专利检索 ap:("Gianni Chessari" OR "Miles Stuart Congreve" OR "Eva Figueroa Navarro" OR "Martyn Frederickson" OR "Christopher Murray" OR "Alison Jo-Anne Woolford" OR "Maria Grazia Carr" OR "Michael Alistair O'Brien" OR "Andrew James Woodhead" OR "Robert Downham" OR "Theresa Rachel Phillips") AND inv:"Miles Stuart Congreve" 第 2 页

11.

发明申请
Pyrimidine Derivatives As HSP90 Inhibitors 审中-公开
标题翻译：嘧啶衍生物作为HSP90抑制剂

公开(公告)号：US20090215777A1

公开(公告)日：2009-08-27

申请号：US11914728

申请日：2006-05-19

申请人： Gianni Chessari , Miles Stuart Congreve , Owen Callaghan , Suzanna Ruth Cowan , Christopher William Murray , Alison Jo-Anne Woolford , Michael Alistair O'Brien , Andrew James Woodhead

发明人： Gianni Chessari , Miles Stuart Congreve , Owen Callaghan , Suzanna Ruth Cowan , Christopher William Murray , Alison Jo-Anne Woolford , Michael Alistair O'Brien , Andrew James Woodhead

IPC分类号： A61K31/5377 , C07D239/42 , A61K31/505 , C07D413/12 , C07D251/42 , A61K31/53

CPC分类号： C07D413/04 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D409/04

摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates or N-oxides thereof; wherein: A is N or a group CR3; R1 is a monocyclic or bicyclic carbocyclic or heterocyclic ring of 5 to 10 ring members of which up to two ring members may be heteroatoms selected from N, O and S and the remainder are carbon atoms, the carbocyclic or heterocyclic ring being optionally substituted by one or more substituent groups independently selected from R10; and R2, R3 and R10 are as defined in the claims.

摘要翻译： 本发明提供了用作Hsp90抑制剂的化合物，具有式（I）的化合物：或其盐，互变异构体，溶剂合物或N-氧化物; 其中：A为N或CR3基团; R 1是5至10个环成员的单环或双环碳环或杂环，其中多至两个环成员可以是选自N，O和S的杂原子，其余是碳原子，碳环或杂环任选被一个或更多个独立地选自R 10的取代基; 并且R 2，R 3和R 10如权利要求中所定义。

12.

发明授权
Imidazole derivatives and their use as modulators of cyclin dependent kinases 失效
标题翻译：咪唑衍生物及其作为细胞周期蛋白依赖性激酶的调节剂的用途

公开(公告)号：US08598217B2

公开(公告)日：2013-12-03

申请号：US13266976

申请日：2010-04-30

申请人： Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'Reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Giraldes , Michael Joseph Luzzio , Lawrence Blas Perez

发明人： Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'Reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Giraldes , Michael Joseph Luzzio , Lawrence Blas Perez

IPC分类号： A61K31/496 , A61K31/4545 , A61K31/4439 , A61K31/4725 , A61K31/4353 , A61K31/4178 , A61K31/4184 , A61P35/00 , C07D471/04 , C07D401/06 , C07D417/10 , C07D413/06 , C07D403/10

CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00

摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O− or CR3; Y is N, N+—O− or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.

摘要翻译： 本发明提供式（I）化合物及其盐，互变异构体，溶剂化物和N-氧化物; 其中Q是CH或N; X是N，N + -O-或CR 3; Y是N，N + -O-或CR3a; R1和R2独立地选自氢和权利要求中定义的各种取代基; 或R 1和R 2与它们所连接的原子一起连接以形成任选取代的4至7个成员的碳环或杂环芳族或非芳族环; R3选自氢和各种取代基; 并且R 3a选自氢和权利要求中定义的各种取代基。还提供含有式（I）化合物，制备化合物的方法和化合物的医疗用途的药物组合物。式（I）化合物具有作为CDK激酶抑制剂的活性，并且可用于治疗尤其是增殖性疾病如癌症。

13.

发明申请
Therapeutic Combinations Of Hydroxybenzamide Derivatives As Inhibitors Of HSP90 有权
标题翻译：羟基苯甲酰胺衍生物作为HSP90抑制剂的治疗组合

公开(公告)号：US20120251545A1

公开(公告)日：2012-10-04

申请号：US13271678

申请日：2011-10-12

申请人： Gianni Chessari , Miles Stuart Congreve , Martyn Frederickson , Christopher William Murray , Eva Figueron Navarro , Alison Jo-Anne Woolford

发明人： Gianni Chessari , Miles Stuart Congreve , Martyn Frederickson , Christopher William Murray , Eva Figueron Navarro , Alison Jo-Anne Woolford

IPC分类号： A61K31/496 , A61K31/4035 , A61P35/00 , A61K31/5377 , A61K31/454 , A61K38/45 , A61K39/395 , A61K31/437

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。

14.

