公开(公告)号：EP1773997B1

公开(公告)日：2011-11-23

申请号：EP05774134.0

申请日：2005-06-14

申请人： Galapagos N.V.

发明人： BRYS, Reginald ,  VANDEGHINSTE, Nick ,  TOMME, Peter, Herwig, Maria

IPC分类号： C12N15/11

CPC分类号： C12Q1/37 ,  C12N9/6491 ,  C12N15/111 ,  C12N2310/14 ,  C12N2320/12 ,  G01N33/6887 ,  G01N2333/96486 ,  G01N2500/04 ,  G01N2800/102

摘要： The present invention relates to in vivo and in vitro methods, agents and compound screening assays for inhibiting extra-cellular matrix degradation, including joint degenerative inhibiting and/or anti-inflammatory pharmaceutical compositions, and the use thereof in treating and/or preventing a disease involving extra-cellular matrix degradation in a subject.

公开(公告)号：EP2361251A1

公开(公告)日：2011-08-31

申请号：EP09781072.5

申请日：2009-07-24

申请人： Galapagos N.V.

发明人： MENET, Christel Jeanne Marie ,  VAN ROMPAEY, Luc Juliaan Corina ,  FLETCHER, Stephen Robert ,  BLANC, Javier ,  JOUANNIGOT, Nolwenn ,  HODGES, Alastair James ,  SMITS, Koen Kurt

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： [1,2,4]Triazolo[1,5-
a ]pyridine compounds are disclosed that have a formula represented by the formula (I). 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, 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 IL6, transplantation rejection (e.g. organ transplant rejection) and proliferative diseases.

公开(公告)号：EP2360474A2

公开(公告)日：2011-08-24

申请号：EP11154007.6

申请日：2005-06-21

申请人： Galapagos N.V.

发明人： Vandeghinste, Nick ,  Tomme, Peter Herwig Maria ,  Michiels, Frits ,  Ma, Libin ,  Mille-Baker, Blandine ,  van Es, Helmuth H.G.

IPC分类号： G01N33/50

CPC分类号： C07H21/04 ,  A61K38/1709 ,  A61K48/00 ,  C12N15/111 ,  C12N2310/14 ,  C12N2320/12 ,  C12Q1/6883 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/5008 ,  G01N33/6887 ,  G01N33/6893 ,  G01N2800/105 ,  Y10T436/143333

摘要： The present invention relates to in vivo and in vitro methods, agents and compound screening assays for inducing anabolic stimulation of chondrocytes, including cartilage formation enhancing pharmaceutical compositions, and the use thereof in treating and/or preventing a disease involving a systemic or local decrease in mean cartilage thickness in a subject.

公开(公告)号：EP2270160A1

公开(公告)日：2011-01-05

申请号：EP10174541.2

申请日：2005-06-14

申请人： Galapagos N.V.

发明人： Brys, Reginald ,  Vandeghinste, Nick ,  Tomme, Peter Herwig Maria

IPC分类号： C12N15/11

CPC分类号： C12Q1/37 ,  C12N9/6491 ,  C12N15/111 ,  C12N2310/14 ,  C12N2320/12 ,  G01N33/6887 ,  G01N2333/96486 ,  G01N2500/04 ,  G01N2800/102

摘要： The present invention relates to in vivo and in vitro methods, agents and compound screening assays for inhibiting extra-cellular matrix degradation, including joint degenerative inhibiting and/or anti-inflammatory pharmaceutical compositions, and the use thereof in treating and/or preventing a disease involving extra-cellular matrix degradation in a subject.

摘要翻译： 本发明涉及一种在体内和体外方法，药剂和化合物的筛选测定法用于抑制的细胞外基质的降解，包括联合变性抑制和/或抗炎的药物组合物，以及治疗和/或预防疾病中的用途 涉及的受试者的细胞外基质降解。

公开(公告)号：EP2259063A2

公开(公告)日：2010-12-08

申请号：EP10174527.1

申请日：2005-04-27

申请人： Galapagos N.V.

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

IPC分类号： G01N33/566 ,  A61P19/10 ,  G01N33/50

CPC分类号： G01N33/566 ,  C12N15/111 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/53 ,  C12N2320/11 ,  C12N2320/12 ,  G01N33/5026 ,  G01N2333/51 ,  G01N2500/04 ,  G01N2800/108

摘要： The present invention relates to methods, agents and compound screening assays for inducing differentiation of undifferentiated mammalian cells into osteoblasts. The invention thus provides a method, comprising contacting a compound with a polypeptide comprising an amino acid sequence selected from the group consisting of SEQ ID No: 194-309; and measuring a compound-polypeptide property related to the differentiation of said cells. The invention further relates to a bone formation enhancing pharmaceutical composition, and the use thereof in treating and/or preventing a disease involving a systemic or local decrease in mean bone density in a subject. Furthermore, the invention relates to a method for the in vitro production of bone tissue.

