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    MACROLIDES AND THEIR USE
    5.
    发明申请
    MACROLIDES AND THEIR USE 有权
    MACROLIDES及其使用

    公开(公告)号：US20110053876A1

    公开(公告)日：2011-03-03

    申请号：US12864921

    申请日：2009-02-09

    申请人： Johannes Laurenz Kellenberger ,  Jürg Dreier ,  Stefan Bernhard Reinelt

    发明人： Johannes Laurenz Kellenberger ,  Jürg Dreier ,  Stefan Bernhard Reinelt

    IPC分类号： A61K31/7076 ,  C07H17/08 ,  A61K31/706 ,  A61P29/00 ,  A61P37/08 ,  A61P35/00 ,  A61P11/06 ,  A61P17/06 ,  A61P25/00 ,  A61P11/00

    CPC分类号： C07H17/08

    摘要： The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with anti-inflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.

    摘要翻译： 本发明涉及式（I）的大环内酯类化合物，所述化合物作为药物的用途，特别是用于治疗或预防炎性和过敏性疾病，含有所述化合物的药物组合物及其制备方法。 本发明特别涉及具有主要通过抑制磷酸二酯酶4（PDE4）介导的抗炎活性的大环内酯类化合物，其使它们可用于治疗和/或预防炎性和过敏性疾病如慢性阻塞性肺病（COPD），哮喘 类风湿性关节炎，特应性皮炎或炎症性肠病或增殖性疾病如癌症。

    Macrolides Useful Against Inflammatory and Allergic Diseases
    6.
    发明申请
    Macrolides Useful Against Inflammatory and Allergic Diseases 有权

    公开(公告)号：US20100120706A1

    公开(公告)日：2010-05-13

    申请号：US12375963

    申请日：2007-08-08

    申请人： Johannes Laurenz Kellenberger ,  Jürg Dreier ,  Stefan Bernhard Reinelt

    发明人： Johannes Laurenz Kellenberger ,  Jürg Dreier ,  Stefan Bernhard Reinelt

    IPC分类号： A61K31/7076 ,  C07H17/08 ,  A61P11/00

    CPC分类号： C07H17/08

    摘要： Macrolide compounds of formula I: with PDF4 inhibiting activity are described, wherein R1 is a residue —Y—X-Q; Y is S, SO or SO2; X is a bond or a linear group consisting of hydrogen atoms and with up to 9 atoms selected from C, N, O and/or S, of which up to 2 atoms can be N and one atom can be O or S, one carbon atom can appear as a CO group and the sulphur atom can appear as an SO2 group and two adjacent C atoms can be present as —CH═CH— or —C≡C— and which group X is unsubstituted or is substituted with —COO—W or —CONH—W; Q is a residue —V-A1-L-A2-W or, if X does not represent a bond, may also be —NR6R7; V is a divalent aromatic or heterocyclic group; W is aryl or heterocyclyl; or in a group —V-A1-L-A2-W, wherein at least one of the groups A1; L or A2 is present, can also be a monovalent substituted or unsubstituted, saturated or unsaturated linear group with up to 5 atoms consisting of C, N, O and/or S of which one carbon can appear as a CO group one sulphur atom can appear as an SO2 group, A1, A2 are independently of each other either absent or a C1-C4alkylene group; L is —O—, —S—, —SO2-, —NH—, —CO—, —(CO)O—, —O(OC)—, —(CO)NH—, —NH(CO)—, —(SO2)NH—, —HN(SO2)—, —HN(CO)NH—, —O(CO)NH—, —NH(CO)O—, or can also be absent if A1 and/or A2 are present; R2 is hydrogen and R3 is and OR4 or R2, R3 taken together form a C═O group; R4 is hydrogen or an saturated or unsaturated aliphatic group with 1 to 6 carbon atoms; R6, R7 are independently selected from aryl; aralkyl; heterocyclyl and heterocyclylalkyl; and one of R6 and R7 can also be a group -L-W; and * indicates a chiral centre which is in the (R) or (S) form.