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。

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。

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。

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。

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。

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。

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，

公开(公告)号：US07531530B2

公开(公告)日：2009-05-12

申请号：US10565308

申请日：2004-07-23

申请人： Thomas Helleday ,  Nicola Curtin

发明人： Thomas Helleday ,  Nicola Curtin

IPC分类号： A61P35/00

CPC分类号： C07D487/06 ,  A61K31/5517 ,  A61K38/005 ,  C12N15/1137 ,  C12N2310/14 ,  C12Y204/0203

摘要： The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.

摘要翻译： 本发明涉及三环内酰胺衍生物和三环内酰胺苯并三唑衍生物及其在抑制PARP酶活性中的应用。 本发明还涉及这些化合物在制备药物中的用途。

公开(公告)号：US07351701B2

公开(公告)日：2008-04-01

申请号：US10898653

申请日：2004-07-23

申请人： Thomas Helleday ,  Nicola Curtin

发明人： Thomas Helleday ,  Nicola Curtin

IPC分类号： A61P35/00

CPC分类号： C07D487/06 ,  A61K31/5517 ,  A61K38/005 ,  C12N15/1137 ,  C12N2310/14 ,  C12Y204/0203

摘要： The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.

摘要翻译： 本发明涉及三环内酰胺衍生物和三环内酰胺苯并三唑衍生物及其在抑制PARP酶活性中的应用。 本发明还涉及这些化合物在制备药物中的用途。

公开(公告)号：US20070072841A1

公开(公告)日：2007-03-29

申请号：US10565308

申请日：2004-07-23

申请人： Thomas Helleday ,  Nicola Curtin

发明人： Thomas Helleday ,  Nicola Curtin

IPC分类号： A61K31/55 ,  A61K31/551 ,  C07D487/04 ,  C07D487/02

CPC分类号： C07D487/06 ,  A61K31/5517 ,  A61K38/005 ,  C12N15/1137 ,  C12N2310/14 ,  C12Y204/0203

摘要： The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.

摘要翻译： 本发明涉及三环内酰胺衍生物和三环内酰胺苯并三唑衍生物及其在抑制PARP酶活性中的应用。 本发明还涉及这些化合物在制备药物中的用途。