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    Substituted oxindole compounds
    2.
    发明授权
    Substituted oxindole compounds 有权
    取代的羟吲哚化合物

    公开(公告)号：US08486931B2

    公开(公告)日：2013-07-16

    申请号：US12529542

    申请日：2008-02-29

    Applicant: Herve Genesle ,  Thorsten Oost ,  Charles W. Hutchins ,  Liliane Unger ,  Wilfried Hornberger ,  Wilfried Lubisch ,  Astrid Netz ,  Alfred Hahn

    Inventor： Herve Genesle ,  Thorsten Oost ,  Charles W. Hutchins ,  Liliane Unger ,  Wilfried Hornberger ,  Wilfried Lubisch ,  Astrid Netz ,  Wolfgang Wernet

    IPC: A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/551

    CPC classification number: C07D401/14 ,  C07D401/04 ,  C07D401/12 ,  C07D471/08

    Abstract: The present invention relates to compounds of the general formula (I) in which A, B, R1, R2 and Het have the meaning given in claim 1; Y is a bivalent group of the formula in which D is C1-C3-alkylene, where D may have a substituent R5; R3 is hydrogen, C1-C8-alkyl or together with R4 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, and R4 is hydrogen, C1-C8-alkyl or together with R3 is C1-C3-alkylene which may have a radical R5a, or together with R5 is C1-C3-alkylene, where R5 together with R5a, where present, are a bond or C1-C3-alkylene; and where one of the following conditions is satisfied: R3 together with R4 is C1-C3-alkylene which may have a radical R5a; or R3 together with R5 is C1-C3-alkylene; or R4 together with R5 is C1-C3-alkylene where the radical A is different from phenyl when the radical B is phenyl or naphthyl; and medicaments which comprise such compounds and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.

    Abstract translation: 本发明涉及通式（I）的化合物，其中A，B，R1，R2和Het具有权利要求1中给出的含义; Y是下式的二价基团，其中D是C 1 -C 3 - 亚烷基，其中D可以具有取代基R 5; R 3是氢，C 1 -C 8烷基或与R 4一起是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，并且R 4是氢，C 1 -C 8 - 烷基或与 R 3是可以具有基团R 5a的C 1 -C 3亚烷基，或与R 5一起为C 1 -C 3 - 亚烷基，其中R 5与存在的R a a为键或C 1 -C 3 - 亚烷基; 并且其中满足以下条件之一：R 3与R 4一起可以具有基团R 5a的C 1 -C 3 - 亚烷基; 或R 3与R 5一起为C 1 -C 3 - 亚烷基; 或R 4与R 5一起为C 1 -C 3 - 亚烷基，其中基团B为苯基或萘基时，基团A不同于苯基; 以及包含这些化合物的药物及其用于预防和/或治疗加压素依赖性和/或催产素依赖性疾病的用途。

    N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR
    5.
    发明申请
    N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR 失效
    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

    Applicant: Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer ,  Sean C. Turner

    Inventor： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer ,  Sean C. Turner

    IPC: A61K31/496 ,  A61P13/12 ,  A61P25/00 ,  C07D401/04 ,  A61K31/4995

    CPC classification number: C07D213/74 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D403/04 ,  C07D403/14 ,  C07D487/08

    Abstract: 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.

    Abstract translation: 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。

    Poly(ADP-ribose) polymerase-gene
    9.
    发明授权
    Poly(ADP-ribose) polymerase-gene 失效
    聚（ADP-核糖）聚合酶基因

    公开(公告)号：US07754459B1

    公开(公告)日：2010-07-13

    申请号：US09701586

    申请日：1999-06-04

    Applicant: Michael Kock ,  Thomas Höger ,  Burkhard Kröger ,  Bernd Otterbach ,  Wilfried Lubisch ,  Hans-Georg Lemaire

    Inventor： Michael Kock ,  Thomas Höger ,  Burkhard Kröger ,  Bernd Otterbach ,  Wilfried Lubisch ,  Hans-Georg Lemaire

    IPC: C12N9/12

    CPC classification number: C12N9/1077 ,  A01K2217/05 ,  A61K38/00 ,  A61K49/00 ,  C07K16/40 ,  C07K2317/76 ,  C07K2319/00 ,  C12Q1/48 ,  C12Y204/0203 ,  G01N2333/91142

    Abstract: The invention relates to poly(ADP-ribose)polymerase (PARP) homologs which have an amino acid sequence which has a) a functional NAD+ binding domain and b) no zinc finger sequence motif of the general formula CX2CXmHX2C  in which  m is an integral value from 28 or 30, and the X radicals are, independently of one another, any amino acid; and the functional equivalents thereof; nucleic acids coding therefor; antibodies with specificity for the novel protein; pharmaceutical and gene therapy compositions which comprise products according to the invention; methods for the analytical determination of the proteins and nucleic acids according to the invention; methods for identifying effectors or binding partners of the proteins according to the invention; novel PARP effectors; and methods for determining the activity of such effectors.

    Abstract translation: 本发明涉及具有氨基酸序列的聚（ADP-核糖）聚合酶（PARP）同系物，该氨基酸序列具有a）功能性的NAD +结合域，b）没有通式CX2CXmHX2C的锌指序列基序，其中m是整数值 28或30个，X基彼此独立地为任何氨基酸; 及其功能等同物; 为此编码的核酸; 对新蛋白具有特异性的抗体; 包括根据本发明的产品的药物和基因治疗组合物; 根据本发明的用于分析测定蛋白质和核酸的方法; 用于鉴定根据本发明的蛋白质的效应物或结合配偶体的方法; 新型PARP效应器; 以及用于确定这种效应物的活性的方法。

    Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor
    10.
    发明申请
    Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor 失效
    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

    Applicant: Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

    Inventor： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

    IPC: C07D223/16 ,  A61K31/55 ,  A61P25/00

    CPC classification number: C07D223/16 ,  C07D409/12

    Abstract: 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.

    Abstract translation: 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。

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