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公开(公告)号：US07407957B2
公开(公告)日：2008-08-05
申请号：US11213504
申请日：2005-08-26
申请人： Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Naill 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 , Naill 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： 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, 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独立地选自氢和C 1-4烷基，或当X是C 1-4烷基时， R 1，X 2，R 2，R 2，R 2，X 2， 与它们所连接的碳原子一起可以形成任选取代的稠合芳环; R 1选自H和卤素; 并且Het选自：其中Y 1选自CH，N，Y 2选自CH和N，Y 3选自 从CH，CF和N，其中Y 1，Y 2和Y 3中只有一个或两个可以是N; 而Q是O或S.
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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：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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公开(公告)号：US20060063767A1
公开(公告)日：2006-03-23
申请号：US11213504
申请日：2005-08-26
申请人： Muhammad Javaid , Graeme Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-lai Loh , Xiao-Ling Cockcroft , Stefano Forte , Keith Menear , Ian Timothy William Matthews
发明人： Muhammad Javaid , Graeme Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-lai Loh , Xiao-Ling Cockcroft , Stefano Forte , Keith Menear , Ian Timothy William Matthews
IPC分类号： A61K31/502 , C07D403/02
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, 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：
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