公开(公告)号：US20150330968A1

公开(公告)日：2015-11-19

申请号：US14367565

申请日：2012-12-20

申请人： Reginald Christophe Xavier BRYS ,  Sonia DUPONT

发明人： Reginald Christophe Xavier BRYS ,  Sonia DUPONT

IPC分类号： G01N33/50 ,  A61K49/00

CPC分类号： G01N33/5029 ,  A61K49/0008 ,  G01N2333/726

摘要： The present invention relates to methods and assays for identifying agents capable of modulating GPR84 activity in cells, in particular agents that inhibit GPR84-agonist stimulated chemotaxis. Inhibition of GPR84-agonist stimulated chemotaxis is useful in the prevention and/or treatment of inflammatory conditions. In particular, the present invention provides methods and assays for identifying agents for use in 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 and/or diseases involving impairment of immune cell functions.

摘要翻译： 本发明涉及用于鉴定能够调节细胞中GPR84活性的试剂的方法和测定法，特别是抑制GPR84-激动剂刺激的趋化性的药物。 GPR84-激动剂刺激趋化性的抑制可用于预防和/或治疗炎性病症。 特别地，本发明提供了用于鉴定用于预防和/或治疗炎性病症（例如炎性肠病（IBD）），类风湿性关节炎，血管炎，肺部疾病（例如慢性阻塞性肺病（COPD） ）和肺间质疾病（例如特发性肺纤维化（IPF）），神经炎症状况，感染性疾病，自身免疫疾病和/或涉及免疫细胞功能损伤的疾病。

公开(公告)号：US08637257B2

公开(公告)日：2014-01-28

申请号：US12214787

申请日：2008-06-19

申请人： Reginald Christophe Xavier Brys ,  Nick Ernest René Vandeghinste

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

IPC分类号： G01N33/53 ,  C12Q1/00 ,  C07H21/00

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能够抑制参与调节破骨细胞发生过程的蛋白质的表达或活性的试剂的方法，所述抑制剂可用于预防和/或治疗骨和关节变性疾病和涉及异常活动或分化的疾病 破骨细胞。 特别地，本发明提供用于鉴定用于预防和/或治疗类风湿性关节炎的药剂的方法。

公开(公告)号：US20090117107A1

公开(公告)日：2009-05-07

申请号：US12214787

申请日：2008-06-19

申请人： Reginald Christophe Xavier Brys ,  Nick Ernest Rene Vandeghinste

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

IPC分类号： A61K39/395 ,  G01N33/566 ,  C40B30/04 ,  C07H21/04 ,  C07H21/02 ,  A61P19/10 ,  C12N15/869 ,  A61K31/711 ,  C12N15/86 ,  C12N15/867 ,  A61P19/00 ,  C12N15/861 ,  A61K31/7105 ,  A61K35/76

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能够抑制参与调节破骨细胞发生过程的蛋白质的表达或活性的试剂的方法，所述抑制剂可用于预防和/或治疗骨和关节变性疾病和涉及异常活动或分化的疾病 破骨细胞。 特别地，本发明提供用于鉴定用于预防和/或治疗类风湿性关节炎的药剂的方法。

公开(公告)号：US20140200258A1

公开(公告)日：2014-07-17

申请号：US14162908

申请日：2014-01-24

申请人： Reginald Christophe Xavier Brys ,  Luc Nelles ,  Nick Ernest Rene Vandeghinste ,  Blandine Mille-Baker ,  Michela Angela Tessari

发明人： Reginald Christophe Xavier Brys ,  Luc Nelles ,  Nick Ernest Rene Vandeghinste ,  Blandine Mille-Baker ,  Michela Angela Tessari

IPC分类号： G01N33/50 ,  C12N15/113

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.

摘要翻译： 本发明涉及药物研究，软骨生理学和涉及软骨组织退化的疾病领域。 更具体地，本发明涉及用于鉴定抑制软骨细胞分解代谢过程并降低软骨和/或ECM降解的化合物的方法和手段。 本发明还涉及可用于治疗骨关节炎的化合物。 本发明还涉及靶的调节，其导致ECM和/或软骨的降解降低并减少炎症。 此外，本发明涉及用于治疗以ECM和/或软骨和炎症降解为特征的病症的组合物和方法。

公开(公告)号：US08663930B2

公开(公告)日：2014-03-04

申请号：US13262634

申请日：2010-04-01

申请人： Reginald Christophe Xavier Brys ,  Luc Nelles ,  Nick Ernest Rene Vandeghinste ,  Blandine Mille-Baker ,  Michela Angela Tessari

发明人： Reginald Christophe Xavier Brys ,  Luc Nelles ,  Nick Ernest Rene Vandeghinste ,  Blandine Mille-Baker ,  Michela Angela Tessari

IPC分类号： G01N33/53

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.