发明申请
IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 失效
标题翻译：咪唑衍生物及其作为细胞周期调节因子的调节剂

公开(公告)号：US20120101064A1

公开(公告)日：2012-04-26

申请号：US13266976

申请日：2010-04-30

申请人： Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Grialdes , Michael Joseph Luzzio , Lawrence Blas Perez

发明人： Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Grialdes , Michael Joseph Luzzio , Lawrence Blas Perez

IPC分类号： A61K31/675 , A61K31/4439 , A61K31/496 , A61K31/4545 , C07D413/06 , A61K31/5377 , C07D417/10 , A61K31/427 , C07D403/10 , A61K31/4178 , C07D409/10 , C07D401/06 , A61K31/4725 , A61K31/551 , C07D471/04 , A61K31/437 , C07F9/6561 , A61P35/00 , A61P35/02 , C07D401/14

CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00

摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O− or CR3; Y is N, N+—O− or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.

摘要翻译： 本发明提供式（I）化合物及其盐，互变异构体，溶剂化物和N-氧化物; 其中Q是CH或N; X是N，N + -O-或CR 3; Y是N，N + -O-或CR3a; R1和R2独立地选自氢和权利要求中定义的各种取代基; 或R 1和R 2与它们所连接的原子一起连接以形成任选取代的4至7个成员的碳环或杂环芳族或非芳族环; R3选自氢和各种取代基; 并且R 3a选自氢和权利要求中定义的各种取代基。还提供含有式（I）化合物，制备化合物的方法和化合物的医疗用途的药物组合物。式（I）化合物具有作为CDK激酶抑制剂的活性，并且可用于治疗尤其是增殖性疾病如癌症。

15.

发明申请
IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES 有权
标题翻译：作为受体酪氨酸激酶抑制剂的咪唑吡啶衍生物

公开(公告)号：US20120208791A1

公开(公告)日：2012-08-16

申请号：US12997754

申请日：2009-06-12

申请人： Valerio Berdini , Maria Grazia Carr , Miles Stuart Congreve , Martyn Frederickson , Charlotte Mary Griffiths-Jones , Christopher Charles Frederick Hamlett , Andrew Madin , Christopher William Murray , Rajdeep Kaur Benning , Gordon Saxty , Emma Vickerstaffe , Brian John Williams , Marian Williams , Andrew James Woodhead , Steven John Woodhead , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Patrick René Angibaud

发明人： Valerio Berdini , Maria Grazia Carr , Miles Stuart Congreve , Martyn Frederickson , Charlotte Mary Griffiths-Jones , Christopher Charles Frederick Hamlett , Andrew Madin , Christopher William Murray , Rajdeep Kaur Benning , Gordon Saxty , Emma Vickerstaffe , Brian John Williams , Marian Williams , Andrew James Woodhead , Steven John Woodhead , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Patrick René Angibaud

IPC分类号： A61K31/437 , A61K31/501 , A61P35/00 , C07D513/04 , A61K31/53 , A61K31/506 , C07D471/04 , A61K31/5377

CPC分类号： C07D471/04 , C07D513/04

摘要： The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

摘要翻译： 本发明涉及新的双环杂环衍生物化合物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途。癌症。

16.

发明授权
Imidazopyridine derivatives as inhibitors of receptor tyrosine kinases 有权
标题翻译：咪唑并吡啶衍生物作为受体酪氨酸激酶的抑制剂

公开(公告)号：US08796244B2

公开(公告)日：2014-08-05

申请号：US12997754

申请日：2009-06-12

申请人： Valerio Berdini , Maria Grazia Carr , Miles Stuart Congreve , Martyn Frederickson , Charlotte Mary Griffiths-Jones , Christopher Charles Frederick Hamlett , Andrew Madin , Christopher William Murray , Rajdeep Kaur Benning , Gordon Saxty , Emma Vickerstaffe , Andrew James Woodhead , Steven John Woodhead , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Patrick René Angibaud , Marian Williams

发明人： Valerio Berdini , Maria Grazia Carr , Miles Stuart Congreve , Martyn Frederickson , Charlotte Mary Griffiths-Jones , Christopher Charles Frederick Hamlett , Andrew Madin , Christopher William Murray , Rajdeep Kaur Benning , Gordon Saxty , Emma Vickerstaffe , Brian John Williams , Andrew James Woodhead , Steven John Woodhead , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Patrick René Angibaud

IPC分类号： A61K31/5025 , C07D413/02

CPC分类号： C07D471/04 , C07D513/04

摘要： The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.

