公开(公告)号：US20180002293A1

公开(公告)日：2018-01-04

申请号：US15538393

申请日：2015-12-18

申请人： GALAPAGOS NV ,  LES LABORATOIRES SERVIER

发明人： Franck Laurent BREBION ,  Luke Jonathan ALVEY ,  David AMANTINI ,  Frédéric André DE CEUNINCK ,  Pierre Marc Marie Joseph DEPREZ ,  Romain Luc Marie GOSMINI ,  Hélène Marie JARY ,  Christophe PEIXOTO ,  Iuliana Ecaterina POP-BOTEZ ,  Marie Laurence Claire VARIN

IPC分类号： C07D233/78 ,  C07D405/12 ,  C07D403/14 ,  C07D401/14 ,  A61K31/496 ,  C07D401/12 ,  C07D401/04 ,  A61K31/5377 ,  C07D417/12 ,  C07D403/06

CPC分类号： C07D233/78 ,  A61K31/496 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/12 ,  C07D417/12

摘要： The present invention discloses compounds according to Formula I: Wherein R1, R2, R3a, R3b, and Cy are as defined herein.The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.

公开(公告)号：US20210309614A1

公开(公告)日：2021-10-07

申请号：US17141902

申请日：2021-01-05

申请人： GALAPAGOS NV ,  LES LABORATOIRES SERVIER

发明人： Franck Laurent BREBION ,  Luke Jonathan ALVEY ,  David AMANTINI ,  Frédéric André DE CEUNINCK ,  Pierre Marc Marie Joseph DEPREZ ,  Romain Luc Marie GOSMINI ,  Hélène Marie JARY ,  Christophe PEIXOTO ,  Iuliana Ecaterina POP-BOTEZ ,  Marie Laurence Claire VARIN

IPC分类号： C07D233/78 ,  C07D403/06 ,  A61P19/02 ,  A61P19/04 ,  A61K31/496 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D417/12 ,  A61K31/55

摘要： The present invention discloses compounds according to Formula I: Wherein R1, R2, R3a, R3b, and Cy are as defined herein.
The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.

公开(公告)号：US20200216397A1

公开(公告)日：2020-07-09

申请号：US16653668

申请日：2019-10-15

申请人： GALAPAGOS NV ,  LES LABORATOIRES SERVIER

发明人： Franck Laurent BREBION ,  Luke Jonathan ALVEY ,  David AMANTINI ,  Frédéric André DE CEUNINCK ,  Pierre Marc Marie Joseph DEPREZ ,  Romain Luc Marie GOSMINI ,  Hélène Marie JARY ,  Christophe PEIXOTO ,  Iuliana Ecaterina POP-BOTEZ ,  Marie Laurence Claire VARIN

IPC分类号： C07D233/78 ,  A61P19/04 ,  A61P19/02 ,  A61K31/55 ,  C07D417/12 ,  C07D405/12 ,  C07D403/14 ,  C07D401/14 ,  C07D401/12 ,  C07D401/04 ,  A61K31/5377 ,  A61K31/496 ,  C07D403/06

摘要： The present invention discloses compounds according to Formula I: Wherein R1, R2, R3a, R3b, and Cy are as defined herein.The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.

公开(公告)号：US20190300503A1

公开(公告)日：2019-10-03

申请号：US16308380

申请日：2017-06-01

申请人： Galapagos NV ,  LES LABORATOIRES SERVIER

发明人： Frédéric Gilbert LABÉGUÈRE ,  Rama HENG ,  Frédéric André DE CEUNINCK ,  Luke Jonathan ALVEY ,  David AMANTINI ,  Franck Laurent BREBION ,  Pierre Marc Marie Joseph DEPREZ ,  Romain Luc Marie GOSMINI ,  Hélène Marie JARY ,  Christophe PEIXOTO ,  Iuliana Ecaterina POP-BOTEZ ,  Marie Laurence Claire VARIN

IPC分类号： C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  A61P19/02

摘要： The present invention discloses compounds according to Formula I: Wherein R1, R2, R3a, R3b, R6, Cy, and the subscript n are as defined herein.The present invention relates to compounds inhibiting ADAMTS, 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, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering the compound of the invention.

