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1. 发明授权

US07754725B2 Dihydroxyphenyl isoindolymethanones 有权
标题翻译：二羟基苯基异吲哚酮
公开(公告)号：US07754725B2
公开(公告)日：2010-07-13
申请号：US11680818
申请日：2007-03-01
申请人： Gianni Chessari , Maria Grazia Carr , Miles Stuart Congreve , Robert Downham , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
发明人： Gianni Chessari , Maria Grazia Carr , Miles Stuart Congreve , Robert Downham , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
IPC分类号： C07D209/44 , A61K31/4035 , A61K31/496 , A61K31/454
CPC分类号： C07D209/44 , C07D401/04 , C07D401/12
摘要： Compounds having the formula (I): and in particular, those of subgenus VIIa are disclosed as inhibits or modulators of the activity of the heat shock protein Hsp90. As such they are useful for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma.
摘要翻译：公开了具有式（I）：特别是亚属VIIa的化合物作为热休克蛋白Hsp90的活性的抑制剂或调节剂。因此，它们可用于治疗癌症，特别是淋巴或骨髓谱系的造血肿瘤，前列腺癌，肺癌，胃肠道间质瘤，乳腺癌和黑素瘤。

2. 发明申请

US20090215772A1 Hydroxybenzamide derivatives and their use as inhibitors of HSP90 有权
标题翻译：羟基苯甲酰胺衍生物及其作为HSP90抑制剂的用途
公开(公告)号：US20090215772A1
公开(公告)日：2009-08-27
申请号：US11911490
申请日：2006-04-13
申请人： Gianni Chessari , Miles Stuart Congreve , Eva Figueroa Navarro , Martyn Frederickson , Christopher Murray , Alison Jo-Anne Woolford , Maria Grazia Carr , Michael Alistair O'Brien , Andrew James Woodhead , Robert Downham , Theresa Rachel Phillips
发明人： Gianni Chessari , Miles Stuart Congreve , Eva Figueroa Navarro , Martyn Frederickson , Christopher Murray , Alison Jo-Anne Woolford , Maria Grazia Carr , Michael Alistair O'Brien , Andrew James Woodhead , Robert Downham , Theresa Rachel Phillips
IPC分类号： A61K31/5377 , C07D209/44 , A61K31/403 , A61K31/454 , C07D401/02 , C07D403/02 , A61K31/497 , C07D413/14
CPC分类号： C07D401/12 , C07C65/21 , C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
摘要： The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbylamino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur.The compounds have activity as Hsp90 inhibitors.
摘要翻译：本发明提供式（I）的化合物：或其盐，互变异构体，溶剂合物和N-氧化物; 其中R1是羟基或氢; R2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的一或二-C 1-5烃基氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。该化合物具有作为Hsp90抑制剂的活性。

3. 发明授权

US08530469B2 Therapeutic combinations of hydroxybenzamide derivatives as inhibitors of HSP90 有权
标题翻译：作为HSP90抑制剂的羟基苯甲酰胺衍生物的治疗组合
公开(公告)号：US08530469B2
公开(公告)日：2013-09-10
申请号：US13271678
申请日：2011-10-12
申请人： Gianni Chessari , Miles Stuart Congreve , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Alison Jo-Anne Woolford , Maria Grazia Carr , Robert Downham , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
发明人： Gianni Chessari , Miles Stuart Congreve , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Alison Jo-Anne Woolford , Maria Grazia Carr , Robert Downham , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
IPC分类号： A61K31/4035 , A61K31/47 , A61K31/496 , A61K31/5377 , C07D209/04 , C07D215/00 , C07D217/00 , C07D227/00 , C07D241/00 , C07D265/30 , C07D401/02 , C07D471/00
CPC分类号： C07D401/12 , C07C65/21 , C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
摘要： The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
摘要翻译：本发明提供了包含式（VII）的Hsp90抑制剂化合物或其互变异构体或其盐和选自拓扑异构酶I抑制剂的一种或多种治疗剂的组合; 抗代谢药物微管蛋白靶向剂; DNA结合剂和拓扑异构酶II抑制剂; 烷基化剂; 单克隆抗体抗激素; 信号转导抑制剂; 蛋白酶体抑制剂; DNA甲基转移酶; 细胞因子; 类视色素和HDAC或HAT调节剂。

