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    Indazolecarboxamides
    26.
    发明公开
    Indazolecarboxamides 失效

    公开(公告)号：EP0732333A1

    公开(公告)日：1996-09-18

    申请号：EP96301682.9

    申请日：1996-03-12

    申请人： ELI LILLY AND COMPANY

    发明人： Catlow, John Thomas ,  Cohen, Marlene Lois ,  Martinelli, Michael John ,  Schaus, John Mehnert ,  Swanson, Steven Phillip ,  Thompson, Dennis Charles ,  Wilson, Thomas Michael

    IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D231/56 ,  A61K31/415 ,  A61K31/445

    CPC分类号： C07D231/56 ,  C07D401/12

    摘要： Indazolecarboxamides are used as antagonists and partial agonists for the serotonin receptor 5-HT 4 and provide therapeutic methods for treatment of disorders caused by or affected by dysfunction of the 5-HT 4 receptor. The indazolecarboxamides are of the formula
    wherein:

    R is hydrogen, C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl;
    R 1 is hydrogen, halo, C 1 -C 4 alkyl, hydroxy, C 1 -C 4 alkoxy or alkylthio, cyano, trifluoromethyl, carboxamido, mono- or di(C 1 -C 4 alkyl)carboxamido;
    m, n and o are independently 0-5, provided that the sum of m, n and o is 2-5;
    R 2 is hydrogen or C 1 -C 4 alkyl;
    R 3 and R 4 combine with the nitrogen atom to which they are attached to form 1-pyrrolidinyl, 1-piperazinyl, 1,2,3,4-tetrahydro-2-isoquinolinyl, 2,3-dihydro-1-indolinyl, 4-morpholinyl, 1-piperidinyl or 1-hexamethyleneiminyl, substituted with
       phenyl, naphthyl, (phenyl or naphthyl) (C 1 -C 3 alkyl), (phenyl or naphthyl) (C 1 -C 3 alkanoyl), amino, mono- or di(C 1 -C 4 alkyl)amino, or a group of the formula -NH-Y-R 5 ; provided that a piperazinyl or morpholinyl group may not be substituted with amino, mono- or di(C 1 -C 4 alkyl)amino, or -NH-Y-R 5 ;
          wherein a phenyl or naphthyl group is unsubstituted or substituted with 1-3 halo, C 1 -C 3 alkyl or C 1 -C 3 alkoxy groups;
    Y is carbonyl, sulfonyl, aminocarbonyl or oxycarbonyl;
    R 5 is C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, C 6 -C 11 bicyclo- or tricycloalkyl, (phenyl or naphthyl)(C 1 -C 3 alkyl), phenyl or naphthyl;
       wherein a cycloalkyl, bicyclo- or tricycloalkyl, phenyl or naphthyl group is unsubstituted or substituted with 1-3 hydroxy, halo, C 1 -C 3 alkyl or C 1 -C 3 alkoxy groups;
    or a pharmaceutically acceptable salt thereof.

    摘要翻译： 吲唑甲酰胺用作5-羟色胺受体5-HT4的拮抗剂和部分激动剂，并提供治疗由5-HT4受体功能障碍引起的或受其影响的疾病的治疗方法。 吲唑羧酰胺具有下式：其中：R为氢，C 1 -C 6烷基，C 3 -C 6环烷基; 卤素，C1-C4烷基，羟基，C1-C4烷氧基或烷硫基，氰基，三氟甲基，甲酰氨基，单或二（C1-C4烷基）甲酰氨基; m，n和o独立地为0-5，条件是m，n和o的和为2-5; R2是氢或C1-C4烷基; R3和R4与它们所连接的氮原子结合形成1-吡咯烷基，1-哌嗪基，1,2,3,4-四氢-2-异喹啉基，2,3-二氢-1-二氢吲哚基，4-吗啉基 （苯基或萘基）（C 1 -C 3烷基），（苯基或萘基）（C 1 -C 3烷酰基），氨基，单或二（C 1 -C 4烷基）取代的1-哌啶基或1-六亚甲基亚胺基 ）氨基或式-NH-Y-R5的基团; 条件是哌嗪基或吗啉基基团可以不被氨基，一或二（C1-C4烷基）氨基或-NH-Y-R5取代; 其中苯基或萘基未被取代或被1-3个卤素，C1-C3烷基或C1-C3烷氧基取代; Y是羰基，磺酰基，氨基羰基或氧羰基; （苯基或萘基）（C 1 -C 3烷基），苯基或萘基; R 5是C 1 -C 6烷基，C 3 -C 8环烷基，C 6 -C 11双环或三环烷基， 其中环烷基，双环或三环烷基，苯基或萘基未被取代或被1-3个羟基，卤素，C 1 -C 3烷基或C 1 -C 3烷氧基取代; 或其药学上可接受的盐。

    Hexahydrobenz[CD]indoles and processes for preparation thereof
    28.
    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。