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    Heteroaromatic modulators of the retinoid-related orphan receptor gamma
    61.
    发明授权
    Heteroaromatic modulators of the retinoid-related orphan receptor gamma 有权

    公开(公告)号：US10934282B2

    公开(公告)日：2021-03-02

    申请号：US16874961

    申请日：2020-05-15

    Applicant: LEO PHARMA A/S

    Inventor： Alan Stuart Jessiman ,  Patrick Stephen Johnson ,  Kristoffer Maansson ,  Morten Dahl Sørensen

    IPC: C07D413/14 ,  C07D413/12 ,  C07D417/14 ,  C07D241/04

    Abstract: The present invention relates to a compound according to general formula (I) wherein X represents N or CH; R1 is —CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C3-C7)cycloalkyl(C1-C4)alkyl, (3-7 membered)heterocycloalkyl-(C1-C4)alkyl or (5-6 membered)heteroaryl-(C1-C4)alkyl; R2 is halogen, cyano, (C1-C4)alkyl or (C3-C7)cycloalkyl; R3 is halogen, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl or (C3-C7)cycloalkyl; R4 is (C1-C4)alkyl or (C1-C4)haloalkyl; R5 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or —ORa. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds.

    HETEROAROMATIC MDOULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA
    62.
    发明申请
    HETEROAROMATIC MDOULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA 审中-公开

    公开(公告)号：US20200291010A1

    公开(公告)日：2020-09-17

    申请号：US16874961

    申请日：2020-05-15

    Applicant: LEO PHARMA A/S

    Inventor： Alan Stuart JESSIMAN ,  Patrick Stephen JOHNSON ,  Kristoffer MAANSSON ,  Morten Dahl SØRENSEN

    IPC: C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D241/04

    Abstract: The present invention relates to a compound according to general formula (I) wherein X represents N or CH; R1 is —CN, (C1-C6)alkyl, (C3-C7)cycloalkyl, (3-7 membered)heterocycloalkyl, (5-6 membered)heteroaryl, (C3-C7)cycloalkyl(C1-C4)alkyl, (3-7 membered)heterocycloalkyl-(C1-C4)alkyl or (5-6 membered)heteroaryl-(C1-C4)alkyl; R2 is halogen, cyano, (C1-C4)alkyl or (C3-C7)cycloalkyl; R3 is halogen, cyano, (C1-C4)alkyl, (C1-C4)haloalkyl or (C3-C7)cycloalkyl; R4 is (C1-C4)alkyl or (C1-C4)haloalkyl; R5 is (C1-C6)alkyl, (C3-C7)cycloalkyl, (C1-C6)alkyl-(C3-C7)cycloalkyl, (C3-C7)cycloalkyl-(C1-C6)alkyl, (3-7 membered)heterocycloalkyl, phenyl, (5-6 membered)heteroaryl or —ORa. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds and to intermediates for preparation of said compounds.

    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
    65.
    发明申请
    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS 审中-公开

    公开(公告)号：US20160022657A1

    公开(公告)日：2016-01-28

    申请号：US14872487

    申请日：2015-10-01

    Applicant: LEO PHARMA A/S

    Inventor： Simon Feldbaek NIELSEN

    IPC: A61K31/4436 ,  A61K31/4433 ,  A61K9/00 ,  A61K31/443

    CPC classification number: C07D495/10 ,  A61K9/0053 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  C07D493/10

    Abstract: Compounds of the general formula I wherein each of m and n is independently 0 or 1; R1 and R2, together with the carbon atom to which they are attached, form a heterocyclic ring comprising one or two heteroatoms selected from oxygen, sulfur, —S(O)— and —S(O)2—; R3 is —CHF2, —CF3, —OCHF2, —OCF3, —SCHF2 or —SCF3; X is a bond, —CH2—, or —NH—; A is aryl, cycloalkyl, cycloalkenyl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycloalkyl or heterocycloalkenyl, optionally substituted with one or more, same or different substituents selected from R4; and R4 is hydrogen, amino, thioxo, alkyl, haloalkyl, hydroxyalkyl, alkoxy, haloalkoxy, halogen, oxo, thia, or hydroxy; or pharmaceutically acceptable salts, hydrates or solvates thereof, have been found to exhibit PDE4 inhibiting activity, and may therefore be useful in the treatment of inflammatory diseases and disorders.

    A METHOD OF INHIBITING THE EXPRESSION OF IL-22 IN ACTIVATED T-CELLS
    66.
    发明申请
    A METHOD OF INHIBITING THE EXPRESSION OF IL-22 IN ACTIVATED T-CELLS 有权
    抑制活化T细胞中IL-22表达的方法

    公开(公告)号：US20150297616A1

    公开(公告)日：2015-10-22

    申请号：US14648480

    申请日：2013-11-28

    Applicant: LEO PHARMA A/S

    Inventor： Paola LOVATO

    IPC: A61K31/59 ,  A61K31/44 ,  A61K45/06

    CPC classification number: A61K31/59 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/593 ,  A61K45/06 ,  A61K2300/00

    Abstract: 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 3) sufficient to inhibit the upregulation of IL-22 expression.

    Abstract translation: 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。

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