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1. 发明申请

WO2019138017A1 FUSED IMIDAZOLE DERIVATIVES AS IL-17 MODULATORS 审中-公开
公开(公告)号：WO2019138017A1
公开(公告)日：2019-07-18
申请号：PCT/EP2019/050594
申请日：2019-01-10
申请人： UCB BIOPHARMA SPRL
发明人： BRACE, Gareth Neil , CHAPPELL, Rose Elizabeth , FOULKES, Gregory , FROST, James Richard , HORSLEY, Helen Tracey , JONES, Elizabeth Pearl , LECOMTE, Fabien Claude , REUBERSON, James Thomas , SCHULZE, Monika-Sarah Elisabeth Dorothea , TAYLOR, Richard David , YAU, Wei Tsung , ZHU, Zhaoning
IPC分类号： C07D403/12 , C07D405/14 , C07D413/14 , C07D403/14 , C07D413/12 , C07D487/04 , A61P29/00 , A61K31/4184
CPC分类号： C07D487/04 , A61K31/4184 , A61P29/00 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D413/14
摘要： A series of substituted fused bicyclic imidazole derivatives, including benzimidazole derivatives and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

2. 发明申请

WO2017144517A1 IMINOTHIADIAZINANE DIOXIDE DERIVATIVES AS PLASMEPSIN V INHIBITORS 审中-公开
标题翻译：作为PLASMEPSIN V抑制剂的亚胺二氮杂二氧化物衍生物
公开(公告)号：WO2017144517A1
公开(公告)日：2017-08-31
申请号：PCT/EP2017/054023
申请日：2017-02-22
申请人： UCB BIOPHARMA SPRL
发明人： DE HARO GARCIA, Teresa , LOWE, Martin Alexander , MACCOSS, Malcolm , TAYLOR, Richard David , ZHU, Zhaoning
IPC分类号： C07D417/10 , C07D417/14 , A61K31/54 , A61P33/06
CPC分类号： C07D417/10 , 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 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.
摘要翻译：一系列式（I）的3-亚氨基-5-甲基-1,2,4-噻二嗪烷-1,1-二氧化物衍生物，其在5位被苯基部分取代，被含有至少一个氮原子的任选取代的稠合双环杂芳族环体系间位取代，它们是plasmepsin V活性的选择性抑制剂，作为药物试剂是有益的，特别是在治疗疟疾中。

3. 发明申请

WO2018229079A1 SPIROCYCLIC INDOLINES AS IL-17 MODULATORS 审中-公开
公开(公告)号：WO2018229079A1
公开(公告)日：2018-12-20
申请号：PCT/EP2018/065558
申请日：2018-06-12
申请人： UCB BIOPHARMA SPRL
发明人： BRACE, Gareth Neil , CHAPPELL, Rose Elizabeth , DEBOVES, Hervé Jean Claude , FOLEY, Anne Marie , FOULKES, Gregory , JONES, Elizabeth Pearl , LECOMTE, Fabien Claude , QUINCEY, Joanna Rachel , SCHULZE, Monika-Sarah Elisabeth Dorothea , SELBY, Matthew Duncan , SMALLEY, Adam Peter , TAYLOR, Richard David , TOWNSEND, Robert James , ZHU, Zhaoning
IPC分类号： A61K31/4155 , A61K31/407 , A61K31/41 , A61K31/4184 , A61K31/421 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D471/10 , C07D487/10 , C07D491/107 , C07D491/20
摘要： A series of substituted spirocyclic 2-oxoindoline derivatives, and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

4. 发明申请

WO2017093435A1 DE NOVO ANTIBODY DESIGN 审中-公开
标题翻译： DE NOVO抗体设计
公开(公告)号：WO2017093435A1
公开(公告)日：2017-06-08
申请号：PCT/EP2016/079497
申请日：2016-12-01
申请人： UCB BIOPHARMA SPRL
发明人： BAKER, Terence Seward , LIU, Xiaofeng , SHI, Jiye , TAYLOR, Richard David
IPC分类号： G06F19/16
CPC分类号： G06F19/16 , G06F19/18
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.
摘要翻译：公开了设计将结合靶表位的抗体的计算机实施的方法。在一种安排中，该方法包括识别一个或多个热点残基，这些热点残余将各自结合靶表位上的一个或多个热点位点中相应的一个。从数据库中选择候选抗体结构，使得抗体结构和热点特征原子内的特征原子可以在平均空间偏差小于预定阈值的情况下在计算上被叠加。设计的抗体是通过用不同的残基替换匹配的残基产生的，从而预测的亲和力增加。

