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    5- [4-(azetidin-3-yloxy)-phenyl]-2-phenyl-5H-thiazolo[5,4-C] pyridin-4-one derivatives and their use as MCH receptor antagonists
    6.
    发明授权
    5- [4-(azetidin-3-yloxy)-phenyl]-2-phenyl-5H-thiazolo[5,4-C] pyridin-4-one derivatives and their use as MCH receptor antagonists 失效
    5- [4-（氮杂环丁烷-3-基氧基） - 苯基] -2-苯基-5H-噻唑并[5,4-C]吡啶-4-酮衍生物及其作为MCH受体拮抗剂

    公开(公告)号：US08049013B2

    公开(公告)日：2011-11-01

    申请号：US12515432

    申请日：2007-11-15

    申请人： Kevin Matthew Gardinier ,  David Joseph Garmene ,  Erik James Hembre ,  Michael Brunavs ,  Helen Jane Szekeres

    发明人： Kevin Matthew Gardinier ,  David Joseph Garmene ,  Erik James Hembre ,  Michael Brunavs ,  Helen Jane Szekeres

    IPC分类号： C07D513/02

    CPC分类号： C07D513/04

    摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “-----” is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, —C1-C2 alkyl, halo, hydroxy, —C1-C2 haloalkyl, —C1-C3 alkoxy, cyano, —O—C3-C4 cycloalkyl, and —OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, —C1-C3 alkyl, hydroxy, —C1-C3 alkoxy, cyano, —C1-C2 haloalkyl, —OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, —C1-C4 alkyl, —C2-C4 haloalkyl, —C2-C4 alkylOH, —C3-C6 cycloalkyl, —CH2C3-C6 cycloalkyl, —C2-C4 alkyl-O—C1-C4 alkyl, —C(O)C1-C4 alkyl, —C(O)C1-C4 haloalkyl, —CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and —C1-C2 haloalkyl; or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture thereof, useful in the treating, preventing or ameliorating of symptoms associated with obesity and related diseases.

    摘要翻译： 本发明涉及式I的黑色素浓缩激素拮抗剂化合物：其中“-----”不存在或任选地是键; q为1或2; R 1独立地选自氢，-C 1 -C 2烷基，卤素，羟基，-C 1 -C 2卤代烷基，-C 1 -C 3烷氧基，氰基，-O-C 3 -C 4环烷基和-OC 1 -C 2卤代烷基; R 2选自氢，-C 1 -C 3烷基，羟基，-C 1 -C 3烷氧基，氰基，-C 1 -C 2卤代烷基，-OC 1 -C 2卤代烷基和卤素; R 3选自氢，-C 1 -C 4烷基，-C 2 -C 4卤代烷基，-C 2 -C 4烷基OH，-C 3 -C 6环烷基，-CH 2 C 3 -C 6环烷基，-C 2 -C 4烷基-O- C4烷基，-C（O）C1-C4烷基，-C（O）C1-C4卤代烷基，-CH2-噻唑，苯基，苄基，四氢噻喃基和四氢吡喃基，其中环烷基，四氢噻喃基，四氢吡喃基和噻唑基任选被取代 具有一个或两个独立地选自卤素，羟基，C 1 -C 2烷基和-C 1 -C 2卤代烷基的基团; 或其药学上可接受的盐，对映异构体，非对映体或其混合物，其可用于治疗，预防或改善与肥胖症和相关疾病相关的症状。

    5- [4-(AZETIDIN-3-YLOXY)-PHENYL]-2-PHENYL-5H-THIAZOLO[5,4-C] PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS MCH RECEPTOR ANTAGONISTS
    7.
    发明申请
    5- [4-(AZETIDIN-3-YLOXY)-PHENYL]-2-PHENYL-5H-THIAZOLO[5,4-C] PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS MCH RECEPTOR ANTAGONISTS 失效
    5- [4-（AZETIDIN-3-乙氧基） - 苯基] -2-苯基-5H-噻唑并[5,4-C]吡啶-4-酮衍生物及其作为MCH受体拮抗剂的用途

    公开(公告)号：US20100069352A1

    公开(公告)日：2010-03-18

    申请号：US12515432

    申请日：2007-11-15

    申请人： Kevin Matthew Gardinier ,  David Joseph Garmene ,  Erik James Hembre ,  Michael Brunavs ,  Helen Jane Szekeres

    发明人： Kevin Matthew Gardinier ,  David Joseph Garmene ,  Erik James Hembre ,  Michael Brunavs ,  Helen Jane Szekeres

    IPC分类号： A61K31/397 ,  C07D471/04 ,  A61P3/04 ,  A61P3/10

    CPC分类号： C07D513/04

    摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “ - - - ” is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, —C1-C2 alkyl, halo, hydroxy, —C1-C2 haloalkyl, —C1-C3 alkoxy, cyano, —O—C3-C4 cycloalkyl, and —OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, —C1-C3 alkyl, hydroxy, —C1-C3 alkoxy, cyano, —C1-C2 haloalkyl, —OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, —C1-C4 alkyl, —C2-C4 haloalkyl, —C2-C4 alkylOH, —C3-C6 cycloalkyl, —CH2C3-C6 cycloalkyl, —C2-C4 alkyl-O—C1-C4 alkyl, —C(O)C1-C4 alkyl, —C(O)C1-C4 haloalkyl, —CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and —C1-C2 haloalkyl; or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture thereof, useful in the treating, preventing or ameliorating of symptoms associated with obesity and related diseases.

    摘要翻译： 本发明涉及式I的黑色素浓缩激素拮抗剂化合物：其中“ - - - ”不存在或任选地是键; q为1或2; R 1独立地选自氢，-C 1 -C 2烷基，卤素，羟基，-C 1 -C 2卤代烷基，-C 1 -C 3烷氧基，氰基，-O-C 3 -C 4环烷基和-OC 1 -C 2卤代烷基; R 2选自氢，-C 1 -C 3烷基，羟基，-C 1 -C 3烷氧基，氰基，-C 1 -C 2卤代烷基，-OC 1 -C 2卤代烷基和卤素; R 3选自氢，-C 1 -C 4烷基，-C 2 -C 4卤代烷基，-C 2 -C 4烷基OH，-C 3 -C 6环烷基，-CH 2 C 3 -C 6环烷基，-C 2 -C 4烷基-O- C4烷基，-C（O）C1-C4烷基，-C（O）C1-C4卤代烷基，-CH2-噻唑，苯基，苄基，四氢噻喃基和四氢吡喃基，其中环烷基，四氢噻喃基，四氢吡喃基和噻唑基任选被取代 具有一个或两个独立地选自卤素，羟基，C 1 -C 2烷基和-C 1 -C 2卤代烷基的基团; 或其药学上可接受的盐，对映异构体，非对映体或其混合物，其可用于治疗，预防或改善与肥胖症和相关疾病相关的症状。