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公开(公告)号：US20190047990A1
公开(公告)日：2019-02-14
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 , A61P35/00 , A61K31/506 , C07D471/04 , C07D487/04 , A61K31/5377 , A61K31/55 , A61K31/553 , C07D498/22 , C07D497/08 , C07D513/04 , C07D403/04 , C07D403/14 , A61K31/444 , C07D409/14 , A61K31/541
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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公开(公告)号：US20210107908A1
公开(公告)日：2021-04-15
申请号：US16976631
申请日：2019-03-01
发明人： Christopher Norbert JOHNSON , Ildiko Maria BUCK , Gianni CHESSARI , James Edward Harvey DAY , Hideto FUJIWARA , Christopher Charles Frederick HAMLETT , Steven Douglas HISCOCK , Rhian Sara HOLVEY , Steven HOWARD , John Walter LIEBESCHUETZ , Nicholas John PALMER , Jeffrey David ST DENIS , David Geoffrey TWIGG , Andrew James WOODHEAD
IPC分类号： C07D487/04 , C07D519/00 , A61K31/4985 , A61K45/06 , A61K31/517 , A61K31/5377
摘要： The invention provides new pyrazine derivatives of formula (I): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising 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：US20230019032A1
公开(公告)日：2023-01-19
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 , A61P35/00 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , C07D403/04 , 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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