5. 发明申请

WO2019192992A1 ANTIMALARIAL HEXAHYDROPYRIMIDINE ANALOGUES 审中-公开
公开(公告)号：WO2019192992A1
公开(公告)日：2019-10-10
申请号：PCT/EP2019/058249
申请日：2019-04-02
申请人： UCB BIOPHARMA SPRL
发明人： DE HARO GARCIA, Teresa , KING, Lloyd Malcolm , LOWE, Martin Alexander , MACCOSS, Malcolm , TAYLOR, Richard David , ZHU, Zhaoning
IPC分类号： C07D239/22 , C07D405/04 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/14 , C07D413/14 , C07D471/04 , C07D493/08 , A61P33/06 , A61K31/513
摘要： The application relates to a series of 2-imino-6-methylhexahydropyrimidin-4-one derivatives and 3-imino-5-methyl-l,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted by an arylaminophenyl or heteroarylaminophenyl moiety. The compounds are potent inhibitors of the growth and propagation of the Plasmodium falciparum parasite in human blood and thus useful as pharmaceutical agents for the treatment of malaria.

6. 发明申请

WO2017089453A1 IMINOTETRAHYDROPYRIMIDINONE DERIVATIVES AS PLASMEPSIN V INHIBITORS 审中-公开
标题翻译：作为抑制剂V抑制剂的亚氨基四氢嘧啶酮衍生物
公开(公告)号：WO2017089453A1
公开(公告)日：2017-06-01
申请号：PCT/EP2016/078664
申请日：2016-11-24
申请人： UCB BIOPHARMA SPRL
发明人： CHARLTON, Rebecca Louise , DE HARO GARCIA, Teresa , LOWE, Martin Alexander , MACCOSS, Malcolm , MORGAN, Trevor , TAYLOR, Richard David , ZHU, Zhaoning
IPC分类号： C07D401/10 , C07D403/10 , C07D417/10 , C07D471/04 , A61K31/513 , A61P33/06
CPC分类号： C07D403/10 , C07D401/10 , C07D417/10 , C07D471/04
摘要： A series of 2-imino-6-methyltetrahydropyrimidin-4(l H )-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.
摘要翻译：一系列在6位被苯基部分取代的2-亚氨基-6-甲基四氢嘧啶-4（1H） - 衍生物，被含有至少一个氮原子的任选取代的不饱和稠合双环体系取代，它们是plasmepsin V活性的选择性抑制剂，作为药物试剂是有益的，尤其是在治疗疟疾中。

7. 发明公开

EP3384415A1 DE NOVO ANTIBODY DESIGN 审中-公开
公开(公告)号：EP3384415A1
公开(公告)日：2018-10-10
申请号：EP16805412.0
申请日：2016-12-01
申请人： UCB Biopharma SPRL
发明人： BAKER, Terence Seward , LIU, Xiaofeng , SHI, Jiye , TAYLOR, Richard David
IPC分类号： G06F19/16
CPC分类号： G06F19/16 , G06F19/18
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.

8. 发明公开

EP3419975A1 IMINOTHIADIAZINANE DIOXIDE DERIVATIVES AS PLASMEPSIN V INHIBITORS 有权转让
公开(公告)号：EP3419975A1
公开(公告)日：2019-01-02
申请号：EP17706753.5
申请日：2017-02-22
申请人： UCB Biopharma SPRL
发明人： DE HARO GARCIA, Teresa , LOWE, Martin Alexander , MACCOSS, Malcolm , TAYLOR, Richard David , ZHU, Zhaoning
IPC分类号： C07D417/10 , C07D417/14 , A61K31/54 , A61P33/06

9. 发明公开

EP3380464A1 IMINOTETRAHYDROPYRIMIDINONE DERIVATIVES AS PLASMEPSIN V INHIBITORS 有权转让
公开(公告)号：EP3380464A1
公开(公告)日：2018-10-03
申请号：EP16800984.3
申请日：2016-11-24
申请人： UCB Biopharma SPRL
发明人： CHARLTON, Rebecca Louise , DE HARO GARCIA, Teresa , LOWE, Martin Alexander , MACCOSS, Malcolm , MORGAN, Trevor , TAYLOR, Richard David , ZHU, Zhaoning
IPC分类号： C07D401/10 , C07D403/10 , C07D417/10 , C07D471/04 , A61K31/513 , A61P33/06
摘要： A series of 2-imino-6-methyltetrahydropyrimidin-4(lH)-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.

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