公开(公告)号：WO2020239656A1

公开(公告)日：2020-12-03

申请号：PCT/EP2020/064364

申请日：2020-05-25

Applicant: GALAPAGOS NV

Inventor： HUCK, Jacques ,  MAMMOLITI, Oscar ,  PALISSE, Adeline, Marie, Elise ,  RICHARD, Sébastien ,  SAVY, Pascal, Pierre, Alexandre

IPC: A61P31/00 ,  C07D495/04 ,  A61K31/4365

Abstract: The present invention discloses compounds according to Formula (I), wherein X, G, R 1 , R 2a , R 2b , R 3 , R 4 , and R 5 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 diseases involving hepatitis B by administering the compound of the invention.

公开(公告)号：WO2020200898A1

公开(公告)日：2020-10-08

申请号：PCT/EP2020/058061

申请日：2020-03-24

Applicant: GALAPAGOS NV

Inventor： MAMMOLITI, Oscar ,  BRYS, Reginald, Christophe, Xavier ,  NEWSOME, Gregory, John, Robert ,  BABEL, Marielle, Gilles

IPC: C07D471/04 ,  A61P29/00 ,  A61K31/416

Abstract: The present invention discloses compounds according to Formula I, wherein R 1 , R 2 , and Cy are as defined herein. The present invention relates to compounds, methods for the production of said compounds, pharmaceutical compositions comprising said compounds and methods for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, pain, fibrosis and/or proliferative diseases by administering said compounds.

公开(公告)号：WO2017060879A1

公开(公告)日：2017-04-13

申请号：PCT/IB2016/056035

申请日：2016-10-07

Applicant: ABBVIE S.À.R.L. ,  GALAPAGOS NV

Inventor： AKKARI, Rhalid ,  ALVEY, Luke Jonathan ,  BOCK, Xavier Marie ,  BROWN, Brian S. ,  CLAES, Pieter Isabelle Roger ,  COWART, Marlon D. ,  CONRATH, Katja E. ,  CYR, Douglas ,  DE LEMOS, Elsa ,  DE WILDE, Gert Jules Hector ,  DESROY, Nicolas ,  DUTHION, Béranger ,  GFESSER, Gregory A. ,  GOSMINI, Romain Luc Marie ,  HOUSSEMAN, Christopher Gaëtan ,  JANSEN, Koen Karel ,  JI, Jianguo ,  KYM, Philip R. ,  LEFRANCOIS, Jean-Michel ,  MAMMOLITI, Oscar ,  MENET, Christel Jeanne Marie ,  MERAYO, Nuria Merayo ,  NEWSOME, Gregory John Robert ,  PALISSE, Adeline Marie Elise ,  PATEL, Sachin V. ,  PIZZONERO, Mathieu Rafaël ,  SHRESTHA, Anurupa ,  SWIFT, Elizabeth C. ,  TSE, Chris ,  VAN DER PLAS, Steven Emiel ,  WANG, Xueqing

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/437 ,  A61P11/00 ,  G01N33/68

CPC classification number: A61K31/4545 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  G01N33/5023 ,  G01N2800/382

Abstract: A corrector agent capable of stabilizing a newly synthesized cystic fibrosis transmembrane conductance regulator (CFTR) protein, useful in the treatment of cystic fibrosis.

Abstract translation: 能够稳定新合成的囊性纤维化跨膜电导调节蛋白（CFTR）蛋白的修正剂，可用于治疗囊性纤维化。

公开(公告)号：WO2017012647A1

公开(公告)日：2017-01-26

申请号：PCT/EP2015/066520

申请日：2015-07-20

Applicant: GALAPAGOS NV

Inventor： MENET, Christel, Jeanne, Marie ,  MAMMOLITI, Oscar ,  QUINTON, Evelyne ,  JOANNESSE, Caroline, Martine, Andrée-Marie ,  DE BLIECK, Ann ,  BLANC, Javier

IPC: C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P37/08 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: The present invention discloses compounds according to Formula (I), wherein R 1 , R 3 , R 4 , R 5 , L1, and Cy are as defined herein. The present invention also provides compounds, methods for the production of said compounds of the invention, pharmaceutical compositions comprising the same and their use in allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 and/or interferons. The present invention also methods for the prevention and/or treatment of the aforementioned diseases by administering a compound of the invention.

Abstract translation: 本发明公开了根据式（I）的化合物，其中R1，R3，R4，R5，L1和Cy如本文所定义。 本发明还提供化合物，制备本发明所述化合物的方法，包含其的药物组合物及其在过敏或炎性病症中的用途，自身免疫性疾病，增殖性疾病，移植排斥反应，涉及软骨周转损伤的疾病，先天性软骨 畸形和/或与IL6和/或干扰素的分泌过多相关的疾病。 本发明还涉及通过给予本发明化合物来预防和/或治疗上述疾病的方法。