N-(3-acyl-2-hydroxyalkyl) cycloalkyl amide derivatives
    4.
    发明公开
    N-(3-acyl-2-hydroxyalkyl) cycloalkyl amide derivatives 有权
    N-(3-酰基-2-羟基烷基)环烷基酰胺衍生物

    公开(公告)号:EP1619189A1

    公开(公告)日:2006-01-25

    申请号:EP05018359.9

    申请日:1999-11-12

    IPC分类号: C07D295/205 A61K31/5375

    摘要: Alcohol derivatives represented by the general formula (IV);

    wherein:

    R 1 represents a substituted C 1 -C 12 alkyl group; a substituted C 2 -C 6 alkenyl group; a substituted amino group; a substituted C 1 -C 6 alkoxy group; a substituted C 1 -C 6 alkylthio group; a substituted carbamoyl group; a substituted sulfonamide group; or a substituted amide group;
    the ring A represents a saturated cyclic alkyl group with 5 to 7 carbon atoms;
    R 2 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group;
    R 3 represents a hydrogen atom, a group represented by the general formula R 4 O- ; or a group represented by the general formula R 5 (R 6 )N-wherein R 4 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group; R 5 and R 6 may be the same or different and each represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted heterocyclic group,

    The cyclic carboxylic acid derivatives of formula (IV) are useful for the synthesis of cyclic amide derivatives useful as cathepsin K inhibitors.

    摘要翻译: 由通式(IV)表示的醇衍生物; 其中:R 1表示取代的C 1 -C 12烷基; 取代的C 2 -C 6烯基; 取代的氨基; 取代的C 1 -C 6烷氧基; 取代的C 1 -C 6烷硫基; 取代的氨基甲酰基; 取代的磺酰胺基团; 或取代的酰胺基团; 环A表示具有5至7个碳原子的饱和环状烷基; R2表示氢原子,取代或未取代的烷基,取代或未取代的芳烃基或取代或未取代的杂环基; R3表示氢原子,由通式R4O-表示的基团; 或由通式R5(R6)N-表示的基团,其中R4表示氢原子,取代或未取代的烷基,取代或未取代的芳族烃基或取代或未取代的杂环基; R5和R6可以相同或不同,并且各自表示氢原子,取代或未取代的烷基,取代或未取代的芳族烃基或取代或未取代的杂环基。式(IV)的环状羧酸衍生物是有用的 用于合成可用作组织蛋白酶K抑制剂的环酰胺衍生物。