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1. 发明申请

US20110294817A1 N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR 失效
标题翻译：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
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
IPC分类号： A61K31/496 , A61P13/12 , A61P25/00 , C07D401/04 , A61K31/4995
CPC分类号： C07D213/74 , C07D213/76 , C07D239/48 , C07D239/50 , C07D403/04 , C07D403/14 , C07D487/08
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。

2. 发明申请

US20090105224A1 Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor 失效
标题翻译：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
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
IPC分类号： C07D223/16 , A61K31/55 , A61P25/00
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。

3. 发明申请

US20060160809A1 N-[(piperazinyl)hetaryl]arylsulfonamide compounds 失效
公开(公告)号：US20060160809A1
公开(公告)日：2006-07-20
申请号：US10823317
申请日：2004-04-13
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer , Sean Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer , Sean Turner
IPC分类号： A61K31/53 , A61K31/506 , A61K31/501
CPC分类号： C07D213/76 , C07D213/74 , C07D239/69 , C07D401/04 , C07D487/08
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.

4. 发明授权

US07786105B2 Pyrimidine compounds and use thereof 有权
标题翻译：嘧啶化合物及其用途
公开(公告)号：US07786105B2
公开(公告)日：2010-08-31
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： C07D401/12 , C07D413/12 , C07D417/12 , A61K31/506
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，对多巴胺D3受体拮抗剂或激动剂的影响。

5. 发明授权

US08207160B2 Tetrahydrobenzazepines and their use in he modulation of the dopamine D3 receptor 失效
标题翻译：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
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
IPC分类号： A61P25/00 , A61K31/55 , C07D223/16 , C07D409/12
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。

6. 发明申请

US20080161322A1 Pyrimidine Compounds and Use Thereof 有权
标题翻译：嘧啶化合物及其用途
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。

7. 发明授权

US07723384B2 Keto lactam compounds and use thereof 有权
标题翻译：酮内酰胺化合物及其用途
公开(公告)号：US07723384B2
公开(公告)日：2010-05-25
申请号：US10582285
申请日：2004-12-10
申请人： Wilfried Lubisch , Andreas Haupt , Wilfried Braje , Herve Geneste
发明人： Wilfried Lubisch , Andreas Haupt , Wilfried Braje , Herve Geneste
IPC分类号： C07D403/12 , C07D401/12 , C07D223/16 , A61K31/55
CPC分类号： C07D401/12 , C07D223/16 , C07D403/12
摘要： The invention relates to novel keto lactam compounds, hydrogenated derivatives and tautomers thereof. These compounds have valuable therapeutic properties and are particularly suited for treating diseases that respond to the modulation of the dopamine D3 receptor. The keto lactams have general formula (I), wherein: (a) represents a group of formulas (b) or (c), wherein D is bound to the nitrogen atom and W, Rp and Rq have the meanings cited in Claim 1; —B— represents a bond or (d), wherein Rm and Rn have the meanings cited in Claim 1; (e) represents a single bond or a double bond; Rv, Rw, Rx and Ry have the meanings cited in Claim 1; D represents a linear or branched 2 to 10-membered alkylene chain that can have, as chain members, a heteroatom group K, which is selected among O, S, S(O), S(O)2, N—R8, CO—O, C(O)NR8 and/or 1 or 2 non-adjacent carbonyl groups and which can have a cycloalkane diyl group and/or a double or triple bond; (f) represents a saturated or monounsaturated monocyclic nitrogen heterocyclic compound having 5 to 8 cyclic members or a bicyclic saturated nitrogen heterocyclic compound having 7 to 12 cyclic members.
摘要翻译：本发明涉及新型酮内酰胺化合物，氢化衍生物及其互变异构体。这些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。酮内酰胺具有通式（I），其中：（a）表示式（b）或（c）中的基团，其中D与氮原子结合，W，Rp和Rq具有权利要求1所述的含义; -B-表示键或（d），其中Rm和Rn具有权利要求1中引用的含义; （e）表示单键或双键; Rv，Rw，Rx和Ry具有权利要求1中引用的含义; D表示可以具有作为链成员的选自O，S，S（O），S（O）2，N-R8，CO（C 1 -C 6）中的杂原子基团K的直链或支链2至10元亚烷基链 -O，C（O）NR 8和/或1或2个不相邻的羰基，并且其可具有环烷烃二基和/或双键或三键; （f）表示具有5〜8个环状成员的饱和或单不饱和单环氮杂环化合物或具有7〜12个环状成员的双环饱和氮杂环化合物。

8. 发明授权

US08476275B2 N-[piperazinyl hetaryl]arylsufonamide compounds with affinity for the dopamine D3 receptor 失效
标题翻译：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
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean Colm Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean Colm Turner
IPC分类号： A61K31/496 , A61K31/506 , C07D213/72 , C07D213/74 , C07D239/48
CPC分类号： C07D213/74 , C07D213/76 , C07D239/48 , C07D239/50 , C07D403/04 , C07D403/14 , C07D487/08
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。

9. 发明申请

US20070054918A1 N-[(piperazinyl)hetary]arylsulfonamide compounds with affinity for the dopamine d3 receptor 审中-公开
公开(公告)号：US20070054918A1
公开(公告)日：2007-03-08
申请号：US10552842
申请日：2004-04-13
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer , Sean Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer , Sean Turner
IPC分类号： A61K31/506 , A61K31/501 , A61K31/496 , C07D403/14 , C07D403/02
CPC分类号： C07D213/74 , C07D213/76 , C07D239/48 , C07D239/50 , C07D403/04 , C07D403/14 , C07D487/08
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.

10. 发明申请

US20050137186A1 Tetrahydrobenzazepines and their use 审中-公开
标题翻译：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
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer
IPC分类号： A61K31/55 , C07D223/16 , C07D409/12
CPC分类号： C07D223/16 , A61K31/55 , 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 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。

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