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公开(公告)号：EP2121687B1
公开(公告)日：2015-10-14
申请号：EP07848681.8
申请日：2007-12-21
发明人： BERDINI, Valerio , BESONG, Gilbert Ebai , CALLAGHAN, Owen , CARR, Maria Grazia , CONGREVE, Miles Stuart , GILL, Adrian Liam , GRIFFITHS-JONES, Charlotte Mary , MADIN, Andrew , MURRAY, Christopher William , NIJJAR, Rajdeep Kaur , O'BRIEN, Michael Alistair , PIKE, Andrew , SAXTY, Gordon , TAYLOR, Richard David , VICKERSTAFFE, Emma
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
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公开(公告)号：EP2563775B1
公开(公告)日：2017-01-04
申请号：EP11724710.6
申请日：2011-04-28
发明人： SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , JOHNSON, Christopher Norbert , WOODHEAD, Steven John , READER, Michael , REES, David Charles , MEVELLEC, Laurence Anne , ANGIBAUD, Patrick René , FREYNE, Eddy Jean Edgard , GOVAERTS, Tom Cornelis Hortense , WEERTS, Johan Erwin Edmond , PERERA, Timothy Pietro Suren , GILISSEN, Ronaldus Arnodus Hendrika Joseph , WROBLOWSKI, Berthold , LACRAMPE, Jean Fernand Armand , PAPANIKOS, Alexandra , QUEROLLE, Olivier Alexis Georges , PASQUIER, Elisabeth Thérèse Jeanne , PILATTE, Isabelle Noëlle Constance , BONNET, Pascal Ghislain André , EMBRECHTS, Werner Constant Johan , AKKARI, Rhalid , MEERPOEL, Lieven
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61P35/00
CPC分类号： C07D403/04 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D491/113 , C07F9/6524
摘要： The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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公开(公告)号：EP2773615A1
公开(公告)日：2014-09-10
申请号：EP12798621.4
申请日：2012-10-31
发明人： WOODHEAD, Andrew James , HAMLETT, Christopher Charles Frederick Hamlett , BESONG, Gilbert Ebai , CHESSARI, Gianni , CARR, Maria Grazia , MILLEMAGGI, Alessia , NORTON, David , SAALAU-BETHELL, Susanne Maria , WILLEMS, Hendrika Maria Gerarda , THOMPSON, Neil Thomas , HISCOCK, Steven Douglas
IPC分类号： C07D213/50 , C07D213/64 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/79 , C07D213/81 , C07D213/84 , C07D213/89 , C07D231/12 , C07D239/26 , C07D239/38 , C07D241/20 , C07D261/08 , C07D277/28
CPC分类号： C07C225/16 , A61K9/0019 , A61K9/19 , A61K9/2018 , A61K9/4858 , A61K31/138 , A61K31/277 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4965 , A61K31/505 , A61K31/5383 , A61K45/06 , A61K47/10 , A61K47/26 , C07B2200/05 , C07C221/00 , C07C225/18 , C07C225/22 , C07C229/38 , C07C237/06 , C07C237/10 , C07C237/24 , C07C237/30 , C07C253/30 , C07C255/58 , C07C313/06 , C07C2601/02 , C07D213/50 , C07D213/64 , C07D213/65 , C07D213/73 , C07D213/74 , C07D213/79 , C07D213/81 , C07D213/84 , C07D213/89 , C07D231/12 , C07D239/26 , C07D239/38 , C07D241/20 , C07D261/08 , C07D275/02 , C07D277/28 , C07D401/04 , C07D498/04
摘要： The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections. The compounds have the formula (1): or a salt, N-oxide, tautomer or stereoisomer thereof, wherein A is CH or N; E is CH or N; R
1 is selected from: an optionally substituted acyclic C
1-8 hydrocarbon group wherein one carbon atom of the acyclic C
1-8 hydrocarbon group may optionally be replaced by O, S, NRC, S(O) or SO
2 , or two adjacent carbon atoms of the acyclic d-β hydrocarbon group may optionally be replaced by CONR
c , NR
c CO, NR
c SO
2 or SO
2 NR
c provided that in each case at least one carbon atom of the acyclic C
1-8 hydrocarbon group remains; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R
2 is hydrogen or X-R
8 ; X is a C
1-8 alkanediyl group wherein one carbon atom of the C
1-8 alkanediyl group may optionally be bonded to a -CH
2 -CH
2 - moiety to form a cyclopropane-1,1-diyl group or two adjacent carbon atoms of the C
1-8 alkanediyl group may optionally be bonded to a -(CH
2 )
