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公开(公告)号:US07981889B2
公开(公告)日:2011-07-19
申请号:US12109260
申请日:2008-04-24
申请人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
发明人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号: A61K31/50 , A61K31/495 , C07D487/00
CPC分类号: A61K31/502 , A61K31/00 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/06 , A61N5/10 , C07D237/32 , C07D243/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , 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NRX或CRXRY; 如果X = NRX则n为1或2,如果X = CRXRY则n为1; RX选自H,任选取代的C 1-20烷基,C 5-20芳基,C 3-20杂环基,酰氨基,硫代酰氨基,酯,酰基和磺酰基; RY选自H,羟基,氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2均为氢,或当X为CRXRY时,RC1,RC2,RX和RY与它们所连接的碳原子一起形成任选取代的稠合芳环; 并且R 1选自H和卤素。
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公开(公告)号:US08912187B2
公开(公告)日:2014-12-16
申请号:US13179353
申请日:2011-07-08
申请人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
发明人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号: A01N43/58 , A61K31/50 , C07D237/30
CPC分类号: A61K31/502 , A61K31/00 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/06 , A61N5/10 , C07D237/32 , C07D243/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , 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NRX或CRXRY; 如果X = NRX则n为1或2,如果X = CRXRY则n为1; RX选自H,任选取代的C 1-20烷基,C 5-20芳基,C 3-20杂环基,酰氨基,硫代酰氨基,酯,酰基和磺酰基; RY选自H,羟基,氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2均为氢,或当X为CRXRY时,RC1,RC2,RX和RY与它们所连接的碳原子一起形成任选取代的稠合芳环; 并且R 1选自H和卤素。
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公开(公告)号:US07662818B2
公开(公告)日:2010-02-16
申请号:US11318155
申请日:2005-12-23
申请人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
发明人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号: A01N43/60 , C07D221/02 , C07D237/30
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NRX或CRXRY; 如果X = NRX,则n为1或2,如果X = CRXRY,则n为1; RX选自H,任选取代的C 1-20烷基,C 5-20芳基,C 3-20杂环基,酰氨基,硫代酰氨基,酯,酰基和磺酰基; RY选自H,羟基,氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2均为氢,或当X为CRXRY时,RC1,RC2,RX和RY与它们所连接的碳原子一起形成任选取代的稠合芳环; 并且R 1选自H和卤素。
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公开(公告)号:US20080200469A1
公开(公告)日:2008-08-21
申请号:US12109260
申请日:2008-04-24
申请人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
发明人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号: A61K31/502 , C07D403/08 , A61P35/04
CPC分类号: A61K31/502 , A61K31/00 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/06 , A61N5/10 , C07D237/32 , C07D243/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , 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:US07449464B2
公开(公告)日:2008-11-11
申请号:US10876080
申请日:2004-06-24
申请人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
发明人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent Junior M Loh , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号: A01N43/60 , A01N43/58 , A61K31/50 , A61K31/495 , C07D487/00
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:US20120010204A1
公开(公告)日:2012-01-12
申请号:US13179353
申请日:2011-07-08
申请人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent M. Loh, JR. , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
发明人: Niall Morrison Barr Martin , Graeme Cameron Smith , Stephen Philip Jackson , Vincent M. Loh, JR. , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Frank Kerrigan , Alan Ashworth
IPC分类号: A61K31/502 , A61P35/00 , A61K31/5377
CPC分类号: A61K31/502 , A61K31/00 , A61K31/506 , A61K31/5377 , A61K31/551 , A61K45/06 , A61N5/10 , C07D237/32 , C07D243/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , 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NRX或CRXRY; 如果X = NRX则n为1或2,如果X = CRXRY则n为1; RX选自H,任选取代的C 1-20烷基,C 5-20芳基,C 3-20杂环基,酰氨基,硫代酰氨基,酯,酰基和磺酰基; RY选自H,羟基,氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2均为氢,或当X为CRXRY时,RC1,RC2,RX和RY与它们所连接的碳原子一起形成任选取代的稠合芳环; 并且R 1选自H和卤素。
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公开(公告)号:US07470688B2
公开(公告)日:2008-12-30
申请号:US11550004
申请日:2006-10-17
申请人: Muhammad Hashim Javaid , Keith Allan Menear , Sylvie Gomez , Marc Geoffrey Hummersone , Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Xiao-Ling Fan Cockcroft , Frank Kerrigan
发明人: Muhammad Hashim Javaid , Keith Allan Menear , Sylvie Gomez , Marc Geoffrey Hummersone , Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Xiao-Ling Fan Cockcroft , Frank Kerrigan
IPC分类号: A61K31/502 , A61K31/5355 , A61K31/53 , C07D487/00 , C07D413/10 , C07D253/04 , C07D253/06 , C07D251/10 , A61P9/10
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) 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 heterocyclic 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.
