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公开(公告)号:US08131527B1
公开(公告)日:2012-03-06
申请号:US11963654
申请日:2007-12-21
申请人: Gordon Saxty , Valerio Berdini , David Richard Newell , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Andrew Madin , Christopher William Murray
发明人: Gordon Saxty , Valerio Berdini , David Richard Newell , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Andrew Madin , Christopher William Murray
CPC分类号: G06F19/706 , C40B30/02 , G01N2333/71 , G01N2500/04
摘要: The present invention relates to FGFR pharmacophores, and in particular to compounds which are capable of binding to FGFR with greater affinity than their binding to VEGFR and methods of identifying such compounds using the pharmacophore. The present invention further relates to compositions, methods and uses of the compounds and the pharmacophores disclosed herein.
摘要翻译: 本发明涉及FGFR药效学,特别是涉及能够以比它们与VEGFR结合的亲和力更高的亲和力结合FGFR的化合物以及使用该药效团鉴别这些化合物的方法。 本发明还涉及本文公开的化合物和药效团的组合物,方法和用途。
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公开(公告)号:US08895745B2
公开(公告)日:2014-11-25
申请号:US12520481
申请日:2007-12-21
申请人: Valerio Berdini , Gilbert Ebai Besong , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Charlotte Mary Griffiths-Jones , Andrew Madin , Christopher William Murray , Rajdeep Kaur Nijjar , Michael Alistair O'Brien , Andrew Pike , Gordon Saxty , Richard David Taylor , Emma Vickerstaffe
发明人: Valerio Berdini , Gilbert Ebai Besong , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Charlotte Mary Griffiths-Jones , Andrew Madin , Christopher William Murray , Rajdeep Kaur Nijjar , Michael Alistair O'Brien , Andrew Pike , Gordon Saxty , Richard David Taylor , Emma Vickerstaffe
IPC分类号: C07D471/04 , A61K31/437 , C07D487/04
CPC分类号: C07D487/04 , A61K31/437 , C07D471/04
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。
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公开(公告)号:US08513276B2
公开(公告)日:2013-08-20
申请号:US12520333
申请日:2007-12-21
申请人: Valerio Berdini , Gilbert Ebai Besong , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Charlotte Mary Griffiths-Jones , Andrew Madin , Christopher William Murray , Rajdeep Kaur Nijjar , Michael Alistair O'Brien , Andrew Pike , Gordon Saxty , Richard David Taylor , Emma Vickerstaffe
发明人: Valerio Berdini , Gilbert Ebai Besong , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Charlotte Mary Griffiths-Jones , Andrew Madin , Christopher William Murray , Rajdeep Kaur Nijjar , Michael Alistair O'Brien , Andrew Pike , Gordon Saxty , Richard David Taylor , Emma Vickerstaffe
IPC分类号: C07D471/04 , A61K31/437 , C07D487/04 , A61K31/519 , A61P35/00
CPC分类号: C07D471/04 , C07D487/04
摘要: The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.
摘要翻译: 本发明涉及式(I)的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以及所述化合物在治疗疾病中的用途。 癌症。 式(I)的化合物是FGFR,VEGFR或PDGFR的抑制剂。
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公开(公告)号:US20100120761A1
公开(公告)日:2010-05-13
申请号:US12520481
申请日:2007-12-21
申请人: Valerio Berdini , Gilbert Ebai Besong , Owen Callaghan , Maria Grazia Carr , MIles Stuart Congreve , Adrian Liam Gill , Charlotte Mary Griffiths-Jones , Andrew Madin , Christopher William Murray , Rajdeep Kaur Nijjar , Michael Alistair O'Brien , Andrew Pike , Gordon Saxty , Richard David Taylor , Emma Vickerstaffe
发明人: Valerio Berdini , Gilbert Ebai Besong , Owen Callaghan , Maria Grazia Carr , MIles Stuart Congreve , Adrian Liam Gill , Charlotte Mary Griffiths-Jones , Andrew Madin , Christopher William Murray , Rajdeep Kaur Nijjar , Michael Alistair O'Brien , Andrew Pike , Gordon Saxty , Richard David Taylor , Emma Vickerstaffe
IPC分类号: A61K31/437 , C07D471/04 , C07D487/04 , A61K31/496 , A61K31/5377 , A61K31/519 , A61P35/00
CPC分类号: C07D487/04 , A61K31/437 , C07D471/04
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。
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公开(公告)号:US20100093718A1
公开(公告)日:2010-04-15
申请号:US12520333
申请日:2007-12-21
申请人: Valerio Berdini , Gilbert Ebai Besong , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Charlotte Mary Griffiths-Jones , Andrew Madin , Christopher William Murray , Rajdeep Kaur Nijjar , Michael Alistair O'Brien , Andrew Pike , Gordon Saxty , Richard David Taylor , Emma Vickerstaffe
发明人: Valerio Berdini , Gilbert Ebai Besong , Owen Callaghan , Maria Grazia Carr , Miles Stuart Congreve , Adrian Liam Gill , Charlotte Mary Griffiths-Jones , Andrew Madin , Christopher William Murray , Rajdeep Kaur Nijjar , Michael Alistair O'Brien , Andrew Pike , Gordon Saxty , Richard David Taylor , Emma Vickerstaffe
IPC分类号: A61K31/5377 , C07D401/14 , A61K31/496 , C07D413/14 , C07D471/02 , A61K31/437 , C07D487/02 , A61K31/519 , A61P35/00
CPC分类号: C07D471/04 , C07D487/04
摘要: The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.
