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1. 发明申请

US20120129855A1 PHTHALAZINONE DERIVATIVES 审中-公开
标题翻译：邻苯二酚衍生物
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。

2. 发明授权

US08129380B2 Phthalazinone derivatives 失效
标题翻译：酞嗪酮衍生物
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。

3. 发明申请

US20090192156A1 PHTHALAZINONE DERIVATIVES 失效
标题翻译：邻苯二酚衍生物
公开(公告)号：US20090192156A1
公开(公告)日：2009-07-30
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： A61K31/5025 , C07D401/10 , C07D401/14 , C07D491/107 , C07D487/04 , C07D413/14 , A61K31/502 , A61K31/5377 , A61P9/00 , A61P25/00 , A61P31/12 , 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。

4. 发明申请

US20090023727A1 PHTHALAZINONE DERIVATIVES 审中-公开
标题翻译：邻苯二酚衍生物
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。

5. 发明申请

US20090048269A1 CHEMICAL COMPOUNDS-821 审中-公开
标题翻译：化学化合物-821
公开(公告)号：US20090048269A1
公开(公告)日：2009-02-19
申请号：US12190008
申请日：2008-08-12
申请人： Maurice Raymond Finlay , Frederick Woolf Goldberg , Craig Anthony Roberts , Nicola Jane Roberts , David Alan Rudge
发明人： Maurice Raymond Finlay , Frederick Woolf Goldberg , Craig Anthony Roberts , Nicola Jane Roberts , David Alan Rudge
IPC分类号： A61K31/497 , C07D401/12 , C07D401/14 , A61K31/444
CPC分类号： C07D213/74 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The invention relates to chemical compounds of the formula (I), or pharmaceutically acceptable salts thereof, which possess ALK5 (TGFβR1) inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及具有ALK5（TGFbetaR1）抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

6. 发明授权

US08247562B2 Benzamide derivatives useful as histone deacetylase inhibitors 有权
标题翻译：可用作组蛋白脱乙酰酶抑制剂的苯甲酰胺衍生物
公开(公告)号：US08247562B2
公开(公告)日：2012-08-21
申请号：US12879367
申请日：2010-09-10
申请人： Elaine Sophie Elizabeth Stokes , Craig Anthony Roberts , Michael James Waring
发明人： Elaine Sophie Elizabeth Stokes , Craig Anthony Roberts , Michael James Waring
IPC分类号： C07D211/32 , C07D401/06 , A61K31/452 , A61P35/00
CPC分类号： C07D239/26 , C07D211/34 , C07D213/56 , C07D213/74 , C07D215/12 , C07D237/08 , C07D239/42 , C07D241/20 , C07D251/18 , C07D277/24 , C07D277/30 , C07D295/155 , C07D307/54 , C07D401/04 , C07D401/06 , C07D403/12 , C07D405/06 , C07D409/04 , C07D417/06 , C07D487/04 , C07D495/04
摘要： The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by histone deacetylase.
摘要翻译：本发明涉及式（I）化合物，其中环A是杂环基; m为0-4，R 1为羟基，卤素，三氟甲基，氰基等基团。 R2为卤素，n为0-2; 并且每个R 4是诸如羟基，卤素，三氟甲基和氰基的基团; p为0-4; 并且R 3是氨基或羟基; 或其药学上可接受的盐或体内可水解的酯或酰胺; 其制备方法，含有它们的药物组合物及其在治疗由组蛋白脱乙酰酶介导的疾病或医学病症中的用途。