摘要翻译： 本发明涉及用于诱导未分化哺乳动物细胞分化成成骨细胞的方法，试剂和化合物筛选试验。 因此，本发明提供了一种方法，包括使化合物与包含选自SEQ ID No：194-309的氨基酸序列的多肽接触; 并测量与所述细胞的分化相关的化合物 - 多肽性质。 本发明进一步涉及骨形成增强药物组合物及其在治疗和/或预防涉及受试者平均骨密度全身或局部减少的疾病中的用途。 此外，本发明涉及体外生产骨组织的方法。

公开(公告)号：EP2248896A2

公开(公告)日：2010-11-10

申请号：EP10174533.9

申请日：2004-12-29

申请人： Galapagos N.V.

发明人： Van Rompaye, 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： 本发明提供了用于诱导未分化的哺乳动物细胞的分化成成骨细胞的方法，以及用于鉴定化合物的方法没有诱导未分化的哺乳动物细胞分化成成骨细胞。 另外，本发明提供的多核苷酸和载体，以及作为用于疾病的涉及平均骨密度全身或局部降低的疾病的药物中的用途。 更完了，本发明提供了用于体外骨组织，成骨细胞和用于诊断的病理状态中涉及的平均骨密度全身或局部减小或易感性的条件的方法的生产方法。

公开(公告)号：EP2214018A2

公开(公告)日：2010-08-04

申请号：EP10158238.5

申请日：2005-04-27

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： G01N33/566 ,  A61P19/10 ,  G01N33/50

CPC分类号： G01N33/566 ,  C12N15/111 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/53 ,  C12N2320/11 ,  C12N2320/12 ,  G01N33/5026 ,  G01N2333/51 ,  G01N2500/04 ,  G01N2800/108

摘要： The present invention relates to methods, agents and compound screening assays for inducing differentiation of undifferentiated mammalian cells into osteoblasts. The invention thus provides a method, comprising contacting a compound with a polypeptide comprising an amino acid sequence selected from the group consisting of SEQ ID No: 194-309; and measuring a compound-polypeptide property related to the differentiation of said cells. The invention further relates to a bone formation enhancing pharmaceutical composition, and the use thereof in treating and/or preventing a disease involving a systemic or local decrease in mean bone density in a subject. Furthermore, the invention relates to a method for the in vitro production of bone tissue.

摘要翻译： 本发明涉及到的方法，试剂和化合物筛选测定法用于诱导未分化的哺乳动物细胞分化成成骨细胞。 因此，本发明提供一种方法，包括与包含选自SEQ ID NO的选择的氨基酸序列的多肽的化合物：194-309; 和测量与细胞分化的化合物的多肽属性说。 本发明还涉及到一个骨形成增强药物组合物，以及治疗和/或预防疾病涉及在受试者中的平均骨密度全身或局部降低其用途。 进一步，本发明涉及一种用于骨组织的体外产生的方法。

公开(公告)号：EP2029602B1

公开(公告)日：2010-04-21

申请号：EP07729660.6

申请日：2007-05-30

申请人： Galapagos N.V.

发明人： ANDREWS, Martin James Inglis ,  EDWARDS, Paul ,  CHAMBERS, Mark Stuart ,  SCHMIDT, Wolfgang ,  CLASE, Juha Andrew ,  BAR, Gregory ,  HIRST, Kim Louise ,  MACLEOD, Angus

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P29/00

CPC分类号： C07D487/04

摘要： Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following (formula I). 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, arthritis, inflammation, and others.

公开(公告)号：EP2027124A1

公开(公告)日：2009-02-25

申请号：EP07729106.0

申请日：2007-05-14

申请人： Galapagos N.V.

发明人： BRYS, Reginald Christophe Xavier ,  EDWARDS, Paul ,  SCHMIDT, Wolfgang ,  ANDREWS, Martin James Inglis ,  CHAMBERS, Mark Stuart ,  CLASE, Juha Andrew ,  BIRAULT, Veronique ,  HIRST, Kim Louise ,  MACLEOD, Angus ,  BAR, Gregory ,  HARRIS, Clifford John ,  HUXLEY, Philip

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P19/02

CPC分类号： C07D487/04

摘要： Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula ( I ) represented by the following: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, arthritis, inflammation, and others.

公开(公告)号：EP1444346B1

公开(公告)日：2008-03-12

申请号：EP02776950.4

申请日：2002-08-29

申请人： Galapagos N.V.

发明人： ARTS, Gert-Jan ,  LANGEMEIJER, Ellen, Vera ,  PIEST, Ivo ,  VAN ES, Helmuth, Hendrikus, Gerardus ,  MICHIELS, Godefridus, Augustinus, Maria

IPC分类号： C12N15/11 ,  C12N5/10 ,  C12N7/00 ,  A61K31/713

CPC分类号： C12N9/22 ,  A01K2217/05 ,  C12N15/111 ,  C12N15/113 ,  C12N2310/111 ,  C12N2310/14 ,  C12N2310/53 ,  C12N2320/12 ,  C12N2330/30 ,  C12N2330/31 ,  C12N2799/022 ,  C12Q1/6876

摘要： The present invention relates to polynucleotide constructs, methods for their preparation, and preparations for their use in methods that lower the amount of RNA and/or protein production in cells based on the intracellular expression of small interfering polyribonucleic acid molecules.