4. 发明授权

US08101648B2 Hydroxybenzamide derivatives and their use as inhibitors of HSP90 有权
标题翻译：羟基苯甲酰胺衍生物及其作为HSP90抑制剂的用途
公开(公告)号：US08101648B2
公开(公告)日：2012-01-24
申请号：US11911490
申请日：2006-04-13
申请人： Gianni Chessari , Miles Stuart Congreve , Eva Figueroa Navarro , Martyn Frederickson , Christopher Murray , Alison Jo-Anne Woolford , Maria Grazia Carr , Michael Alistair O'Brien , Andrew James Woodhead , Robert Downham , Theresa Rachel Phillips
发明人： Gianni Chessari , Miles Stuart Congreve , Eva Figueroa Navarro , Martyn Frederickson , Christopher Murray , Alison Jo-Anne Woolford , Maria Grazia Carr , Michael Alistair O'Brien , Andrew James Woodhead , Robert Downham , Theresa Rachel Phillips
IPC分类号： A01N43/38 , A61K31/40 , C07D209/44
CPC分类号： C07D401/12 , C07C65/21 , C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
摘要： The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydrogen; R2 is hydroxy or methoxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
摘要翻译：本发明提供式（I）的化合物：或其盐，互变异构体，溶剂合物和N-氧化物; 其中R1是氢; R2是羟基或甲氧基; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。该化合物具有作为Hsp90抑制剂的活性。

5. 发明授权

US08106057B2 Dihydroxyphenyl isoindolylmethanones 有权
标题翻译：二羟基苯基异吲哚甲酮
公开(公告)号：US08106057B2
公开(公告)日：2012-01-31
申请号：US12782996
申请日：2010-05-19
申请人： Gianni Chessari , Maria Grazia Carr , Miles Stuart Congreve , Robert Downham , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
发明人： Gianni Chessari , Maria Grazia Carr , Miles Stuart Congreve , Robert Downham , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
IPC分类号： A61K31/497 , A61K31/445 , A61K31/405
CPC分类号： C07D209/44 , C07D401/04 , C07D401/12
摘要： This invention provides methods for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I): and in particular, those of subgenus VIIa These compounds inhibit or modulate the activity of the heat shock protein Hsp90.
摘要翻译：本发明提供了治疗癌症，特别是淋巴或骨髓谱系造血肿瘤，前列腺癌，肺癌，胃肠道间质瘤，乳腺癌和黑素瘤的方法，其包括向哺乳动物施用化合物，盐，水合物，互变异构体或N-氧化物根据式（I）：特别是亚属VIIa的化合物这些化合物抑制或调节热休克蛋白Hsp90的活性。

