公开(公告)号：EP4410375A2

公开(公告)日：2024-08-07

申请号：EP24179691.1

申请日：2019-09-11

申请人： iTeos Belgium SA

发明人： CROSIGNANI, Stefano ,  DICKINSON, Paul ,  DE MATAS, Marcel ,  HOUTHUYS, Erica Joke Katelijne Heleen ,  MARILLIER, Reece Gerrad ,  MARTINOLI, Chiara ,  DE HENAU, Olivier ,  DRIESSENS, Gregory

IPC分类号： A61P35/00

CPC分类号： A61K9/4858 ,  A61K9/4866 ,  A61K31/337 ,  A61K31/513 ,  A61K31/519 ,  A61K31/555 ,  A61K31/704 ,  A61K31/7068 ,  A61K45/06 ,  A61P35/00 ,  C07D513/14 ,  A61K31/5377 ,  A61K33/243 ,  A61K39/3955 ,  C07K16/2803 ,  C07K16/2818 ,  C07K16/2827 ,  C07K2317/7620130101

摘要： The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors

Especially, the present invention relates to a pharmaceutical composition comprising an A2A inhibitor of Formula (I) and a lipid carrier such as lauroyl macrogol-32 glycerides, D-α-tocopherol-polyethylene glycol-1000 succinate or a mixture thereof. The pharmaceutical composition of the invention is particularly useful for oral dosing in the treatment of cancers.
The present invention also relates to a combination comprising an A2A receptor inhibitor of Formula (I) and an anticancer agent. The anticancer agent is for example an immunotherapeutic agent, such as a checkpoint inhibitor. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination. Additionally, the combination of the invention is particularly useful for the treatment and/or prevention of cancers.

公开(公告)号：EP4410375A3

公开(公告)日：2024-11-06

申请号：EP24179691.1

申请日：2019-09-11

申请人： iTeos Belgium SA

发明人： CROSIGNANI, Stefano ,  DICKINSON, Paul ,  DE MATAS, Marcel ,  HOUTHUYS, Erica Joke Katelijne Heleen ,  MARILLIER, Reece Gerrad ,  MARTINOLI, Chiara ,  DE HENAU, Olivier ,  DRIESSENS, Gregory

IPC分类号： A61K31/519 ,  C07D497/14 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/22 ,  A61K9/20 ,  A61K9/16 ,  A61K9/48 ,  A61P35/00 ,  A61K47/20 ,  A61K47/30 ,  A61K47/32 ,  A61K47/34 ,  A61K47/38

摘要： The present invention relates to thiocarbamate derivatives of Formula (I) which are useful as A2A adenosine receptor (A2AR) inhibitors

Especially, the present invention relates to a pharmaceutical composition comprising an A2A inhibitor of Formula (I) and a lipid carrier such as lauroyl macrogol-32 glycerides, D-α-tocopherol-polyethylene glycol-1000 succinate or a mixture thereof. The pharmaceutical composition of the invention is particularly useful for oral dosing in the treatment of cancers.
The present invention also relates to a combination comprising an A2A receptor inhibitor of Formula (I) and an anticancer agent. The anticancer agent is for example an immunotherapeutic agent, such as a checkpoint inhibitor. The invention further relates to a pharmaceutical composition and a kit of parts comprising such combination. Additionally, the combination of the invention is particularly useful for the treatment and/or prevention of cancers.

公开(公告)号：EP4413007A1

公开(公告)日：2024-08-14

申请号：EP22800911.4

申请日：2022-10-06

申请人： iTeos Belgium SA

发明人： DE MATAS, Marcel ,  DICKINSON, Paul ,  SCHNEIDER, Manfred ,  ROSS, Sally ,  GANGOLLI, Esha ,  SRIVASTAVA, Shouraydeep ,  LAGER, Joanne ,  MADASAMY, Pratheepan ,  ARET, Edwin ,  VAN BERKEL, Chantalle ,  ROSSETTI, Maura ,  MARTINOLI, Chiara

IPC分类号： C07D497/14 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D497/14

公开(公告)号：EP3849558A1

公开(公告)日：2021-07-21

申请号：EP19772998.1

申请日：2019-09-11

申请人： iTeos Belgium SA

发明人： CROSIGNANI, Stefano ,  DICKINSON, Paul ,  DE MATAS, Marcel ,  HOUTHUYS, Erica Joke Katelijne Heleen ,  MARILLIER, Reece Gerrad ,  MARTINOLI, Chiara ,  DE HENAU, Olivier ,  DRIESSENS, Gregory

IPC分类号： A61K31/519 ,  C07D497/14 ,  A61K31/337 ,  A61K31/513 ,  A61K31/555 ,  A61K31/704 ,  A61K31/7068 ,  A61K45/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/22 ,  A61K9/20 ,  A61K9/16 ,  A61K9/48 ,  A61P35/00