摘要翻译： 本发明涉及新的双环杂环衍生物化合物，包含该化合物的药物组合物和该化合物在治疗疾病中的用途。癌症。

17.

发明授权
Pharmaceutical compounds 失效
标题翻译：药物化合物

公开(公告)号：US08779132B2

公开(公告)日：2014-07-15

申请号：US12445154

申请日：2007-10-12

申请人： Miles Stuart Congreve , Lynsey Helen Fazal , Martyn Frederickson , Christopher William Murray , Michael Alistair O'Brien , Andrew James Woodhead , John Francis Lyons , Neil Thomas Thompson

发明人： Miles Stuart Congreve , Lynsey Helen Fazal , Martyn Frederickson , Christopher William Murray , Michael Alistair O'Brien , Andrew James Woodhead , John Francis Lyons , Neil Thomas Thompson

IPC分类号： C07D403/06 , A61K31/497

CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18

摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C═O, (C═O)O, (C═O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C═O or (C═O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims. The compounds of formula (VI0) are pro-drugs of parent compounds wherein R1 and/or R2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.

摘要翻译： 本发明提供了一种用于医药的化合物，该化合物为式（VI0）化合物或其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团：选自结构C1，C5和C6：其中n为0,1,2或3; R1是氢，羟基或O-Rz; R2a是羟基，甲氧基或O-Rz; 条件是R1和R2a中的至少一个是O-Rz; Rz是Lp-Rp1; SO3H; 葡萄糖苷酸残基; 单，二或三肽残基; 或Lp为键，C = O，（C = O）O，（C = O）NRp1或S（O）xNRp1; x为1或2; Rp1是氢或任选取代的含有0,1或2个碳环和0,1,2,3,4,5或6个碳 - 碳多重键的C1〜25烃基，条件是当Lp为一个键，C = O或（C = O）O; 并且还提供O-Rz不含有O-O部分; 并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，并且各自为基团Rp1; R3，R4a，R8和R10如权利要求中所定义。式（VI0）化合物是其中R 1和/或R 2a是羟基的母体化合物的前药，其中母体化合物具有Hsp90抑制活性。

18.

发明申请
PHARMACEUTICAL COMPOUNDS 失效
标题翻译：药物化合物

公开(公告)号：US20100152184A1

公开(公告)日：2010-06-17

申请号：US12445154

申请日：2007-10-12

申请人： Miles Stuart Congreve , Lynsey Helen Fazal , Martyn Frederickson , Christopher William Murray , Michael Alistair O'Brien , Andrew James Woodhead , John Francis Lyons , Neil Thomas Thompson

发明人： Miles Stuart Congreve , Lynsey Helen Fazal , Martyn Frederickson , Christopher William Murray , Michael Alistair O'Brien , Andrew James Woodhead , John Francis Lyons , Neil Thomas Thompson

IPC分类号： A61K31/5377 , C07D209/44 , C07D215/14 , C07D221/20 , C07D471/04 , C07D403/10 , C07D413/12 , A61K31/4035 , A61K31/47 , A61K31/438 , A61K31/497 , A61P35/00

CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18

摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C═O, (C═O)O, (C═O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C═O or (C═O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims.The compounds of formula (VI0) are pro-drugs of parent compounds wherein R1 and/or R2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.

摘要翻译： 本发明提供了一种用于医药的化合物，该化合物为式（VI0）化合物或其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团：选自结构C1，C5和C6：其中n为0,1,2或3; R1是氢，羟基或O-Rz; R2a是羟基，甲氧基或O-Rz; 条件是R1和R2a中的至少一个是O-Rz; Rz是Lp-Rp1; SO3H; 葡萄糖苷酸残基; 单，二或三肽残基; 或Lp为键，C = O，（C = O）O，（C = O）NRp1或S（O）xNRp1; x为1或2; Rp1是氢或任选取代的含有0,1或2个碳环和0,1,2,3,4,5或6个碳 - 碳多重键的C1〜25烃基，条件是当Lp为一个键，C = O或（C = O）O; 并且还提供O-Rz不含有O-O部分; 并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，并且各自为基团Rp1; R3，R4a，R8和R10如权利要求中所定义。式（VI0）化合物是其中R 1和/或R 2a是羟基的母体化合物的前药，其中母体化合物具有Hsp90抑制活性。