6. 发明申请

US20100286167A1 DIHYDROXYPHENYL ISOINDOLYLMETHANONES 有权
标题翻译：二羟基苯并恶唑酮
公开(公告)号：US20100286167A1
公开(公告)日：2010-11-11
申请号：US12782996
申请日：2010-05-19
申请人： Gianni Chessari , Maria Grazia Carr , Miles Stuart Congreve , Robert Downham , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
发明人： Gianni Chessari , Maria Grazia Carr , Miles Stuart Congreve , Robert Downham , Martyn Frederickson , Christopher William Murray , Eva Figueroa Navarro , Michael Alistair O'Brien , Theresa Rachel Phillips , Andrew James Woodhead
IPC分类号： A61K31/496 , A61K31/404 , A61K31/454 , A61P35/00 , A61P35/04
CPC分类号： C07D209/44 , C07D401/04 , C07D401/12
摘要： This invention provides methods for treating cancer, particularly hematopoietic tumors of lymphoid or myeloid lineage, prostate cancer, lung cancer, gastrointestinal stromal tumor, breast cancer and melanoma, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I): and in particular, those of subgenus VIIa These compounds inhibit or modulate the activity of the heat shock protein Hsp90.
摘要翻译：本发明提供了治疗癌症，特别是淋巴或骨髓谱系造血肿瘤，前列腺癌，肺癌，胃肠道间质瘤，乳腺癌和黑素瘤的方法，其包括向哺乳动物施用化合物，盐，水合物，互变异构体或N-氧化物根据式（I）：特别是亚属VIIa的化合物这些化合物抑制或调节热休克蛋白Hsp90的活性。

7. 发明申请

US20080312223A1 Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases 审中-公开
标题翻译：调节CDK，GSK和Aurora激酶活性的噻唑和异噻唑衍生物
公开(公告)号：US20080312223A1
公开(公告)日：2008-12-18
申请号：US11813173
申请日：2005-12-30
申请人： Valerio Berdini , Michael Alistair O'Brien , Theresa Rachel Phillips , Paul Graham Wyatt
发明人： Valerio Berdini , Michael Alistair O'Brien , Theresa Rachel Phillips , Paul Graham Wyatt
IPC分类号： A61K31/5377 , C07D277/38 , A61K31/426 , A61P35/02 , A61P35/00 , C07D417/14
CPC分类号： C07D417/14 , C07D417/04
摘要： The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR5 or N; each of Q1 and Q2 is a carbon atom; Q3 is selected from S and CH; Q4 is selected from CR2 and S; provided that one of Q3 and Q4 is S and the other of Q3 and Q4 is not S; wherein when Q3 is S, there is a double bond between Q1 and Q4 and a double bond between Q2 and the adjacent ring nitrogen atom N; and when Q4 is S, there is a double bond between Q1 and Q2, and a double bond between Q3 and the adjacent ring nitrogen atom N; A is a bond or —(CH2)m—(B)n—; B is C═O, NR8(C═O) or O(C═O) wherein R1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; Ro is hydrogen or, together with NRg when present, forms a group —(CH2)p— wherein p is 2 to 4; R1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C1-8 hydrocarbyl group; R2 is hydrogen, halogen, methoxy, or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R3 and R4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, O and S; and R5 is hydrogen, a group R2 or a group R10 wherein R10 is as defined in the claims. The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物，互变异构体或其溶剂化物，其中X为CR 5或N; Q1和Q2中的每一个是碳原子; Q3选自S和CH; Q4选自CR2和S; 条件是Q3和Q4中的一个是S，Q3和Q4中的另一个不是S; 其中当Q3为S时，在Q1和Q4之间存在双键并且Q2和相邻的环氮原子之间存在双键; 当Q4为S时，Q1与Q2之间存在双键，Q3与相邻环氮原子之间的双键为N; A是键或 - （CH 2）m - （B）n-; B为C-O，NR8（C-O）或O（C-O），其中R 1为氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; m为0,1或2; n为0或1; Ro是氢或与存在的NR g一起形成基团 - （CH 2）p - ，其中p是2至4; R 1是氢，具有3至12个环成员的碳环或杂环基或任选取代的C 1-8烃基; R2是氢，卤素，甲氧基或任选被卤素，羟基或甲氧基取代的C 1-4烃基; R3和R4与它们所连接的碳原子一起形成具有5至7个环成员的任选取代的稠合碳环或杂环，其中多达3个可以是选自N，O和S的杂原子; 并且R 5是氢，基团R 2或基团R 10，其中R 10如权利要求中所定义。该化合物具有作为细胞周期蛋白依赖性激酶，糖原合成酶激酶和极光激酶抑制剂的活性。

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