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    Chemical Compounds
    4.
    发明申请
    Chemical Compounds 审中-公开
    化学化合物

    公开(公告)号：US20090042897A1

    公开(公告)日：2009-02-12

    申请号：US12022327

    申请日：2008-01-30

    申请人： Jonathan Bentley ,  Matteo Biagetti ,  Thorsten Genski ,  Silvia Rosalia Kopf ,  Colin Philip Leslie ,  Sergio Melotto

    发明人： Jonathan Bentley ,  Matteo Biagetti ,  Thorsten Genski ,  Silvia Rosalia Kopf ,  Colin Philip Leslie ,  Sergio Melotto

    IPC分类号： C07D413/02 ,  A61K31/501 ,  A61K31/4439 ,  A61K31/423 ,  A61P3/00 ,  A61P25/00 ,  A61P25/24

    CPC分类号： C07D413/14

    摘要： The present invention relates to novel compounds or a pharmaceutically acceptable salt or solvate thereof, selected from a group consisting of: (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(2-fluoro-3-pyridinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(3-pyridazinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(1-methyl-1H-pyrazol-3-yl)-1-oxa-3-azaspiro[4.5]decan-2-one; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.

    摘要翻译： 本发明涉及选自以下的新的化合物或其药学上可接受的盐或溶剂化物：（反）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基} 甲基）-3-（2-氟-3-吡啶基）-1-氧杂-3-氮杂螺[4.5]癸-2-酮; （反式）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（3-哒嗪基）-1-氧杂-3-氮杂螺[4.5] 2-one; （反式）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（1-甲基-1H-吡唑-3-基）-1-氧杂 - 3-氮杂螺[4.5]癸-2-酮; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

    Spiro Compounds As NPY Y5 Receptor Antagonists
    5.
    发明申请
    Spiro Compounds As NPY Y5 Receptor Antagonists 审中-公开
    螺环化合物作为NPY Y5受体拮抗剂

    公开(公告)号：US20090203705A1

    公开(公告)日：2009-08-13

    申请号：US12360166

    申请日：2009-01-27

    申请人： Matteo Biagetti ,  Stefania Anna Contini ,  Thorsten Genski ,  Sebastien Guery ,  Colin Philip Leslie ,  Angelica Mazzali ,  Domenica Antonia Pizzi ,  Fabio Maria Sabbatini ,  Catia Seri

    发明人： Matteo Biagetti ,  Stefania Anna Contini ,  Thorsten Genski ,  Sebastien Guery ,  Colin Philip Leslie ,  Angelica Mazzali ,  Domenica Antonia Pizzi ,  Fabio Maria Sabbatini ,  Catia Seri

    IPC分类号： A61K31/501 ,  C07D413/14 ,  A61P3/04

    CPC分类号： C07D413/12 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z1 is H, C1-C4 alkyl or F; Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond; A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or —C(═O)—X; or —O(CH2)0-1R1; B is hydrogen or is a 5-6 membered heteroaryl, or a 4-6 membered heterocycle, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom; R1 is —(C1-C4)alkyl(C1-C4)alkoxy; or C3-C8 cycloalkyl; or R1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; X is OR2 or NR3R4; R2 is C1-C4 alkyl; R3 is hydrogen or together with R4 and the nitrogen form a 5-6 saturated membered ring; R4 is C3-C8 cycloalkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.

    摘要翻译： 本发明涉及新的式（I）化合物或其药学上可接受的盐，其中R是可被一个或多个取代的芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C4卤代烷基，C1-C4卤代烷氧基，氰基; Z 1是H，C 1 -C 4烷基或F; Z是CH 2，CH（C 1 -C 4烷基），C（C 1 -C 4烷基）2或键; A是6-10元芳基或杂芳基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 或-C（-O）-X; 或-O（CH 2）0-1R1; B是氢或是5-6元杂芳基或4-6元杂环，或苯基，其可被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C4卤代烷氧基，羟基，氰基; A和B通过任何原子相连; R1是 - （C1-C4）烷基（C1-C4）烷氧基; 或C 3 -C 8环烷基; 或者R 1是可被一个或多个卤素取代的芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 或R 1是4-6元杂环，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; X为OR2或NR3R4; R2是C1-C4烷基; R3是氢或与R4一起形成5-6饱和的元环; R4是C3-C8环烷基; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。