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    Triazole Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor
    5.
    发明申请
    Triazole Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor 失效
    适用于治疗多巴胺D3受体调节反应的三唑化合物

    公开(公告)号：US20080171751A1

    公开(公告)日：2008-07-17

    申请号：US11792596

    申请日：2005-12-01

    申请人： Liliane Unger ,  Andreas Haupt ,  Armin Beyerbach ,  Karla Drescher ,  Wilfried Braje ,  John Darbyshire ,  Sean C. Turner ,  Gisela Backfisch

    发明人： Liliane Unger ,  Andreas Haupt ,  Armin Beyerbach ,  Karla Drescher ,  Wilfried Braje ,  John Darbyshire ,  Sean C. Turner ,  Gisela Backfisch

    IPC分类号： A61K31/496 ,  C07D403/14 ,  A61P25/00

    CPC分类号： C07D403/12

    摘要： The invention relates to compounds of the formula I: wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

    摘要翻译： 本发明涉及式I化合物：其中n是1或2，Ar是在剩余的碳原子上带有自由基R 1的C结合的1,2,4-三唑基，和 其中一个氮原子上的基团R 1a， R 1是氢，C 1 -C 6烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 氟化C 1 -C 6烷基，氟化C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6位的C 1 -C 6烷基， 杂芳基; R 1a是氢或C 1 -C 4烷基; R 2是C 1 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基， 氟化C 1 -C 6烷基或氟化C 3 -C 6环烷基; 以及这些化合物的生理上耐受的酸加成盐。 本发明还涉及一种药物组合物，其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐，还涉及治疗有益于多巴胺D 3的病症的方法 受体拮抗剂或多巴胺D 3激动剂，所述方法包括向有需要的受试者施用有效量的至少一种式III的三唑化合物或生理耐受的酸加成盐。

    Triazole compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    7.
    发明授权
    Triazole compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
    适用于治疗对多巴胺D3受体调节作出反应的三唑化合物

    公开(公告)号：US08101754B2

    公开(公告)日：2012-01-24

    申请号：US11792596

    申请日：2005-12-01

    申请人： Liliane Unger ,  Andreas Haupt ,  Armin Beyerbach ,  Karla Drescher ,  Wilfried Braje ,  John Darbyshire ,  Sean C. Turner ,  Gisela Backfisch

    发明人： Liliane Unger ,  Andreas Haupt ,  Armin Beyerbach ,  Karla Drescher ,  Wilfried Braje ,  John Darbyshire ,  Sean C. Turner ,  Gisela Backfisch

    IPC分类号： C07D403/14 ,  C07D403/12 ,  A61K31/506 ,  A61P25/18

    CPC分类号： C07D403/12

    摘要： The invention relates to compounds of the formula I: wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionially substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

    摘要翻译： 本发明涉及式I化合物：其中n为1或2，Ar为在其余碳原子上携带基团R 1的C结合的1,2,4-三唑基团，其中一个氮气上具有基团R 1a 原子 R 1是氢，C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 4烷氧基甲基，氟化C 1 -C 6烷基，氟化C 3 -C 6环烷基，氟化C 1 -C 4烷氧基甲基或选择性取代的苯基或5或6元杂芳基; R 1a是氢或C 1 -C 4烷基; 和R2是C1-C6烷基，C3-C6环烷基，氟化C1-C6烷基或氟化C3-C6环烷基; 以及这些化合物的生理上耐受的酸加成盐。 本发明还涉及一种药物组合物，其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐，还涉及治疗有益于多巴胺D3受体拮抗剂或多巴胺的病症的方法 D3激动剂，所述方法包括向有需要的受试者施用有效量的至少一种式III的三唑化合物或生理耐受的酸加成盐。

    TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    8.
    发明申请
    TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
    适用于治疗多巴胺D3受体调节症状的三唑化合物

    公开(公告)号：US20120095015A1

    公开(公告)日：2012-04-19

    申请号：US13333702

    申请日：2011-12-21

    申请人： Liliane Unger ,  Andreas Haupt ,  Armin Beyerbach ,  Karla Drescher ,  Wilfried Braje ,  John Darbyshire ,  Sean C. Turner ,  Gisela Backfisch

    发明人： Liliane Unger ,  Andreas Haupt ,  Armin Beyerbach ,  Karla Drescher ,  Wilfried Braje ,  John Darbyshire ,  Sean C. Turner ,  Gisela Backfisch

    IPC分类号： A61K31/506 ,  A61P25/00 ,  A61P25/18 ,  C07D403/14

    CPC分类号： C07D403/12

    摘要： The invention relates to compounds of formula (I), wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of there compounds. The invention also relates to a pharmaceutically composition that comprises at least one triazole compound of the formula (I) and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula (I) to a subject in need thereof.

