公开(公告)号：EP2445911A1

公开(公告)日：2012-05-02

申请号：EP10724881.7

申请日：2010-06-25

申请人： Galapagos N.V.

发明人： MENET, Christel Jeanne Marie ,  SMITS, Koen Kurt

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

CPC分类号： A61K31/541 ,  A61K45/06 ,  C07D471/04

摘要： A novel compound able to inhibit JAK is disclosed, 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, 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. (I)

公开(公告)号：EP2414829A1

公开(公告)日：2012-02-08

申请号：EP10712085.9

申请日：2010-04-01

申请人： Galapagos N.V.

发明人： BRYS, Reginald Christophe Xavier ,  NELLES, Luc ,  VANDEGHINSTE, Nick Ernest Rene ,  MILLE-BAKER, Blandine ,  TESSARI, Michela Angela

IPC分类号： G01N33/50

CPC分类号： C12N15/1137 ,  C12N15/113 ,  C12N15/1138 ,  C12N2310/14 ,  G01N33/5032 ,  G01N33/6887 ,  G01N2333/726 ,  G01N2333/912 ,  G01N2333/9121 ,  G01N2333/96486 ,  G01N2333/96494 ,  G01N2500/04 ,  G01N2500/10 ,  G01N2500/20 ,  G01N2800/105

摘要： The invention relates to the field of medicinal research, cartilage physiology and diseases involving the degeneration of cartilage tissue. More specifically, the invention relates to methods and means for identifying compounds that inhibit catabolic processes in chondrocytes and that decrease the degradation of cartilage and/or ECM. The invention also relates to the compounds that are useful in the treatment of osteoarthritis. The invention also relates to targets, the modulation of which results in a decrease in the degradation of ECM and /or cartilage and decrease inflammation. In addition, the invention relates to compositions and methods for the use thereof in treating conditions that are characterized by the degradation of ECM and /or cartilage and inflammation.

公开(公告)号：EP2360478A1

公开(公告)日：2011-08-24

申请号：EP11154125.6

申请日：2005-10-17

申请人： Galapagos N.V.

发明人： Brys, Reginald ,  Vandeghinste, Nick ,  Tomme, Peter Herwig Maria ,  Klaassen, Hubertus Johanus Matheus

IPC分类号： G01N33/566 ,  C12N15/113 ,  A61K31/7088

CPC分类号： G01N33/6887 ,  A61K31/7088 ,  A61K38/00 ,  A61K48/00 ,  C12N7/00 ,  C12N15/1137 ,  C12N15/1138 ,  C12N2310/11 ,  C12N2310/12 ,  C12N2310/14 ,  C12N2710/10343 ,  C12Y304/24007 ,  G01N33/564 ,  G01N2333/9121 ,  G01N2800/102 ,  G01N2800/105

摘要： The application discloses methods for identifying and using compounds that inhibit extra-cellular matrix (ECM) degradation and inflammation, using a polypeptide sequence including SEQ ID NO: 17-127 (hereinafter "TARGETS") and fragments thereof, expression inhibitory agents such as antisense polynucleotide, a ribozyme, and a small interfering RNA (siRNA), comprising a nucleic acid sequence complementary to, or engineered from, a naturally occurring polynucleotide sequence encoding a polypeptide of SEQ ID NO: 17-127, useful in pharmaceutical compositions comprising said agent, for the treatment, or prevention, of chronic joint degenerative and/or inflammatory diseases such as rheumatoid arthritis.

摘要翻译： 用于鉴定和使用的化合物中的应用无盘方法确实抑制的细胞外基质（ECM）降解和炎症，使用的多肽序列包含SEQ ID NO：17至127（在“目标”之后），以及它们的片段，表达抑制剂：例如反义 多核苷酸，核酶和小干扰RNA（siRNA），其特征在于互补的，或从编码SEQ ID NO的多肽的天然存在的多核苷酸序列工程化的核酸序列：17-127，用于药物组合物含有所述试剂 ，用于治疗，或预防，慢性关节退行性和/或炎性疾病：如类风湿性关节炎。

公开(公告)号：EP2214018A3

公开(公告)日：2011-02-09

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： 本发明涉及用于诱导未分化的哺乳动物细胞分化成成骨细胞的方法，试剂和化合物筛选分析。 本发明因此提供了一种方法，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; 并测量与所述细胞分化有关的化合物 - 多肽特性。 本发明进一步涉及增强骨形成的药物组合物，及其在治疗和/或预防涉及受试者的平均骨密度全身或局部降低的疾病中的用途。 此外，本发明涉及用于体外生产骨组织的方法。

公开(公告)号：EP2267458A2

公开(公告)日：2010-12-29

申请号：EP10174532.1

申请日：2005-04-20

申请人： Galapagos N.V.

