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    Substituted acetophenones useful as PDE4 inhibitors
    52.
    发明授权
    Substituted acetophenones useful as PDE4 inhibitors 有权
    用作PDE4抑制剂的取代苯乙酮

    公开(公告)号：US08148537B2

    公开(公告)日：2012-04-03

    申请号：US12520325

    申请日：2007-12-21

    Applicant: Jakob Felding ,  Simon Feldbæk Nielsen

    Inventor： Jakob Felding ,  Simon Feldbæk Nielsen

    IPC: C07D213/46 ,  A61K31/435

    CPC classification number: C07D213/61 ,  C07D413/12 ,  C07D417/12

    Abstract: 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, alkenyl, 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, hydrates, 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.

    Abstract translation: 本发明涉及式（I）化合物： 其中X1，X2，X3，X4和X5彼此独立地表示-CH-或N; 或X3，X4和X5彼此独立地表示-CH-或N，并且X 1和X 2彼此独立地表示C并且形成另外的6元芳环的一部分; R 1表示氢，烷基，烯基，炔基，卤代烷基，羟基烷基或烷基羰基，它们均为任选取代的; R2和R3独立地表示氢，-CH2-C（O）NR-R'，烷基，环烷基，烯基，环烯基，炔基，卤代烷基，羟基烷基，杂链烯基，烷基芳基，烷基烷氧基羰基，烷基羰氧基或烷氧基烷基， ; R 11表示氢，卤素，氰基，氨基，烷氧基或烷基氨基，X 1 -X 5表示-CH-或N，包括N-氧化物，对映体和非对映体; 及其药学上可接受的盐，水合物或溶剂化物。 本发明进一步涉及制备所述化合物，所述化合物用于治疗的方法，包含所述化合物的药物组合物，治疗疾病的方法。 所述化合物的皮肤病，以及所述化合物在制备药物中的用途。

    Cyanoguanidine compounds
    53.
    发明授权
    Cyanoguanidine compounds 有权
    氰基胍化合物

    公开(公告)号：US08053446B2

    公开(公告)日：2011-11-08

    申请号：US11793867

    申请日：2005-12-20

    Applicant: Fredrik Bjorkling ,  Heinz Wilhelm Dannacher

    Inventor： Fredrik Bjorkling ,  Heinz Wilhelm Dannacher

    IPC: C07D401/12 ,  A61K31/44

    CPC classification number: C07D213/75 ,  C07D401/12

    Abstract: Novel pyridyl cyanoguanidine compounds of general formula I (I) wherein R1, X, R2 and R3 are as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neo-plastic diseases.

    Abstract translation: 其中R1，X，R2和R3如本文所定义的通式I（I）的新型吡啶基氰基胍化合物表现出高的抗增殖活性，可用于治疗过度增殖和新生塑料疾病。

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