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11. 发明授权

US08710059B2 N-phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds suitable for treating disorders that respond to the modulation of the serotonin 5-HT6 receptor 有权
标题翻译： N-苯基 - （高）哌嗪基 - 苯磺酰基或苯磺酰胺化合物，适用于治疗对5-羟色胺5-HT 6受体的调节作用的病症
公开(公告)号：US08710059B2
公开(公告)日：2014-04-29
申请号：US13286446
申请日：2011-11-01
申请人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
发明人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： C07D295/096 , C07D243/08
摘要： The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
摘要翻译：本发明涉及式I的N-苯基 - （同）哌嗪基 - 苯磺酰基或苯磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。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-HT6受体的调节作出反应的疾病。

12. 发明申请

US20120142674A1 N-PHENYL-(HOMO)PIPERAZINYL-BENZENESULFONYL OR BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译： N-苯基 - （HOMO）哌嗪二苯并呋喃或苯并呋喃半导体化合物，适用于治疗依托莫司汀5-HT6受体调节的病症
公开(公告)号：US20120142674A1
公开(公告)日：2012-06-07
申请号：US13286446
申请日：2011-11-01
申请人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
发明人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
IPC分类号： A61K31/551 , C07D243/08 , A61K31/495 , A61P25/18 , A61P25/30 , A61P3/04 , A61P25/28 , C07D295/135 , A61P25/00
CPC分类号： C07D295/096 , C07D243/08
摘要： The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
摘要翻译：本发明涉及式I的N-苯基 - （同）哌嗪基 - 苯磺酰基或苯磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。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-HT6受体的调节作出反应的疾病。

13. 发明申请

US20120129883A1 BENZENESULFONYL OR SULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OFTHE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译：适用于治疗血清丝素5-HT6受体调节障碍的苯并呋喃或磺酰胺化合物
公开(公告)号：US20120129883A1
公开(公告)日：2012-05-24
申请号：US13286387
申请日：2011-11-01
申请人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
发明人： Andreas Haupt , Frauke Pohlki , Liliane Unger , Ana Lucia Relo , Karsten Wicke , Min Zhang
IPC分类号： A61K31/435 , C07D211/28 , A61K31/451 , A61K31/40 , A61P3/04 , A61P25/30 , A61P25/28 , A61P25/18 , C07D209/52 , C07D221/04 , A61K31/403 , C07D207/09 , A61P25/00
CPC分类号： C07D209/52 , C07D211/24 , C07D221/06
摘要： The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
摘要翻译：本发明涉及式IA和IB的苯磺酰基或磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。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-HT6受体的调节作出反应的疾病。

14. 发明授权

US08492540B2 1,2,4,-triazin-3,5-dione compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译： 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。

15. 发明授权

US07790727B2 Benzenesulfonanilide compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor 有权
标题翻译：苯磺酰苯胺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：US07790727B2
公开(公告)日：2010-09-07
申请号：US12262455
申请日：2008-10-31
申请人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
发明人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
IPC分类号： A61K31/495 , A61K31/496 , C07D295/135 , C07D317/62
CPC分类号： C07D295/12 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.
摘要翻译：本发明涉及式I和I'的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。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R1是氢或甲基R2是氢或甲基R3氢，氟C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基或氟化C1-C4烷基; R5是氢，氟，C1-C2烷基，氟化C1-C2烷基，C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟或氯。

16. 发明申请

US20110086863A1 BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译：适用于治疗依托莫司汀5-HT6受体调节的病症的苯并呋喃半导体化合物
公开(公告)号：US20110086863A1
公开(公告)日：2011-04-14
申请号：US12851466
申请日：2010-08-05
申请人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
发明人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
IPC分类号： A61K31/496 , C07D241/04 , A61K31/495 , C07D405/12 , A61P25/00 , A61P3/04
CPC分类号： C07D295/12 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine and chlorine.
摘要翻译：本发明涉及式I和I'的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。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R1是氢或甲基R2是氢或甲基R3氢，氟C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基或氟化C1-C4烷基; R5是氢，氟，C1-C2烷基，氟化C1-C2烷基，C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟和氯。

17. 发明申请

US20090131452A1 BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译：适用于治疗依托莫司汀5-HT6受体调节的病症的苯并呋喃半导体化合物
公开(公告)号：US20090131452A1
公开(公告)日：2009-05-21
申请号：US12262455
申请日：2008-10-31
申请人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
发明人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
IPC分类号： A61K31/496 , C07D295/182 , C07D405/12 , A61P25/00 , A61K31/495
CPC分类号： C07D295/12 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl fluorinated C1-C2 alkyl C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.
摘要翻译：本发明涉及式I和I'的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。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R1是氢或甲基R2是氢或甲基R3氢，氟C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基或氟化C1-C4烷基; R5是氢，氟，C1-C2烷基氟化C1-C2烷基C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟或氯。

18. 发明申请

US20080171751A1 Triazole Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor 失效
标题翻译：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。

19. 发明申请

US20120095015A1 TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
标题翻译：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。

20. 发明申请

US20110160176A1 HETEROCYCLIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 失效
标题翻译：适用于治疗多巴胺D3受体调节障碍的异种化合物
公开(公告)号：US20110160176A1
公开(公告)日：2011-06-30
申请号：US12868480
申请日：2010-08-25
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry , Gisela Backfisch , Armin Beyerbach , Wilfried Lubisch
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry , Gisela Backfisch , Armin Beyerbach , Wilfried Lubisch
IPC分类号： A61K31/397 , C07D207/08 , A61K31/40 , C07D401/02 , C07D205/02 , C07D403/02 , A61K31/506 , C07D417/02 , A61K31/433 , C07D413/14 , A61K31/422 , C07D211/08 , A61K31/445 , A61P25/28
CPC分类号： C07D413/14 , C07D205/04 , C07D207/09 , C07D211/28 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12
摘要： The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; and physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
摘要翻译：本发明涉及式（I）化合物，其中n为0,1或2; G是CH 2或CHR 3; R 1是被C 3 -C 6 - 环烷基取代的C 1 -C 6 - 烷基，C 1 -C 6 - 烷基，C 1 -C 6羟基烷基，氟化C 1 -C 6 - 烷基，C 3 -C 6环烷基，氟化C 3 -C 6 - 环烷基，C3-C6烯基，氟化C3-C6-烯基，甲酰基，乙酰基或丙酰基; R2，R3和R4彼此独立地为H，甲基，氟甲基，二氟甲基或三氟甲基; A是可以被一个或多个选自卤素，甲基，甲氧基和CF 3的取代基取代的亚苯基，亚吡啶基，亚嘧啶基，吡嗪基，哒嗪基或噻吩基; E是NR5或CH2，其中R5是H或C1-C3-烷基; Ar是选自苯基，5或6元杂芳族基团的环状基团，其包含选自N，O和S的环成员1,2或3个杂原子和与饱和或不饱和5 - 或6-元碳环或杂环，其中杂环包含作为环成员1,2或3个选自N，O和S的杂原子和/或1,2或3个各自独立地选自NR8的含杂原子的基团，其中 R8是H，C1-C4-烷基，氟化C1-C4-烷基，C1-C4烷基羰基或氟化C1-C4-烷基羰基，其中环状基团Ar可以带有1,2或3个取代基Ra，其中变量Ra具有在权利要求和说明书中给出的含义; 和其生理学耐受的酸加成盐。本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。

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