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    1,2,4,-TRIAZIN-3,5-DIONE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    11.
    发明申请
    1,2,4,-TRIAZIN-3,5-DIONE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 有权
    1,2,4，-TRIAZIN-3,5-DIONE适用于治疗多巴胺D3受体调节障碍的化合物

    公开(公告)号：US20100311755A1

    公开(公告)日：2010-12-09

    申请号：US12740714

    申请日：2008-10-31

    申请人： Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Herve' Geneste ,  Karla Drescher ,  Liliane Unger ,  Ana Lucia Jongen-Relo ,  Anton Bespalov

    发明人： Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Herve' Geneste ,  Karla Drescher ,  Liliane Unger ,  Ana Lucia Jongen-Relo ,  Anton Bespalov

    IPC分类号： A61K31/53 ,  C07D253/07 ,  A61P25/00 ,  A61P25/18 ,  A61P25/30 ,  A61P13/12

    CPC分类号： C07D403/12

    摘要： The invention relates to compounds of the formula I: wherein A is a saturated or unsaturated hydrocarbon chain having a chain length of 4 to 6 carbon atoms, the hydrocarbon chain being unsubstituted or substituted by 1, 2 or 3 methyl groups; R1 is selected from the group consisting of hydrogen, C1-C3 alkyl and fluorinated C1-C3 alkyl; R2 is hydrogen, halogen, cyano, C1-C3 alkyl, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R3 is selected from the group consisting of branched C4-C6 alkyl and C3-C6 cycloalkyl, and R4 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C3-alkyl and fluorinated C3-C6 cycloalkyl. and the physiologically tolerated salts of these compounds and the N-oxides thereof. The invention also relates to a pharmaceutical composition that comprises at least one 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 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A是链长为4-6个碳原子的饱和或不饱和烃链，烃链未被取代或被1,2或3个甲基取代; R1选自氢，C1-C3烷基和氟化C1-C3烷基; R2是氢，卤素，氰基，C1-C3烷基，C1-C3烷氧基，氟化C1-C3烷基或氟化C1-C3烷氧基; R3选自支链C4-C6烷基和C3-C6环烷基，R4为C1-C6烷基，C3-C6环烷基，氟化C1-C3-烷基和氟化C3-C6环烷基。 以及这些化合物的生理上耐受的盐及其N-氧化物。 本发明还涉及包含至少一种式I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受体拮抗剂或多巴胺D3的病症的方法 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化合物或生理学上耐受的酸加成盐。

    AZETIDIN COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR
    13.
    发明申请
    AZETIDIN COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
    适用于治疗响应调节SEROTONIN 5-HT6受体的疾病的AZETIDIN化合物

    公开(公告)号：US20100137280A1

    公开(公告)日：2010-06-03

    申请号：US12532406

    申请日：2008-03-20

    申请人： Thomas Schultz, SR. ,  Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Matthias Mayrer

    发明人： Thomas Schultz, SR. ,  Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Matthias Mayrer

    IPC分类号： A61K31/404 ,  A61K31/437 ,  A61K31/4184 ,  A61K31/416 ,  C07D403/10 ,  C07D413/02 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/506 ,  A61P25/00 ,  A61P3/04 ,  A61P25/30 ,  A61P25/18

    CPC分类号： C07D471/04 ,  C07D403/04

    摘要： The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl, is a single or double bond; X1 and X2 are N, CRx1, NRx2, or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; wherein a maximum of 3 of the radicals X1, X2, Y1, Y2 and Y3 are selected from NRx1 and N; R1 is hydrogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, etc.; R2 is C1-C4-alkyl or C1-C4-haloalkyl; n is 0, 1 or 2; physiologically tolerated acid addition salts and the N-oxides thereof, pharmaceutical composition comprising them, a method for treating medical disorders selected from diseases of the central nervous system, addiction diseases or obesity, said method comprising administering an effective amount of such compounds to a subject in need and the use of such a compound for preparing a pharmaceutical compositions.

    摘要翻译： 本发明涉及式（I）化合物，其中A为C 1 -C 6 - 烷基，C 1 -C 6 - 卤代烷基，C 1 -C 6羟基烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 卤代烯基，C 3 -C 6 - 环烷基，芳基-C 1 -C 4烷基，芳基-C 2 -C 4 - 烯基，芳基或杂芳基，是单键或双键; X1和X2是N，CRx1，NRx2或CRx3Rx4; Rx1，Rx3和Rx4是H，卤素，CN，NO2，C1-C6-烷基，C1-C6-烷氧基，C1-C6-烷基羰基等，或两个偕根基Rx3和Rx4与它们所在的碳原子一起 结合可形成羰基或3-至6-元碳环或杂环螺环状环; Rx2是氢，C1-C6-烷基，C1-C6-烷基羰基，C1-C6-卤代烷基等; 或两个连位基Rx1，Rx2，Rx3或Rx4与X1和X2一起形成五元或六元碳环或杂环稠环; Y1，Y2和Y3为N或CRy; Ry是H，卤素，CN，NO 2，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基羰基，C 1 -C 6 - 卤代烷基等; 其中基团X1，X2，Y1，Y2和Y3中的最多3个选自NRx1和N; R1是氢，C1-C6-烷基，C1-C6-羟基烷基，C1-C6-卤代烷基等; R2是C1-C4-烷基或C1-C4卤代烷基; n为0,1或2; 生理耐受的酸加成盐及其N-氧化物，包含它们的药物组合物，治疗选自中枢神经系统疾病，成瘾疾病或肥胖症的医学病症的方法，所述方法包括向受试者施用有效量的这些化合物 并且使用这种化合物来制备药物组合物。