摘要翻译： 本发明涉及药物研究，软骨生理学和涉及软骨组织退化的疾病领域。 更具体地，本发明涉及用于鉴定抑制软骨细胞分解代谢过程并降低软骨和/或ECM降解的化合物的方法和手段。 本发明还涉及可用于治疗骨关节炎的化合物。 本发明还涉及靶的调节，其导致ECM和/或软骨的降解降低并减少炎症。 此外，本发明涉及用于治疗以ECM和/或软骨和炎症降解为特征的病症的组合物和方法。

公开(公告)号：US20130303515A1

公开(公告)日：2013-11-14

申请号：US13980798

申请日：2012-01-10

申请人： Laurent Raymond Maurice Sanière ,  Mathieu Rafaël Pizzonero ,  Nicolas Triballeau ,  Nick Ernest René Vandeghinste ,  Steve Irma Joel De Vos ,  Reginald Christophe Xavier Brys ,  Christelle Dominique Bénédicte Pourbaix-L'ebraly

发明人： Laurent Raymond Maurice Sanière ,  Mathieu Rafaël Pizzonero ,  Nicolas Triballeau ,  Nick Ernest René Vandeghinste ,  Steve Irma Joel De Vos ,  Reginald Christophe Xavier Brys ,  Christelle Dominique Bénédicte Pourbaix-L'ebraly

IPC分类号： C07D205/04 ,  C07D409/06 ,  C07D405/06 ,  C07D413/06 ,  A61K31/422 ,  A61K31/5377 ,  C07D403/12 ,  A61K31/4025 ,  A61K31/41 ,  C07D413/12 ,  A61K31/4245 ,  A61K31/4155 ,  A61K31/404 ,  C07D417/12 ,  C07D471/04 ,  A61K45/06 ,  A61K31/496 ,  A61K31/437 ,  A61K31/428 ,  A61K31/397

CPC分类号： C07D471/04 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D205/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： Compounds are disclosed that have a formula represented by the following: These compounds 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, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.

摘要翻译： 公开了具有下列化学式的化合物：这些化合物可以制备为药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括作为非限制性实例的炎症 疾病，感染性疾病，自身免疫疾病，涉及免疫细胞功能受损的疾病，心脏代谢疾病和/或增殖性疾病。

公开(公告)号：US20110218178A1

公开(公告)日：2011-09-08

申请号：US12970659

申请日：2010-12-16

申请人： Martin James Inglis Andrews ,  Paul Edwards ,  Reginald Christophe Xavier Brys ,  Philip Huxley ,  Wolfgang Schmidt ,  Veronique Birault ,  Mark Stuart Chambers ,  Clifford John Harris ,  Angus Macleod ,  Kim Louise Hirst ,  Juha Andrew Clase ,  Gregory Bar

发明人： Martin James Inglis Andrews ,  Paul Edwards ,  Reginald Christophe Xavier Brys ,  Philip Huxley ,  Wolfgang Schmidt ,  Veronique Birault ,  Mark Stuart Chambers ,  Clifford John Harris ,  Angus Macleod ,  Kim Louise Hirst ,  Juha Andrew Clase ,  Gregory Bar

IPC分类号： A61K31/635 ,  C07D487/04 ,  A61K31/4985 ,  C07D413/14 ,  A61K31/5377 ,  A61P19/02 ,  A61P29/00

CPC分类号： C07D487/04

摘要： Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula 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.

摘要翻译： 公开了具有下列表示的式的新型咪唑并[1,2-a]吡嗪化合物：该化合物可以制备为药物组合物，并且可用于预防和治疗包括人在内的哺乳动物中的多种病症， 包括作为非限制性实例的关节炎，炎症等。

公开(公告)号：US20140155461A1

公开(公告)日：2014-06-05

申请号：US14106951

申请日：2013-12-16

申请人： Reginald Christophe Xavier Brys ,  Nick Ernest Rene Vandeghinste

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

IPC分类号： G01N33/53 ,  A61K31/7088 ,  A61K45/06 ,  A61K31/713

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能够抑制参与调节破骨细胞发生过程的蛋白质的表达或活性的试剂的方法，所述抑制剂可用于预防和/或治疗骨和关节变性疾病和涉及异常活动或分化的疾病 破骨细胞。 特别地，本发明提供用于鉴定用于预防和/或治疗类风湿性关节炎的药剂的方法。

公开(公告)号：US20120027766A1

公开(公告)日：2012-02-02

申请号：US13262634

申请日：2010-04-01

申请人： Reginald Christophe Xavier Brys ,  Luc Nelles ,  Nick Ernest Rene Vandeghinste ,  Blandine Mille-Baker ,  Michela Angela Tessari

发明人： Reginald Christophe Xavier Brys ,  Luc Nelles ,  Nick Ernest Rene Vandeghinste ,  Blandine Mille-Baker ,  Michela Angela Tessari

IPC分类号： A61K39/395 ,  A61K31/711 ,  A61K38/00 ,  C40B30/04 ,  A61K31/7105

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.

摘要翻译： 本发明涉及药物研究，软骨生理学和涉及软骨组织退化的疾病领域。 更具体地，本发明涉及用于鉴定抑制软骨细胞分解代谢过程并降低软骨和/或ECM降解的化合物的方法和手段。 本发明还涉及可用于治疗骨关节炎的化合物。 本发明还涉及靶的调节，其导致ECM和/或软骨的降解降低并减少炎症。 此外，本发明涉及用于治疗以ECM和/或软骨和炎症降解为特征的病症的组合物和方法。

公开(公告)号：US20160296529A1

公开(公告)日：2016-10-13

申请号：US15069130

申请日：2016-03-14

申请人： Gerben Albert Eleutherius van't Klooster ,  Florence Sylvie Namour ,  Reginald Christophe Xavier Brys ,  Luc Juliaan Corina van Rompaey

发明人： Gerben Albert Eleutherius van't Klooster ,  Florence Sylvie Namour ,  Reginald Christophe Xavier Brys ,  Luc Juliaan Corina van Rompaey

IPC分类号： A61K31/541 ,  A61K45/06

CPC分类号： A61K31/541 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

摘要： The present invention relates to the compound according to Formula I, and to its use in medicine, in particular in the treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound inhibits JAK a family of tyrosine kinases, and more particularly JAK1. The present invention also provides pharmaceutical compositions comprising the compound, methods for the prophylaxis and/or treatment of diseases involving inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound.