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292 条记录 (耗时 0.022 秒)

    Process for the preparation of 5-substituted-1-azabicyclo (3.3.0) octanes
    43.
    发明公开
    Process for the preparation of 5-substituted-1-azabicyclo (3.3.0) octanes 失效
    一种制备5-取代的-1-氮杂双环（3.3.0）辛烷过程

    公开(公告)号：EP0703233A3

    公开(公告)日：1996-09-25

    申请号：EP95111702.7

    申请日：1995-07-25

    申请人： SANWA KAGAKU KENKYUSHO CO., LTD.

    发明人： Oka, Mitsuru, c/o Sanwa Kagaku Kenkyusho Co., Ltd. ,  Suzuki, Tomoo, c/o Sanwa Kagaku Kenkyusho Co.,Ltd. ,  Baba, Yutaka, c/o Sanwa Kagaku Kenkyusho Co.,Ltd.

    IPC分类号： C07D487/02

    CPC分类号： C07D487/04

    摘要： There is disclosed a process for the preparation of 5-substituted-1-azabicyclo[3.3.0]octanes of the Formula

       wherein R¹ is a cyano radical or group of -CO₂R³, in which R³ is a lower alkyl group.
    The derivative is prepared by reacting 1,7-disubstituted-4-heptanone of the Formula

       wherein X is a chlorine, bromine or iodine atom, or a group of -OSO₂R, in which R is a methyl, tolyl or tri-fuloromethyl radical,
    with a substituted acetic acid derivative of the Formula
            R¹CH₂CO₂Y
       wherein R¹ has the meaning as referred to; and Y is a hydrogen, sodium or potassium atom, or -NH₄,
    an alkali metal salt or ammonium salt of the derivative, in the presence of ammonia. Among the 5-substituted-1-azabicyclo[3.3.0]octanes, 5-cyanomethyl-1-azabicyclo[3.3.0]octane can be converted into 5-(2-aminoethyl)-1-azabicyclo[3.3.0]octane through a catalystic reduction which is carried out in atmospheric pressure, in alkali condition, and in the presence of Raney nickel.

    Process for the preparation of 5-substituted-1-azabicyclo (3.3.0) octanes
    44.
    发明公开
    Process for the preparation of 5-substituted-1-azabicyclo (3.3.0) octanes 失效
    制备5-取代-1-氮杂双环（3.3.0）辛烷的方法

    公开(公告)号：EP0703233A2

    公开(公告)日：1996-03-27

    申请号：EP95111702.7

    申请日：1995-07-25

    申请人： SANWA KAGAKU KENKYUSHO CO., LTD.

    发明人： Oka, Mitsuru, c/o Sanwa Kagaku Kenkyusho Co., Ltd. ,  Suzuki, Tomoo, c/o Sanwa Kagaku Kenkyusho Co.,Ltd. ,  Baba, Yutaka, c/o Sanwa Kagaku Kenkyusho Co.,Ltd.

    IPC分类号： C07D487/02

    CPC分类号： C07D487/04

    摘要： There is disclosed a process for the preparation of 5-substituted-1-azabicyclo[3.3.0]octanes of the Formula

       wherein R¹ is a cyano radical or group of -CO₂R³, in which R³ is a lower alkyl group.
    The derivative is prepared by reacting 1,7-disubstituted-4-heptanone of the Formula

       wherein X is a chlorine, bromine or iodine atom, or a group of -OSO₂R, in which R is a methyl, tolyl or tri-fuloromethyl radical,
    with a substituted acetic acid derivative of the Formula

            R¹CH₂CO₂Y


       wherein R¹ has the meaning as referred to; and Y is a hydrogen, sodium or potassium atom, or -NH₄,
    an alkali metal salt or ammonium salt of the derivative, in the presence of ammonia. Among the 5-substituted-1-azabicyclo[3.3.0]octanes, 5-cyanomethyl-1-azabicyclo[3.3.0]octane can be converted into 5-(2-aminoethyl)-1-azabicyclo[3.3.0]octane through a catalystic reduction which is carried out in atmospheric pressure, in alkali condition, and in the presence of Raney nickel.

