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21. 发明申请

US20090042865A1 DNA-PK INHIBITORS 审中-公开
标题翻译： DNA-PK抑制剂
公开(公告)号：US20090042865A1
公开(公告)日：2009-02-12
申请号：US12175542
申请日：2008-07-18
申请人： Mark Frigerio , Marc Geoffrey Hummersone , Keith Allan Menear , Christine Sarah Bailey , Heather Mary Ellen Duggan , Sylvie Gomez , Niall Morrison Barr Martin
发明人： Mark Frigerio , Marc Geoffrey Hummersone , Keith Allan Menear , Christine Sarah Bailey , Heather Mary Ellen Duggan , Sylvie Gomez , Niall Morrison Barr Martin
IPC分类号： A61K31/5377 , C07D413/14 , A61K31/551 , A61P35/00 , C07D243/08
CPC分类号： C07D409/04 , C07D409/14
摘要： A compound of formula I: 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; X is CH or N; n is 1 or 2; RC1 and RC2 are independently selected from H and methyl; when X is N, RX is selected from the group consisting of H, and optionally substituted C1-7 alkyl, C3-20 heterocyclyl, C5-20 aryl, acyl, ester, amido and sulfonyl; and when X is CH, RX is selected from the group consisting of H, and optionally substituted C1-7 alkyl, C3-20 heterocyclyl, C5-20 aryl, acyl, ester, amido, sulfonyl, amino and ether.
摘要翻译：式I的化合物：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，或者可以一起与氮原子一起形成它们所连接的是具有4至8个环原子的任选取代的杂环; X是CH或N; n为1或2; RC1和RC2独立地选自H和甲基; 当X是N时，RX选自H和任选取代的C 1-7烷基，C 3-20杂环基，C 5-20芳基，酰基，酯，酰氨基和磺酰基; 当X是CH时，RX选自H和任选取代的C 1-7烷基，C 3-20杂环基，C 5-20芳基，酰基，酯，酰氨基，磺酰基，氨基和醚。

22. 发明申请

US20080280910A1 PHTHALAZINONE DERIVATIVES 审中-公开
标题翻译：邻苯二酚衍生物
公开(公告)号：US20080280910A1
公开(公告)日：2008-11-13
申请号：US12051219
申请日：2008-03-19
申请人： Keith Allan Menear , Marc Geoffrey Hummersone , Sylvie Gomez , Muhammad Hashim Javaid , Niall Morrison Barr Martin , Frank Kerrigan
发明人： Keith Allan Menear , Marc Geoffrey Hummersone , Sylvie Gomez , Muhammad Hashim Javaid , Niall Morrison Barr Martin , Frank Kerrigan
IPC分类号： A61K31/502 , C07D237/32 , A61P35/04
CPC分类号： C07D237/32 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D405/14 , C07D409/06 , C07D409/10 , C07D409/14 , C07D411/10 , C07D413/10 , C07D417/06 , C07D417/10 , C07D417/14
摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring or an optionally substituted, fused cyclohexene ring; D is selected from: where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N and Y4 is selected from CH and N; where Y1 is selected from CH and N and Y2 is selected from CH and N; where Q is O or S; and where Q is O or S; and RD is an optionally substituted C5-20 aryl group, bound to D by a carbon-carbon bond.
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或任选取代的稠合环己烯环; D选自：其中Y 1是选自CH和N，Y 2选自CH和N，Y 3选自： CH，CF和N和Y 4选自CH和N; 其中Y 1选自CH，N和Y 2选自CH和N; 其中Q是O或S; Q为O或S; R D是通过碳 - 碳键与D结合的任意取代的C 5-20-20芳基。

