公开(公告)号：US20220242855A1

公开(公告)日：2022-08-04

申请号：US17621877

申请日：2020-06-24

Applicant: UCB Biopharma SRL

Inventor： Shuyu Chu ,  Helen Tracey Horsley ,  James Thomas Reuberson ,  Richard David Taylor ,  Zhaoning Zhu ,  Rose Elizabeth Chappell ,  Gregory William Haslett ,  Adam Peter Smalley ,  Nathaniel Julius Thomas Monck ,  Gareth Neil Brace ,  Prafulkumar Tulshibhai Chovatia

IPC: C07D405/14 ,  C07D487/04 ,  A61K45/06 ,  A61K31/501 ,  A61K31/519 ,  A61K31/4353 ,  C07D498/04 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/497 ,  C07D417/14

Abstract: A series of substituted fused bicyclic imidazole derivatives of formula (I), 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, wherein i. a. A represents C—R1 or N; B represents C—R2 or N; D represents C—R3 or N; E represents C—R4 or N; Z represents —CH(R5)N(H)CH2R6, —CH(R5)N(H)S(O)2R6, —C(═CR5aR5b)N(H)C(O)R6, —CH(R5)R7, —CH(R5)N(H)R7 or —CH(R5)C(O)N(H)R7; R0 represents hydrogen or C1-6 alkyl.

公开(公告)号：US11052076B2

公开(公告)日：2021-07-06

申请号：US16619573

申请日：2018-06-12

Applicant: UCB BIOPHARMA SRL

Inventor： Gareth Neil Brace ,  Rose Elizabeth Chappell ,  Hervé Jean Claude Deboves ,  Anne Marie Foley ,  Gregory Foulkes ,  Elizabeth Pearl Jones ,  Fabien Claude Lecomte ,  Joanna Rachel Quincey ,  Monika-Sarah Elisabeth Dorothea Schulze ,  Matthew Duncan Selby ,  Adam Peter Smalley ,  Richard David Taylor ,  Robert James Townsend ,  Zhaoning Zhu

IPC: C07D471/10 ,  C07D487/10 ,  C07D495/10 ,  C07D491/20 ,  A61K31/4439 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  C07D491/107 ,  C07D519/00

Abstract: 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.

公开(公告)号：US10906919B2

公开(公告)日：2021-02-02

申请号：US16220847

申请日：2018-12-14

Applicant: UCB Biopharma SRL ,  Sanofi

Inventor： Teresa De Haro Garcia ,  Michael Deligny ,  Jag Paul Heer ,  Joanna Rachel Quincey ,  Mengyang Xuan ,  Zhaoning Zhu ,  Daniel Christopher Brookings ,  Mark Daniel Calmiano ,  Yves Evrard ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Sophie Jadot ,  Jean Keyaerts ,  Malcolm Mac Coss ,  Matthew Duncan Selby ,  Michael Alan Shaw ,  Dominique Louis Leon Swinnen ,  Laurent Schio ,  Yann Foricher ,  Bruno Filoche-Romme

IPC: C07D519/00 ,  C07F7/18 ,  C07D491/08 ,  A61K31/4184 ,  A61K31/506 ,  A61K31/55 ,  C07D487/08 ,  C07D491/18 ,  C07D495/08 ,  C07D471/18 ,  C07D487/18 ,  C07D493/18 ,  C07D495/18 ,  C07D513/18

Abstract: A series of fused pentacyclic imidazole derivatives, being potent modulators of human TNFa 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. In particular, the present invention is concerned with 6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one derivatives and analogs thereof.

公开(公告)号：US11479546B2

公开(公告)日：2022-10-25

申请号：US17044550

申请日：2019-04-02

Applicant: UCB Biopharma SRL

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

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

Abstract: 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

Applicant: UCB BIOPHARMA SRL

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

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

Abstract: 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：US10980814B2

公开(公告)日：2021-04-20

申请号：US16497217

申请日：2018-04-24

Applicant: UCB Biopharma SRL ,  SANOFI

Inventor： Daniel Christopher Brookings ,  Teresa De Haro Garcia ,  Yann Foricher ,  Helen Tracey Horsley ,  Martin Clive Hutchings ,  James Andrew Johnson ,  Malcolm Maccoss ,  Mengyang Xuan ,  Zhaoning Zhu

IPC: C07D487/18 ,  A61K31/55

Abstract: Disclosed herein are compounds of formula (I) and pharmaceutically acceptable salt thereof, wherein variables X, R1, R2, and R3 are defined herein. These compounds are potent modulators of human TNFα activity and, 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：US20210094941A1

公开(公告)日：2021-04-01

申请号：US17044550

申请日：2019-04-02

Applicant: UCB Biopharma SRL

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

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

Abstract: 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.