C 1-7 - 烷基,C 5-20-20芳基,或 C 3-20杂环基或R 4和R 5可以一起与它们所连接的氮原子一起形成一个 具有4至8个环原子的任选取代的杂环; 如果Q是-O-,X另外选自-C(-O)-NR 6 R 7,其中R 6和R 独立地选自氢,任选取代的C 1-7 - 烷基,C 5-20-20芳基或C 3-20 或者R 6和R 7可以与它们所连接的氮原子一起形成任选取代的杂环,其具有4个 至8个环原子; 并且如果Q是-NH-C(-O) - ,-Y-X可另外选自C 1-7烷基。
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公开(公告)号:US20070238731A1
公开(公告)日:2007-10-11
申请号:US11575606
申请日:2005-09-20
申请人: Graeme Smith , Niall Martin , Roger Griffin , Bernard Golding , Ian Hardcastle , Kappusamy Saravanan , David Newell , Hilary Calvert , Nicola Curtin , Keith Menear , Marc Hummersone
发明人: Graeme Smith , Niall Martin , Roger Griffin , Bernard Golding , Ian Hardcastle , Kappusamy Saravanan , David Newell , Hilary Calvert , Nicola Curtin , Keith Menear , Marc Hummersone
IPC分类号: A61K31/5355 , C07D413/14
CPC分类号: C07D413/14 , C07D409/04 , C07D409/14
摘要: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(═O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3 or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(═O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R6 and R7 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and if Q is —NH—C(═O)—, —Y—X may additionally be selected from C1-7 alkyl.
摘要翻译: 式I化合物及其异构体,盐,溶剂合物,化学保护形式及其前药,其中:R 1和R 2独立地选自氢,任选地 取代的C 1-7烷基,C 3-20杂环基或C 5-20-20芳基,或者可以一起形成 与它们所连接的氮原子一起形成具有4至8个环原子的任选取代的杂环; Q是-NH-C(-O) - 或-O-; Y是任选取代的C 1-5亚烷基; X选自SR 3或NR 4 R 5,其中,R 3或R 4 R 5和R 5独立地选自氢,任选取代的C 1-7 - 烷基,C 5-20芳基或C 3-20个杂环基或R 4和R 5可以一起与它们所连接的氮原子一起形成任选地 具有4至8个环原子的取代杂环; 如果Q是-O-,X另外选自-C(-O)-NR 6 R 7,其中R 6和R 独立地选自氢,任选取代的C 1-7 - 烷基,C 5-20-20芳基或C 3-20 或者R 6和R 7可以与它们所连接的氮原子一起形成任选取代的杂环,其具有4个 至8个环原子; 并且如果Q是-NH-C(-O) - ,-Y-X可另外选自C 1-7烷基。
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公开(公告)号:US20060264427A1
公开(公告)日:2006-11-23
申请号:US11403606
申请日:2006-04-13
申请人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Xiao-ling Cockcroft , Mark Frigerio , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , HiIary Calvert , Nicola Curtin , Kappusamy Saravanan , Marine Desage-El Murr
发明人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Xiao-ling Cockcroft , Mark Frigerio , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , HiIary Calvert , Nicola Curtin , Kappusamy Saravanan , Marine Desage-El Murr
IPC分类号: A61K31/541 , A61K31/5377 , C07D487/02
CPC分类号: C07D413/00 , C07D401/14 , C07D405/04 , C07D407/04 , C07D407/14 , C07D409/04 , C07D471/04
摘要: Compounds of formula I: wherein A, B and D are respectively selected from the group consisting of: (i) CH, NH, C; (ii) CH, N, N;and (iii) CH, O, C; the dotted lines represent two double bonds in the appropriate locations; and where Z is selected from S, O, C(═O), CH2 and NH are disclosed for use in inhibiting DNA-PK.
摘要翻译: 式I化合物:其中A,B和D分别选自:(i)CH,NH,C; (ii)CH,N,N;和(iii)CH,O,C; 虚线表示适当位置的两个双键; 并且其中Z选自S,O,C(-O),CH 2和NH,用于抑制DNA-PK。
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公开(公告)号:US20060264623A1
公开(公告)日:2006-11-23
申请号:US11403763
申请日:2006-04-13
申请人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Xiao-ling Cockcroft , Mark Frigerio , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , Hilary Calvert , Nicola Curtin , Marine Desage-El Murr
发明人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Xiao-ling Cockcroft , Mark Frigerio , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , Hilary Calvert , Nicola Curtin , Marine Desage-El Murr
IPC分类号: C07D413/00
CPC分类号: C07D413/00 , C07D401/14 , C07D405/04 , C07D407/04 , C07D407/14 , C07D409/04 , C07D471/04
摘要: Compounds of formula l: wherein A, B and D are respectively selected from the group consisting of: (i) CH, NH, C; (ii) CH, N, N;and (iii) CH, O, C; are disclosed for use in inhibiting DNA-PK.
