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    HETEROCYCLIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
    7.
    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。

    Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (VR1) and uses thereof
    8.
    发明授权
    Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (VR1) and uses thereof 有权
    抑制香草素受体亚型1（VR1）的噻吩并吡啶基化合物及其用途

    公开(公告)号：US07875627B2

    公开(公告)日：2011-01-25

    申请号：US11293012

    申请日：2005-12-02

    申请人： Sean C. Turner ,  Tammie K. Jinkerson ,  Arthur R. Gomtsyan ,  Chih-Hung Lee

    发明人： Sean C. Turner ,  Tammie K. Jinkerson ,  Arthur R. Gomtsyan ,  Chih-Hung Lee

    IPC分类号： A61K31/4743 ,  C07D498/02

    CPC分类号： C07D495/04 ,  C07D498/04

    摘要： The present invention discloses fused thienopyridyl compounds of general formula (I) wherein X1-X6, R5-R7, Z1 and L are as defined in the description. The resent invention also discloses a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain, urinary incontinence, bladder overactivity, and inflammatory thermal hyperalgesia in mammals, and pharmaceutical compositions including those compounds.

    摘要翻译： 本发明公开了通式（I）的稠合噻吩并吡啶基化合物，其中X1-X6，R5-R7，Z1和L如说明书中所定义。 本发明还公开了使用这些化合物抑制哺乳动物中的VR1受体的方法，用于控制哺乳动物中的疼痛，尿失禁，膀胱过度活动和炎性热痛觉过敏的方法，以及包括那些化合物的药物组合物。

    Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    10.
    发明授权
    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：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。