23. 发明授权

US08129380B2 Phthalazinone derivatives 失效
标题翻译：酞嗪酮衍生物
公开(公告)号：US08129380B2
公开(公告)日：2012-03-06
申请号：US12357957
申请日：2009-01-22
申请人： Keith Allan Menear , Muhammad Hashim Javaid , Sylvie Gomez , Marc Geoffrey Hummersone , Carlos Fenandez Lence , Niall Morrison Barr Martin , David Alan Rudge , Craig Anthony Roberts , Kevin Blades
发明人： Keith Allan Menear , Muhammad Hashim Javaid , Sylvie Gomez , Marc Geoffrey Hummersone , Carlos Fenandez Lence , Niall Morrison Barr Martin , David Alan Rudge , Craig Anthony Roberts , Kevin Blades
IPC分类号： C07D237/02 , A61K31/502 , A61P35/04
CPC分类号： C07D401/10 , C07D401/14 , C07D405/14 , C07D487/04 , C07D491/10
摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; RC is selected from H, C1-4 alkyl; and R1 is selected from C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl, which groups are optionally substituted; or RC and R1 together with the carbon and oxygen atoms to which they are attached form a spiro-C5-7 oxygen-containing heterocyclic group, which is optionally substituted or fused to a C5-7 aromatic ring.
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和Y分别选自CH和CH，CF和CH，CH和CF以及N和CH; RC选自H，C 1-4烷基; 并且R 1选自C 1-7烷基，C 3-20杂环基和C 5-20芳基，该基团任选被取代; 或RC和R 1与它们所连接的碳原子和氧原子一起形成含有C 5-7的含氧杂环基团，其任选被取代或稠合至C5-7芳环。

24. 发明申请

US20090192156A1 PHTHALAZINONE DERIVATIVES 失效
标题翻译：邻苯二酚衍生物
公开(公告)号：US20090192156A1
公开(公告)日：2009-07-30
申请号：US12357957
申请日：2009-01-22
申请人： Keith Allan MENEAR , Muhammad Hashim Javaid , Sylvie Gomez , Marc Geoffrey Hummersone , Carlos Fenandez Lence , Niall Morrison Barr Martin , David Alan Rudge , Craig Anthony Roberts , Kevin Blades
发明人： Keith Allan MENEAR , Muhammad Hashim Javaid , Sylvie Gomez , Marc Geoffrey Hummersone , Carlos Fenandez Lence , Niall Morrison Barr Martin , David Alan Rudge , Craig Anthony Roberts , Kevin Blades
IPC分类号： A61K31/5025 , C07D401/10 , C07D401/14 , C07D491/107 , C07D487/04 , C07D413/14 , A61K31/502 , A61K31/5377 , A61P9/00 , A61P25/00 , A61P31/12 , A61P35/00
CPC分类号： C07D401/10 , C07D401/14 , C07D405/14 , C07D487/04 , C07D491/10
摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; RC is selected from H, C1-4 alkyl; and R1 is selected from C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl, which groups are optionally substituted; or RC and R1 together with the carbon and oxygen atoms to which they are attached form a spiro-C5-7 oxygen-containing heterocyclic group, which is optionally substituted or fused to a C5-7 aromatic ring.
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和Y分别选自CH和CH，CF和CH，CH和CF以及N和CH; RC选自H，C 1-4烷基; 并且R 1选自C 1-7烷基，C 3-20杂环基和C 5-20芳基，该基团任选被取代; 或RC和R 1与它们所连接的碳原子和氧原子一起形成含有C 5-7的含氧杂环基团，其任选被取代或稠合至C5-7芳环。

