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1. 发明授权

US08912187B2 Phthalazinone derivatives 有权
标题翻译：酞嗪衍生物
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。

2. 发明申请

US20140248378A1 PYRIMIDINONE COMPOUNDS AND THEIR USE 审中-公开
标题翻译：吡咯烷酮化合物及其用途
公开(公告)号：US20140248378A1
公开(公告)日：2014-09-04
申请号：US14131337
申请日：2012-07-05
申请人： Xiao-Ling Fan Cockcroft , William Farnaby , Natasha Kinsella , Kevin Merchant , David Miller
发明人： Xiao-Ling Fan Cockcroft , William Farnaby , Natasha Kinsella , Kevin Merchant , David Miller
IPC分类号： A61K31/513 , C07D239/22 , C07D403/12 , C07D401/12 , A61K45/06 , C07D471/04 , C07D413/12 , C07D405/12
CPC分类号： A61K31/513 , A61K45/06 , C07D239/22 , C07D239/54 , C07D239/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供式（1）化合物及其药学上可接受的盐，其中R1，R2，Y和Z如说明书中所定义，其制备方法，含有它们的药物组合物及其在治疗中的用途。

3. 发明申请

US20100130473A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：US20100130473A1
公开(公告)日：2010-05-27
申请号：US11817134
申请日：2006-02-24
申请人： Marc Geoffrey Hummersone , Sylvie Gomez , Keith Allan Menear , Xiao-Ling Fan Cockcroft , Graeme Cameron Murray Smith
发明人： Marc Geoffrey Hummersone , Sylvie Gomez , Keith Allan Menear , Xiao-Ling Fan Cockcroft , Graeme Cameron Murray Smith
IPC分类号： A61K31/5377 , C07D413/04 , C07D413/14 , C07D471/04 , A61P35/00 , A61K31/53 , A61K31/551 , A61K31/553 , A61K31/519
CPC分类号： C07D251/70 , C07D239/48 , C07D239/50 , C07D239/94 , C07D295/135 , C07D403/04 , C07D403/12 , C07D405/04 , C07D413/12 , C07D417/04 , C07D471/04
摘要： Compounds of formula (I): A-B—C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an optionally substituted N-containing C5-7 heterocyclic group; RC5 is a group selected from formula (iv) which group may be selected by one or two C1-4 alkyl groups or a carboxy group; RC6 is H; or, when X and Y are N, RC5 and RC6 (when Z is CRC6) together with the carbon atoms to which they are attached may form a fused C6 aromatic ring selected from the group consisting of formula (v).
摘要翻译：式（I）化合物：A-B-C及其异构体，盐，溶剂合物，化学保护形式及其前药。其中：B选自式（ⅰ），其中RN为H或Me; 或B是含有一个或两个环杂原子的二价C5杂环残基; A是式（ⅱ）RA 3和RA 5独立地选自卤素，ORO和RAC，其中RO是H或Me，RAC是H或C 1-4烷基; XA选自N和CRA4，其中RA4选自H，ORO，CH2OH，CO2H，NHSO2Me和NHCOMe; RA2和RA6独立地选自H，卤素和ORO; 或RA3和RA4与它们所连接的碳原子一起，或RA2和RA3与它们所连接的碳原子一起可以形成含有至少一个氮环原子的C 5-6杂环或杂芳环; 其中如果X不是RA，RA6的N，1,2或3不是H; C是式（ⅲ），其中X选自N和CH，Y选自N和CH，Z选自N和CRC 6; RC3选自H，卤素和任选取代的含N的C 5-7杂环基; RC5是选自式（iv）的基团，该基团可以被一个或两个C 1-4烷基或羧基选择; RC6为H; 或者当X和Y为N时，RC5和RC6（当Z为CRC6时）与它们所连接的碳原子一起形成选自式（v）的稠合C 6芳环。

4. 发明授权

US07504397B2 mTOR inhibitor compounds 失效
标题翻译： mTOR抑制剂化合物
公开(公告)号：US07504397B2
公开(公告)日：2009-03-17
申请号：US11361599
申请日：2006-02-24
申请人： Marc Geoffrey Hummersone , Sylvie Gomez , Keith Allan Menear , Xiao-Ling Fan Cockcroft , Graeme Cameron Murray Smith
发明人： Marc Geoffrey Hummersone , Sylvie Gomez , Keith Allan Menear , Xiao-Ling Fan Cockcroft , Graeme Cameron Murray Smith
IPC分类号： A01N43/58 , A61K31/50 , C07D239/00 , C07D239/02
CPC分类号： C07D251/54 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D417/04 , C07D471/04
摘要： Compounds of formula I: A-B-C (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof are provided, wherein variables A, B and C are defined herein and wherein such compounds act as mTor inhibitors.
摘要翻译：式I化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> ABC（I）<？in-line-formula description =“In-line Formulas”end =“tail 提供了异构体，盐，溶剂化物，化学保护形式和前体药物，其中变量A，B和C在本文中定义，并且其中这些化合物作为mTor抑制剂。

5. 发明授权

US07470688B2 Phthalazinone derivatives 失效
标题翻译：酞嗪衍生物
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。

6. 发明授权

US07981889B2 Phthalazinone derivatives 有权
标题翻译：酞嗪衍生物
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。

7. 发明申请

US20090043091A1 ATM INHIBITORS 审中-公开
标题翻译： ATM抑制剂
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。

8. 发明申请

US20090209520A1 2 -OXYBENZAMIDE DERIVATIVES AS PARP INHIBITORS 审中-公开
标题翻译： 2 - 苯甲酰胺衍生物作为PARP抑制剂
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.

9. 发明申请

US20090163477A1 PHTHALAZINONE DERIVATIVES 失效
标题翻译：邻苯二酚衍生物
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.

10. 发明授权

US10085986B2 Pyrimidinone compounds and their use 有权
公开(公告)号：US10085986B2
公开(公告)日：2018-10-02
申请号：US14131337
申请日：2012-07-05
申请人： Xiao-Ling Fan Cockcroft , William Farnaby , Natasha Kinsella , Kevin Merchant , David Miller
发明人： Xiao-Ling Fan Cockcroft , William Farnaby , Natasha Kinsella , Kevin Merchant , David Miller
IPC分类号： C07F9/02 , A61K31/513 , C07D239/54 , C07D239/60 , A61K45/06 , C07D239/22 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

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