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公开(公告)号：US07049313B2
公开(公告)日：2006-05-23
申请号：US10373114
申请日：2003-02-24
申请人： Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Stephen Philip Jackson , Mark James O'Connor , Alan Yin Kai Lau , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Laurent Jean Martin Rigoreau , Marc Geoffery Hummersone , Roger John Griffin
发明人： Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Stephen Philip Jackson , Mark James O'Connor , Alan Yin Kai Lau , Xiao-Ling Fan Cockcroft , Ian Timothy Williams Matthews , Keith Allan Menear , Laurent Jean Martin Rigoreau , Marc Geoffery Hummersone , Roger John Griffin
IPC分类号： A61K31/535 , C07D413/00 , A61P35/00
CPC分类号： C07D409/04 , C07D417/04
摘要： The application concerns a compound of formula I: wherein one of P and Q is O, and the other of P and Q is CH, where there is a double bond between whichever of Q and P is CH and the carbon atom bearing the R3 group; Y is either O or S; 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 an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; R3 is a phenyl or pyridyl group, attached by a first bridge group selected from —S—, —S(═O)—, —S(═O)2—, —O—, —NRN— and CRC1RC2— to an optionally substituted C5-20 carboaryl group, the phenyl or pyridyl group and optionally substituted C5-20 carboaryl group being optionally further linked by a second bridge group, so as to form an optionally substituted C5-7 ring, the phenyl or pyridyl group being further optionally substituted.
摘要翻译： 本申请涉及式I化合物：其中P和Q中的一个为O，P和Q中的另一个为CH，其中Q和P中的任一个为CH且具有R 1的碳原子之间为双键， SUP> 3 组; Y是O或S; R 1和R 2独立地是氢，任选取代的C 1-7烷基，C 3-20 或杂环基，或C 5-20-20芳基，或者可以一起形成任选取代的具有4至8个环原子的杂环; R 3是通过选自-S - ， - S（-O） - ， - S（-O）2 N的第一桥基团连接的苯基或吡啶基） - ， - O - ， - NR N - 和CR C1 - C2 - 与任选取代的C 5-20 - 苯基或吡啶基和任选取代的C 5-20碳芳基任选地通过第二桥基进一步连接，从而形成任选取代的C 5-7 苯基或吡啶基进一步任选被取代。
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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。
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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。
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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。
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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：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：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：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：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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