25. 发明申请

US20120129855A1 PHTHALAZINONE DERIVATIVES 审中-公开
标题翻译：邻苯二酚衍生物
公开(公告)号：US20120129855A1
公开(公告)日：2012-05-24
申请号：US13361911
申请日：2012-01-30
申请人： Keith Allan Menear , Muhammad Hashim Javaid , Sylvie Gomez , Marc Geoffrey Hummersone , Carlos Fernandez Lence , Niall Morrison Barr Martin , David Alan Rudge , Craig Anthony Roberts , Kevin Blades
发明人： Keith Allan Menear , Muhammad Hashim Javaid , Sylvie Gomez , Marc Geoffrey Hummersone , Carlos Fernandez Lence , Niall Morrison Barr Martin , David Alan Rudge , Craig Anthony Roberts , Kevin Blades
IPC分类号： A61K31/502 , A61K31/5377 , A61P35/00
CPC分类号： C07D401/10 , C07D401/14 , C07D405/14 , C07D487/04 , C07D491/10
摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; RC is selected from H, C1-4 alkyl; and R1 is selected from C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl, which groups are optionally substituted; or RC and R1 together with the carbon and oxygen atoms to which they are attached form a spiro-C5-7 oxygen-containing heterocyclic group, which is optionally substituted or fused to a C5-7 aromatic ring.
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和Y分别选自CH和CH，CF和CH，CH和CF以及N和CH; RC选自H，C 1-4烷基; 并且R 1选自C 1-7烷基，C 3-20杂环基和C 5-20芳基，该基团任选被取代; 或RC和R 1与它们所连接的碳原子和氧原子一起形成含有C 5-7的含氧杂环基团，其任选被取代或稠合至C5-7芳环。

26. 发明申请

US20080255128A1 PHTHALAZINONE DERIVATIVES 审中-公开
标题翻译：邻苯二酚衍生物
公开(公告)号：US20080255128A1
公开(公告)日：2008-10-16
申请号：US12100614
申请日：2008-04-10
申请人： Muhammad Hashim Javaid , Marc Geoffrey Hummersone , Keith Allan Menear , Sylvie Gomez , Niall Morrison Barr Martin
发明人： Muhammad Hashim Javaid , Marc Geoffrey Hummersone , Keith Allan Menear , Sylvie Gomez , Niall Morrison Barr Martin
IPC分类号： A61K31/502 , C07D237/30 , A61P35/04 , A61P3/00 , A61P9/00 , A61P19/00 , A61P25/00
CPC分类号： C07D403/10 , C07D403/14 , C07D407/14 , C07D413/14 , C07D417/14
摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X is selected from H and F; R1 and R2 are independently selected from H and methyl; RN1 is selected from H and optionally substituted C1-7 alkyl; RN2 is selected from H, optionally substituted C1-7 alkyl, C3-7 heterocyclyl and C5-6 aryl; or RN1 and RN2 and the nitrogen atom to which they are bound form an optionally substituted nitrogen containing C5-7 heterocyclic group.
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选自H和F; R 1和R 2独立地选自H和甲基; R 11选自H和任选取代的C 1-7烷基; R N2选自H，任选取代的C 1-7 - 烷基，C 3-7 - 杂环基和C 5-6杂环基， / SUB>芳基; 或R 1 N 2和R 2 N 2和它们所连接的氮原子形成任选取代的含有C 5〜5-7杂环基的氮。

27. 发明授权

US07750006B2 Phthalazinone derivatives 有权
标题翻译：酞嗪衍生物
公开(公告)号：US07750006B2
公开(公告)日：2010-07-06
申请号：US11352178
申请日：2006-02-10
申请人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Charles Richard White , Roger Frank Newton , Diane Gillian Douglas , Penny Jane Eversley , Julia Vile
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Charles Richard White , Roger Frank Newton , Diane Gillian Douglas , Penny Jane Eversley , Julia Vile
IPC分类号： A01N43/58 , A61K31/50 , C07D237/26
CPC分类号： C07D401/12 , A61K31/50 , A61K31/502 , C07D237/32 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by -L-RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(═O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, —(CH2)n3— (if present) and part of RL; and RL is optionally substituted C5-20 aryl; and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, and C5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone.
摘要翻译：一种治疗由PARP介导的人体或动物体的疾病的方法，包括向所述受试者施用治疗有效量的式：或其异构体，盐，溶剂化物，化学保护形式及其前药的化合物，其中： A和B一起表示任选取代的稠合芳环; RC由-L-RL表示，其中L为下式： - （CH2）n1-Qn2-（CH2）n3-，其中n1，n2和n3各自选自0,1,2和3，n1 ，n2和n3是1,2或3，Q选自O，S，NH，C（= O）或-CR1R2-，其中R1和R2独立地选自氢，卤素或任选取代的C 1-7烷基，或者可以与它们所连接的碳原子一起形成可以是饱和的（C 3-7环烷基）或不饱和的（C 3-7环烯基）或R 1和R 2中的一个的C 3-7环烷基可以连接到RL中的原子以形成不饱和的C 3-7环烯基，其包含在Q， - （CH 2）n 3-（如果存在）和部分RL中R 1和R 2连接的碳原子; 并且RL是任选取代的C 5-20芳基; 并且RN选自氢，任选取代的C 1-7烷基，C 3-20杂环基和C 5-20芳基，羟基，醚，硝基，氨基，酰胺基，硫醇，硫醚，亚砜和砜。

