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    Adamantyl pyrrolidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
    6.
    发明授权
    Adamantyl pyrrolidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
    金刚烷基吡咯烷-2-酮衍生物作为11-β羟基类固醇脱氢酶抑制剂

    公开(公告)号：US07687644B2

    公开(公告)日：2010-03-30

    申请号：US11632195

    申请日：2005-04-29

    申请人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Buyck ,  Louis Jozef Elisabeth Van der Veken

    发明人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Buyck ,  Louis Jozef Elisabeth Van der Veken

    IPC分类号： C07D207/00 ,  A61K31/40

    CPC分类号： C07D207/26 ,  C07D207/267 ,  C07D211/76 ,  C07D453/06

    摘要： the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl-, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl-; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy-optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, hydroxy, cyano or C1-4alkyloxy-optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, C1-4alkyl or Ar2—C1-4alkyl-; R6 represents hydrogen, hydroxy, halo, C1-4alkyl or C1-4alkyoxy-; R7 represents hydrogen or R7 and R5 taken together with the carbon atom to which they are attached from a —C2-alkyl-linker; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl.

    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n为1或2; M表示直接键或任选被一个或两个选自C 1-4烷基，C 1-3烷氧基-C 1-4 - 烷基 - ，羟基-C 1-4 - 烷基 - ，羟基，C 1-3烷氧基 - 或苯基-C 1 -4-烷基 - ; R 1和R 2各自独立地表示氢，卤素，氰基，羟基，任选被卤素取代的C 1-4烷基，C 1-4烷氧基 - 任选被一个或可能的两个或三个选自羟基，Ar 1和卤素的取代基取代; R 3表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R 4表示氢，卤素，C 1-4烷基，羟基，氰基或C 1-4烷氧基 - 任选地被一个或其中可能的两个或三个选自羟基和卤素的取代基取代; R5表示氢，C1-4烷基或Ar2-C1-4烷基 - ; R 6表示氢，羟基，卤代，C 1-4烷基或C 1-4烷氧基 - ; R 7代表氢或R 7和R 5与它们所连接的碳原子一起从-C2-烷基 - 连接基中取代; Ar 1和Ar 2各自独立地表示苯基或萘基，其中所述苯基和萘基任选被C 1-4烷基，C 1-4烷氧基或苯基-C 1-4烷基取代。

    N-2 adamantanyl-2-phenoxy-acetamide derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
    7.
    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。

    Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
    9.
    发明授权
    Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors 有权
    吡咯烷-2-酮和哌啶-2-酮衍生物作为11-β羟基类固醇脱氢酶抑制剂

    公开(公告)号：US09012494B2

    公开(公告)日：2015-04-21

    申请号：US11632675

    申请日：2005-04-29

    申请人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Nestor Buyck ,  Louis Jozef Elisabeth Van Der Veken ,  Vladimir Dimtchev Dimitrov ,  Theo Teofanov Nikiforov

    发明人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Nestor Buyck ,  Louis Jozef Elisabeth Van Der Veken ,  Vladimir Dimtchev Dimitrov ,  Theo Teofanov Nikiforov

    IPC分类号： A61K31/4015 ,  C07D207/12 ,  C07D207/267 ,  C07D207/26 ,  C07D211/76 ,  C07D405/06

    CPC分类号： C07D211/76 ,  C07D207/26 ,  C07D207/267 ,  C07D405/06

    摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.

    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n为1或2; L表示任选被一个或两个选自C 1-4烷基，C 1-3烷氧基-C 1-4烷基 - ，羟基-C 1-4烷基，羟基，C 1-3烷氧基或苯基-C 1-4烷基的取代基取代的C 1-3烷基接头。 M表示直接键或任选被一个或两个选自羟基，C 1-4烷基或C 1-4烷氧基的取代基取代的C 1-3烷基接头; R 1和R 2各自独立地表示氢，卤素，氰基，羟基，任选被卤素取代的C 1-4烷基，C 1-4烷氧基 - 任选被一个或可能的两个或三个选自羟基，Ar 1和卤素的取代基取代; 或者R 1和R 2与它们所连接的苯环一起形成萘基或1,3-苯并二恶唑基，其中所述萘基或1,3-苯并二恶唑基任选被卤素取代; R 3表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R4代表氢，卤素，C1-4烷基，C1-4烷氧基，氰基或羟基; R5表示氢，C1-4烷基或Ar2-C1-4烷基; R 6表示氢，卤素，C 1-4烷基或C 1-4烷氧基 - ; Ar1和Ar2各自独立地表示苯基或萘基，其中所述苯基和萘基任选被C 1-4烷基，C 1-4烷氧基 - 或苯基-C 1-4烷基取代; 用作药物。

    Tricyclic lactam derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
    10.
    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。