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1. 发明申请

US20070049588A1 ATM INHIBITOR 审中-公开
标题翻译： ATM抑制剂
公开(公告)号：US20070049588A1
公开(公告)日：2007-03-01
申请号：US11468315
申请日：2006-08-30
申请人： Graeme Smith , Niall Martin , Andrew Slade , Keith Menear , Marc Hummersone , Xiao-Ling Cockcroft , Ian Matthews , Laurent Rigoreau , Roger Griffin , David Newell , Nicola Curtin
发明人： Graeme Smith , Niall Martin , Andrew Slade , Keith Menear , Marc Hummersone , Xiao-Ling Cockcroft , Ian Matthews , Laurent Rigoreau , Roger Griffin , David Newell , Nicola Curtin
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D409/04
摘要： A compound of formula (I): and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, and their use in treating diseases ameliorated by the inhibition of ATM.
摘要翻译：式（I）的化合物及其异构体，盐，溶剂化物，化学保护形式及其前药，以及它们在治疗通过抑制ATM而改善的疾病中的用途。

2. 发明申请

US20050054657A1 ATM inhibitors 失效
标题翻译： ATM抑制剂
公开(公告)号：US20050054657A1
公开(公告)日：2005-03-10
申请号：US10918180
申请日：2004-08-13
申请人： Graeme Smith , Niall Martin , Xiao-Ling Cockcroft , Ian Matthews , Keith Menear , Laurent Rigoreau , Marc Hummersone , Roger Griffin
发明人： Graeme Smith , Niall Martin , Xiao-Ling Cockcroft , Ian Matthews , Keith Menear , Laurent Rigoreau , Marc Hummersone , Roger Griffin
IPC分类号： A61P31/12 , A61P35/00 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/04 , A61K31/496 , C07D49/14
CPC分类号： C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/04
摘要： A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 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 RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.
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 2一起与它们所连接的氮原子一起形成任选取代的杂环具有4至8个环原子的环; 并且R N1选自氢，任选取代的C 1-7烷基，任选取代的C 3-20杂环基，任选取代的C 5-20芳基，酰基，酯基和酰胺基，以及其用作药物。

3. 发明申请

US20060264623A1 DNA-PK inhibitors 审中-公开
标题翻译： DNA-PK抑制剂
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。

4. 发明申请

US20060264427A1 DNA-PK inhibitors 失效
标题翻译： DNA-PK抑制剂
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。

5. 发明申请

US20060106025A1 DNA-PK inhibitors 失效
标题翻译： DNA-PK抑制剂
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。

6. 发明申请

US20060178361A1 ATM inhibitors 失效
标题翻译： ATM抑制剂
公开(公告)号：US20060178361A1
公开(公告)日：2006-08-10
申请号：US11351052
申请日：2006-02-09
申请人： Marc Hummersone , Keith Menear , Laurent Rigoreau , Graeme Smith , Niall Martin , Roger Griffin
发明人： Marc Hummersone , Keith Menear , Laurent Rigoreau , Graeme Smith , Niall Martin , Roger Griffin
IPC分类号： A61K31/55 , A61K31/453 , C07D409/14
CPC分类号： 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 together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms; and R3 is selected from hydroxy and —NRN1RN2, where RN1 and RN2 are independently selected from hydrogen, optionally substituted C1-7 alkyl groups, optionally substituted C3-20 heterocyclyl groups and optionally substituted C5-20 aryl groups, or together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms, and its use in inhibiting ATM.
摘要翻译：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 2一起与氮原子一起形成它们所连接的是具有4-8个环原子的任选取代的含氮杂环; R 3和R 3选自羟基和-NR N 1 N 2 N 2，其中R 11和R 10独立地选自氢， N 2独立地选自氢，任选取代的C 1-7烷基，任选取代的C 3-20杂环基和任选取代的C 5 -20个芳基，或者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含氮杂环，以及其在抑制ATM中的用途。

7. 发明申请

US20070093489A1 PHTHALAZINONE DERIVATIVES 失效
公开(公告)号：US20070093489A1
公开(公告)日：2007-04-26
申请号：US11550004
申请日：2006-10-17
申请人： Muhammad Javaid , Keith Menear , Sylvie Gomez , Marc Hummersone , Niall Martin , Graeme Smith , Xiao-Ling Cockcroft
发明人： Muhammad Javaid , Keith Menear , Sylvie Gomez , Marc Hummersone , Niall Martin , Graeme Smith , Xiao-Ling Cockcroft
IPC分类号： A61K31/53
CPC分类号： C07D403/10 , C07D403/14 , C07D411/14 , C07D413/14 , C07D487/04
摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) and where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2; RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.

8. 发明申请

US20070238729A1 DNA-PK INHIBITORS 失效
标题翻译： DNA-PK抑制剂
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 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。

9. 发明申请

US20060149059A1 Phthalazinone derivatives 有权
标题翻译：酞嗪衍生物
公开(公告)号：US20060149059A1
公开(公告)日：2006-07-06
申请号：US11318155
申请日：2005-12-23
申请人： Niall Martin , Graeme Smith , Stephen Jackson , Vincent Loh , Xiao-Ling Cockcroft , Ian Matthews , Keith Menear , Frank Kerrigan , Alan Ashworth
发明人： Niall Martin , Graeme Smith , Stephen Jackson , Vincent Loh , Xiao-Ling Cockcroft , Ian Matthews , Keith Menear , Frank Kerrigan , Alan Ashworth
IPC分类号： C07D403/02 , A61K31/502
CPC分类号： A61K31/00 , C07D237/32 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D495/04
摘要： Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
摘要翻译：式（I）的化合物：其中A和B一起表示任选取代的稠合芳环; X可以是NR X或X X R O Y; 如果X = NR X，则n为1或2，并且如果X = CR X R Y Y，则n为1; R X选自H，任选取代的C 1-20烷基，C 5-20-20芳基，C 1〜酰胺基，磺酰基，磺酰基，酰基和磺酰基; R Y选自H，羟基，氨基; 或R X和R Y可以一起形成螺C 3-7环烷基或杂环基; R C1和R C2都是氢，或者当X是CR X R Y，R O， C 1，R 2，R 2，X和R Y以及它们所连接的碳原子可以形成任选取代的稠合芳环; R 1和R 2选自H和卤素。

10. 发明申请

US20070238731A1 Dna-Pk Inhibitors 审中-公开
标题翻译： Dna-Pk抑制剂
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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