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; D选自:(i)其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N; 和(ii)其中Q为O或S; RD是:其中RN1选自H和任选取代的C 1-10烷基; X选自单键NRN2,CRC3RC4和C-O; RN2选自H和任选取代的C 1-10烷基; RC3和RC4独立地选自H,R,C(-O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; Y选自NRN3和CRC1RC2; RC1和RC2独立地选自H,R,C(-O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; RC1和RC2与它们所连接的碳原子一起可以形成任选取代的螺 - 稠合的C 5-7碳环或杂环; 当X是单键时,RN1和RC2可以与它们所结合的N和C原子一起形成任选取代的C 5-7杂环; 并且当X是CRC3RC4时,RC2和RC4可以一起形成附加键,使得在被RC1和RC3取代的原子之间存在双键。
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公开(公告)号:US20090163477A1
公开(公告)日:2009-06-25
申请号:US12143208
申请日:2008-06-20
申请人: Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-lai Loh , Xiao-Ling Fan Cockcroft , Stefano Forte , Keith Allan Menear , Ian Timothy William Matthews , Frank Kerrigan
发明人: Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-lai Loh , Xiao-Ling Fan Cockcroft , Stefano Forte , Keith Allan Menear , Ian Timothy William Matthews , Frank Kerrigan
IPC分类号: A61K31/502 , C07D401/14 , C07D413/14 , A61K31/551 , A61P9/00 , A61P35/00 , A61P29/00 , A61K31/5377 , C07D405/14 , C07D409/14
CPC分类号: C07D401/06 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06
摘要: A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, 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 independently selected from the group consisting of hydrogen and C1-4 alkyl, or when X is CRXRY, RC1, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het 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, where only one or two of Y1, Y2 and Y3 can be N; and where Q is O or S.
摘要翻译: 式(I)的化合物:用于治疗通过抑制PARP而改善的癌症或其它疾病,其中:A和B一起表示任选取代的稠合芳环; X可以是NRX或CRXRY; 如果X-NRX则n为1或2,如果X-CRXRY则n为1; RX选自H,任选取代的C 1-20烷基,C 5-20芳基,C 3-20杂环基,酰氨基,硫代酰氨基,酯,酰基和磺酰基; RY选自H,羟基,氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2独立地选自氢和C 1-4烷基,或当X是CRXRY,RC1,RC1,RC2,RX和RY时,连同它们所连接的碳原子一起可以形成任选取代的 稠合芳环; R1选自H和卤素; Het选自:其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N,其中Y1,Y2和Y3中只有一个可以是N; 而Q是O或S.
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公开(公告)号:US07902193B2
公开(公告)日:2011-03-08
申请号:US12271308
申请日:2008-11-14
申请人: Muhammad Hashim Javaid , Keith Allan Menear , Sylvie Gomez , Marc Geoffrey Hummersone , Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Xiao-Ling Fan Cockcroft , Frank Kerrigan
发明人: Muhammad Hashim Javaid , Keith Allan Menear , Sylvie Gomez , Marc Geoffrey Hummersone , Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Xiao-Ling Fan Cockcroft , Frank Kerrigan
IPC分类号: C07D237/32 , A61K31/502 , A61P35/00
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) 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.
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; D选自:(i)其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N; 和(ii)其中Q为O或S; RD是:其中RN1选自H和任选取代的C 1-10烷基; X选自单键NRN2,CRC3RC4和C = O; RN2选自H和任选取代的C 1-10烷基; RC3和RC4独立地选自H,R,C(= O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; Y选自NRN3和CRC1RC2。 RC1和RC2独立地选自H,R,C(= O)OR,其中R是任选取代的C 1-10烷基,任选取代的C 5-20芳基或任选取代的C 3-20杂环基; RC1和RC2与它们所连接的碳原子一起可以形成任选取代的螺 - 稠合的C 5-7碳环或杂环; 当X是单键时,RN1和RC2可以与它们所结合的N和C原子一起形成任选被取代的C5-7杂环; 并且当X是CRC3RC4时,RC2和RC4可以一起形成附加键,使得在被RC1和RC3取代的原子之间存在双键。
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公开(公告)号:US07666870B2
公开(公告)日:2010-02-23
申请号:US12143208
申请日:2008-06-20
申请人: Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-Iai Loh , Xiao-Ling Fan Cockcroft , Stefano Forte , Keith Allan Menear , Ian Timothy William Matthews , Frank Kerrigan
发明人: Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-Iai Loh , Xiao-Ling Fan Cockcroft , Stefano Forte , Keith Allan Menear , Ian Timothy William Matthews , Frank Kerrigan
IPC分类号: C07D403/02 , A61K31/502
CPC分类号: C07D401/06 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06
摘要: A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, 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 independently selected from the group consisting of hydrogen and C1-4 alkyl, or when X is CRXRY, RC1, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het 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, where only one or two of Y1, Y2 and Y3 can be N; and where Q is O or S.
摘要翻译: 式(I)的化合物:用于治疗通过抑制PARP而改善的癌症或其它疾病,其中:A和B一起表示任选取代的稠合芳环; X可以是NRX或CRXRY; 如果X = NRX则n为1或2,如果X = CRXRY则n为1; RX选自H,任选取代的C 1-20烷基,C 5-20芳基,C 3-20杂环基,酰氨基,硫代酰氨基,酯,酰基和磺酰基; RY选自H,羟基,氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2独立地选自氢和C 1-4烷基,或当X是CRXRY,RC1,RC1,RC2,RX和RY时,连同它们所连接的碳原子一起可以形成任选取代的 稠合芳环; R1选自H和卤素; Het选自:其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N,其中Y1,Y2和Y3中只有一个可以是N; 而Q是O或S.
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