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    Aminoethylaromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    21.
    发明授权
    Aminoethylaromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
    适用于治疗响应于多巴胺D3受体调节的疾病的氨基乙基芳族化合物

    公开(公告)号：US08232426B2

    公开(公告)日：2012-07-31

    申请号：US11665288

    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： C07C303/00 ,  A61K31/18

    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 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; 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, 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, or R1a and R2 together are (CH2)n with n being 2, 3 or 4, or R1a and R2a together are (CH2)n with n being 2, 3 or 4; R2 and R2a are are independently of each other H, C1-C4-alkyl or fluorinated C1-C4-alkyl or R2a and R2 together are (CH2)m with m being 1, 2, 3, 4 or 5; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, fluorine, C1-C4-alkyl and fluorinated C1-C4-alkyl or together form a moiety (CH2)p with p being 2, 3, 4 or 5; 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; 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; R 1a是H，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 - 烯基，氟化C 1 -C 4 - 烷基，氟化C 3 -C 4 - 环烷基，氟化的C 3 -C 4环烷基甲基， C 3 -C 4 - 烯基或R 1a和R 2一起为（CH 2）n，其中n为2,3或4，或者R 1a和R 2a一起为（CH 2）n，n为2,3或4; R2和R2a彼此独立地为H，C1-C4-烷基或氟化C1-C4-烷基或R2a和R2一起为（CH2）m，其中m为1,2,3,4或5; R3是H或C1-C4-烷基; R 6，R 7彼此独立地选自H，氟，C 1 -C 4 - 烷基和氟化的C 1 -C 4 - 烷基或一起形成部分（CH 2）p，其中p为2,3,4或5; 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。

    Aminomethyl Substituted Bicyclic Aromatic Compounds Suitable for Treating Disorders That Respond to Modulation of the Dopamine D3 Receptor
    22.
    发明申请
    Aminomethyl Substituted Bicyclic Aromatic Compounds Suitable for Treating Disorders That Respond to Modulation of the Dopamine D3 Receptor 失效

    公开(公告)号：US20110144146A1

    公开(公告)日：2011-06-16

    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： A61K31/437 ,  C07D209/04 ,  A61K31/405 ,  A61K31/16 ,  C07C331/00 ,  C07D235/00 ,  A61K31/415 ,  C07D471/02 ,  A61K31/40 ,  A61P25/00

    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 wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, 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, 0 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; X is a covalent bond or N—R2, CHR2, CHR2CH2, N or C—R2; Y is N—R2a, CHR2a, CHR2aCH2 or CHR2aCH2CH2; is a single bond or a double bond; E is CH2 or NR3; R1 is H, 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, C1C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl, R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3 or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2 or 3; R3 is H or C1C4-alkyl; R4 and R5 independently of each other are H, C1-C4-alkyl, fluorinated C1-C4-alkyl or C1-C4-alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring; R6 and R7 independently of each other are H or halogen; and the physiologically tolerated acid addition salts thereof.

    6-amino(aza)indane compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    23.
    发明授权
    6-amino(aza)indane compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 失效
    适用于治疗对多巴胺D3受体调节作出反应的病症的6-氨基（氮杂）二氢化茚化合物

    公开(公告)号：US07759397B2

    公开(公告)日：2010-07-20

    申请号：US11665420

    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： A61K31/135 ,  C07C211/00

    CPC分类号： C07D239/38 ,  C07C311/21 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2602/08 ,  C07D221/06 ,  C07D333/34 ,  C07D401/12 ,  C07D409/12

    摘要： The present invention relates to 6-amino(aza)indane compound 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 I or 2 radicals Rb; X is N or CH; 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 or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及式（I）的6-氨基（氮杂）二氢化茚化合物，其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基，其中Ar可以带有1个基团Ra，其中Ar也可以 携带I或2个基团Rb; X为N或CH; 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是H或R1a，R2或R1a和R2a同时为（CH2）n，n为1,2,3或4; R2和R2a各自独立地为H，CH3，CH2F，CHF2或CF3; R3是H或C，-C4-烷基; 和这些化合物的生理上耐受的酸加成盐。 本发明还涉及包含至少一种式（I）化合物或其药学上可接受的盐的药物组合物和治疗易受多巴胺D3受体配体治疗的医学疾病的方法，所述方法包括施用有效量 的至少一种式（I）化合物或其药学上可接受的盐。

    6-Amino(Aza)Indane Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor
    24.
    发明申请
    6-Amino(Aza)Indane 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受体调节的疾病的6-氨基（氮杂）吲哚化合物

    公开(公告)号：US20080318996A1

    公开(公告)日：2008-12-25

    申请号：US11665420

    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： A61K31/435 ,  C07C311/15 ,  A61K31/18 ,  A61P25/00 ,  C07D221/06

    CPC分类号： C07D239/38 ,  C07C311/21 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2602/08 ,  C07D221/06 ,  C07D333/34 ,  C07D401/12 ,  C07D409/12

    摘要： The present invention relates to 6-amino(aza)indane compound 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 R6 and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; 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 or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及式（I）的6-氨基（氮杂）二氢化茚化合物，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可以携带1个基团R6，并且其中Ar也可以 携带I或2个基团Rb; X为N或CH; 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是H或R1a，R2或R1a和R2a同时为（CH2）n，n为1,2,3或4; R2和R2a各自独立地为H，CH3，CH2F，CHF2或CF3; R3是H或C，-C4-烷基; 和这些化合物的生理上耐受的酸加成盐。 本发明还涉及包含至少一种式（I）化合物或其药学上可接受的盐的药物组合物和治疗易受多巴胺D3受体配体治疗的医学疾病的方法，所述方法包括施用有效量 的至少一种式（I）化合物或其药学上可接受的盐。