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    A METHOD OF INHIBITING THE EXPRESSION OF IL-22 IN ACTIVATED T-CELLS
    2.
    发明公开
    A METHOD OF INHIBITING THE EXPRESSION OF IL-22 IN ACTIVATED T-CELLS 审中-公开
    VERFAHREN ZUR HEMMUNG DER EXPRESSION VON IL-22 IN AKTIVIERTEN T-ZELLEN

    公开(公告)号：EP2925364A1

    公开(公告)日：2015-10-07

    申请号：EP13798642.8

    申请日：2013-11-28

    申请人： Leo Pharma A/S

    发明人： LOVATO, Paola

    IPC分类号： A61K45/06 ,  A61K31/44 ,  A61K31/443 ,  A61K31/593 ,  A61P29/00 ,  A61P17/06

    CPC分类号： A61K31/59 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/593 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to a method of inhibiting the upregulation of the expression of the proinflammatory cytokine interleukin-22 (IL-22) in activated and differentiated human T-cells, said upregulation being induced by administration of a therapeutically effective amount of a phosphodiesterase 4 (PDE4) inhibitor. The method comprises administering, either sequentially to or simultaneously with the administration of the PDE4 inhibitor, a vitamin D receptor agonist in an amount sufficient to inhibit the upregulation of IL-22 expression.

    摘要翻译： 本发明涉及抑制活化和分化的人T细胞中促炎细胞因子白细胞介素-22（IL-22）表达上调的方法，所述上调是通过施用治疗有效量的磷酸二酯酶4 （PDE4）抑制剂。 该方法包括向PDE4抑制剂的依次施用或同时施用足以抑制IL-22表达上调的量3）的维生素D受体激动剂。

    SUBSTITUTED ACETOPHENONES USEFUL AS PDE4 INHIBITORS
    7.
    发明授权
    SUBSTITUTED ACETOPHENONES USEFUL AS PDE4 INHIBITORS 有权
    作为PDE4抑制剂的合适的取代的苯乙酮

    公开(公告)号：EP2125736B1

    公开(公告)日：2011-03-30

    申请号：EP07846434.4

    申请日：2007-12-21

    申请人： LEO PHARMA A/S

    发明人： FELDING, Jakob ,  NIELSEN, Simon, Feldbæk

    IPC分类号： C07D213/61 ,  C07D413/12 ,  C07D417/12 ,  A61K31/44 ,  A61K31/4427 ,  A61P25/00 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00

    CPC分类号： C07D213/61 ,  C07D413/12 ,  C07D417/12

    摘要： The present invention relates to a compound according to formula: (I); wherein X1, X2, X3, X4 and X5 independently of each other represent -CH- or N; or X3, X4 and X5 independently of each other represent -CH- or N, and Xi and X2 independently of each other represent C and form part of an additional 6- membered aromatic ring; R1 represents hydrogen, alkyl, alke nyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, -CH2-C(O)NR-R', alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, alkylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent -CH- or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hyd rates, or solvates thereof. The invention relates further to processes for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.

    SUBSTITUTED ACETOPHENONES USEFUL AS PDE4 INHIBITORS
    8.
    发明公开
    SUBSTITUTED ACETOPHENONES USEFUL AS PDE4 INHIBITORS 有权
    作为PDE4抑制剂的合适的取代的苯乙酮

    公开(公告)号：EP2125736A1

    公开(公告)日：2009-12-02

    申请号：EP07846434.4

    申请日：2007-12-21

    申请人： LEO PHARMA A/S

    发明人： FELDING, Jakob ,  NIELSEN, Simon, Feldbæk

    IPC分类号： C07D213/61 ,  C07D413/12 ,  C07D417/12 ,  A61K31/44 ,  A61K31/4427 ,  A61P25/00 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00

    CPC分类号： C07D213/61 ,  C07D413/12 ,  C07D417/12

    摘要： The present invention relates to a compound according to formula: (I); wherein X1, X2, X3, X4 and X5 independently of each other represent -CH- or N; or X3, X4 and X5 independently of each other represent -CH- or N, and Xi and X2 independently of each other represent C and form part of an additional 6- membered aromatic ring; R1 represents hydrogen, alkyl, alke nyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, -CH2-C(O)NR-R', alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, alkylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent -CH- or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hyd rates, or solvates thereof. The invention relates further to processes for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.

    CYANOGUANIDINE PRODUGS
    10.
    发明公开
    CYANOGUANIDINE PRODUGS 审中-公开
    氰基胍产品

    公开(公告)号：EP1507759A1

    公开(公告)日：2005-02-23

    申请号：EP03720293.4

    申请日：2003-05-15

    申请人： LEO PHARMA A/S

    发明人： BINDERUP, Ernst, Torndal

    IPC分类号： C07D213/02 ,  A61K31/4425 ,  A61P35/00

    CPC分类号： C07D213/75

    摘要： Pyridyl cyanoguanidine compounds according to formula I wherein A, R1, R2, R5, R6, X1, X2, X3, X4, Y1, Y2, Y3, Y4 and n are as indicated in the description are useful as produgs in human and veterinary therapy of poliferative disease such as cancers.

    摘要翻译： 其中A，R 1，R 2，R 5，R 6，X 1，X 2，X 3，X 4，Y 1，Y 2，Y 3，Y 4和n如说明书中所示的吡啶基氰基胍化合物可用作人和兽医疗法 诸如癌症之类的增殖性疾病。