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公开(公告)号：US10272087B2
公开(公告)日：2019-04-30
申请号：US15203424
申请日：2016-07-06
发明人： Gordon Saxty , Christopher Charles Frederick Hamlett , Valerio Berdini , Christopher William Murray , Patrick René Angibaud , Olivier Alexis Georges Querolle , Virginie Sophie Poncelet
IPC分类号： C07D475/00 , A61K31/519 , A61K45/06
摘要： The invention relates to new pteridine 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：US09447098B2
公开(公告)日：2016-09-20
申请号：US14404175
申请日：2013-05-30
发明人： Gordon Saxty , Christopher Charles Frederick Hamlett , Valerio Berdini , Christopher William Murray , Patrick René Angibaud , Olivier Alexis Georges Querolle , Virginie Sophie Poncelet
IPC分类号： A61K31/4985 , A61K31/519 , C07D475/00 , A61K45/06
CPC分类号： A61K31/519 , A61K45/06 , C07D475/00
摘要： The invention relates to new pteridine 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
摘要翻译： 本发明涉及新的蝶啶衍生物化合物，包含所述化合物的药物组合物，用于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：US20150291589A1
公开(公告)日：2015-10-15
申请号：US14404175
申请日：2013-05-30
发明人： Gordon Saxty , Christopher Charles Frederick Hamlett , Valerio Berdini , Christopher William Murray , Patrick René Angibaud , Olivier Alexis Georges Querolle , Virginie Sophie Poncelet
IPC分类号： C07D475/00 , A61K45/06 , A61K31/519
CPC分类号： A61K31/519 , A61K45/06 , C07D475/00
摘要： The invention relates to new pteridine 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： 本发明涉及新的蝶啶衍生物化合物，包含所述化合物的药物组合物，用于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：US09145354B2
公开(公告)日：2015-09-29
申请号：US14355786
申请日：2012-10-31
发明人： Andrew James Woodhead , Christopher Charles Frederick Hamlett , Gilbert Ebai Besong , Gianni Chessari , Maria Grazia Carr , Alessia Millemaggi , David Norton , Susanne Maria Saalau-Bethell , Hendrika Maria Gerarda Willems , Neil Thomas Thompson , Steven Douglas Hiscock
IPC分类号： C07C225/16 , C07D213/73 , C07D213/74 , C07C255/58 , C07D213/79 , C07D213/81 , C07D213/84 , C07D213/89 , C07D231/12 , C07D401/04 , C07D239/26 , C07D239/38 , C07C225/18 , C07D241/20 , C07D261/08 , C07D277/28 , C07D498/04 , C07D213/50 , C07D213/64 , C07D213/65 , C07C225/22 , C07C229/38 , C07C237/06 , C07C237/10 , C07C237/24 , C07C237/30 , A61K9/00 , A61K9/20 , A61K9/48 , C07C313/06 , A61K31/138 , A61K31/277 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4965 , A61K31/505 , A61K31/5383 , A61K45/06 , C07C221/00 , C07C253/30 , C07D275/02 , A61K47/10 , A61K47/26 , A61K9/19
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; R1 is selected from: an optionally substituted acyclic C1-8 hydrocarbon group wherein one carbon atom of the acyclic C1-8 hydrocarbon group may optionally be replaced by O, S, NRc, S(O) or SO2, or two adjacent carbon atoms of the acyclic C1-8 hydrocarbon group may optionally be replaced by CONRc, NRcCO, NRcSO2 or SO2NRc provided that in each case at least one carbon atom of the acyclic C1-8 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; R2 is hydrogen or X—R8; X is a C1-8 alkanediyl group wherein one carbon atom of the C1-8 alkanediyl group may optionally be bonded to a —CH2—CH2— moiety to form a cyclopropane-1,1-diyl group or two adjacent carbon atoms of the C1-8 alkanediyl group may optionally be bonded to a —(CH2)n moiety, where n is 1 to 5, to form a C3-7-cycloalkane-1,2-diyl group; R3 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; R4 is hydrogen or R4a wherein R4a is halogen; cyano; C1-4 alkyl; fluoro-1-4 alkyl; C1-4 alkoxy; fluoro-C1-4 alkoxy; hydroxy-C1-4 alkyl; or C1-2 alkoxy-C1-4 alkyl; R5 is hydrogen or R5a wherein R5a is selected from C1-2 alkyl optionally substituted with fluorine; C1-3 alkoxy optionally substituted with fluorine; halogen; cyclopropyl; and cyano; R8 is hydroxy or C(═O)NR10R11; 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; R10 is hydrogen or C1-4 alkyl; and R11 is hydrogen; amino-C2-4 alkyl or hydroxy-C2-4 alkyl; but excluding the compounds 1-(3-benzoylphenyl)-ethylamine and 1-(3-furan-2-oylcarbonylphenyl)-ethylamine.
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公开(公告)号：US20150051199A1
公开(公告)日：2015-02-19
申请号：US14355786
申请日：2012-10-31
发明人： Andrew James Woodhead , Christopher Charles Frederick Hamlett , Gilbert Ebai Besong , Gianni Chessari , Maria Grazia Carr , Alessia Millemaggi , David Norton , Susanne Maria Saalau-Bethell , Hendrika Maria Gerarda Willems , Neil Thomas Thompson , Steven Douglas Hiscock
IPC分类号： C07C225/16 , A61K31/44 , A61K45/06 , C07C221/00 , C07D213/50 , C07D241/20 , A61K31/4965 , A61K31/138 , C07C255/58 , A61K31/277 , C07D239/26 , A61K31/505 , C07D275/02 , A61K31/425 , C07D213/65 , C07D261/08 , A61K31/42 , C07D498/04 , A61K31/5383 , C07C253/30 , C07D213/73
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; R1 is selected from: an optionally substituted acyclic C1-8 hydrocarbon group wherein one carbon atom of the acyclic C1-8 hydrocarbon group may optionally be replaced by O, S, NRc, S(O) or SO2, or two adjacent carbon atoms of the acyclic C1-8 hydrocarbon group may optionally be replaced by CONRc, NRcCO, NRcSO2 or SO2NRc provided that in each case at least one carbon atom of the acyclic C1-8 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; R2 is hydrogen or X—R8; X is a C1-8 alkanediyl group wherein one carbon atom of the C1-8 alkanediyl group may optionally be bonded to a —CH2—CH2— moiety to form a cyclopropane-1,1-diyl group or two adjacent carbon atoms of the C1-8 alkanediyl group may optionally be bonded to a —(CH2)n moiety, where n is 1 to 5, to form a C3-7-cycloalkane-1,2-diyl group; R3 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; R4 is hydrogen or R4a wherein R4a is halogen; cyano; C1-4 alkyl; fluoro-1-4 alkyl; C1-4 alkoxy; fluoro-C1-4 alkoxy; hydroxy-C1-4 alkyl; or C1-2 alkoxy-C1-4 alkyl; R5 is hydrogen or R5a wherein R5a is selected from C1-2 alkyl optionally substituted with fluorine; C1-3 alkoxy optionally substituted with fluorine; halogen; cyclopropyl; and cyano; R8 is hydroxy or C(═O)NR10R11; 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; R10 is hydrogen or C1-4 alkyl; and R11 is hydrogen; amino-C2-4 alkyl or hydroxy-C2-4 alkyl; but excluding the compounds 1-(3-benzoylphenyl)-ethylamine and 1-(3-furan-2-oylcarbonylphenyl)-ethylamine.
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