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    • 10. 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
    • 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
    • US08049013B2
    • 2011-11-01
    • US12515432
    • 2007-11-15
    • Kevin Matthew GardinierDavid Joseph GarmeneErik James HembreMichael BrunavsHelen Jane Szekeres
    • Kevin Matthew GardinierDavid Joseph GarmeneErik James HembreMichael BrunavsHelen Jane Szekeres
    • C07D513/02
    • C07D513/04
    • 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.
    • 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。