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。

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。

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。

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。

公开(公告)号：US20090069303A1

公开(公告)日：2009-03-12

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： A61K31/551 ,  C07D237/30 ,  A61K31/502 ,  C07D253/06 ,  A61K31/53 ,  A61P9/00 ,  A61P29/00 ,  A61P3/10 ,  A61P25/00 ,  A61P35/00 ,  C07D413/14 ,  A61K31/5377 ,  C07D243/08

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。

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。

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。

公开(公告)号：US20090023727A1

公开(公告)日：2009-01-22

申请号：US12167567

申请日：2008-07-03

申请人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  David Alan Rudge ,  Craig Anthony Roberts

发明人： Muhammad Hashim Javaid ,  Keith Allan Menear ,  Niall Morrison Barr Martin ,  Graeme Cameron Murray Smith ,  David Alan Rudge ,  Craig Anthony Roberts

IPC分类号： A61K31/5377 ,  A61K31/502 ,  C07D403/08 ,  A61K31/53 ,  A61P35/00 ,  C07D403/14 ,  C07D413/14

CPC分类号： C07D237/32 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12

摘要： A compound of the formula (I): wherein: R represents one or more optional substituents on the fused cyclohexene ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; if X=NRX, then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted ester, optionally substituted acyl, and optionally substituted sulfonyl groups; if X=CRXRY then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted sulfonamino, optionally substituted ether, optionally substituted ester, optionally substituted acyl, optionally substituted acylamido, and optionally substituted sulfonyl groups and RY is selected from H, hydroxy, optionally substituted amino, or RX and RY may together form an optionally substituted 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：R表示稠合环己烯环上的一个或多个任选的取代基; 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; 如果X = NRX，则RX选自H，任选取代的C 1-20烷基，任选取代的C 5-20芳基，任选取代的C 3-20杂环基，任选取代的酰胺基，任选取代的硫代酰氨基，任选取代的酯，任选地 取代的酰基和任选取代的磺酰基; 如果X = CRXRY，则RX选自H，任选取代的C 1-20烷基，任选取代的C 5-20芳基，任选取代的C 3-20杂环基，任选取代的酰胺基，任选取代的硫代酰氨基，任选取代的磺酰氨基，任选取代的 醚，任选取代的酯，任选取代的酰基，任选取代的酰基酰氨基和任选取代的磺酰基，RY选自H，羟基，任选取代的氨基，或RX和RY可以一起形成任选取代的螺C 3-7环烷基或杂环基 组; 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。

公开(公告)号：US20090209520A1

公开(公告)日：2009-08-20

申请号：US12304636

申请日：2007-06-15

申请人： Muhammad Hashim Javaid ,  Sylvie Gomez ,  Xiao-Ling Fan Cockcroft ,  Keith Allan Menear ,  Niall Morrison Barr Martin

发明人： Muhammad Hashim Javaid ,  Sylvie Gomez ,  Xiao-Ling Fan Cockcroft ,  Keith Allan Menear ,  Niall Morrison Barr Martin

IPC分类号： A61K31/55 ,  C07D295/192 ,  A61K31/495 ,  C07D223/04 ,  C07D211/32 ,  A61K31/4453 ,  C12N5/06 ,  A61P35/00

CPC分类号： C07D295/192 ,  C07C235/60 ,  C07D211/16 ,  C07D211/18 ,  C07D211/70 ,  C07D213/74 ,  C07D217/06 ,  C07D295/205

摘要： A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; Y is —CRRC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2′ together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20heterocyclyl 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 formula (ii): 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.

摘要翻译： 式（I）的化合物及其药学上可接受的盐，其中：R 2，R 3，R 4和R 5独立地选自H，C 1-7烷氧基，氨基，卤素或羟基; Y是-CRRC2-（CH2）m-，其中m是0或1，RC1选自H，CH3和CF3，RC2选自H和CH3，或RC1和RC2'与它们所代表的碳原子一起 连接形成1,1-环亚丙基基团（A）：RN1和RN2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杂环基和C 5-20芳基; 或RN1和RN2与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为式（ⅱ）：其中Y1和Y3独立地选自CH和N，Y2选自CX和N，X是H，Cl或F.

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.