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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.
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公开(公告)号:US20060135770A1
公开(公告)日:2006-06-22
申请号:US11315528
申请日:2005-12-22
申请人: Muhammad Javaid , Graeme Smith , Niall Martin , Sylvie Gomez , Vincent Loh , Xiao-Ling Cockcroft , Keith Menear
发明人: Muhammad Javaid , Graeme Smith , Niall Martin , Sylvie Gomez , Vincent Loh , Xiao-Ling Cockcroft , Keith Menear
IPC分类号: C07D403/14
CPC分类号: C07C235/60 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D215/36 , C07D231/14 , C07D231/18 , C07D231/20 , C07D241/44 , C07D261/10 , C07D261/18 , C07D263/32 , C07D271/12 , C07D277/18 , C07D295/14 , C07D295/18 , C07D295/26 , C07D307/14 , C07D307/52 , C07D317/68 , C07D333/34 , C07D333/62 , C07D401/06 , C07D403/06 , C07D413/06 , C07D495/04
摘要: A compound of the formula (I): and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; n is 1 or 2; RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; Het is selected from: where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F; and where Q is O or S.
摘要翻译: 式(I)的化合物及其异构体,盐,溶剂合物,化学保护形式及其前药,其中:R 2,R 3,R 3, 4和R 5独立地选自H,C 1-7烷氧基,氨基,卤素或羟基; n为1或2; R N1和R N2独立地选自H和R,其中R是任选取代的C 1-10烷基,C 3 -20个杂环基和C 5-20-20芳基; 或R N1和R N2,以及它们所连接的氮原子一起形成任选取代的5-7元含氮杂环; Het选自:其中Y 1和Y 3独立地选自CH和N,Y 2选自CX和N和X 是H,Cl或F; 而Q是O或S.
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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: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。
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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: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。
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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。
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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。
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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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