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：US20220169653A1

公开(公告)日：2022-06-02

申请号：US17466230

申请日：2021-09-03

申请人： Galapagos NV

发明人： David AMANTINI ,  Milan MESIC ,  Gordon SAXTY ,  Tanja POLJAK ,  Ines VUJASINOVIC ,  Dinko ZIHER ,  David WITTY ,  Karl Richard GIBSON

IPC分类号： C07D487/04 ,  A61P1/16 ,  A61P19/02 ,  A61P25/04 ,  A61P11/00 ,  C07D471/04

摘要： The present invention relates to pyrrolopyrimidine compounds according to Formula I and their use in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. In a particular aspect, the present compounds are ASK inhibitors, particularly ASK1 inhibitors. The present invention also provides methods for the production of a compound of the invention, pharmaceutical compositions comprising a compound of the invention, the use of the compounds in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases.

公开(公告)号：US20230310433A1

公开(公告)日：2023-10-05

申请号：US18146698

申请日：2022-12-27

申请人： Galapagos NV

发明人： Steven Emiel VAN DER PLAS ,  Oscar MAMMOLITI ,  Sebastien Laurent Xavier MARTINA ,  Pieter Isabelle Roger CLAES ,  Ghjuvanni Petru Diunisu COTI ,  Denis Maurice ANNOOT ,  Miriam LÓPEZ RAMOS ,  René Alexandre GALIEN ,  David AMANTINI ,  Réginald Christophe Xavier BRYS

IPC分类号： A61K31/506 ,  A61P37/06 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5355 ,  C07D471/04 ,  C07D519/00

CPC分类号： A61K31/506 ,  A61P37/06 ,  A61P35/00 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5355 ,  C07D471/04 ,  C07D519/00 ,  C07B2200/05

摘要： The present invention discloses compounds according to Formula I:






Wherein R1, L1, R2, L2, R3, Cy, and the subscript n 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 allergic diseases, inflammatory diseases, metabolic diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IFNα, IL12 and/or IL23 by administering the compound of the invention.

公开(公告)号：US20200165259A1

公开(公告)日：2020-05-28

申请号：US16632202

申请日：2018-07-12

申请人： GALAPAGOS NV ,  CALCHAN LIMITED

发明人： David AMANTINI ,  Milan MESIC ,  Gordon SAXTY ,  Tanja POLJAK ,  Ines VUJASINOVIC ,  Dinko ZIHER ,  David WITTY ,  Karl Richard GIBSON

IPC分类号： C07D487/04 ,  C07D471/04 ,  A61P25/04 ,  A61P1/16 ,  A61P11/00 ,  A61P19/02

摘要： The present invention relates to pyrrolopyrimidine compounds according to Formula I and their use in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases. In a particular aspect, the present compounds are ASK inhibitors, particularly ASK1 inhibitors. The present invention also provides methods for the production of a compound of the invention, pharmaceutical compositions comprising a compound of the invention, the use of the compounds in the prophylaxis and/or treatment of pain, inflammatory conditions, cardiovascular diseases, neurodegenerative diseases, neurological diseases, complications of type I diabetes, cancer and/or fibrotic diseases.

公开(公告)号：US20220402911A1

公开(公告)日：2022-12-22

申请号：US17252146

申请日：2019-05-29

申请人： GALAPAGOS NV

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

IPC分类号： C07D471/04 ,  A61P19/02 ,  A61P17/06 ,  A61P1/00

摘要： The present invention discloses compounds according to Formula I: wherein R1, R2a, 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.

公开(公告)号：US20210169879A1

公开(公告)日：2021-06-10

申请号：US16757189

申请日：2018-10-11

申请人： Galapagos NV

发明人： Steven Emiel VAN DER PLAS ,  Oscar MAMMOLITI ,  Sébastien Laurent Xavier MARTINA ,  Pieter Isabelle Roger CLAES ,  Ghjuvanni Petru Diunisu COTI ,  Denis Maurice ANNOOT ,  Miriam LÓPEZ RAMOS ,  René Alexandre GALIEN ,  David AMANTINI ,  Reginald Christophe Xavier BRYS

IPC分类号： A61K31/506 ,  C07D471/04 ,  C07D519/00 ,  A61K31/496 ,  A61K31/5355 ,  A61K31/444 ,  A61K31/501 ,  A61K31/4545 ,  A61P37/06 ,  A61P35/00

摘要： The present invention discloses compounds according to Formula I: Wherein R1, L1, R2, L2, R3, Cy, and the subscript n 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 allergic diseases, inflammatory diseases, metabolic diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IFNα, IL12 and/or IL23 by administering the compound of the invention.