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    METABOLITES AND DERIVATIVES OF AMBRISENTAN
    2.
    发明申请
    METABOLITES AND DERIVATIVES OF AMBRISENTAN 审中-公开
    AMBRISENTAN的代谢产物和衍生物

    公开(公告)号：WO2009017777A3

    公开(公告)日：2009-04-09

    申请号：PCT/US2008009236

    申请日：2008-07-31

    Applicant: GILEAD COLORADO INC ,  ABBOTT GMBH & KG CO ,  MELVIN JR LAWRENCE S ,  ULLRICH MARTINA ,  HEGE HANS-GUENTHER ,  WEYMANN JUERGEN

    Inventor： MELVIN JR LAWRENCE S ,  ULLRICH MARTINA ,  HEGE HANS-GUENTHER ,  WEYMANN JUERGEN

    IPC: C07D239/34 ,  A61K31/505 ,  A61P9/00

    CPC classification number: C07D239/34 ,  C07D403/12 ,  Y10T436/143333 ,  Y10T436/147777

    Abstract: The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R1 is -H or -OCH3; R2 is-H, lower alkyl (e.g. C1-C4 alkyl) or glycosidyl; and R3 and R4 are independently -CH3, -C(O)H or -CH2OR6, wherein R6 is -H or a hydrocarbyl group having 1 to 20 carbon atoms. In some embodiments, compounds of Formula (I) exhibit selective affinity for ETA receptors and serve as endothelin receptor antagonists. In some embodiments, the compounds correspond to metabolites of ambrisentan produced by the enzymatic action of cytochrome P450 or uridine diphosphate glucuronosyl transferase enzymes, for example as elucidated in pre-clinical or clinical studies.

    Abstract translation: 本发明涉及安立生坦的衍生物和代谢物，包括通式（I）的化合物或其盐，水合物，溶剂合物，外消旋物或旋光异构体，其中R 1是-H或-OCH 3; R2是-H，低级烷基（例如C1-C4烷基）或糖苷基; 并且R 3和R 4独立地为-CH 3，-C（O）H或-CH 2 OR 6，其中R 6为-H或具有1至20个碳原子的烃基。 在一些实施方案中，式（I）的化合物对ETA受体显示出选择性亲和力并充当内皮素受体拮抗剂。 在一些实施方案中，所述化合物对应于由细胞色素P450或尿苷二磷酸葡糖醛酸基转移酶的酶促作用产生的安立生坦的代谢物，例如在临床前或临床研究中阐明的。

    METABOLITES AND DERIVATIVES OF AMBRISENTAN
    3.
    发明申请
    METABOLITES AND DERIVATIVES OF AMBRISENTAN 审中-公开
    代谢物的衍生物和衍生物

    公开(公告)号：WO2009017777A2

    公开(公告)日：2009-02-05

    申请号：PCT/US2008/009236

    申请日：2008-07-31

    Applicant: GILEAD COLORADO, INC. ,  ABBOTT GMBH & KG Co. ,  MELVIN, JR., Lawrence S. ,  ULLRICH, Martina ,  HEGE, Hans-guenther ,  WEYMANN, Jürgen

    Inventor： MELVIN, JR., Lawrence S. ,  ULLRICH, Martina ,  HEGE, Hans-guenther ,  WEYMANN, Jürgen

    IPC: C07D239/34 ,  A61K31/505 ,  A61P9/00

    CPC classification number: C07D239/34 ,  C07D403/12 ,  Y10T436/143333 ,  Y10T436/147777

    Abstract: The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R 1 is -H or -OCH 3 ; R 2 is -H, lower alkyl (e.g. C 1 -C 4 alkyl) or glycosidyl; and R 3 and R 4 are independently -CH3, -C(O)H or -CH 2 OR 6 , wherein R 6 is -H or a hydrocarbyl group having 1 to 20 carbon atoms. In some embodiments, compounds of Formula (I) exhibit selective affinity for ET A receptors and serve as endothelin receptor antagonists. In some embodiments, the compounds correspond to metabolites of ambrisentan produced by the enzymatic action of cytochrome P450 or uridine diphosphate glucuronosyl transferase enzymes, for example as elucidated in pre-clinical or clinical studies.

    Abstract translation: 本发明涉及包括通式（I）的化合物或其盐，水合物，溶剂化物，外消旋体或其旋光异构体的其中R1为-H或-OCH3的安立森定的衍生物和代谢物; R2是-H，低级烷基（例如C1-C4烷基）或糖基; 且R 3和R 4独立地为-CH 3，-C（O）H或-CH 2 OR 6，其中R 6为-H或具有1至20个碳原子的烃基。 在一些实施方案中，式（I）化合物对ETA受体表现出选择性亲和力并且用作内皮素受体拮抗剂。 在一些实施方案中，化合物对应于通过细胞色素P450或尿苷二磷酸葡萄糖醛酸转移酶的酶作用产生的安立生坦的代谢物，例如在临床前或临床研究中阐明。

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