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1. 发明申请

US20070259871A1 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：US20070259871A1
公开(公告)日：2007-11-08
申请号：US11680830
申请日：2007-03-01
申请人： Gianni Chessari , Maria Carr , Miles Congreve , Robert Downham , Martyn Frederickson , Christopher Murray , Eva Navarro , Michael O'Brien , Theresa Phillips , Andrew Woodhead , Alison Woolford
发明人： Gianni Chessari , Maria Carr , Miles Congreve , Robert Downham , Martyn Frederickson , Christopher Murray , Eva Navarro , Michael O'Brien , Theresa Phillips , Andrew Woodhead , Alison Woolford
IPC分类号： A61K31/4035 , A61K31/47 , A61K31/496 , A61K31/5377 , A61P35/00 , 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 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 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R 1是羟基或氢; R 2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; R 3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; R 4选自氢; 其中n为0或1且R 7为任选取代的无环C 1 - （O）N - ， - -5个烃基或具有3〜7个环成员的单环碳环或杂环基; 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。

2. 发明申请

US20070276026A1 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：US20070276026A1
公开(公告)日：2007-11-29
申请号：US11680805
申请日：2007-03-01
申请人： Gianni Chessari , Miles Congreve , Martyn Frederickson , Christopher Murray , Eva Navarro , Alison Woolford
发明人： Gianni Chessari , Miles Congreve , Martyn Frederickson , Christopher Murray , Eva Navarro , Alison Woolford
IPC分类号： A61K31/40 , C07D209/00
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 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 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）化合物或其盐，互变异构体，溶剂合物和N-氧化物，其中R 1是羟基或氢; R 2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; R 3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; R 4选自氢; 其中n为0或1且R 7为任选取代的无环C 1 - （O）N - ， - -5个烃基或具有3〜7个环成员的单环碳环或杂环基; 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。

3. 发明申请

US20070135477A1 Benzimidazole derivatives and their use as protein kinases inhibitors 失效
标题翻译：苯并咪唑衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：US20070135477A1
公开(公告)日：2007-06-14
申请号：US10564166
申请日：2004-07-05
申请人： Valerio Berdini , Michael O'Brien , Maria Carr , Theresa Early , Eva Navarro , Adrian Gill , Steven Howard , Gary Trewartha , Alison Woolford , Andrew Woodhead , Paul Wyatt
发明人： Valerio Berdini , Michael O'Brien , Maria Carr , Theresa Early , Eva Navarro , Adrian Gill , Steven Howard , Gary Trewartha , Alison Woolford , Andrew Woodhead , Paul Wyatt
IPC分类号： A61K31/4745 , A61K31/4184 , C07D403/04
CPC分类号： A61K31/5377 , A61K31/00 , A61K31/4184 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D513/04
摘要： The invention provides compounds of the formula (1): The compounds have activity against cyclin depdenent kinases, glycogen synthase kinase and Auroa kinases and are therefore useful to treat cancer and viral diseases.
摘要翻译：本发明提供式（1）化合物：该化合物对细胞周期蛋白依赖性激酶，糖原合酶激酶和Auroa激酶具有活性，因此可用于治疗癌症和病毒性疾病。

