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    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
    3.
    发明申请
    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS 审中-公开
    作为磷酸二酯酶抑制剂的苯二酚或苯并二氧杂环己烷化合物

    公开(公告)号：US20150111915A1

    公开(公告)日：2015-04-23

    申请号：US14586681

    申请日：2014-12-30

    Applicant: LEO PHARMA A/S

    Inventor： Simon Feldbaek NIELSEN

    IPC: C07D495/10 ,  C07D493/10

    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。

    BENZODIOXOLE OR BENZODIOXEPINE HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
    5.
    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.

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