公开(公告)号：US07105518B2

公开(公告)日：2006-09-12

申请号：US10486811

申请日：2002-08-14

申请人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Roger John Griffin ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  Laurent Jean Martin Rigoreau ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Paul Workman ,  Florence Irene Raynaud ,  Bernard Paul Nutley

发明人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Roger John Griffin ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  Laurent Jean Martin Rigoreau ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Paul Workman ,  Florence Irene Raynaud ,  Bernard Paul Nutley

IPC分类号： A61K31/382 ,  C07D335/02 ,  A61N5/00 ,  A61K31/5355 ,  C07D413/04

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：US07674823B2

公开(公告)日：2010-03-09

申请号：US11758332

申请日：2007-06-05

申请人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Roger John Griffin ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Laurent Jean Martin Rigoreau ,  Xiao-ling Fan Cockcroft ,  Vincent Junior Ming-lai Loh ,  Paul Workman ,  Florence Irene Raynaud ,  Bernard Paul Nutley

发明人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Roger John Griffin ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Laurent Jean Martin Rigoreau ,  Xiao-ling Fan Cockcroft ,  Vincent Junior Ming-lai Loh ,  Paul Workman ,  Florence Irene Raynaud ,  Bernard Paul Nutley

IPC分类号： A61K31/351

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R1和R2独立地为氢 ，任选取代的C 1-7烷基，C 3-20杂环基或C 5-20芳基，或者可以与它们所连接的氮原子一起形成任选取代的具有4-8个环的杂环 原子 X和Y选自CR4和O，O和CR'4和NR "4和N，其中不饱和键在环中的适当位置，并且其中R3和R4或R'4之一是任选取代的C3 -20杂芳基或C5-20芳基，R3和R4或R'4中的另一个为H，或R3和R4或R“4一​​起为-A-B-，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：US07226918B2

公开(公告)日：2007-06-05

申请号：US10486816

申请日：2002-08-14

申请人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Roger John Griffin ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Laurent Jean Martin Rigoreau ,  Xiao-ling Fan Cockcroft ,  Vincent Junior Ming-lai Loh ,  Paul Workman ,  Florence Irene Raynaud ,  Bernard Paul Nutley

发明人： Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  Roger John Griffin ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Laurent Jean Martin Rigoreau ,  Xiao-ling Fan Cockcroft ,  Vincent Junior Ming-lai Loh ,  Paul Workman ,  Florence Irene Raynaud ,  Bernard Paul Nutley

IPC分类号： A61K31/353 ,  A61K31/5377 ,  C07D265/30 ,  C07D311/58

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4-8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：US07732483B2

公开(公告)日：2010-06-08

申请号：US12133837

申请日：2008-06-05

申请人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Laurent Jean Martin Rigoreau ,  Roger John Griffin ,  Bernard Thomas Golding ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Ian Robert Hardcastle ,  Kappusamy Saravanan

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Laurent Jean Martin Rigoreau ,  Roger John Griffin ,  Bernard Thomas Golding ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Ian Robert Hardcastle ,  Kappusamy Saravanan

IPC分类号： A61K31/381 ,  C07D333/74 ,  C07D409/04

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，任选取代的C 1-7烷基，C 3-20杂环基或C 5- 20芳基，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; 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杂环基，或者R 4和R 5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; 如果Q是-O-，X另外选自-C（= O）-NR 6 R 7，其中R 6和R 7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杂环基， 或R6和R7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; 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：US20080242664A1

公开(公告)日：2008-10-02

申请号：US12133837

申请日：2008-06-05

申请人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Laurent Jean Martin Rigoreau ,  Roger John Griffin ,  Bernard Thomas Golding ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Ian Robert Hardcastle ,  Kappusamy Saravanan

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Laurent Jean Martin Rigoreau ,  Roger John Griffin ,  Bernard Thomas Golding ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Ian Robert Hardcastle ,  Kappusamy Saravanan

IPC分类号： A61K31/5377 ,  C07D409/10 ,  A61K31/381 ,  C07D409/14 ,  A61P35/04 ,  A61K31/496 ,  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, C3-20 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：US07402607B2

公开(公告)日：2008-07-22

申请号：US11231041

申请日：2005-09-20

申请人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Laurent Jean Martin Rigoreau ,  Roger John Griffin ,  Bernard Thomas Golding ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Ian Robert Hardcastle ,  Kappusamy Saravanan

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Laurent Jean Martin Rigoreau ,  Roger John Griffin ,  Bernard Thomas Golding ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Ian Robert Hardcastle ,  Kappusamy Saravanan

IPC分类号： A61K31/381 ,  C07D333/76

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：US07696203B2

公开(公告)日：2010-04-13

申请号：US11403606

申请日：2006-04-13

申请人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Xiao-ling Cockcroft ,  Mark Frigerio ,  Roger John Griffin ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Kappusamy Saravanan ,  Marine Desage-El Murr

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Keith Allan Menear ,  Marc Geoffrey Hummersone ,  Xiao-ling Cockcroft ,  Mark Frigerio ,  Roger John Griffin ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  David Richard Newell ,  Hilary Alan Calvert ,  Nicola Jane Curtin ,  Kappusamy Saravanan ,  Marine Desage-El Murr

IPC分类号： A61K31/535 ,  C07D413/14

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：US20090043091A1

公开(公告)日：2009-02-12

申请号：US12233736

申请日：2008-09-19

申请人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Marc Geoffrey Hummersone ,  Roger John Griffin

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Marc Geoffrey Hummersone ,  Roger John Griffin

IPC分类号： C07D243/08 ,  C07D413/14 ,  C07D223/02 ,  C07D279/18

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具有4至8个的杂环 环原子 并且RN1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，其用作 制药。

公开(公告)号：US07642254B2

公开(公告)日：2010-01-05

申请号：US11351052

申请日：2006-02-09

申请人： Marc Geoffrey Hummersone ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Roger John Griffin

发明人： Marc Geoffrey Hummersone ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Roger John Griffin

IPC分类号： A61K31/535 ,  A61K31/38 ,  A61K31/35 ,  C07D413/14 ,  C07D409/14 ,  C07D407/14

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含氮杂环，其具有4个 至8个环原子; 并且R 3选自羟基和-NRN 1 R N 2，其中RN 1和RN 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芳基，或一起形成， 与它们相连的氮原子，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。

公开(公告)号：US07429660B2

公开(公告)日：2008-09-30

申请号：US10918180

申请日：2004-08-13

申请人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Marc Geoffrey Hummersone ,  Roger John Griffin

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Marc Geoffrey Hummersone ,  Roger John Griffin

IPC分类号： A61K413/00

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 与它们相连的任选取代的具有4至8个环原子的杂环; 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，以及其作为药物的用途。