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    N-2 adamantanyl-2-phenoxy-acetamide derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
    1.
    发明授权
    N-2 adamantanyl-2-phenoxy-acetamide derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
    N-2金刚烷基-2-苯氧基乙酰胺衍生物作为11-β羟基类固醇脱氢酶抑制剂

    公开(公告)号：US08344181B2

    公开(公告)日：2013-01-01

    申请号：US11661470

    申请日：2005-08-26

    申请人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Louis Jozef Elisabeth Van Der Veken ,  Gustaaf Henri Maria Willemsens ,  François Paul Bischoff

    发明人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Louis Jozef Elisabeth Van Der Veken ,  Gustaaf Henri Maria Willemsens ,  François Paul Bischoff

    IPC分类号： C07C233/05 ,  A61K31/16

    CPC分类号： A61K31/165 ,  C07C235/22 ,  C07C237/04 ,  C07C271/38 ,  C07C307/08 ,  C07C311/07 ,  C07C311/09 ,  C07C311/20 ,  C07C2603/74 ,  C07D207/27 ,  C07D263/20 ,  C07D265/36 ,  C07D295/32 ,  C07D307/85 ,  C07D311/66 ,  C07D319/20

    摘要： the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, S, NR6, SO or SO2; R1 represents hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of —O—CH2— (a), —NR7—CH2— (b), —(CR8R9)m- (c) and —CR10═ (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR13R14 or C1-4alkyl substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR15R16; R6 represents hydrogen; R11 and R12 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R13 and R14 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R15 and R16 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R17 and R18 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-.

    摘要翻译： N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中Z表示O，S，NR6，SO或SO2; R 1表示氢，氰基，羟基或任选被卤素取代的C 1-4烷基，R 2表示氢，C 1-4烷基或C 1-4烷氧基 - ; R 3表示氢，C 1-4烷基，C 1-4烷氧基或与R 2结合的R 3一起形成选自-O-CH 2 - （a），-NR 7 -CH 2 - （b）， - （CR 8 R 9） m-（c）和-CR 10 =（d）其中m表示1或2，并且R 7，R 8，R 9和R 10各自独立地选自氢或C 1-4烷基; R 4表示氢，卤素，羟基，氰基，氨基，NR 11 R 12，C 1-4烷氧基 - 任选地被一个或可能的两个或三个选自羟基和卤素的取代基取代，或者R 4表示任选地被一个或两个或三个 选自羟基和卤素的取代基; R 5表示氢，卤素，氰基，氨基，苯基，羟基，C 1-4烷氧基羰基，羟基羰基，NR 13 R 14或被一个或多个选自羟基羰基，苯基，C 1-4烷氧基或NR 15 R 16的取代基取代的C 1-4烷基; R6代表氢; R 11和R 12各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 13和R 14各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 15和R 16各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; R 17和R 18各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基。

    Tricyclic lactam derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
    2.
    发明授权
    Tricyclic lactam derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
    三环内酰胺衍生物作为11-β羟基类固醇脱氢酶抑制剂

    公开(公告)号：US08563591B2

    公开(公告)日：2013-10-22

    申请号：US11661468

    申请日：2005-08-26

    申请人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Louis Jozef Elisabeth Van Der Veken ,  Gustaaf Henri Maria Willemsens

    发明人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Louis Jozef Elisabeth Van Der Veken ,  Gustaaf Henri Maria Willemsens

    IPC分类号： C07D209/62 ,  A61K31/403 ,  A61K31/404

    CPC分类号： C07D471/04 ,  A61K31/4745 ,  A61K45/06 ,  C07D209/58 ,  C07D209/60 ,  C07D209/64 ,  C07D495/04

    摘要： the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents C or N; Y represents C or N; L represents a methyl or a direct bond; Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b); Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b); R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydroxycarbonyl, NR3R4 or C1-4alkyl optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8; R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-; R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; R7 and R8 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-; A represents phenyl or a monocyclic heterocycle selected from the group consisting of thiophenyl, furanyl, oxazolyl, thiazolyl, imidazolyl, isoxazolyl, isothiazolyl, pyrridinyl, pyridazinyl, pyrimidinyl and piperazinyl.

    摘要翻译： N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中X表示C或N; Y表示C或N; L表示甲基或直接键; Z 1表示直接键，C 1-2烷基 - 或式-CH 2 -CH =（a）或-CH =（b））的二价基团。 Z2表示直接键，C1-2烷基 - 或式-CH2-CH =（a）或-CH =（b）的二价基团; R 1表示氢，卤素，氰基，氨基，苯基，羟基，C 1-4烷氧基羰基，羟基羰基，NR 3 R 4或任选被一个或多个选自羟基羰基，苯基，C 1-4烷氧基或NR 5 R 6的取代基取代的C 1-4烷基或R 1表示C 1-4烷氧基 - 任选地被一个或多个选自羟基羰基，苯基，C 1-4烷氧基或NR 7 R 8的取代基取代; R 2表示氢，卤素，C 1-4烷基或C 1-4烷氧基 - ; R3和R4各自独立地表示氢，C1-4烷基或C1-4烷基羰基; R5和R6各自独立地表示氢，C1-4烷基或C1-4烷基羰基 - ; R 7和R 8各自独立地表示氢，C 1-4烷基或C 1-4烷基羰基 - ; A表示苯基或选自噻吩基，呋喃基，恶唑基，噻唑基，咪唑基，异恶唑基，异噻唑基，吡啶基，哒嗪基，嘧啶基和哌嗪基的单环杂环。