Tetrahydrobenzazepines and their use in he modulation of the dopamine D3 receptor
    1.
    发明授权
    Tetrahydrobenzazepines and their use in he modulation of the dopamine D3 receptor 失效
    四氢苯并吖嗪及其在多巴胺D3受体调节中的应用

    公开(公告)号:US08207160B2

    公开(公告)日:2012-06-26

    申请号:US10583590

    申请日:2004-12-17

    CPC分类号: C07D223/16 C07D409/12

    摘要: The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.

    摘要翻译: 本发明涉及通式Ⅰ的四氢苯并吖庚因,其中变量Ar,A,B,Y,R 1和R 2具有权利要求1所示的含义,以及这些化合物的N-氧化物,生理上耐受的酸加成盐 的这些化合物和N-氧化物的生理上耐受的酸加成盐。 本发明还涉及药物组合物,其包含至少一种式I的四氢苯并氮杂化合物,I的物理耐受的酸加成盐,式I化合物的N-氧化物和/或其物理上耐受的酸加成盐 I的N-氧化物,并且进一步使用根据本发明的化合物用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3激动剂的病症。 根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。

    N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR
    2.
    发明申请
    N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR 失效
    具有多巴胺D3受体亲和性的N- [哌嗪基]维生素A亚磺酰胺化合物

    公开(公告)号:US20110294817A1

    公开(公告)日:2011-12-01

    申请号:US13117269

    申请日:2011-05-27

    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。

    Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor
    3.
    发明申请
    Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor 失效
    四氢苯并吖嗪及其在调节多巴胺d3受体中的用途

    公开(公告)号:US20090105224A1

    公开(公告)日:2009-04-23

    申请号:US10583590

    申请日:2004-12-17

    CPC分类号: C07D223/16 C07D409/12

    摘要: The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides.The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.

    摘要翻译: 本发明涉及通式Ⅰ的四氢苯并吖庚因,其中变量Ar,A,B,Y,R 1和R 2具有权利要求1所示的含义,以及这些化合物的N-氧化物,生理上耐受的酸加成盐 的这些化合物和N-氧化物的生理上耐受的酸加成盐。 本发明还涉及药物组合物,其包含至少一种式I的四氢苯并氮杂化合物,I的物理耐受的酸加成盐,式I化合物的N-氧化物和/或其物理上耐受的酸加成盐 I的N-氧化物,并且进一步使用根据本发明的化合物用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3激动剂的病症。 根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。

    N-[piperazinyl hetaryl]arylsufonamide compounds with affinity for the dopamine D3 receptor
    4.
    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

    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。

    N-[(piperazinyl)hetaryl]arylsulfonamide compounds

    公开(公告)号:US20060160809A1

    公开(公告)日:2006-07-20

    申请号:US10823317

    申请日:2004-04-13

    摘要: The invention relates 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.

    N-[(piperazinyl)hetary]arylsulfonamide compounds with affinity for the dopamine d3 receptor

    公开(公告)号:US20070054918A1

    公开(公告)日:2007-03-08

    申请号:US10552842

    申请日:2004-04-13

    摘要: The invention relates 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.

    Tetrahydrobenzazepines and their use
    7.
    发明申请
    Tetrahydrobenzazepines and their use 审中-公开
    四氢苯并吖嗪及其用途

    公开(公告)号:US20050137186A1

    公开(公告)日:2005-06-23

    申请号:US10740092

    申请日:2003-12-18

    摘要: The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meaninigs indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical compositon that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond benefically to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.

    摘要翻译: 本发明涉及通式I的四氢苯并吖庚因,其中变量Ar,A,B,Y,R 1和R 2 2具有权利要求1所示的平均分子,如 以及这些化合物的N-氧化物,这些化合物的生理上耐受的酸加成盐和N-氧化物的生理上耐受的酸加成盐。 本发明还涉及药物组合物,其包含至少一种式I的四氢苯并氮杂化合物,I的物理耐受的酸加成盐,式I化合物的N-氧化物和/或物理上耐受的酸加成盐 I的N-氧化物,并且还涉及使用根据本发明的化合物治疗对多巴胺D 3受体拮抗剂或多巴胺D 3激动剂有益的反应的病症 。 根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。