28. 发明授权

US07196085B2 Phthalazinone derivatives 失效
标题翻译：酞嗪衍生物
公开(公告)号：US07196085B2
公开(公告)日：2007-03-27
申请号：US10426147
申请日：2003-04-29
申请人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Penny Jane Eversley , Xiao-Ling Cockcroft , Frank Kerrigan , Janet Hoare , Lesley Dixon
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Penny Jane Eversley , Xiao-Ling Cockcroft , Frank Kerrigan , Janet Hoare , Lesley Dixon
IPC分类号： A01N43/60 , A01N43/58 , A61K31/50 , A61K31/495 , C07D487/00
CPC分类号： C07D401/10 , C07D237/32 , C07D403/10 , C07D495/04
摘要： A compound of formula: or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein A and B together represent an optionally substituted, fused aromatic ring; RL is a C5-7 aryl group substituted in the meta position by the group R2, and optionally further substituted; wherein R2 is selected from: and its use as a pharmaceutical, in particular for the treatment of diseases ameliorated by inhibiting the activity of PARP.
摘要翻译：式的化合物：

29. 发明授权

US07151102B2 Phthalazinone derivatives 有权
公开(公告)号：US07151102B2
公开(公告)日：2006-12-19
申请号：US10021506
申请日：2001-10-30
申请人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Charles Richard White , Roger Frank Newton , Diane Gillian Douglas , Penny Jane Eversley , Julia Vile
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Charles Richard White , Roger Frank Newton , Diane Gillian Douglas , Penny Jane Eversley , Julia Vile
IPC分类号： C07D237/26 , C07D487/00 , A01N43/58 , A61K31/50
CPC分类号： C07D401/12 , A61K31/50 , A61K31/502 , C07D237/32 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by —L—RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(═O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are attached in Q, —(CH2)n3— (if present) and part of RL; and RL is optionally substituted C5-20 aryl; and RN is selected from hydrogen, optionally substituted C1-7 alkyl, C3-20 heterocyclyl, and C5-20 aryl, hydroxy, ether, nitro, amino, amido, thiol, thioether, sulfoxide and sulfone.

30. 发明授权

US08435985B2 Pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mTOR inhibitors 有权
公开(公告)号：US08435985B2
公开(公告)日：2013-05-07
申请号：US13307342
申请日：2011-11-30
申请人： Keith Menear , Graeme Cameron Murray Smith , Karine Malagu , Heather Mary Ellen Duggan , Niall Morrison Barr Martin , Frederic Georges Marie Leroux
发明人： Keith Menear , Graeme Cameron Murray Smith , Karine Malagu , Heather Mary Ellen Duggan , Niall Morrison Barr Martin , Frederic Georges Marie Leroux
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： A61K31/5377 , A61K31/565 , A61K45/06 , C07D413/14 , C07D471/04 , C07D475/08 , C07D475/10
摘要： There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.

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