n moiety, where n is 1 to 5, to form a C
3-7 -cycloalkane-1,2-diyl group; R
3 is an optionally substituted 3- to 10-membered monocyclic or bicyclic carbocyclic or heterocyclic ring containing 0-3 heteroatom ring members selected from N, O and S; R
4 is hydrogen or R
43 wherein R
43 is halogen; cyano; C
1-4 alkyl; fluoro-1.4 alkyl; C
1-4 alkoxy; fluoro-C
1-4 alkoxy; hydroxy-C
1-4 alkyl; or C
1-2 alkoxy-C
1-4 alkyl; R
5 is hydrogen or R
53 wherein R
53 is selected from C
1-2 alkyl optionally substituted with fluorine; C
1-3 alkoxy optionally substituted with fluorine; halogen; cyclopropyl; and cyano; R
8 is hydroxy or C(=O)NR
10 R
11 ; provided that when R8 is hydroxy, there are at least two carbon atoms in line between the hydroxy group and the nitrogen atom to which X is attached; R
10 is hydrogen or C
1-4 alkyl; and R
11 is hydrogen; amino-C
2-4 alkyl or hydroxy-C
2-4 alkyl; but excluding the compounds 1-(3-benzoylphenyl)-ethylamine and 1-(3-furan-2-oylcarbonylphenyl)-ethylamine.摘要翻译： 本发明提供可用于治疗丙型肝炎病毒（HCV）感染的化合物。 化合物具有式（1）：或其盐，N-氧化物，互变异构体或立体异构体，其中A是CH或N; E为CH或N; R1选自：任选取代的非环C 1-8烃基，其中无环C 1-8烃基的一个碳原子可以任选地被O，S，NR c，S（O）或SO 2取代，或两个相邻的碳原子 非环式C 1-8烃基可以任选地被CONRc，NRcCO，NRcSO2或SO2NRc替代，条件是在每种情况下残留至少一个无环C 1-8烃基的碳原子; 和3至7个环成员的任选取代的单环碳环或杂环基，其中0,1,2,3或4是选自O，N和S的杂原子环成员; R2是氢或X-R8; X是C 1-8烷二基，其中C 1-8烷二基的一个碳原子可以任选地与-CH 2 -CH 2 - 部分键合形成环丙烷-1,1-二基或C1的两个相邻碳原子 -8烷二基可以任选地键合到 - （CH 2）n部分，其中n为1至5，以形成C 3-7 - 环烷烃-1,2-二基; R3是含有0-3个选自N，O和S的杂原子环成员的任选取代的3至10元单环或双环碳环或杂环; R4是氢或R4a，其中R4a是卤素; 氰基; C 1-4烷基; 氟-1- C 1-4烷氧基; 氟-C1-4烷氧基; 羟基-C 1-4烷基; 或C 1-2烷氧基-C 1-4烷基; R5是氢或R5a，其中R5a选自任选被氟取代的C 1-2烷基; 任选被氟取代的C 1-3烷氧基; 卤素; 环丙基; 和氰基; R8是羟基或C（= O）NR10R11; 条件是当R 8为羟基时，X与X连接的羟基与氮原子之间具有至少两个碳原子; R 10是氢或C 1-4烷基; R11为氢; 氨基-C 2-4烷基或羟基-C 2-4烷基; 但不包括化合物1-（3-苯甲酰基苯基） - 乙胺和1-（3-呋喃-2-基羰基苯基） - 乙胺。
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公开(公告)号：EP2563775A1
公开(公告)日：2013-03-06
申请号：EP11724710.6
申请日：2011-04-28
发明人： SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , JOHNSON, Christopher Norbert , WOODHEAD, Steven John , READER, Michael , REES, David Charles , MEVELLEC, Laurence Anne , ANGIBAUD, Patrick René , FREYNE, Eddy Jean Edgard , GOVAERTS, Tom Cornelis Hortense , WEERTS, Johan Erwin Edmond , PERERA, Timothy Pietro Suren , GILISSEN, Ronaldus Arnodus Hendrika Joseph , WROBLOWSKI, Berthold , LACRAMPE, Jean Fernand Armand , PAPANIKOS, Alexandra , QUEROLLE, Oliver Alexis Georges , PASQUIER, Elisabeth Thérèse Jeanne , PILATTE, Isabelle Noëlle Constance , BONNET, Pascal Ghislain André , EMBRECHTS, Werner Constant Johan , AKKARI, Rhalid , MEERPOEL, Lieven
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61P35/00
CPC分类号： C07D403/04 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D491/113 , C07F9/6524
摘要： The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译： 本发明涉及新的喹喔啉衍生物化合物，涉及包含所述化合物的药物组合物，制备所述化合物的方法以及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：EP3178818A1
公开(公告)日：2017-06-14
申请号：EP16207610.3
申请日：2011-04-28
发明人： SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , JOHNSON, Christopher Norbert , WOODHEAD, Steven John , READER, Michael , REES, David Charles , MEVELLEC, Laurence Anne , ANGIBAUD, Patrick René , FREYNE, Eddy Jean Edgard , GOVAERTS, Tom Cornelis Hortense , WEERTS, Johan Erwin Edmond , PERERA, Timothy Pietro Suren , GILISSEN, Ronaldus Arnodus Hendrika Joseph , WROBLOWSKI, Berthold , LACRAMPE, Jean Fernand Armand , PAPANIKOS, Alexandra , QUEROLLE, Olivier Alexis Georges , PASQUIER, Elisabeth Thérèse Jeanne , PILATTE, Isabelle Noëlle Constance , BONNET, Pascal Ghislain André , EMBRECHTS, Werner Constant Johan , AKKARI, Rhalid , MEERPOEL, Lieven
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61P35/00
CPC分类号： C07D403/04 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , C07D491/113 , C07F9/6524
