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1. 发明授权

US07407957B2 Phthalazinone derivatives 失效
标题翻译：酞嗪衍生物
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.

2. 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.

3. 发明授权

US07666870B2 Phthalazinone derivatives 失效
标题翻译：酞嗪衍生物
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.

4. 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。

5. 发明申请

US20090069303A1 PHTHALAZINONE DERIVATIVES 失效
标题翻译：邻苯二酚衍生物
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。

6. 发明授权

US07902193B2 Phthalazinone derivatives 失效
标题翻译：酞嗪衍生物
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。

7. 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。

8. 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。

9. 发明授权

US07674823B2 DNA-PK inhibitors 失效
标题翻译： DNA-PK抑制剂
公开(公告)号：US07674823B2
公开(公告)日：2010-03-09
申请号：US11758332
申请日：2007-06-05
申请人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Roger John Griffin , Bernard Thomas Golding , Ian Robert Hardcastle , David Richard Newell , Hilary Alan Calvert , Nicola Jane Curtin , Laurent Jean Martin Rigoreau , Xiao-ling Fan Cockcroft , Vincent Junior Ming-lai Loh , Paul Workman , Florence Irene Raynaud , Bernard Paul Nutley
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Roger John Griffin , Bernard Thomas Golding , Ian Robert Hardcastle , David Richard Newell , Hilary Alan Calvert , Nicola Jane Curtin , Laurent Jean Martin Rigoreau , Xiao-ling Fan Cockcroft , Vincent Junior Ming-lai Loh , Paul Workman , Florence Irene Raynaud , Bernard Paul Nutley
IPC分类号： A61K31/351
CPC分类号： C07D417/04 , C07D309/38 , C07D311/22 , C07D311/92 , C07D471/04
摘要： The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein 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, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR′4 and NR″4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R′4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R′4 is H, or R3 and R4 or R″4 together are —A—B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.
摘要翻译：本发明涉及式（I）化合物及其异构体，盐，溶剂合物，化学保护形式及其前药在制备用于抑制DNA-PK活性的药物中的用途，其中R1和R2独立地为氢，任选取代的C 1-7烷基，C 3-20杂环基或C 5-20芳基，或者可以与它们所连接的氮原子一起形成任选取代的具有4-8个环的杂环原子 X和Y选自CR4和O，O和CR'4和NR "4和N，其中不饱和键在环中的适当位置，并且其中R3和R4或R'4之一是任选取代的C3 -20杂芳基或C5-20芳基，R3和R4或R'4中的另一个为H，或R3和R4或R“4一起为-A-B-，它们共同表示稠合的任选取代的芳环。与PI3-激酶和/或ATM相比，化合物还选择性地抑制DNA-PK的活性。

10. 发明授权

US07226918B2 DNA-PK inhibitors 有权
标题翻译： DNA-PK抑制剂
公开(公告)号：US07226918B2
公开(公告)日：2007-06-05
申请号：US10486816
申请日：2002-08-14
申请人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Roger John Griffin , Bernard Thomas Golding , Ian Robert Hardcastle , David Richard Newell , Hilary Alan Calvert , Nicola Jane Curtin , Laurent Jean Martin Rigoreau , Xiao-ling Fan Cockcroft , Vincent Junior Ming-lai Loh , Paul Workman , Florence Irene Raynaud , Bernard Paul Nutley
发明人： Niall Morrison Barr Martin , Graeme Cameron Murray Smith , Roger John Griffin , Bernard Thomas Golding , Ian Robert Hardcastle , David Richard Newell , Hilary Alan Calvert , Nicola Jane Curtin , Laurent Jean Martin Rigoreau , Xiao-ling Fan Cockcroft , Vincent Junior Ming-lai Loh , Paul Workman , Florence Irene Raynaud , Bernard Paul Nutley
IPC分类号： A61K31/353 , A61K31/5377 , C07D265/30 , C07D311/58
CPC分类号： C07D417/04 , C07D309/38 , C07D311/22 , C07D311/92 , C07D471/04
摘要： The invention relates to the use of compounds of formula (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, in the preparation of a medicament for inhibiting the activity of DNA-PK, wherein 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, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X and Y are selected from CR4 and O, O and CR′4 and NR″4 and N, where the unsaturation is in the appropriate place in the ring, and where one of R3 and R4 or R′4 is an optionally substituted C3-20 heteroaryl or C5-20 aryl group, and the other of R3 and R4 or R′4 is H, or R3 and R4 or R″4 together are -A-B—, which collectively represent a fused optionally substituted aromatic ring. The compounds also selectively inhibit the activity of DNA-PK compared to PI 3-kinase and/or ATM.
摘要翻译：本发明涉及式（I）化合物及其异构体，盐，溶剂合物，化学保护形式及其前药在制备用于抑制DNA-PK活性的药物中的用途，其中R 1， R 2和R 2各自独立地为氢，任选取代的C 1-7 - 烷基，C 3-20杂环基或C 或者可以与它们所连接的氮原子一起形成具有4-8个环原子的任选取代的杂环; X和Y选自CR 4和O，O和CR'4和NR“4和N，其中不饱和键处于 R 2中的一个是R 3，R 4，R 4和R 4中的一个是任选取代的C 3 -20个杂芳基或C 5-20-20芳基，R 3和R 4中的另一个或R' > 4 是H，或R 3和R 4或R“4”一起是-AB-，它们共同表示稠合的任选取代的芳环。与PI3-激酶和/或ATM相比，化合物还选择性地抑制DNA-PK的活性。

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