7. 发明申请

US20100331329A1 BENZAMIDE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS 有权
标题翻译：苯甲酸衍生物有用作组织脱乙酰酶抑制剂
公开(公告)号：US20100331329A1
公开(公告)日：2010-12-30
申请号：US12879367
申请日：2010-09-10
申请人： Elaine Sophie Elizabeth Stokes , Craig Anthony Roberts , Michael James Waring
发明人： Elaine Sophie Elizabeth Stokes , Craig Anthony Roberts , Michael James Waring
IPC分类号： A61K31/5377 , C07D213/56 , C07D215/14 , C07D241/12 , C07D307/54 , C07D277/30 , C07D239/42 , C07D239/30 , C07D265/30 , C07D211/34 , C07D413/04 , C07D403/12 , C07D401/12 , C07D413/12 , C07D495/04 , C07D239/38 , C07D473/00 , C07D251/48 , A61P35/00 , A61K31/4418 , A61K31/47 , A61K31/4965 , A61K31/341 , A61K31/426 , A61K31/505 , A61K31/5375 , A61K31/451 , A61K31/506 , A61K31/496 , A61K31/519 , A61K31/4365 , A61K31/52 , A61K31/53
CPC分类号： C07D239/26 , C07D211/34 , C07D213/56 , C07D213/74 , C07D215/12 , C07D237/08 , C07D239/42 , C07D241/20 , C07D251/18 , C07D277/24 , C07D277/30 , C07D295/155 , C07D307/54 , C07D401/04 , C07D401/06 , C07D403/12 , C07D405/06 , C07D409/04 , C07D417/06 , C07D487/04 , C07D495/04
摘要： The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.
摘要翻译：本发明涉及式（I）化合物，其中环A是杂环基; m为0-4，R 1为羟基，卤素，三氟甲基，氰基等基团。 R2为卤素，n为0-2; 并且每个R 4是诸如羟基，卤素，三氟甲基和氰基的基团; p为0-4; 并且R 3是氨基或羟基; 或其药学上可接受的盐或体内可水解的酯或酰胺; 其制备方法，含有它们的药物组合物及其在治疗由组蛋白脱乙酰酶介导的疾病或医学条件中的用途。

8. 发明申请

US20100075942A1 N-PHENYL-4-PYRIDIN-2-YL-BENZAMIDE DERIVATIVES AS HISTONE DEACYLASE (HDAC) INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：作为治疗癌症的HISTONE DEACYLASE（HDAC）抑制剂的N-苯基-4-吡啶-2-基-L-苯甲酰胺衍生物
公开(公告)号：US20100075942A1
公开(公告)日：2010-03-25
申请号：US11813838
申请日：2006-01-12
申请人： Keith Hopkinson Gibson , Elaine Sophie, Elizabeth Stokes , Michael James Waring , David Michael Andrews , Zbigniew Stanley Matusiak , Mark Maybury , Craig Anthony Roberts
发明人： Keith Hopkinson Gibson , Elaine Sophie, Elizabeth Stokes , Michael James Waring , David Michael Andrews , Zbigniew Stanley Matusiak , Mark Maybury , Craig Anthony Roberts
IPC分类号： A61K31/4418 , C07D213/61 , C07D401/12 , C07D213/82 , C07D401/06 , A61K31/496 , A61K31/4523
CPC分类号： C07D213/82 , C07D213/61 , C07D213/65
摘要： The invention concerns benzamide derivatives of Formula (I) wherein R1a, R1b, R1c, R2, R3, R4, W, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).
摘要翻译：本发明涉及式（I）的苯甲酰胺衍生物，其中R1a，R1b，R1c，R2，R3，R4，W，m和n具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对组蛋白脱乙酰酶（HDAC）的抑制敏感的肿瘤或其它增殖病症中的抗增殖剂的药物中的用途。

9. 发明申请

US20090029991A1 BENZAMIDE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：苯甲酸衍生物有用作组织脱乙酰酶抑制剂
公开(公告)号：US20090029991A1
公开(公告)日：2009-01-29
申请号：US12211510
申请日：2008-09-16
申请人： Elaine Sophie Elizabeth Stokes , Craig Anthony Roberts , Michael James Waring
发明人： Elaine Sophie Elizabeth Stokes , Craig Anthony Roberts , Michael James Waring
IPC分类号： A61K31/5377 , C07D495/04 , A61K31/519
CPC分类号： C07D239/26 , C07D211/34 , C07D213/56 , C07D213/74 , C07D215/12 , C07D237/08 , C07D239/42 , C07D241/20 , C07D251/18 , C07D277/24 , C07D277/30 , C07D295/155 , C07D307/54 , C07D401/04 , C07D401/06 , C07D403/12 , C07D405/06 , C07D409/04 , C07D417/06 , C07D487/04 , C07D495/04
摘要： The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by histone deacetylase.
摘要翻译：本发明涉及式（I）化合物，其中环A是杂环基; m为0-4，R 1为羟基，卤素，三氟甲基，氰基等基团。 R2为卤素，n为0-2; 并且每个R 4是诸如羟基，卤素，三氟甲基和氰基的基团; p为0-4; 并且R 3是氨基或羟基; 或其药学上可接受的盐或体内可水解的酯或酰胺，其制备方法，含有它们的药物组合物及其在治疗由组蛋白脱乙酰酶介导的疾病或医学病症中的用途。

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