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    Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
    1.
    发明授权
    Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor 有权
    适用于治疗对5-羟色胺5-HT 6受体的调节作用的疾病的氮杂环丁啶化合物

    公开(公告)号：US08507469B2

    公开(公告)日：2013-08-13

    申请号：US12532406

    申请日：2008-03-20

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

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

    IPC分类号： A61K31/397 ,  C07D403/04 ,  C07D471/04

    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 - 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。

    AZETIDIN COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR
    2.
    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。

    Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
    4.
    发明授权
    Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor 有权
    喹啉化合物适用于治疗对血清素5-HT6受体调节作用的疾病

    公开(公告)号：US08242102B2

    公开(公告)日：2012-08-14

    申请号：US12532407

    申请日：2008-03-23

    申请人： Sean Colm Turner ,  Andreas Haupt ,  Wilfried Braje ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Wolfgang Wernet ,  Alfred Hahn, legal representative ,  Matthias Mayrer

    发明人： Sean Colm Turner ,  Andreas Haupt ,  Wilfried Braje ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Wolfgang Wernet ,  Matthias Mayrer

    IPC分类号： A61K31/397 ,  C07D215/00

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R is a moiety of the formula wherein A, R1 to R4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; Ra, Rb are independently selected from the group consisting of halogen, CN, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C(O)Raa, C(O)NRccRbb and NRccRbb; X is CH2, C(O), S, S(O) or S(O)2; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar1, Ar2—Ar3 or Ar2—O—Ar3, wherein Ar1, Ar2 and Ar3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents Rx, wherein and physiologically tolerated acid addition salts and the N-oxides thereof.

    摘要翻译： 本发明涉及新颖的喹啉化合物。 该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT 6受体调节作出反应的疾病。 其中R是下式的部分，其中A，R 1至R 4如权利要求和说明书中所定义，n为0,1或2; m为0,1,2或3; R a，R b独立地选自卤素，CN，C 1 -C 4 - 烷基，C 1 -C 4卤代烷基，C 1 -C 4 - 烷氧基，C 1 -C 4卤代烷氧基，C（O）R aa，C（O）NR c R b b 和NRccRbb; X是CH 2，C（O），S，S（O）或S（O）2; 其位于喹啉环的3-或4-位; Ar是Ar1，Ar2-Ar3或Ar2-O-Ar3基团，其中Ar1，Ar2和Ar3各自独立地选自芳基或杂芳基，其中芳基或杂芳基部分可以是未取代的或可以携带1,2,3 取代基Rx，其中和生理上耐受的酸加成盐及其N-氧化物。