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    TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    23.
    发明申请
    TRIAZOLE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开
    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。

    Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the Dopamine D3 receptor
    24.
    发明申请
    Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the Dopamine D3 receptor 有权
    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。

    N-[piperazinyl hetaryl]arylsufonamide compounds with affinity for the dopamine D3 receptor
    25.
    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

    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。

    HETEROCYCLIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    27.
    发明申请
    HETEROCYCLIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 失效
    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。

    N-[(piperazinyl)hetary]arylsulfonamide compounds with affinity for the dopamine d3 receptor
    29.
    发明申请
    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.

    Tetrahydrobenzazepines and their use
    30.
    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

    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。