公开(公告)号：US10654861B2

公开(公告)日：2020-05-19

申请号：US16086408

申请日：2017-03-31

申请人： UCB Biopharma SRL ,  Sanofi

发明人： Michael Louis Robert Deligny ,  Jag Paul Heer ,  Jean Keyaerts ,  Luce Elsa Lepissier ,  Martin Alexander Lowe

IPC分类号： C07D487/18 ,  C07D487/04

摘要： A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

公开(公告)号：US11479546B2

公开(公告)日：2022-10-25

申请号：US17044550

申请日：2019-04-02

申请人： UCB Biopharma SRL

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

IPC分类号： A61P33/06 ,  C07D403/12 ,  C07D493/08 ,  C07D471/04 ,  C07D239/22 ,  C07D401/12 ,  C07D413/14 ,  C07D405/06 ,  C07D405/14 ,  C07D405/04

摘要： The application relates to a series of 2-imino-6-methylhexahydropyrimidin-4-one derivatives and 3-imino-5-methyl-1,2,4-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.

公开(公告)号：US20220289685A1

公开(公告)日：2022-09-15

申请号：US17632336

申请日：2020-08-17

申请人： UCB BIOPHARMA SRL

发明人： Teresa De Haro Garcia ,  Martin Alexander Lowe ,  Malcolm MacCoss ,  Richard David Taylor ,  Zhaoning Zhu ,  Rose Elizabeth Chappell

IPC分类号： C07D239/22 ,  C07D407/04 ,  C07D471/04 ,  C07D407/14 ,  A61P33/06 ,  A61K47/06

摘要： A series of 2-imino-6-methylhexahydropyrimidin-4-one derivatives, and analogues thereof, substituted in the 6-position by an arylcarbonylaminophenyl or heteroarylcarbonylaminophenyl moiety, being potent inhibitors of the growth and propagation of the Plasmodium falciparum parasite in human blood, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

公开(公告)号：US20210094941A1

公开(公告)日：2021-04-01

申请号：US17044550

申请日：2019-04-02

申请人： UCB Biopharma SRL

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

IPC分类号： C07D405/14 ,  C07D239/22 ,  C07D405/04 ,  C07D471/04 ,  C07D413/14 ,  C07D401/12 ,  C07D403/12 ,  C07D493/08 ,  C07D405/06

摘要： The application relates to a series of 2-imino-6-methylhexahydropyrimidin-4-one derivatives and 3-imino-5-methyl-1,2,4-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.

公开(公告)号：US20190100525A1

公开(公告)日：2019-04-04

申请号：US16086408

申请日：2017-03-31

申请人： UCB Biopharma SPRL ,  Sanofi

发明人： Michael Louis Robert Deligny ,  Jag Paul Heer ,  Jean Keyaerts ,  Luce Elsa Lepissier ,  Martin Alexander Lowe

IPC分类号： C07D487/18

摘要： A series of substituted fused pentacyclic benzimidazole derivatives, and analogues thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.