摘要翻译: 本发明涉及式(I)的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以及所述化合物在治疗疾病中的用途。 癌症化学式(I)的化合物是FGFR,VEGFR或PDGFR的抑制剂。
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6.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。
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7.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。
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公开(公告)号:US07365196B2
公开(公告)日:2008-04-29
申请号:US10239233
申请日:2001-03-15
申请人: Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
发明人: Patrice Charles Belanger , Ian James Collins , Joanne Claire Hannam , Timothy Harrison , Stephen John Lewis , Andrew Madin , Edward Giles McIver , Alan John Nadin , Joseph George Neduvelil , Mark Steven Shearman , Adrian Leonard Smith , Timothy Jason Sparey , Graeme Irvine Stevenson , Martin Richard Teall
IPC分类号: C07D413/14 , C07D413/12 , C07D213/71 , C07D213/52 , C07D333/34 , C07D409/14 , C07D409/12 , C07D249/12 , C07D233/84 , C07D207/48 , C07D277/16 , C07D307/64 , A61P25/28
CPC分类号: C07D213/30 , A61K31/18 , A61K31/40 , C07C311/07 , C07C311/09 , C07C311/11 , C07C311/14 , C07C311/20 , C07C311/24 , C07C323/67 , C07C2601/08 , C07C2601/14 , C07C2602/44 , C07C2602/46 , C07C2603/72 , C07C2603/78 , C07D207/36 , C07D211/14 , C07D211/18 , C07D213/71 , C07D213/81 , C07D215/12 , C07D223/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D271/107 , C07D277/36 , C07D285/14 , C07D285/16 , C07D295/088 , C07D295/135 , C07D295/26 , C07D307/64 , C07D307/81 , C07D319/18 , C07D333/34 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10 , C07D513/10
摘要: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
摘要翻译: 公开了一类化合物,其包含磺酰氨基取代的桥连双环烷基结构。 这些化合物是γ-分泌酶的抑制剂,因此可用于治疗和/或预防阿尔茨海默氏病。
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公开(公告)号:US07205434B2
公开(公告)日:2007-04-17
申请号:US10484290
申请日:2002-07-31
IPC分类号: C07C303/00 , A61K31/18
CPC分类号: C07D333/34
摘要: There is disclosed a novel class of sulphonamido-substituted bridged bicycloalkyl derivatives comprising a substitute on the bridgehead position. The compounds modulate the production of the β-amyloid precursor protein, and hence are useful in the treatment of Alzheimer's Disease.
摘要翻译: 公开了一种新型磺酰胺取代的桥连双环烷基衍生物,其包含在桥头头位置上的替代物。 该化合物调节β-淀粉样蛋白前体蛋白的产生,因此可用于治疗阿尔茨海默病。
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公开(公告)号:US20060293373A1
公开(公告)日:2006-12-28
申请号:US10571717
申请日:2004-09-16
申请人: Ian Collins , Joanne Hannam , Andrew Madin , Mark Ridgill
发明人: Ian Collins , Joanne Hannam , Andrew Madin , Mark Ridgill
IPC分类号: A01N43/80
CPC分类号: C07D233/64 , C07D249/08 , C07D409/12 , C07D417/04 , C07D417/12
摘要: Compounds of formula I: are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of β-amyloid.
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