发明人： Merchiers, Pascal Gerard ,  Spittaels, Koenraad Frederik Florentina ,  Hoffmann, Marcel

IPC分类号： G01N33/68 ,  G01N33/566

CPC分类号： C12Q1/37 ,  G01N33/566 ,  G01N33/6896 ,  G01N2333/4709 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2800/2821

摘要： A method for identifying compounds that inhibit amyloid-beta precursor protein processing in cells, comprising contacting a test compound with a GPCR polypeptide (GPR12), or fragment thereof, and measuring a compound-GPCR property related to the production of amyloid-beta peptide. Cellular assays of the method measure indicators including second messenger and/or amyloid beta peptide levels. Therapeutic methods, and pharmaceutical compositions including effective amyloid-beta precursor processing-inhibiting amounts of GPCR expression inhibitors, are useful for treating conditions involving cognitive impairment such as Alzheimers Disease.

摘要翻译： 用于鉴定抑制细胞中淀粉样蛋白β前体蛋白加工的化合物的方法，包括使测试化合物与GPCR多肽（GPR12）或其片段接触，并测量与淀粉状蛋白-β肽的产生相关的化合物-GPCR性质。 所述方法的细胞测定测量指标，包括第二信使和/或淀粉样蛋白β肽水平。 包括有效淀粉样蛋白-β前体加工抑制量的GPCR表达抑制剂的治疗方法和药物组合物可用于治疗涉及认知障碍的疾病如阿尔茨海默病。

公开(公告)号：EP2248898A2

公开(公告)日：2010-11-10

申请号：EP10174538.8

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 ,  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哺乳动物细胞分化为成骨细胞的方法，以及用于鉴定诱导未分化哺乳动物细胞分化成成骨细胞的化合物的方法。 此外，本发明提供多核苷酸和载体，以及其用作治疗涉及全身或局部平均骨密度降低的疾病的药物的用途。 此外，本发明提供了用于体外生产骨组织，成骨细胞的方法和用于诊断涉及全身或局部平均骨密度降低或对该病症易感性的病理状态的方法。

公开(公告)号：EP2240768A1

公开(公告)日：2010-10-20

申请号：EP09708266.3

申请日：2009-02-03

申请人： Galapagos N.V.

发明人： FISCHER, David Frederik ,  JANSSEN, Richard Antonius Jozef ,  DE PRIL, Remko ,  VAN STEENHOVEN, Desire Maria Petronella Catharina ,  KWAK, Seung ,  HOWLAND, David S. ,  SIGNER, Ethan

IPC分类号： G01N33/50

CPC分类号： G01N33/5023 ,  G01N2500/04 ,  G01N2800/2835

摘要： The present invention relates to methods and assays for identifying agents capable of inhibiting the mutant huntingtin protein, inhibiting or reducing cell death, in particular cell death associated with polyglutamine-induced protein aggregation, which inhibition is useful in the prevention, amelioration and / or treatment of neurodegenerative diseases, and Huntington's disease more generally. In particular, the present invention provides methods and assays for identifying agents for use in the prevention and / or treatment of Huntingtons disease. The invention provides polypeptide and nucleic acid TARGETs and siRNA sequences based on these TARGETS.

公开(公告)号：EP2162747A2

公开(公告)日：2010-03-17

申请号：EP08774155.9

申请日：2008-06-19

申请人： Galapagos N.V.

发明人： BRYS, Reginald Christophe Xavier ,  VANDEGHINSTE, NickErnest 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.

公开(公告)号：EP2029602A2

公开(公告)日：2009-03-04

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：EP1817411A2

公开(公告)日：2007-08-15

申请号：EP05803408.3

申请日：2005-10-17

申请人： Galapagos N.V.

发明人： BRYS, Reginald ,  VANDEGHINSTE, Nick ,  TOMME, Peter, Herwig, Maria ,  KLAASSEN, Hubertus, Johanus, Matheus

IPC分类号： C12N9/12 ,  C12N9/02 ,  C12N15/11 ,  C07K14/705 ,  G01N33/53 ,  A61K48/00

CPC分类号： G01N33/6887 ,  A61K31/7088 ,  A61K38/00 ,  A61K48/00 ,  C12N7/00 ,  C12N15/1137 ,  C12N15/1138 ,  C12N2310/11 ,  C12N2310/12 ,  C12N2310/14 ,  C12N2710/10343 ,  C12Y304/24007 ,  G01N33/564 ,  G01N2333/9121 ,  G01N2800/102 ,  G01N2800/105

摘要： The application discloses methods for identifying and using compounds that inhibit extra-cellular matrix (ECM) degradation and inflammation, using a polypeptide sequence including SEQ ID NO: 17-127 (hereinafter 'TARGETS') and fragments thereof, expression inhibitory agents such as antisense polynucleotide, a ribozyme, and a small interfering RNA (siRNA), comprising a nucleic acid sequence complementary to, or engineered from, a naturally occurring polynucleotide sequence encoding a polypeptide of SEQ ID NO: 17-127, useful in pharmaceutical compositions comprising said agent, for the treatment, or prevention, of chronic joint degenerat ive and/or inflammatory diseases such as rheumatoid arthritis.