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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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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: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。
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公开(公告)号:US20080287399A1
公开(公告)日:2008-11-20
申请号:US11721779
申请日:2005-12-12
申请人: Jeffrey Scott Albert , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Suzanna Cowan , Miles Stuart Congreve , Phil Edwards , Martyn Frederickson , Christopher William Murray , Sahil Patel
发明人: Jeffrey Scott Albert , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Suzanna Cowan , Miles Stuart Congreve , Phil Edwards , Martyn Frederickson , Christopher William Murray , Sahil Patel
IPC分类号: A61K31/675 , A61K31/497 , A61K31/47 , C07D215/12 , C07F9/28 , C07D413/02 , C07D401/02 , A61K31/5377 , A61P25/28
CPC分类号: C07D213/73 , C07D213/74 , C07D213/81 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/10 , C07D409/14 , C07D413/12
摘要: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译: 本发明涉及具有结构式(I)的新化合物及其药学上可接受的盐,组合物和使用方法。 这些新化合物提供了认知障碍,阿尔茨海默病,神经变性和痴呆症的治疗或预防。
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公开(公告)号:US20090062282A1
公开(公告)日:2009-03-05
申请号:US11577154
申请日:2005-10-14
申请人: Jeffrey Scott Albert , Don Andisik , James Arnold , Dean Brown , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Miles Stuart Congreve , Phil Edwards , James R. Empfield , Martyn Frederickson , Gerard M. Koether , Jennifer Krumrine , Russ Mauger , Christopher William Murray , Sahil Patel , Mark Sylvester , Scott Throner
发明人: Jeffrey Scott Albert , Don Andisik , James Arnold , Dean Brown , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Miles Stuart Congreve , Phil Edwards , James R. Empfield , Martyn Frederickson , Gerard M. Koether , Jennifer Krumrine , Russ Mauger , Christopher William Murray , Sahil Patel , Mark Sylvester , Scott Throner
IPC分类号: A61K31/5377 , C07D239/22 , A61K31/513 , C12N9/99 , A61P25/28 , C07D413/10
CPC分类号: C07D239/47 , C07D401/10 , C07D403/06 , C07D403/10 , C07D405/10 , C07D405/14 , C07D409/10
摘要: This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia, Ib), and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译: 本发明涉及具有结构式Ia或式Ib的新化合物:(Ia,Ib)及其药学上可接受的盐,互变异构体或体内可水解的前体,组合物及其使用方法。 这些新型化合物提供治疗或预防Abeta相关病理学,如认知障碍,阿尔茨海默病,神经变性和痴呆。
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公开(公告)号:US20090221579A1
公开(公告)日:2009-09-03
申请号:US11577155
申请日:2005-10-14
申请人: Jeffrey Scott Albert , Don Andisik , James Arnold , Dean Brown , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Miles Stuart Congreve , Phil Edwards , James R. Empfield , Martyn Frederickson , Gerard M. Koether , Jennifer Krumrine , Russ Mauger , Christopher William Murray , Sahil Patel , Mark Sylvester , Scott Throner
发明人: Jeffrey Scott Albert , Don Andisik , James Arnold , Dean Brown , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Miles Stuart Congreve , Phil Edwards , James R. Empfield , Martyn Frederickson , Gerard M. Koether , Jennifer Krumrine , Russ Mauger , Christopher William Murray , Sahil Patel , Mark Sylvester , Scott Throner
IPC分类号: A61K31/5377 , C07D239/47 , A61K31/513 , C07D413/10 , C12N9/99 , A61P25/28
CPC分类号: C07D239/47 , C07D401/06 , C07D401/08 , C07D403/08 , C07D405/08 , C07D405/12 , C07D405/14 , C07D409/08
摘要: This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译: 本发明涉及具有结构式Ia或式Ib:Ia Ib的新化合物及其药学上可接受的盐,互变异构体或体内可水解的前体,组合物及其使用方法。 这些新型化合物提供治疗或预防Abeta相关病理学,如认知障碍,阿尔茨海默病,神经变性和痴呆。
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公开(公告)号:US20180243125A1
公开(公告)日:2018-08-30
申请号:US15559099
申请日:2016-03-30
申请人: Owen CALLAGHAN , Cornelis P. M. GOVERS , Mario A.A. DE ZEEUW , Jesper LAURSEN , Klaas SIPKENS , Joris M. SWAAK , Marco A. VOOGSGERD , Merck Sharp & Dohme B.V.
发明人: Owen Callaghan , Cornelis P. M. Govers , Joris M. Swaak , Marco A. Voogsgerd , Mario A. A. de Zeeuw , Jesper Laursen , Klaas Sipkens
IPC分类号: A61F6/12 , A61K9/00 , A61L31/14 , A61K31/565 , B29C45/26
CPC分类号: A61F6/12 , A61F6/08 , A61F13/26 , A61F13/266 , A61F13/28 , A61K9/0036 , A61K31/565 , A61L31/14 , A61L2400/10 , B29C45/261 , B29K2023/12 , B29L2031/753
摘要: Described herein is a vaginal ring applicator comprising a barrel comprising a polymer and at least one friction reducing agent, wherein the barrel is a flattened cylinder having two slightly curved and opposing sides connected by two arcs, wherein the barrel extends between an insertion end and a plunger end; and a plunger extending between distal and proximal ends, wherein the distal end of the plunger engages the plunger end of the barrel and wherein the plunger fits telescopically within the barrel.
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