公开(公告)号：US20180258052A1

公开(公告)日：2018-09-13

申请号：US15896779

申请日：2018-02-14

申请人： GALAPAGOS NV ,  LES LABORATOIRES SERVIER

发明人： Franck Laurent BREBION ,  Luke Jonathan ALVEY ,  David AMANTINI ,  Frédéric André DE CEUNINCK ,  Pierre Marc Marie Joseph DEPREZ ,  Romain Luc Marie GOSMINI ,  Hélène Marie JARY ,  Christophe PEIXOTO ,  Iuliana Ecaterina POP-BOTEZ ,  Marie Laurence Claire VARIN

IPC分类号： C07D233/78 ,  C07D403/14 ,  A61K31/5377 ,  A61K31/496 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D401/04 ,  C07D401/14 ,  C07D403/06

摘要： The present invention discloses compounds according to Formula I: Wherein R1, R2, R3a, R3b, and Cy are as defined herein.The present invention relates to compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory conditions, and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis by administering a compound of the invention.

公开(公告)号：US20190002458A1

公开(公告)日：2019-01-03

申请号：US15971245

申请日：2018-05-04

申请人： GALAPAGOS NV

发明人： Frédéric Gilbert LABÉGUÈRE ,  Gregory John Robert NEWSOME ,  Luke Jonathan ALVEY ,  Laurent Raymond Maurice SANIÈRE ,  Stephen Robert FLETCHER

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

摘要： A compound according to Formula Ia: wherein L1, G, and R1 are as described herein.The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

公开(公告)号：US20160244442A1

公开(公告)日：2016-08-25

申请号：US14966879

申请日：2015-12-11

申请人： GALAPAGOS NV

发明人： Frédéric Gilbert LABÉGUÈRE ,  Gregory John Robert NEWSOME ,  Luke Jonathan ALVEY ,  Laurent Raymond Maurice SANIÈRE ,  Stephen Robert FLETCHER

IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/519

CPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

摘要： A compound according to Formula Ia: wherein L1, G, and R1 are as described herein.The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

公开(公告)号：US20140121204A1

公开(公告)日：2014-05-01

申请号：US14148057

申请日：2014-01-06

申请人： GALAPAGOS NV

发明人： Frédéric Gilbert Labéguère ,  Gregory John Robert NEWSOME ,  Luke Jonathan ALVEY ,  Laurent Raymond Maurice Sanière ,  Stephen Robert FLETCHER

IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/519

CPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

摘要： A compound according to Formula Ia: wherein L1, G, and R1 are as described herein.The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.

摘要翻译： 根据式Ia的化合物：其中L 1，G和R 1如本文所述。 本发明涉及拮抗GPR84的式I的新型化合物，涉及炎性病症的G蛋白偶联受体，以及这些新化合物的制备方法，包含这些化合物的药物组合物，以及预防方法 炎症性疾病（IBD），类风湿性关节炎，血管炎，肺部疾病（如慢性阻塞性肺疾病（COPD）和肺间质性疾病（如特发性肺纤维化（IPF）））和/或治疗炎症性疾病 ，传染病，自身免疫性疾病，内分泌和/或代谢疾病，和/或涉及免疫细胞功能损害的疾病，通过施用本发明的化合物。

公开(公告)号：US20220340548A1

公开(公告)日：2022-10-27

申请号：US17614854

申请日：2020-05-25

申请人： Galapagos NV

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

IPC分类号： C07D405/10 ,  C07D401/10 ,  C07D235/16 ,  C07D471/04 ,  C07D519/00 ,  A61P1/00 ,  A61P19/02 ,  A61P9/00 ,  A61P11/00 ,  A61P37/00

摘要： The present invention discloses compounds according to Formula I: wherein R1a, R1b, R1c, R2a, W1, W2, X1, X2, X3, 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：US20220227751A1

公开(公告)日：2022-07-21

申请号：US17454712

申请日：2021-11-12

申请人： GALAPAGOS NV

发明人： Frédéric Gilbert LABÉGUÈRE ,  Gregory John Robert NEWSOME ,  Luke Jonathan ALVEY ,  Laurent Raymond Maurice SANIÈRE ,  Stephen Robert FLETCHER

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06

摘要： A compound according to Formula Ia: wherein L1, G, and R1 are as described herein.
The present invention relates to novel compounds according to Formula I that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis, lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.