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。

公开(公告)号：US20100292271A1

公开(公告)日：2010-11-18

申请号：US12664394

申请日：2008-08-06

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

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

IPC分类号： A61K31/47 ,  C07D215/36 ,  A61P25/28 ,  A61P25/18 ,  A61P25/30 ,  A61P3/04 ,  A61P25/00

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X′, Y, Q, R1, R2, R3, R4, R5, m, n, p, q, R1, Rb, X and Ar are as defined in claim 1.

摘要翻译： 本发明涉及式（I）的新颖喹啉化合物及其盐。 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。 在式（I）中，R是式（R）的部分，其中*表示与喹啉基的结合位点，其中A，B，X'，Y，Q，R 1，R 2，R 3，R 4，R 5， n，p，q，R 1，R b，X和Ar如权利要求1中所定义。

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。

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。

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。

公开(公告)号：US06919342B2

公开(公告)日：2005-07-19

申请号：US10860823

申请日：2004-06-04

申请人： Andreas Haupt ,  Roland Grandel ,  Wilfried Braje ,  Hervé Geneste ,  Karla Drescher ,  Dorothea Starck ,  Hans-Jürgen Teschendorf

发明人： Andreas Haupt ,  Roland Grandel ,  Wilfried Braje ,  Hervé Geneste ,  Karla Drescher ,  Dorothea Starck ,  Hans-Jürgen Teschendorf

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

CPC分类号： C07D403/12

摘要： The invention relates to triazole compounds of the general formula I wherein R1 is hydrogen or methyl, and R2 is C3-C4 alkyl or C1-C2 fluoroalkyl, as well as 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： 本发明涉及通式Ⅰ的三唑化合物，其中R 1是氢或甲基，R 2是C 3 -C 3 > 4个烷基或C 1 -C 2 - 氟代烷基，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。

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。

公开(公告)号：US08440694B2

公开(公告)日：2013-05-14

申请号：US13613344

申请日：2012-09-13

申请人： Sean Colm Turner ,  Wilfried Braje ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Matthias Mayrer ,  Andrea Hager-Wernet

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

IPC分类号： A61K31/47 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P25/30 ,  C07D215/36

CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D519/00

摘要： The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X′, Y, Q, R1, R2, R3, R4, R5, m, n, p, q, Ra, Rb, X and Ar are as defined in claim 1.

摘要翻译： 本发明涉及式（I）的新颖喹啉化合物及其盐。 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。 在式（I）中，R是式（R）的部分，其中*表示与喹啉基的结合位点，其中A，B，X'，Y，Q，R 1，R 2，R 3，R 4，R 5， n，p，q，Ra，Rb，X和Ar如权利要求1所定义。

公开(公告)号：US20110009380A1

公开(公告)日：2011-01-13

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 ,  Matthias Mayrer

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

IPC分类号： A61K31/4709 ,  C07D401/02 ,  A61K31/4725 ,  C07D401/14 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18

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。

公开(公告)号：US20080161322A1

公开(公告)日：2008-07-03

申请号：US11628658

申请日：2005-06-03

申请人： Herve Geneste ,  Andreas Haupt ,  Wilfried Braje ,  Wilfried Lubisch ,  Gerd Steiner

发明人： Herve Geneste ,  Andreas Haupt ,  Wilfried Braje ,  Wilfried Lubisch ,  Gerd Steiner

IPC分类号： A61K31/497 ,  C07D401/02 ,  A61P25/00

CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D413/12

摘要： The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.

摘要翻译： 本发明涉及通式（I）的嘧啶化合物，以及这些化合物（I）的化合物和化合物（I）的生理上相容的酸加成盐在制备用于治疗疾病的药剂中的用途， 受多巴胺D 3受体拮抗剂或激动剂的影响。