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11. 发明授权

US07851463B2 Heterocyclic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的疾病的杂环化合物
公开(公告)号：US07851463B2
公开(公告)日：2010-12-14
申请号：US11665399
申请日：2005-10-14
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 , A61K31/506 , A61K31/4439 , A61K31/40 , C07D239/42 , C07D401/04 , C07D207/04
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). 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.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。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。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。

12. 发明授权

US08202868B2 4-piperazinyl-pyrimidine compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
标题翻译：适用于治疗对多巴胺D3受体的调节作出反应的病症的4-哌嗪基 - 嘧啶化合物
公开(公告)号：US08202868B2
公开(公告)日：2012-06-19
申请号：US11659063
申请日：2005-08-08
申请人： Andreas Haupt , Liliane Unger , Karla Drescher , Ana Lucia Jongen-Relo , Roland Grandel , Wilfried Braje , Herve Geneste
发明人： Andreas Haupt , Liliane Unger , Karla Drescher , Ana Lucia Jongen-Relo , Roland Grandel , Wilfried Braje , Herve Geneste
IPC分类号： C07D417/12 , C07D403/12 , A61K31/505
CPC分类号： C07D239/42 , C07D239/52 , C07D239/56 , C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention relates to novel 4-piperazinylpyrimidine compounds. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. The 4-piperzinylpyrimidine compounds have the general formula I wherein Ar, X, A, R1 and R1a are as defined in the claims.
摘要翻译：本发明涉及新的4-哌嗪基嘧啶化合物。该化合物具有有价值的治疗特性，特别适用于治疗对多巴胺D3受体调节作出反应的疾病。 4-哌嗪基嘧啶化合物具有通式I，其中Ar，X，A，R 1和R 1a如权利要求中所定义。

13. 发明申请

US20090264437A1 4-Piperazinyl-Pyrimidine Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor 失效
标题翻译：适用于治疗响应多巴胺D3受体调节的疾病的4-哌嗪基 - 嘧啶化合物
公开(公告)号：US20090264437A1
公开(公告)日：2009-10-22
申请号：US11659063
申请日：2005-08-08
申请人： Andreas Haupt , Liliane Unger , Karla Drescher , Ana Lucia Jongen-Relo , Roland Grandel , Wilfried Braje , Herve Geneste
发明人： Andreas Haupt , Liliane Unger , Karla Drescher , Ana Lucia Jongen-Relo , Roland Grandel , Wilfried Braje , Herve Geneste
IPC分类号： A61K31/506 , A61P25/00 , C07D417/14 , C07D403/14 , C07D401/14 , C07D403/04
CPC分类号： C07D239/42 , C07D239/52 , C07D239/56 , C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention relates to novel 4-piperazinylpyrimidine compounds. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. The 4-piperzinylpyrimidine compounds have the general formula I wherein Ar, X, A, R1 and R1a are as defined in the claims.
摘要翻译：本发明涉及新的4-哌嗪基嘧啶化合物。该化合物具有有价值的治疗特性，特别适用于治疗对多巴胺D3受体调节作出反应的疾病。 4-哌嗪基嘧啶化合物具有通式I，其中Ar，X，A，R 1和R 1a如权利要求中所定义。

14. 发明授权

US08969552B2 Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译：芳基磺酰基甲基或芳基磺酰胺取代的芳族化合物，适用于治疗对多巴胺D3受体调节作用的疾病
公开(公告)号：US08969552B2
公开(公告)日：2015-03-03
申请号：US11665428
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry
IPC分类号： C07C311/44 , C07D207/10 , C07D211/10 , C07D215/38 , C07D263/32 , C07D413/04 , C07C311/21 , C07C311/29 , C07D239/84 , C07D277/82 , C07D311/04 , C07D491/04
CPC分类号： C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2602/10 , C07D207/10 , C07D211/10 , C07D215/38 , C07D239/84 , C07D263/32 , C07D277/82 , C07D311/04 , C07D413/04 , C07D491/04
摘要： The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH═N—, —CH═CH— or —N═CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the 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的芳族化合物，其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基团，其中Ar可以带有1个基团R a，并且其中Ar也可以带有1个或2个基团Rb; X为N或CH; Y是O，S，-CH = N - ， - CH = CH-或-N = CH-; A是CH 2，O或S; E为CR6R7或NR3; R 1是C 1 -C 4烷基，C 3 -C 4环烷基，C 3 -C 4环烷基甲基，C 3 -C 4链烯基，氟化C 1 -C 4烷基，氟化C 3 -C 4环烷基，氟化C 3 -C 4环烷基甲基， C4-烯基，甲酰基或C1-C3-烷基羰基; R1a为H，C2-C4-烷基，C3-C4-环烷基，C3-C4-烯基，氟化C1-C4-烷基，氟化C3-C4-环烷基或R1a和R2一起为（CH2）n，n为2 或3，或R 1a和R 2a一起为（CH 2）n，其中n为2或3; R2和R2a彼此独立地为H，CH3，CH2F，CHF2或CF3; R3是H或C1-C4-烷基; R6，R7彼此独立地选自H，C1-C2-烷基和氟化C1-C2-烷基; 及其生理上耐受的酸加成盐。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。

15. 发明申请

US20080045493A1 Heterocyclic Compounds Suitable For Treating Disorders That Respond To Modulation Of The Dopamine D3 Receptor 有权
公开(公告)号：US20080045493A1
公开(公告)日：2008-02-21
申请号：US11665399
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean Turner , Wilfried Braje , Roland Grandel , Christophe Henry , Gisela Backfisch , Armin Beyerbach , Wilfried Lubisch
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean Turner , Wilfried Braje , Roland Grandel , Christophe Henry , Gisela Backfisch , Armin Beyerbach , Wilfried Lubisch
IPC分类号： A61K31/397 , A61K31/4025 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/433 , A61K31/445 , A61K31/4523 , A61K31/496 , A61K31/4965 , A61K31/501 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/5375 , A61K31/538 , A61K31/541 , A61P25/16 , C07D205/04 , C07D207/08 , C07D211/28 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D411/12 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12
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, C1-C6-alkyl, C1-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C1-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-C4-alkylcarbonyl 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.