摘要： The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译： 本发明涉及新的喹喔啉衍生物化合物，涉及包含所述化合物的药物组合物，制备所述化合物的方法以及所述化合物在治疗疾病中的用途， 癌症。
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6.发明公开SUBSTITUTED BENZOPYRAZIN DERIVATIVES AS FGFR KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES 有权代入为BENZOPYRAZINDERIVATE FGFR激酶抑制剂用于癌症治疗
公开(公告)号：EP2646432A1
公开(公告)日：2013-10-09
申请号：EP11805567.2
申请日：2011-11-29
发明人： BERDINI, Valerio , SAXTY, Gordon , MURRAY, Christopher William , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , WOODHEAD, Steven John , LIGNY, Yannick Aimé Eddy , ANGIBAUD, Patrick René
IPC分类号： C07D403/04 , A61K31/502 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14
摘要： The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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公开(公告)号：EP2121687A2
公开(公告)日：2009-11-25
申请号：EP07848681.8
申请日：2007-12-21
发明人： BERDINI, Valerio , BESONG, Gilbert Ebai , CALLAGHAN, Owen , CARR, Maria Grazia , CONGREVE, Miles Stuart , GILL, Adrian Liam , GRIFFITHS-JONES, Charlotte Mary , MADIN, Andrew , MURRAY, Christopher William , NIJJAR, Rajdeep Kaur , O'BRIEN, Michael Alistair , PIKE, Andrew , SAXTY, Gordon , TAYLOR, Richard David , VICKERSTAFFE, Emma
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , 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.
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公开(公告)号：EP3590934A1
公开(公告)日：2020-01-08
申请号：EP19175481.1
申请日：2011-04-28
发明人： SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , JOHNSON, Christopher Norbert , WOODHEAD, Steven John , READER, Michael , REES, David Charles , MEVELLEC, Laurence Anne , ANGIBAUD, Patrick Rene , FREYNE, Eddy Jean Edgard , GOVAERTS, Tom Cornelis Hortense , WEERTS, Johan Erwin Edmond , PERERA, Timothy Pietro Suren , GILISSEN, Ronaldus Arnodus Hendrika Joseph , WROBLOWSKI, Berthold , LACRAMPE, Jean Fernand Armand , PAPANIKOS, Alexandra , QUEROLLE, Olivier Alexis Georges , PASQUIER, Elisabeth Therese Jeanne , PILATTE, Isabelle Noelle Constance , BONNET, Pascal Ghislain Andre , EMBRECHTS, Werner Constant Johan , AKKARI, Rhalid , MEERPOEL, Lieven
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61P35/00
摘要： The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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公开(公告)号：EP3178818B1
公开(公告)日：2019-05-22
申请号：EP16207610.3
申请日：2011-04-28
发明人： SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , JOHNSON, Christopher Norbert , WOODHEAD, Steven John , READER, Michael , REES, David Charles , MEVELLEC, Laurence Anne , ANGIBAUD, Patrick René , FREYNE, Eddy Jean Edgard , GOVAERTS, Tom Cornelis Hortense , WEERTS, Johan Erwin Edmond , PERERA, Timothy Pietro Suren , GILISSEN, Ronaldus Arnodus Hendrika Joseph , WROBLOWSKI, Berthold , LACRAMPE, Jean Fernand Armand , PAPANIKOS, Alexandra , QUEROLLE, Olivier Alexis Georges , PASQUIER, Elisabeth Thérèse Jeanne , PILATTE, Isabelle Noëlle Constance , BONNET, Pascal Ghislain André , EMBRECHTS, Werner Constant Johan , AKKARI, Rhalid , MEERPOEL, Lieven
IPC分类号： C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61P35/00
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10.发明授权SUBSTITUTED BENZOPYRAZIN DERIVATIVES AS FGFR KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES 有权代入为BENZOPYRAZINDERIVATE FGFR激酶抑制剂用于癌症治疗
公开(公告)号：EP2646432B1
公开(公告)日：2015-04-08
申请号：EP11805567.2
申请日：2011-11-29
发明人： BERDINI, Valerio , SAXTY, Gordon , MURRAY, Christopher William , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , WOODHEAD, Steven John , LIGNY, Yannick Aimé Eddy , ANGIBAUD, Patrick René
IPC分类号： C07D403/04 , A61K31/502 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14
摘要： The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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