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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
    1.
    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
    3.
    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。

    Macroporous ion exchange resins
    10.
    发明申请
    Macroporous ion exchange resins 失效
    大孔离子交换树脂

    公开(公告)号：US20050261385A1

    公开(公告)日：2005-11-24

    申请号：US11059858

    申请日：2005-02-17

    申请人： Jerald Rasmussen ,  James Hembre

    发明人： Jerald Rasmussen ,  James Hembre

    IPC分类号： B01J39/18 ,  B01J39/20 ,  B01J39/22 ,  B01J39/26 ,  B01J41/12 ,  B01J41/14 ,  B01J41/20 ,  C08J5/20

    CPC分类号： B01J39/20 ,  B01J20/28085 ,  B01J39/26 ,  B01J41/14 ,  B01J41/20 ,  Y10S526/909 ,  Y10T428/249953

    摘要： Ion exchange resins are described that are hydrophilic, crosslinked (meth)acrylic copolymers. The ion exchange resins are macroporous, have a surface area of at least 50 m2/g, and an average particle size of at least 20 micrometers. Additionally, chromatographic columns containing the ion exchange resins, composite materials containing the ion exchange resin, filtration elements containing the ion exchange resin, methods of preparing the ion exchange resins, and methods of separating or purifying negatively or positively charged materials with the ion exchange resins are described.

    摘要翻译： 描述了亲水交联（甲基）丙烯酸共聚物的离子交换树脂。 离子交换树脂是大孔的，表面积至少为50m 2 / g，平均粒度至少为20微米。 此外，含有离子交换树脂的色谱柱，含有离子交换树脂的复合材料，含离子交换树脂的过滤元件，离子交换树脂的制备方法以及用离子交换树脂分离或纯化带正电或带正电的材料的方法 被描述。