公开(公告)号：US11136310B2

公开(公告)日：2021-10-05

申请号：US15774332

申请日：2016-11-24

申请人： UCB Biopharma SPRL

发明人： Rebecca Louise Charlton ,  Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm Maccoss ,  Trevor Morgan ,  Richard David Taylor ,  Zhaoning Zhu

IPC分类号： C07D403/10 ,  C07D417/10 ,  C07D471/04

摘要： A series of 2-imino-6-methyltetrahydropyrimidin-4(1H)-one derivatives, substituted in the 6-position by a phenyl moiety which in turn is meta-substituted by an optionally substituted unsaturated fused bicyclic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

公开(公告)号：US10464932B2

公开(公告)日：2019-11-05

申请号：US16076387

申请日：2017-02-22

申请人： UCB Biopharma SPRL

发明人： Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm Maccoss ,  Richard David Taylor ,  Zhaoning Zhu

IPC分类号： C07D417/10 ,  C07D417/14 ,  A61P33/06

摘要： A series of 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted in the 5-position by a phenyl moiety NH which in turn is meta-substituted by an optionally substituted fused bicyclic heteroaromatic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

公开(公告)号：US20190040053A1

公开(公告)日：2019-02-07

申请号：US16076387

申请日：2017-02-22

申请人： UCB Biopharma SPRL

发明人： Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm Maccoss ,  Richard David Taylor ,  Zhaoning Zhu

IPC分类号： C07D417/10 ,  C07D417/14 ,  A61P33/06

CPC分类号： C07D417/10 ,  A61P33/06 ,  C07D417/14

摘要： A series of 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted in the 5-position by a phenyl moiety NH which in turn is meta-substituted by an optionally substituted fused bicyclic heteroaromatic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

公开(公告)号：US20200168293A1

公开(公告)日：2020-05-28

申请号：US15781228

申请日：2016-12-01

申请人： UCB Biopharma SPRL

发明人： Terence Seward Baker ,  Xiaofeng Liu ,  Jiye Shi ,  Richard David Taylor

IPC分类号： G16B20/30 ,  G16B15/00 ,  G06F30/20

摘要： Computer-implemented methods of designing an antibody that will bind to a target epitope are disclosed. In one arrangement, the method comprises identifying one or more hotspot residues that will each bind to a corresponding one of one or more hotspot sites on the target epitope. Candidate antibody structures are selected from a database such that characteristic atoms within the antibody structure and hotspot characteristic atoms can be superimposed computationally with an averaged spatial deviation less than a predetermined threshold. A designed antibody is generated by replacing matching residues with different residues such that a predicted affinity is increased.

公开(公告)号：US20200283416A1

公开(公告)日：2020-09-10

申请号：US15774332

申请日：2016-11-24

申请人： UCB Biopharma SPRL

发明人： Rebecca Louise Charlton ,  Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm Maccoss ,  Trevor Morgan ,  Richard David Taylor ,  Zhaoning Zhu

IPC分类号： C07D403/10 ,  C07D471/04 ,  C07D417/10

摘要： A series of 2-imino-6-methyltetrahydropyrimidin-4(1H)-one derivatives, substituted in the 6-position by a phenyl moiety which in turn is meta-substituted by an optionally substituted unsaturated fused bicyclic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.