摘要翻译: 式I化合物:其中A,B和D分别选自:(i)CH,NH,C; (ii)CH,N,N;和(iii)CH,O,C; 被公开用于抑制DNA-PK。
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公开(公告)号:US20070238729A1
公开(公告)日:2007-10-11
申请号:US11758332
申请日:2007-06-05
申请人: Niall Martin , Graeme Smith , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , Hilary Calvert , Nicola Curtin , Laurent Rigoreau , Xiao-ling Cockcroft , Vincent Junior Loh , Paul Workman , Florence Raynaud , Bernard Nutley
发明人: Niall Martin , Graeme Smith , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , Hilary Calvert , Nicola Curtin , Laurent Rigoreau , Xiao-ling Cockcroft , Vincent Junior Loh , Paul Workman , Florence Raynaud , Bernard Nutley
IPC分类号: A61K31/351 , A61K31/519 , A61K31/5377 , A61P35/00
CPC分类号: C07D417/04 , C07D309/38 , C07D311/22 , C07D311/92 , C07D471/04
摘要: The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR′4 and NR″4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R′4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R′4 is H, or R3 and R4 or R″4 together are -A-B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.
摘要翻译: 本发明涉及式(I)化合物及其异构体,盐,溶剂合物,化学保护形式及其前药在制备用于抑制DNA-PK活性的药物中的用途,其中R 1, R 2和R 2各自独立地为氢,任选取代的C 1-7 - 烷基,C 3-20杂环基或C 或者可以与它们所连接的氮原子一起形成具有4至8个环原子的任选取代的杂环; X和Y选自CR 4和O,O和CR'4和NR“4和N,其中不饱和键处于 R 2中的一个是R 3,R 4,R 4和R 4中的一个是任选取代的C 3 -20个杂芳基或C 5-20-20芳基,R 3和R 4中的另一个或R' > 4 SUP>是H,或R 3和R 4或R“4”一起是-AB-,它们共同表示 稠合的任选取代的芳环。 与PI3-激酶和/或ATM相比,化合物还选择性地抑制DNA-PK的活性。
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公开(公告)号:US20050107367A1
公开(公告)日:2005-05-19
申请号:US10486811
申请日:2002-08-14
申请人: Niall Martin , Graeme Cameron Smith , Roger Griffin , Bernard Golding , Ian Hardcastle , Laurent Rigoreau , David Newell , Hilary Calvert , Nicola Curtin , Paul Workman , Florence Raynaud , Bernard Nutley
发明人: Niall Martin , Graeme Cameron Smith , Roger Griffin , Bernard Golding , Ian Hardcastle , Laurent Rigoreau , David Newell , Hilary Calvert , Nicola Curtin , Paul Workman , Florence Raynaud , Bernard Nutley
IPC分类号: C12N9/99 , A61K31/5377 , A61P31/12 , A61P35/00 , A61P43/00 , C07D335/02 , C07D409/10 , A61K31/541 , A61K31/496 , C07D413/04 , C07D417/04 , C07D49/04
CPC分类号: C07D335/02
摘要: The present invention provides compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein R1 and R2 are independently hydrogen, an option ally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and R3 is an optionally substituted C3-20 heterocyclyl or C5-20 aryl group, and their use as pharmaceuticals, particularly in treating diseases which are retroviral mediated or ameliorated by the inhibition of DNA-PK,
摘要翻译: 本发明提供式(I)化合物及其异构体,盐,溶剂化物,化学保护形式及其前药,其中R 1和R 2独立地为氢, 选择性地取代C 1-7烷基,C 3-20杂环基或C 5-20-20芳基,或可一起形成 与它们所连接的氮原子一起形成具有4-8个环原子的任选取代的杂环; 并且R 3是任选取代的C 3-20杂环基或C 5-20芳基,并且它们作为药物的用途,特别是在治疗 通过抑制DNA-PK介导或改善的逆转录病毒的疾病,
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公开(公告)号:US09945789B2
公开(公告)日:2018-04-17
申请号:US11653568
申请日:2007-01-16
申请人: Ian Hardcastle , Carol T. Schembri , John Francis Petrilla , Rene B. Helbing , Daniel B. Roitman
发明人: Ian Hardcastle , Carol T. Schembri , John Francis Petrilla , Rene B. Helbing , Daniel B. Roitman
CPC分类号: G01N21/78 , G01N21/253 , G01N21/8483
摘要: A multiple analyte detection system includes a carrier having reagents disposed thereat, with each of the reagents capable of optically changing in response to exposure to a respective analyte. The system further includes a photodetector positioned to collectively detect light interacted with each of the reagents, a processor to determine a presence or an absence of each of the analytes in response to the light collectively-detected, and an indicator to provide an indication of the presence or the absence of each of the analytes. A method of detecting multiple analytes includes exposing reagents capable of optically changing in response to exposure to a respective analyte to a sample. The method further includes collectively detecting light interacted with each of the reagents, determining a presence or an absence of each of the analytes in response to the light collectively detected, and indicating the presence or the absence of each of the analytes determined.