    摘要翻译： 本发明涉及式（I）化合物，其中n为1或2，Ar为在其余碳原子上携带基团R1的C结合的1,2,4-三唑基团， 氮原子; R 1是氢，C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 4烷氧基甲基，氟化C 1 -C 6烷基，氟化C 3 -C 6环烷基，氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6-元杂芳基; R 1a是氢或C 1 -C 4烷基; 和R2是C1-C6烷基，C3-C6环烷基，氟化C1-C6烷基或氟化C3-C6环烷基; 以及该化合物的生理耐受酸加成盐。 本发明还涉及包含至少一种式（I）的三唑化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D3受体拮抗剂的病症的方法 或多巴胺D3激动剂，所述方法包括向有需要的受试者施用有效量的至少一种式（I）的三唑化合物或生理上耐受的酸加成盐。

    Apparatus for agglomeration
    10.
    发明授权
    Apparatus for agglomeration 失效
    用于凝聚的装置

    公开(公告)号：US4815958A

    公开(公告)日：1989-03-28

    申请号：US224818

    申请日：1988-07-27

    申请人： Marcel Buhler ,  John Darbyshire ,  Michel Jaccard

    发明人： Marcel Buhler ,  John Darbyshire ,  Michel Jaccard

    IPC分类号： A23C9/16 ,  A23G1/00 ,  A23G1/04 ,  A23G1/30 ,  A23G3/26 ,  A23L1/00 ,  A23L1/164 ,  A23L1/18 ,  A23P1/02 ,  A23P1/08 ,  B01J2/12 ,  B29C67/06

    CPC分类号： B01J2/12 ,  A23L7/122 ,  A23P10/20 ,  Y10S425/02

    摘要： Apparatus particularly for agglomerating particles of different products. A rotatable drum, which has a wall which defines a cylinder and a cylinder void, is mounted on a frame in a horizontal or inclined position. The apparatus includes provision for rotating the cylinder in one direction thereby defining ascending and descending halves of the cylinder. A first part of the cylinder receives particles of a product and has means, such as projecting elements, to rotate the particles for forming a vortex of particles about an axis within the ascending half of the cylinder void such that the axis of the vortex is displaced from and substantially parallel to a central longitudinal axis of the cylinder. The apparatus also includes provision for introducing a product into a second part of the cylinder in the ascending half of the cylinder void, the second part being displaced from the first end of the cylinder and abutting the first part of the cylinder, for distributing secondary product into the vortex of particles within a zone about which the vortex rotates. A spraying device is positioned in the second part of the cylinder void in the descending half of the cylinder for spraying an agglomerating agent onto the particles of the vortex from outside of the vortex.

    摘要翻译： 特别是用于聚集不同产品的颗粒的装置。 具有限定气缸和气缸空隙的壁的可旋转滚筒以水平或倾斜的位置安装在框架上。 该装置包括用于在一个方向上旋转气缸的装置，从而限定气缸的上升和下降两半。 气缸的第一部分接收产品的颗粒并且具有诸如突出元件的装置以使颗粒旋转以形成围绕汽缸空隙的上升半部内的轴线的颗粒涡旋，使得涡流的轴线被移位 从并且基本上平行于圆柱体的中心纵向轴线。 该设备还包括用于将产品引入汽缸的上半部分中的第二部分中的第二部分，第二部分从气缸的第一端移动并邻接气缸的第一部分，用于分配二次产品 进入涡旋旋转的区域内的颗粒涡流。 喷射装置位于气缸的第二部分中，在气缸的下半部分中具有空隙，用于从涡流外部将附聚剂喷射到涡流颗粒上。