公开(公告)号：EP3976189B1

公开(公告)日：2024-07-03

申请号：EP20728465.4

申请日：2020-05-25

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

CPC分类号： C07D471/04 ,  C07D487/04 ,  A61P29/00 ,  A61P35/00 ,  A61P11/00 ,  A61P9/00 ,  A61P37/00 ,  C07D519/00

公开(公告)号：EP3736267B1

公开(公告)日：2021-05-05

申请号：EP20183405.8

申请日：2018-09-13

发明人： ALTENBACH, Robert J ,  BOGDAN, Andrew ,  COUTY, Sylvain ,  DESROY, Nicolas ,  GFESSER, Gregory A. ,  HOUSSEMAN, Christopher Gaëtan ,  KYM, Philip R. ,  LIU, Bo ,  MAI, Thi Thu Trang ,  MALAGU, Karine Fabienne ,  MERAYO MERAYO, Nuria ,  PICOLET, Olivier Laurent ,  PIZZONERO, Mathieu Rafaël ,  SEARLE, Xenia B. ,  VAN DER PLAS, Steven Emiel ,  WANG, Xueqing ,  YEUNG, Ming C.

IPC分类号： C07D215/36 ,  C07D213/64 ,  C07D213/71 ,  C07D231/56 ,  C07D235/28 ,  C07D401/12 ,  C07D471/04 ,  C07C311/45 ,  A61P11/00 ,  A61K31/4709

公开(公告)号：EP3736267A1

公开(公告)日：2020-11-11

申请号：EP20183405.8

申请日：2018-09-13

申请人： AbbVie Overseas S.à r.l. ,  Galapagos N.V.

发明人： ALTENBACH, Robert J ,  BOGDAN, Andrew ,  COUTY, Sylvain ,  DESROY, Nicolas ,  GFESSER, Gregory A. ,  HOUSSEMAN, Christopher Gaëtan ,  KYM, Philip R. ,  LIU, Bo ,  MAI, Thi Thu Trang ,  MALAGU, Karine Fabienne ,  MERAYO MERAYO, Nuria ,  PICOLET, Olivier Laurent ,  PIZZONERO, Mathieu Rafaël ,  SEARLE, Xenia B. ,  VAN DER PLAS, Steven Emiel ,  WANG, Xueqing ,  YEUNG, Ming C.

IPC分类号： C07D215/36 ,  C07D213/64 ,  C07D213/71 ,  C07D231/56 ,  C07D235/28 ,  C07D401/12 ,  C07D471/04 ,  C07C311/45 ,  A61P11/00 ,  A61K31/4709

摘要： Compounds of Formula (I) are disclosed:

wherein A 1 , R 1 , R 2 , R 3 , R 4 , and n are as defined herein. Also disclosed is the use of the compounds in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering the compounds.

公开(公告)号：EP2565649B1

公开(公告)日：2015-04-15

申请号：EP12183326.3

申请日：2008-06-19

申请人： Galapagos N.V.

发明人： Brys, Reginald Christophe Xavier ,  Vandeghinste, Nick Ernest René

IPC分类号： G01N33/50 ,  G01N33/68 ,  C12N15/11

CPC分类号： G01N33/5308 ,  A61K31/7088 ,  A61K31/713 ,  A61K45/06 ,  C12N15/111 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/53 ,  C12N2320/12 ,  C12Y111/01006 ,  G01N33/6887 ,  G01N2500/04 ,  G01N2800/102 ,  G01N2800/105

公开(公告)号：EP2702059A1

公开(公告)日：2014-03-05

申请号：EP12717289.8

申请日：2012-04-26

申请人： Galapagos N.V.

发明人： MENET, Christel, Jeanne, Marie ,  HODGES, Alastair, James ,  VATER, Huw, David

IPC分类号： C07D471/04 ,  A61K31/4162 ,  A61P19/02

CPC分类号： A61K31/496 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D471/04 ,  C07D491/107

摘要： Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.

公开(公告)号：EP2565649A1

公开(公告)日：2013-03-06

申请号：EP12183326.3

申请日：2008-06-19

申请人： Galapagos N.V.

发明人： Brys, Reginald Christophe Xavier ,  Vandeghinste, Nick Ernest René

IPC分类号： G01N33/68 ,  C12N15/11

CPC分类号： G01N33/5308 ,  A61K31/7088 ,  A61K31/713 ,  A61K45/06 ,  C12N15/111 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/53 ,  C12N2320/12 ,  C12Y111/01006 ,  G01N33/6887 ,  G01N2500/04 ,  G01N2800/102 ,  G01N2800/105

摘要： The present invention relates to methods for identifying agents capable of inhibiting the expression or activity of proteins involved in the processes modulating osteoclastogenesis, which inhibition is useful in the prevention and / or treatment of bone and joint degenerative diseases and diseases involving aberrant activity or differentiation of osteoclasts. In particular, the present invention provides methods for identifying agents for use in the prevention and / or treatment of rheumatoid arthritis.