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公开(公告)号:US08998478B2
公开(公告)日:2015-04-07
申请号:US13448688
申请日:2012-04-17
申请人: Timothy A. McCollum , Jeffery R. Parker , Fumitomo Hide , Alexey Titov , Ian Hardcastle , Robert M. Ezell
发明人: Timothy A. McCollum , Jeffery R. Parker , Fumitomo Hide , Alexey Titov , Ian Hardcastle , Robert M. Ezell
IPC分类号: F21S8/06 , F21V7/05 , F21V8/00 , F21S6/00 , F21S8/00 , F21Y101/02 , F21Y105/00
CPC分类号: G02B6/0063 , F21S6/002 , F21S8/033 , F21S8/06 , F21V7/05 , F21Y2105/00 , F21Y2115/10 , F21Y2115/15 , G02B6/0011 , G02B6/003 , G02B6/0031 , G02B6/0073
摘要: A lighting assembly includes a light guide having a first major surface, a second major surface opposite the first major surface, a light input edge, and an end edge distal the light input edge. Light input to the light guide through the light input edge propagates by total internal reflection toward the end edge. The lighting assembly further includes light extracting elements at least one of the major surfaces of the light guide, the light extracting elements configured to extract light through the first major surface in a direction away from the light input edge and away from the first major surface, and a banding reduction element at the end edge configured to redirect light incident thereon in a direction away from the light input edge.
摘要翻译: 照明组件包括具有第一主表面,与第一主表面相对的第二主表面,光输入边缘和远离光输入边缘的端边缘的光导。 通过光输入边缘输入到光导的光通过全内反射向端边缘传播。 所述照明组件还包括所述导光体的至少一个主表面的光提取元件,所述光提取元件被配置为沿远离所述光输入边缘并远离所述第一主表面的方向提取穿过所述第一主表面的光, 以及端部边缘处的带状减少元件,被配置成在远离光输入边缘的方向上重定向其上入射的光。
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公开(公告)号:US08864360B2
公开(公告)日:2014-10-21
申请号:US13440197
申请日:2012-04-05
申请人: Jeffery R. Parker , Timothy A. McCollum , Martin E. Ligas , Joseph Crookston , Fumitomo Hide , Alexey Titov , Ian Hardcastle
发明人: Jeffery R. Parker , Timothy A. McCollum , Martin E. Ligas , Joseph Crookston , Fumitomo Hide , Alexey Titov , Ian Hardcastle
CPC分类号: G02B6/0031 , F21K9/00 , F21V7/00 , F21V29/004 , F21V29/70 , F21V29/76 , F21V29/80 , F21V2200/20 , F21Y2115/10
摘要: A lighting assembly includes a light guide having opposed major surfaces between which light propagates by total internal reflection and a light input edge. The light assembly also includes a light engine. The light engine has a heat conductive armature having a receptacle for a portion of the light guide that includes the light input edge and a light source retained by and thermally coupled to the armature. The armature functions as a heat sink for dissipating heat generated by the light source. The light guide is mechanically retained in the receptacle, and the light guide and the armature cooperate to align the light input edge with the light source for inputting light from the light source into the light guide through the light input edge.
摘要翻译: 照明组件包括具有相对的主表面的光导,光之间通过全内反射传播光和光输入边。 灯组件还包括光引擎。 光引擎具有导热电枢,其具有用于导光体的一部分的插座,该插座包括光输入边缘和由电枢保持并热耦合的光源。 电枢用作散热器,用于散发由光源产生的热量。 导光体被机械地保持在插座中,并且光导和电枢协调使光输入边缘与光源对准,用于将来自光源的光通过光输入边缘输入到光导中。
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公开(公告)号:US20120281432A1
公开(公告)日:2012-11-08
申请号:US13440197
申请日:2012-04-05
申请人: Jeffery R. Parker , Timothy A. McCollum , Martin E. Ligas , Joseph Crookston , Fumitomo Hide , Alexey Titov , Ian Hardcastle
发明人: Jeffery R. Parker , Timothy A. McCollum , Martin E. Ligas , Joseph Crookston , Fumitomo Hide , Alexey Titov , Ian Hardcastle
CPC分类号: G02B6/0031 , F21K9/00 , F21V7/00 , F21V29/004 , F21V29/70 , F21V29/76 , F21V29/80 , F21V2200/20 , F21Y2115/10
摘要: A lighting assembly includes a light guide having opposed major surfaces between which light propagates by total internal reflection and a light input edge. The light assembly also includes a light engine. The light engine has a heat conductive armature having a receptacle for a portion of the light guide that includes the light input edge and a light source retained by and thermally coupled to the armature. The armature functions as a heat sink for dissipating heat generated by the light source. The light guide is mechanically retained in the receptacle, and the light guide and the armature cooperate to align the light input edge with the light source for inputting light from the light source into the light guide through the light input edge.
摘要翻译: 照明组件包括具有相对的主表面的光导,光之间通过全内反射传播光和光输入边。 灯组件还包括光引擎。 光引擎具有导热电枢,其具有用于导光体的一部分的插座,该插座包括光输入边缘和由电枢保持并热耦合的光源。 电枢用作散热器,用于散发由光源产生的热量。 导光体被机械地保持在插座中,并且光导和电枢协调使光输入边缘与光源对准,用于将来自光源的光通过光输入边缘输入到光导中。
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