    摘要翻译： 公开了一种制备下式的5-取代-1-氮杂二环[3.3.0]辛烷的方法，其中R 1是氰基或-CO 2 R 3基，其中R 3是低级烷基。 该衍生物是通过式（Ⅰ）的1,7-二取代-4-庚酮（其中X为氯，溴或碘原子）或-OSO 2 R（其中R为甲基，甲苯基或三氟甲基） 与式R 1 CH 2 CO 2 Y的取代的乙酸衍生物反应，其中R 1具有所提及的含义; Y是氢，钠或钾原子或-NH 4，衍生物的碱金属盐或铵盐，在氨的存在下进行。 在5-取代-1-氮杂二环[3.3.0]辛烷中，5-氰甲基-1-氮杂双环[3.3.0]辛烷可以转化成5-（2-氨基乙基）-1-氮杂双环[3.3.0]辛烷 通过在大气压下，碱性条件下和在雷尼镍存在下进行的催化还原来进行。

    Hexahydrobenz[CD]indoles and processes for preparation thereof
    45.
    发明公开
    Hexahydrobenz[CD]indoles and processes for preparation thereof 失效
    六氢苯并[cd]吲哚和Verfahren zu deren Herstellung。

    公开(公告)号：EP0444851A2

    公开(公告)日：1991-09-04

    申请号：EP91301500.4

    申请日：1991-02-26

    申请人： ELI LILLY AND COMPANY

    发明人： Kress, Thomas Joseph ,  Leanna, Marvin Robert ,  Martinelli, Michael John ,  Peterson, Barry Curtis

    IPC分类号： C07D209/90 ,  C07D487/02

    CPC分类号： C07D487/06 ,  C07D209/90

    摘要： New intermediates, and processes therefor, provide an efficient method for deriving 4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indoles, which are themselves intermediates to useful CNS agents, from the Kornfeld-Woodward ketone and like compounds. Preferred embodiments provide means for the preparation of substantially pure enantiomers of the desired 4-amino-1,2,2a,3,4,5-hexahydrobenz[cd]indole.

    摘要翻译： 新的中间体及其方法提供了一种有效的方法，用于得到来自Kornfeld-Woodward酮的4-氨基-1,2,2a，3,4,5-六氢苯并[cd]吲哚，它们本身是有用的CNS剂的中间体 和类似化合物。 优选的实施方案提供了制备所需4-氨基-1,2,2a，3,4,5-六氢苯并[cd]吲哚的基本上纯的对映异构体的方法。

    Derivatives of tryptophan as CCK antagonists
    46.
    发明公开
    Derivatives of tryptophan as CCK antagonists 失效
    色氨酸衍生物，verwendbar als CCK-Gegner。

    公开(公告)号：EP0336356A2

    公开(公告)日：1989-10-11

    申请号：EP89105864.6

    申请日：1989-04-04

    申请人： ABBOTT LABORATORIES

    发明人： Kerwin, James F. ,  Nadzan, Alex M.

    IPC分类号： C07D209/42 ,  C07D209/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D487/02 ,  A61K31/40 ,  A61K31/44 ,  A61K31/47 ,  A61K31/415 ,  A61K31/495

    CPC分类号： C07D401/12 ,  C07D209/20 ,  C07D209/42 ,  C07D401/14 ,  C07D403/12 ,  C07D487/04 ,  C07K5/0202 ,  C07K5/06139

    摘要： A compound of the formula:
    wherein R₁ and R₂ are independently selected from hydrogen, loweralkyl, cycloalkyl, loweralkenyl, adamantyl, aryl, substituted aryl, heterocyclic group, substituted alkyl, substituted amide, functionalized carbonyl, and nitrogen containing ring wherein R₁, R₂ and the adjacent nitrogen atom form a ring;
    R₁₁ is hydrogen, loweralkyl, or loweralkenyl;
    R₂₀ is hydrogen, loweralkyl, or loweralkenyl;
    B is -(CH₂) m -, substituted alkenylene, -QCH₂- wherein Q is O, S, NH or substituted amino, -CH₂Q- wherein Q is as defined or B is NH;
    Z is C=O, S(O)₂, or C=S;
    Ar is a heterocyclic group, aryl or substituted aryl;
    D is unsubstituted or substituted indol-3-yl, indolin-3-yl or oxindol-3-yl; and m is 0 to 4;
    or a pharmaceutically acceptable salt thereof.

    摘要翻译： 下式的化合物，其中R 1和R 2独立地选自氢，低级烷基，环烷基，低级烯基，金刚烷基，芳基，取代的芳基，杂环基，取代的烷基，取代的酰胺，官能化的羰基和含氮环，其中R1 R2和相邻的氮原子形成环; R11是氢，低级烷基或低级烯基; R 20是氢，低级烷基或低级烯基; B是 - （CH 2）m - ，取代的亚烯基，-Q CH 2 - 其中Q是O，S，NH或取代的氨基，-CH 2 Q-，其中Q定义或B是NH; Z为C = O，S（O）2或C = S; Ar是杂环基，芳基或取代的芳基; D是未取代或取代的吲哚-3-基，二氢吲哚-3-基或羟吲哚-3-基; m为0〜4; 或其药学上可接受的盐。