    1,2,4,-triazin-3,5-dione compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    16.
    发明授权
    1,2,4,-triazin-3,5-dione compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
    1,2,4-三嗪-3,5-二酮化合物，适用于治疗对多巴胺D3受体调节作用的疾病

    公开(公告)号：US08492540B2

    公开(公告)日：2013-07-23

    申请号：US12740714

    申请日：2008-10-31

    申请人： Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Hervé Geneste ,  Karla Drescher ,  Liliane Unger ,  Ana Lucia Relo ,  Anton Bespalov

    发明人： Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Hervé Geneste ,  Karla Drescher ,  Liliane Unger ,  Ana Lucia Relo ,  Anton Bespalov

    IPC分类号： C07D253/075 ,  C07D403/14 ,  A61K31/53 ,  A61P25/18 ,  A61P25/30 ,  A61P25/00

    CPC分类号： C07D403/12

    摘要： The invention relates to compounds of the formula I: wherein A is a saturated or unsaturated hydrocarbon chain having a chain length of 4 to 6 carbon atoms, the hydrocarbon chain being unsubstituted or substituted by 1, 2 or 3 methyl groups; R1 is selected from the group consisting of hydrogen, C1-C3 alkyl and fluorinated C1-C3 alkyl; R2 is hydrogen, halogen, cyano, C1-C3 alkyl, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R3 is selected from the group consisting of branched C4-C6 alkyl and C3-C6 cycloalkyl, and R4 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C3-alkyl and fluorinated C3-C6 cycloalkyl. and the physiologically tolerated salts of these compounds and the N-oxides thereof. The invention also relates to a pharmaceutical composition that comprises at least one 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 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A是链长为4-6个碳原子的饱和或不饱和烃链，烃链未被取代或被1,2或3个甲基取代; R1选自氢，C1-C3烷基和氟化C1-C3烷基; R2是氢，卤素，氰基，C1-C3烷基，C1-C3烷氧基，氟化C1-C3烷基或氟化C1-C3烷氧基; R3选自支链C4-C6烷基和C3-C6环烷基，R4为C1-C6烷基，C3-C6环烷基，氟化C1-C3-烷基和氟化C3-C6环烷基。 以及这些化合物的生理上耐受的盐及其N-氧化物。 本发明还涉及包含至少一种式I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受体拮抗剂或多巴胺D3的病症的方法 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化合物或生理学上耐受的酸加成盐。

    N-[piperazinyl hetaryl]arylsufonamide compounds with affinity for the dopamine D3 receptor
    17.
    发明授权
    N-[piperazinyl hetaryl]arylsufonamide compounds with affinity for the dopamine D3 receptor 失效
    对多巴胺D3受体具有亲和力的N- [哌嗪基杂芳基]芳基磺酰胺化合物

    公开(公告)号：US08476275B2

    公开(公告)日：2013-07-02

    申请号：US13117269

    申请日：2011-05-27

    申请人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer ,  Sean Colm Turner

    发明人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer ,  Sean Colm Turner

    IPC分类号： A61K31/496 ,  A61K31/506 ,  C07D213/72 ,  C07D213/74 ,  C07D239/48

    CPC分类号： C07D213/74 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D403/04 ,  C07D403/14 ,  C07D487/08

    摘要： The invention related to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula (I) in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

    摘要翻译： 本发明涉及通式（I）的N - [（哌嗪基）杂芳基]芳基磺酰胺化合物，其中Q是具有1或2个N原子作为环成员的二价，6元杂芳族基团，并且任选地带有一个或两个 被卤素，CN，NO 2，CO 2 R 4，COR 5，C 1 -C 4 - 烷基和C 1 -C 4卤代烷基独立地选择的取代基R a; Ar是苯基或6元杂芳族基，其具有1或2个N原子作为环成员，并且任选地带有一个或两个选自卤素，NO 2，CN，CO 2 R 4，COR 5，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 4 - 烷基和C 1 -C 4卤代烷基， 与Ar的相邻C原子一起C3-C4-亚烷基; R 1是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 3 -C 6环烷基，C 3 -C 6环烷基-C 1 -C 4烷基，C 1 -C 4羟烷基，C 1 -C 4烷氧基-C 1 -C 4 - 烷基，C 3 -C 4 - 烯基或C 3 -C 4 - 炔基; 具有如专利权利要求中给出的含义的基团n，R 1，R 2，R 3，R 4和R 5与这些化合物的N-氧化物和生理上耐受的酸加成盐以及包含至少一种N- 和/或至少一种I的生理学耐受的酸加成盐和/或I的N-氧化物，其中适宜地与生理上可接受的载体和/或 用于治疗对多巴胺D3受体拮抗剂或激动剂影响的疾病的辅助物质，特别是用于治疗中枢神经系统疾病和肾功能障碍。