4. 发明申请

US20060135589A1 1h-Indazole-3-carboxamide compounds as cyclin dependent kinase (cdk) inhibitors 审中-公开
公开(公告)号：US20060135589A1
公开(公告)日：2006-06-22
申请号：US10524784
申请日：2003-08-08
申请人： Valerio Berdino , Alessandro Padova , Paul Wyatt , Gordon Saxty , Alison Woolford
发明人： Valerio Berdino , Alessandro Padova , Paul Wyatt , Gordon Saxty , Alison Woolford
IPC分类号： A61K31/416
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The invention provides a compound of the formula (I) for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase: wherein A is a group R2 or CH2—R2 where R2 is a carbocyclic or heterocyclic group having from 3 to 12 ring members; B is a bond or an acyclic linker group having a linking chain length of up to 3 atoms selected from C, N, S and O; R1 is hydrogen or a group selected from SO2Rb, SO2NR7R8, CONR7R8, NR7R9 and carbocyclic and heterocyclic groups having from 3 to 7 ring members; R3, R4, R5 and R6 are the same or different and are each selected from hydrogen, halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group Ra—Rb wherein Ra is a bond, O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; and Rb is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 12 ring members, and a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1; Rc is hydrogen or C1-4 hydrocarbyl; X1 is O, S or NRc and X2 is ═O, ═S or ═NRc; R7 is selected from hydrogen and a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, amino, mono- or di-C1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 or X1C(X2)X1; R8 is selected from R7 and carbocyclic and heterocyclic groups having from 3 to 12 ring members; R9 is selected from R8, COR8 and SO2R8; or NR7R8 or NR7R9 may each form a heterocyclic group having from 5 to 12 ring members; but excluding the compounds N-[(morpholin-4-yl)phenyl-1H-indazole-3-carboxamide and N-[4-(acetylaminosulphonyl)phenyl-1H-indazole-3-carboxamide.

5. 发明申请

US20060194843A1 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators 有权
公开(公告)号：US20060194843A1
公开(公告)日：2006-08-31
申请号：US11336599
申请日：2006-01-20
申请人： Valerio Berdini , Michael O'Brien , Maria Carr , Theresa Early , Adrian Gill , Gary Trewartha , Alison Woolford , Andrew Woodhead , Paul Wyatt
发明人： Valerio Berdini , Michael O'Brien , Maria Carr , Theresa Early , Adrian Gill , Gary Trewartha , Alison Woolford , Andrew Woodhead , Paul Wyatt
IPC分类号： A61K31/454 , A61K31/416 , A61K31/4152 , C07D403/02
CPC分类号： C07D231/38 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C04B35/632 , C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04
摘要： The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or O(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

6. 发明申请

US20060135516A1 3-(Carbonyl) 1h-indazole compounds as cyclin dependent kinases (cdk) inhibitors 审中-公开
标题翻译： 3-（羰基）1h-吲唑化合物作为细胞周期蛋白依赖性激酶（cdk）抑制剂
公开(公告)号：US20060135516A1
公开(公告)日：2006-06-22
申请号：US10524760
申请日：2003-08-08
申请人： Valerio Berdini , Maria Carr , Gordon Saxty , Alison Woolford , Paul Wyatt
发明人： Valerio Berdini , Maria Carr , Gordon Saxty , Alison Woolford , Paul Wyatt
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/43 , C07D498/02
CPC分类号： C07D513/04
摘要： The invention provides a compound of the formula (I): wherein E is O, S, or NH; G is selected from hydrogen; carbocyclic and heterocyclic groups having from 3 to 12 ring members; and acyclic C1-8 hydrocarbyl groups optionally substituted; provided that E—G is not OH or SH and further provided that E—G does not contain the group O—O; two adjacent moieties selected from R3, R4, R5 and R6, together with the carbon atoms to which they are attached, form a fused heterocyclic group having from 5 to 7 ring members and 1, 2 or 3 ring heteroatoms selected from N, O and S; and the other two moieties selected from R3, R4, R5 and R6 are the same or different and are each as defined in the description. The Invention also provides compounds of the formula (I) for use as inhibitors of cyclin dependent kinases and for use in the treatment of disease states and conditions mediated by cyclin dependent kinases.
摘要翻译：本发明提供式（I）的化合物：其中E是O，S或NH; G选自氢; 具有3至12个环成员的碳环和杂环基; 和任选取代的非环状C 1-8烃基; 条件是E-G不是OH或SH，并且进一步规定E-G不含O-O基团; 选自R 3，R 4，R 5和R 6的两个相邻部分与碳原子一起形成具有5至7个环成员和1,2或3个选自N，O和S的环杂原子的稠合杂环基; 并且选自R 3，R 4，R 5和R 6的另外两个部分是相同或不同的并且各自如说明书中所定义。本发明还提供用作细胞周期蛋白依赖性激酶抑制剂的式（I）化合物，并用于治疗由细胞周期蛋白依赖性激酶介导的疾病状态和状况。

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