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    Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them
    7.
    发明公开
    Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them 审中-公开
    环氧羧基芥酸酰胺，叠氮和氨基烷醇洗涤剂Verfahren zur Herstellung von Alpha-Ketoamiden damit

    公开(公告)号：EP2289888A2

    公开(公告)日：2011-03-02

    申请号：EP10011261.4

    申请日：2001-06-29

    申请人： SEIKAGAKU CORPORATION

    发明人： Kobayashi, Nubuo ,  Koji, Tsuneo ,  Fujita, Takashi ,  Nishimura, Tomofumi ,  Hosoda, Akihiko

    IPC分类号： C07D303/48 ,  C07D295/20 ,  C07D317/66 ,  C07D207/16 ,  C07C247/12 ,  C07C237/22 ,  C07C271/22 ,  C07C231/12 ,  C07C231/16

    CPC分类号： C07D295/215 ,  C07C231/12 ,  C07C231/16 ,  C07C237/22 ,  C07C247/12 ,  C07C271/22 ,  C07C2601/14 ,  C07D207/16 ,  C07D295/18 ,  C07D303/46 ,  C07D303/48 ,  C07D317/66 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12

    摘要： The present invention is to provide manufacturing intermediates which can be led to useful α-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide amino alcohol compounds represented by the following formula:

    wherein R 1 and R 2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R 6 -O- or R 7 -N(R 8 )-; where R 6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 7 and R 8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R 4 and R 5 represent the same groups as R 7 and R 8 , respectively, and R 9 and R 5 optionally form a ring together; and X represents -O- or -N(R 9 )-, where R 9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R 4 or R 5 ,
    and processes for preparing α-keto amide compound using the same.

    摘要翻译： 本发明提供制造中间体，其可以被极端经济和立体选择性地引入具有蛋白酶抑制活性的有用的± - 酮酰胺化合物，并提供由下式表示的氨基醇化合物：其中R 1和R 2各自表示烷基 ，烯基，芳族烃基或杂环基; R 3表示烷基，烯基，芳香族烃基，杂环基，R 6 -O-或R 7 -N（R 8） - ; 其中R 6表示烷基，烯基，芳族烃基或杂环基; R 7和R 8各自表示氢原子，烷基，烯基，芳香族烃基或杂环基，R 4和R 5分别表示与R 7和R 8相同的基团，R 9和R 5任选地 一起形成一个戒指 并且X表示-O-或-N（R 9） - ，其中R 9表示氢原子或烷基，X任选地与R 4或R 5一起形成环，以及使用 相同。

    Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them
    9.
    发明公开
    Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them 审中-公开
    环氧羧基芥酸酰胺，叠氮和氨基烷醇洗涤剂Verfahren zur Herstellung von Alpha-Ketoamiden damit

    公开(公告)号：EP2289888A3

    公开(公告)日：2011-07-13

    申请号：EP10011261.4

    申请日：2001-06-29

    申请人： SEIKAGAKU CORPORATION

    发明人： Kobayashi, Nubuo ,  Koji, Tsuneo ,  Fujita, Takashi ,  Nishimura, Tomofumi ,  Hosoda, Akihiko

    IPC分类号： C07D303/48 ,  C07D295/20 ,  C07D317/66 ,  C07D207/16 ,  C07C247/12 ,  C07C237/22 ,  C07C271/22 ,  C07C231/12 ,  C07C231/16

    CPC分类号： C07D295/215 ,  C07C231/12 ,  C07C231/16 ,  C07C237/22 ,  C07C247/12 ,  C07C271/22 ,  C07C2601/14 ,  C07D207/16 ,  C07D295/18 ,  C07D303/46 ,  C07D303/48 ,  C07D317/66 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12

    摘要： The present invention is to provide manufacturing intermediates which can be led to useful α-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide amino alcohol compounds represented by the following formula:

    wherein R 1 and R 2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R 6 -O- or R 7 -N(R 8 )-; where R 6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 7 and R 8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R 4 and R 5 represent the same groups as R 7 and R 8 , respectively, and R 9 and R 5 optionally form a ring together; and X represents -O- or -N(R 9 )-, where R 9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R 4 or R 5 ,
    and processes for preparing α-keto amide compound using the same.

    摘要翻译： 本发明提供制造中间体，其可以被极端经济和立体选择性地引入具有蛋白酶抑制活性的有用的α-酮酰胺化合物，并提供由下式表示的环氧羧酰胺化合物，叠氮化合物和氨基醇化合物： CHEM> 其中R 1和R 2各自表示烷基，烯基，芳族烃基或杂环基; R 3表示烷基，烯基，芳族烃基，杂环基，R 6 -O-或R 7 -N（R 8） - ; 其中R 6表示烷基，烯基，芳族烃基或杂环基; R 7和R 8各自表示氢原子，烷基，链烯基，芳香族烃基或杂环基，R 4和R 5表示与R 7和R 7相同的基团， 8>，R 4和R 5任选地形成环; 并且X表示-O-或-N（R 9） - ，其中R 9表示氢原子或烷基，X任选地与R 4或R 5一起形成环，并且 用相同的方法制备α-酮酰胺化合物。

    N-(3-acyl-2-hydroxyalkyl) cycloalkyl amide derivatives
    10.
    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

    申请人： SEIKAGAKU CORPORATION

    发明人： Hosoda, Akihiko ,  Kobayashi, Nobuo ,  Tanabe, Naoko ,  Koji, Tsuneo ,  Shibata, Masahiro ,  Sekine, Akihiro ,  Dozen, Masaharu

    IPC分类号： C07D295/205 ,  A61K31/5375

    CPC分类号： C07D213/71 ,  C07C271/24 ,  C07C275/26 ,  C07C311/20 ,  C07C311/29 ,  C07C311/43 ,  C07C311/46 ,  C07C317/44 ,  C07C323/60 ,  C07C2601/14 ,  C07D211/46 ,  C07D211/58 ,  C07D213/75 ,  C07D223/10 ,  C07D223/12 ,  C07D231/40 ,  C07D243/08 ,  C07D277/48 ,  C07D277/68 ,  C07D277/82 ,  C07D295/215 ,  C07D307/14 ,  C07D307/33 ,  C07D307/52 ,  C07D309/20 ,  C07D317/28 ,  C07D317/46 ,  C07D317/58 ,  C07D317/66 ,  C07D317/68 ,  C07D317/72 ,  C07D319/06

    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。