摘要翻译： 本发明涉及用于鉴定试剂能够抑制在过程中所涉及的蛋白质的表达或活性来调节破骨细胞形成，其中抑制是在预防和/或骨关节退行性疾病和疾病的治疗中有用涉及异常活性或分化 破骨细胞。 特别地，本发明提供用于鉴定剂在类风湿性关节炎的预防和/或治疗方法。

公开(公告)号：EP2346864B1

公开(公告)日：2013-03-06

申请号：EP09781073.3

申请日：2009-07-24

申请人： Galapagos N.V.

发明人： MENET, Christel Jeanne Marie ,  BLANC, Javier

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P19/02

CPC分类号： A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  C07D471/04

公开(公告)号：EP2248896A3

公开(公告)日：2012-07-25

申请号：EP10174533.9

申请日：2004-12-29

申请人： Galapagos N.V.

发明人： Van Rompaey, Luc Juliaan Corina ,  Tomme, Peter Herwig Maria ,  Brown, Robin John

IPC分类号： C12N15/113 ,  A61K31/713 ,  C12Q1/68 ,  C12N5/10 ,  G01N33/68 ,  A61P19/08 ,  A61P19/10

CPC分类号： C12N15/1137 ,  C12N5/0654 ,  C12N2310/11 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/315 ,  C12N2310/53 ,  C12N2510/00 ,  C12N2799/021 ,  C12Y207/11001 ,  G01N33/6893

摘要： The present invention provides methods for inducing differentiation of undifferentiated mammalian cells into osteoblasts, and methods for identifying a compound that induces differentiation of undifferentiated mammalian cells into osteoblasts. In addition, the present invention provides polynucleotides and vectors, and the use thereof as a medicament for the treatment of a disease involving a systemic or local decrease in mean bone density. Moreover, the present invention provides methods for in vitro production of bone tissue, osteoblast cells and methods for diagnosing a pathological condition involving a systemic or local decrease in mean bone density or a susceptibility to the condition.

摘要翻译： 本发明提供诱导未分化的哺乳动物细胞分化成成骨细胞的方法，以及鉴定诱导未分化的哺乳动物细胞分化成成骨细胞的化合物的方法。 此外，本发明提供了多核苷酸和载体，以及它们作为用于治疗涉及平均骨密度全身或局部降低的疾病的药物的用途。 此外，本发明提供了用于体外产生骨组织，成骨细胞的方法以及用于诊断涉及平均骨密度或对该病症的易感性的系统或局部降低的病理状态的方法。

公开(公告)号：EP2346864A1

公开(公告)日：2011-07-27

申请号：EP09781073.3

申请日：2009-07-24

申请人： Galapagos N.V.

发明人： MENET, Christel Jeanne Marie ,  BLANC, Javier

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P19/02

CPC分类号： A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  C07D471/04

摘要： A novel [1,2,4]triazolo[1,5-a]pyridine compound is disclosed that has a formula represented by the formula (I). This compound may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diseases involving cartilage degradation, bone and/or joint degradation, for example osteoarthritis; and/or conditions involving inflammation or immune responses, such as Crohn's disease, rheumatoid arthritis, psoriasis, allergic airways disease (e.g. asthma, rhinitis), juvenile idiopathic arthritis, colitis, inflammatory bowel diseases, endotoxin-driven disease states (e.g. complications after bypass surgery or chronic endotoxin states contributing to e.g. chronic cardiac failure), diseases involving impairment of cartilage turnover (e.g. diseases involving the anabolic stimulation of chondrocytes), congenital cartilage malformations, diseases associated with hypersecretion of IL6and transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

公开(公告)号：EP2344460A1

公开(公告)日：2011-07-20

申请号：EP09782854.5

申请日：2009-09-10

申请人： Galapagos N.V.

发明人： NIQUE, François ,  JAGERSCHMIDT, Catherine ,  BLANQUÉ, Roland ,  LEFRANÇOIS, Jean-Michel ,  PEIXOTO, Christophe ,  DEPREZ, Pierre ,  TRIBALLEAU, Nicolas ,  WIGERINCK, Piet, Tom, Bert, Paul ,  NAMOUR, Florence, Sylvie

IPC分类号： C07D233/60 ,  C07D233/66 ,  A61K31/4166 ,  A61P35/00

CPC分类号： C07D233/60 ,  C07D233/66

摘要： Novel compounds are disclosed that have a Formula represented by the following: wherein X, R
1 , R
2a , R
2b , R
2c , R
3a R
3b , R
4a , R
4b , R
4c , and ml are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non- limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.