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    HETEROAROMATIC MODULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA
    13.
    发明申请
    HETEROAROMATIC MODULATORS OF THE RETINOID-RELATED ORPHAN RECEPTOR GAMMA 审中-公开

    公开(公告)号：US20190284177A1

    公开(公告)日：2019-09-19

    申请号：US16317655

    申请日：2017-07-11

    Applicant: LEO PHARMA A/S

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

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

    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
    19.
    发明授权
    Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors 有权
    苯并二氧杂环戊烯或苯并二氧杂环杂环化合物作为磷酸二酯酶抑制剂

    公开(公告)号：US09273064B2

    公开(公告)日：2016-03-01

    申请号：US14586681

    申请日：2014-12-30

    Applicant: LEO PHARMA A/S

    Inventor： Simon Feldbaek Nielsen

    IPC: C07D495/10 ,  C07D493/10 ,  A61K31/4427 ,  A61K31/4433

    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.

    Abstract translation: 通式I的化合物，其中m和n各自独立地为0或1; R1和R2与它们连接的碳原子一起形成包含一个或两个选自氧，硫，-S（O） - 和-S（O）2 - 的杂原子的杂环; R3是-CHF2，-CF3，-OCHF2，-OCF3，-SCHF2或-SCF3; X是键，-CH 2 - 或-NH-; A是任选被一个或多个相同或不同的选自R4的取代基取代的芳基，环烷基，环烯基，芳基烷基，杂芳基，杂芳基烷基，杂环烷基或杂环烯基。 R 4是氢，氨基，硫代，烷基，卤代烷基，羟基烷基，烷氧基，卤代烷氧基，卤素，氧代，硫杂或羟基; 已发现其药学上可接受的盐，水合物或溶剂化物表现出PDE4抑制活性，因此可用于治疗炎性疾病和病症。

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