16. 发明申请

US20120220635A1 AMINOETHYLAROMATIC 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受体调节障碍的氨基甲醛化合物
公开(公告)号：US20120220635A1
公开(公告)日：2012-08-30
申请号：US13405646
申请日：2012-02-27
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
IPC分类号： A61K31/18 , C07D213/71 , A61P25/00 , C07D207/09 , A61K31/40 , C07C311/21 , A61K31/44
CPC分类号： C07D213/76 , C07C311/21 , C07C311/29 , C07C2601/02 , C07D207/09
摘要： The present invention relates to aromatic compounds of the formula (I) and the 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）的芳族化合物及其生理上耐受的酸加成盐。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病症的药物组合物中的用途。

17. 发明申请

US20090012074A1 Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the Dopamine D3 receptor 有权
标题翻译：芳基磺酰基甲基或芳基磺酰胺取代的芳族化合物，适用于治疗对多巴胺D3受体调节作用的疾病
公开(公告)号：US20090012074A1
公开(公告)日：2009-01-08
申请号：US11665428
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry
IPC分类号： A61K31/5375 , A61P25/00 , C07C311/01 , A61K31/18 , A61K31/47 , C07D215/00 , A61K31/473 , A61K31/436 , A61K31/4162 , C07D498/04 , C07D265/28
CPC分类号： C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2602/10 , C07D207/10 , C07D211/10 , C07D215/38 , C07D239/84 , C07D263/32 , C07D277/82 , C07D311/04 , C07D413/04 , C07D491/04
摘要： The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH═N—, —CH═CH— or —N═CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the 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的芳族化合物，其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基团，其中Ar可以带有1个基团R a，并且其中Ar也可以带有1个或2个基团Rb; X为N或CH; Y是O，S，-CH-N-，-CH-CH-或-N-CH-; A是CH 2，O或S; E为CR6R7或NR3; R 1是C 1 -C 4烷基，C 3 -C 4环烷基，C 3 -C 4环烷基甲基，C 3 -C 4链烯基，氟化C 1 -C 4烷基，氟化C 3 -C 4环烷基，氟化C 3 -C 4环烷基甲基， C4-烯基，甲酰基或C1-C3-烷基羰基; R1a为H，C2-C4-烷基，C3-C4-环烷基，C3-C4-烯基，氟化C1-C4-烷基，氟化C3-C4-环烷基或R1a和R2一起为（CH2）n，n为2 或3，或R 1a和R 2a一起为（CH 2）n，其中n为2或3; R2和R2a彼此独立地为H，CH3，CH2F，CHF2或CF3; R3是H或C1-C4-烷基; R6，R7彼此独立地选自H，C1-C2-烷基和氟化C1-C2-烷基; 及其生理上耐受的酸加成盐。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。

18. 发明授权

US08486984B2 Aminomethyl substituted bicyclic aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的疾病的氨基甲基取代的二环芳族化合物
公开(公告)号：US08486984B2
公开(公告)日：2013-07-16
申请号：US11665287
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
IPC分类号： A61K31/404 , A61K31/4184 , C07D209/14 , C07D235/14
CPC分类号： C07D471/04 , C07D209/14 , C07D209/62 , C07D235/14
摘要： The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I 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的氨基甲基取代的双环芳族化合物。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治疗的医学疾病的药物组合物中的用途与多巴胺D3受体配体。

19. 发明授权

US07834048B2 Azabicycloheptyl compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的疾病的氮杂双环庚基化合物
公开(公告)号：US07834048B2
公开(公告)日：2010-11-16
申请号：US11665421
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D401/12 , C07D209/52 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound of the formula (I) wherein R1 is H, C1-C6-alkyl which may be substituted by C3-C6-cycloalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; 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-C4-alkylcarbonyl 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R 1是H，可以被C 3 -C 6环烷基取代的C 1 -C 6烷基，氟化的C 1 -C 6 - 烷基，C 3 -C 6环烷基， C 3 - C 6 - 烯基，氟化C 3 -C 6 - 烯基，甲酰基，乙酰基或丙酰基; 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R a; 其中变量Ra具有权利要求书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。

20. 发明申请

US20090048326A1 Azabicycloheptyl compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的疾病的氮杂双环庚基化合物
公开(公告)号：US20090048326A1
公开(公告)日：2009-02-19
申请号：US11665421
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
IPC分类号： A61K31/403 , A61P25/00 , C07D209/52
CPC分类号： C07D401/12 , C07D209/52 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound of the formula (I) wherein R1 is H, C1-C6-alkyl which may be substituted by C3-C6-cycloalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; 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-C4-alkylcarbonyl 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R 1是H，可以被C 3 -C 6环烷基取代的C 1 -C 6烷基，氟化的C 1 -C 6 - 烷基，C 3 -C 6环烷基， C 3 - C 6 - 烯基，氟化C 3 -C 6 - 烯基，甲酰基，乙酰基或丙酰基; 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R a; 其中变量Ra具有权利要求书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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