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公开(公告)号：US11001575B1
公开(公告)日：2021-05-11
申请号：US16541863
申请日：2019-08-15
发明人： Valerio Berdini , Ildiko Maria Buck , James Edward Harvey Day , Charlotte Mary Griffiths-Jones , Thomas Daniel Heightman , Steven Howard , Christopher William Murray , David Norton , Marc O'Reilly , Alison Jo-Anne Woolford , Michael Liam Cooke , David Cousin , Stuart Thomas Onions , Jonathan Martin Shannon , John Paul Watts
IPC分类号： C07D405/14 , A61K31/55 , C07D487/04 , A61P35/00 , A61K31/553 , C07D403/14 , C07D471/08 , C07D403/04 , C07D413/14 , A61K31/506 , C07D498/22 , A61K31/5377 , C07D417/14 , C07D409/14 , C07D513/04 , A61K31/444 , C07D401/14 , C07D471/04 , C07D497/08 , A61K31/541
摘要： The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—Rz and N; R1 is selected from: -(Alk1)t-Cyc1; wherein t is 0 or 1; Optionally substituted C1-6 acyclic hydrocarbon groups R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R3 is hydrogen or a group L-R7; R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and R4a is selected from hydrogen and a C1-3 alkyl group; wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
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公开(公告)号：US10457669B2
公开(公告)日：2019-10-29
申请号：US15767775
申请日：2016-10-20
发明人： Valerio Berdini , Ildiko Maria Buck , James Edward Harvey Day , Charlotte Mary Griffiths-Jones , Thomas Daniel Heightman , Steven Howard , Christopher William Murray , David Norton , Marc O'Reilly , Alison Jo-Anne Woolford , Michael Liam Cooke , David Cousin , Stuart Thomas Onions , Jonathan Martin Shannon , John Paul Watts
IPC分类号： C07D405/14 , C07D401/14 , C07D413/14 , C07D403/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D403/04 , C07D487/04 , C07D497/08 , C07D498/22 , C07D513/04 , A61P35/00 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553
摘要： The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—Rz and N; R1 is selected from: -(Alk1)t-Cyc1; wherein t is 0 or 1; Optionally substituted C1-6 acyclic hydrocarbon groups R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R3 is hydrogen or a group L1-R7; R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and R4a is selected from hydrogen and a C1-3 alkyl group; wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof. The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
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公开(公告)号：US11939321B2
公开(公告)日：2024-03-26
申请号：US17224733
申请日：2021-04-07
发明人： Valerio Berdini , Ildiko Maria Buck , James Edward Harvey Day , Charlotte Mary Griffiths-Jones , Thomas Daniel Heightman , Steven Howard , Christopher William Murray , David Norton , Marc O'Reilly , Alison Jo-Anne Woolford , Michael Liam Cooke , David Cousin , Stuart Thomas Onions , Jonathan Martin Shannon , John Paul Watts
IPC分类号： C07D405/14 , C07D403/14 , C07D409/14 , C07D471/04 , C07D413/14 , C07D471/08 , C07D401/14 , C07D417/14 , C07D403/04 , C07D487/04 , C07D497/08 , C07D498/22 , C07D513/04 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , A61P35/00
CPC分类号： C07D405/14 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , A61P35/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D497/08 , C07D498/22 , C07D513/04
摘要： The invention provides a compound of formula (0):
or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein:
n is 1 or 2;
X is CH or N;
Y is selected from CH and C—F;
Z is selected from C—Rz and N;
R1 is selected from:
-(Alk1)t-Cyc1; wherein t is 0 or 1;
Optionally substituted C1-6 acyclic hydrocarbon groups
R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms;
R3 is hydrogen or a group L1-R7;
R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and
R4a is selected from hydrogen and a C1-3 alkyl group;
wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein;
provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
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