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182 条记录 (耗时 0.047 秒)

    Aminoalkyl-substituted 2-aminothiazoles and therapeutic agents containing them
    134.
    发明授权
    Aminoalkyl-substituted 2-aminothiazoles and therapeutic agents containing them 失效
    氨基取代的2-氨基丁酸和含有它们的治疗剂

    公开(公告)号：US5071864A

    公开(公告)日：1991-12-10

    申请号：US544900

    申请日：1990-06-28

    申请人： Beatrice Rendenbach-Mueller ,  Liliane Unger ,  Hans-Juergen Teschendorf

    发明人： Beatrice Rendenbach-Mueller ,  Liliane Unger ,  Hans-Juergen Teschendorf

    IPC分类号： C07D277/20 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/505 ,  A61P25/00 ,  A61P43/00 ,  C07D277/38 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46 ,  C07D417/00 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

    CPC分类号： C07D417/06 ,  C07D277/40 ,  C07D277/42 ,  C07D417/12

    摘要： Aminoalkyl-substituted 2-aminothiazole derivatives of the general formula I ##STR1## where R.sup.1 and R.sup.2, which may be identical or different, are each hydrogen, C.sub.1 -C.sub.5 -alkyl, phenyl or C.sub.1 -C.sub.5 -alkanoyl, R.sup.3 is C.sub.1 -C.sub.5 -alkyl, phenyl which is unsubstituted or monosubstituted by halogen, C.sub.1 -C.sub.5 -alkyl or C.sub.1 -C.sub.5 -alkoxy, or thienyl,n is an integer of from 2 to 6, andNR.sup.4 R.sup.5 is one of the groups a, b, c or d ##STR2## where Ar is a phenyl ring which is unsubstituted or monosubstituted by C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, halogen, hydroxyl, nitro or trifluoromethyl, or is pyridyl, pyrimidinyl or thienyl, R.sup.5 is H or C.sub.1 -C.sub.5 -alkyl and R.sup.7 is phenyl which is unsubstituted or monosubstituted by C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, halogen, hydroxyl or trifluoromethyl, or R.sup.7 is thienyl, with the proviso that R.sup.3 is C.sub.1 -C.sub.5 alkyl only when either R.sup.1 and R.sup.2 are not both simultaneously H or when NR.sup.4 R.sup.5 is the group d, and their salts with physiologically tolerated acids, their preparation, their use for the preparation of a drug, and the drugs.

    摘要翻译： 通式I的氨基烷基取代的2-氨基噻唑衍生物其中R 1和R 2可以相同或不同，各自为氢，C 1 -C 5 - 烷基，苯基或C 1 -C 5 - 烷酰基，R 3为C1- C 5 - 烷基，未被卤素，C 1 -C 5 - 烷基或C 1 -C 5 - 烷氧基或噻吩基单取代的苯基，n为2至6的整数，并且NR 4 R 5为a，b，c之一 或者其中Ar是未被取代或被C 1 -C 5 - 烷基，C 1 -C 5 - 烷氧基，卤素，羟基，硝基或三氟甲基单取代的苯环，或者是吡啶基，嘧啶基或噻吩基，R 5是 H或C1-C5-烷基，R7是未被取代或被C1-C5-烷基，C1-C5-烷氧基，卤素，羟基或三氟甲基单取代的苯基，或R7是噻吩基，条件是R3仅为C1-C5烷基 当R 1和R 2不同时为H时，或当NR4R5为基团d时，及其与生理上耐受的酸的盐，其制备方法，其用于制备药物的用途， 和药物。

    Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
    138.
    发明授权
    Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor 有权
    适用于治疗对5-羟色胺5-HT 6受体的调节作用的疾病的氮杂环丁啶化合物

    公开(公告)号：US08507469B2

    公开(公告)日：2013-08-13

    申请号：US12532406

    申请日：2008-03-20

    申请人： Thomas Schultz ,  Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Matthias Mayrer

    发明人： Thomas Schultz ,  Wilfried Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Matthias Mayrer

    IPC分类号： A61K31/397 ,  C07D403/04 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D403/04

    摘要： The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl; is a single or double bond; X1 and X2 are N, CRx1, NRx2 or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; wherein a maximum of 3 of the radicals X1, X2, Y1, Y2 and Y3 are selected from NRx1 and N; R1 is hydrogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, etc.; R2 is C1-C4-alkyl or C1-C4-haloalkyl; n is 0, 1 or 2; physiologically tolerated acid addition salts and the N-oxides thereof, pharmaceutical composition comprising them, a method for treating medical disorders selected from diseases of the central nervous system, addiction diseases or obesity, said method comprising administering an effective amount of such compounds to a subject in need and the use of such a compound for preparing a pharmaceutical compositions.

    摘要翻译： 本发明涉及式（I）化合物，其中A为C 1 -C 6 - 烷基，C 1 -C 6 - 卤代烷基，C 1 -C 6羟基烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 卤代烯基，C 3 -C 6 - 芳基-C 1 -C 4 - 烷基，芳基-C 2 -C 4 - 烯基，芳基或杂芳基; 是单键或双键; X1和X2是N，CRx1，NRx2或CRx3Rx4; Rx1，Rx3和Rx4是H，卤素，CN，NO2，C1-C6-烷基，C1-C6-烷氧基，C1-C6-烷基羰基等，或两个偕根基Rx3和Rx4与它们所在的碳原子一起 结合可形成羰基或3-至6-元碳环或杂环螺环状环; Rx2是氢，C1-C6-烷基，C1-C6-烷基羰基，C1-C6-卤代烷基等; 或两个连位基Rx1，Rx2，Rx3或Rx4与X1和X2一起形成五元或六元碳环或杂环稠环; Y1，Y2和Y3为N或CRy; Ry是H，卤素，CN，NO 2，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基羰基，C 1 -C 6 - 卤代烷基等; 其中基团X1，X2，Y1，Y2和Y3中的最多3个选自NRx1和N; R1是氢，C1-C6-烷基，C1-C6-羟基烷基，C1-C6-卤代烷基等; R2是C1-C4-烷基或C1-C4卤代烷基; n为0,1或2; 生理耐受的酸加成盐及其N-氧化物，包含它们的药物组合物，治疗选自中枢神经系统疾病，成瘾疾病或肥胖症的医学病症的方法，所述方法包括向受试者施用有效量的这些化合物 并且使用这种化合物来制备药物组合物。

    Heterocyclic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor
    139.
    发明授权
    Heterocyclic 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疾病的杂环化合物

    公开(公告)号：US08470810B2

    公开(公告)日：2013-06-25

    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 ,  C07D413/02

    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。