公开(公告)号：WO2019105886A1

公开(公告)日：2019-06-06

申请号：PCT/EP2018/082537

申请日：2018-11-26

Applicant: GALAPAGOS NV

Inventor： ALVEY, Luke, Jonathan ,  ANNOOT, Denis, Maurice ,  BONNATERRE, Florence, Marie-Emilie ,  BUCHER, Denis ,  DUTHION, Béranger ,  JARY, Hélène ,  PEIXOTO, Christophe ,  TEMAL-LAIB, Taoues ,  TIRERA, Amynata

IPC: C07D403/04 ,  C07D471/04 ,  A61K31/437 ,  A61P9/00 ,  A61P37/00

Abstract: The present invention discloses compounds according to Formula (I): wherein R 1 , R 2 , R 3a , R 3b , X, Y 1 , Y 2 , Y 3 , and Z are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of TNFα, interferons, IL-6, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

公开(公告)号：WO2021032323A1

公开(公告)日：2021-02-25

申请号：PCT/EP2020/054086

申请日：2020-02-17

Applicant: GALAPAGOS NV

Inventor： TEMAL-LAÏB, Taoues ,  HECKMANN, Bertrand ,  COUTY, Sylvain ,  RICHARD, Sébastien ,  ANNOOT, Denis, Maurice ,  TIRERA, Amynata ,  MESIC, Milan ,  TRIBALLEAU, Nicolas

IPC: C07D487/04 ,  C07D471/04 ,  C07D519/00 ,  A61K31/519 ,  A61P9/00 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P35/00

Abstract: The present invention discloses compounds according to Formula I, wherein A, B, R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, pain, and/or abnormal angiogenesis associated diseases by administering the compounds of the invention.

公开(公告)号：WO2020239658A1

公开(公告)日：2020-12-03

申请号：PCT/EP2020/064368

申请日：2020-05-25

Applicant: GALAPAGOS NV

Inventor： ALVEY, Luke, Jonathan ,  BUCHER, Denis ,  DESROY, Nicolas ,  JARY, Hélène, Marie ,  PEIXOTO, Christophe ,  TEMAL-LAÏB, Taoues ,  TIRERA, Amynata ,  BONNATERRE, Florence, Marie-Emilie ,  DUTHION, Béranger

IPC: A61P29/00 ,  A61P35/00 ,  C07D471/04 ,  C07D487/04 ,  A61P11/00 ,  A61K31/437 ,  A61P9/00 ,  A61P37/00

Abstract: The present invention discloses compounds according to Formula (I), wherein R 1a , R 1b , R 1c , R 2a , W 1 , W 2 , X 1 , X 2 , X 3 , Y, and Z are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of IL-6, diseases associated with hypersecretion of TNFα, interferons, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.

公开(公告)号：WO2019238424A1

公开(公告)日：2019-12-19

申请号：PCT/EP2019/063956

申请日：2019-05-29

Applicant: GALAPAGOS NV

Inventor： DESROY, Nicolas ,  JONCOUR, Agnès, Marie ,  PEIXOTO, Christophe ,  TEMAL-LAIB, Taoues ,  TIRERA, Amynata ,  BUCHER, Denis ,  AMANTINI, David ,  DE VOS, Steve, Irma, Joel ,  BRYS, Reginald, Christophe, Xavier

IPC: A61K31/437 ,  C07D471/04 ,  A61P25/00 ,  A61P11/00 ,  A61P9/00 ,  A61P35/00 ,  A61P37/00

Abstract: The present invention discloses compounds according to Formula I: wherein R 1 , R 2a , X, Y, and Z are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of IL-6, diseases associated with hypersecretion of TNFα, interferons, IL-12 and/or IL-23, respiratory diseases, endocrine and/or metabolic diseases, cardiovascular diseases, dermatological diseases, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.