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    2-AMINOQUINOLINE DERIVATIVES AS 5-HT ( 5A) RECEPTOR ANTAGONISTS
    1.
    发明申请
    2-AMINOQUINOLINE DERIVATIVES AS 5-HT ( 5A) RECEPTOR ANTAGONISTS 审中-公开
    作为5-HT（5A）受体拮抗剂的2-氨基喹啉衍生物

    公开(公告)号：WO2009109493A3

    公开(公告)日：2009-10-29

    申请号：PCT/EP2009052195

    申请日：2009-02-25

    Applicant: HOFFMANN LA ROCHE ,  KOLCZEWSKI SABINE ,  RIEMER CLAUS ,  ROCHE OLIVIER ,  STEWARD LUCINDA ,  WICHMANN JUERGEN ,  WOLTERING THOMAS

    Inventor： KOLCZEWSKI SABINE ,  RIEMER CLAUS ,  ROCHE OLIVIER ,  STEWARD LUCINDA ,  WICHMANN JUERGEN ,  WOLTERING THOMAS

    IPC: C07D215/38 ,  A61K31/47 ,  A61K31/4709 ,  A61P25/00 ,  C07D405/12

    CPC classification number: C07D215/38 ,  C07D405/12

    Abstract: The present invention is concerned with 2-Aminoquinoline derivatives as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders. In particular, the present invention is concerned with compounds of the general Formula (I) wherein R1 and -Z-Ar1 are as described herein.

    Abstract translation: 本发明涉及作为5-HT5A受体拮抗剂的2-氨基喹啉衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。 本发明的活性化合物可用于预防和/或治疗抑郁症，焦虑症，精神分裂症，恐慌症，广场恐怖症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆，病症 饮食行为，性功能障碍，睡眠障碍，滥用药物，运动障碍如帕金森病，精神病或胃肠道疾病。 特别地，本发明涉及通式（I）的化合物，其中R1和-Z-Ar1如本文所述。

    CHLORO-SUBSTITUTED GUANIDINES
    2.
    发明申请
    CHLORO-SUBSTITUTED GUANIDINES 审中-公开
    氯取代的瓜氨酸

    公开(公告)号：WO2007000392A3

    公开(公告)日：2007-04-05

    申请号：PCT/EP2006063267

    申请日：2006-06-16

    Applicant: HOFFMANN LA ROCHE ,  ALANINE ALEXANDER ,  GOBBI LUCA CLAUDIO ,  KOLCZEWSKI SABINE ,  LUEBBERS THOMAS ,  PETERS JENS-UWE ,  STEWARD LUCINDA

    Inventor： ALANINE ALEXANDER ,  GOBBI LUCA CLAUDIO ,  KOLCZEWSKI SABINE ,  LUEBBERS THOMAS ,  PETERS JENS-UWE ,  STEWARD LUCINDA

    IPC: C07D239/84 ,  A61K31/517 ,  A61P25/18 ,  A61P25/24

    CPC classification number: C07D239/42 ,  C07D403/12 ,  C07D405/12

    Abstract: The present invention relates to compounds of formula wherein R 1 is hydrogen or halogen; R 2 is lower alkyl; R 3 is hydrogen, lower alkyl, -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -phenyl optionally substituted by halogen, or is lower alkyl substituted by halogen, or is -(CH 2 ) n -heterocyclyl, -(CH 2 ) n N-di-lower alkyl, -(CH 2 ) n NHC(O)-lower alkyl, adamantly or -(CH 2 ) n -O-lower alkyl; n is 0, 1, 2 or 3; and pharmaceutically acceptable acid addition salts and tautomers thereof. It has been found that the compounds of formula I have a good activity on the 5-HT 5A receptor. Therefore, the invention provides the use of a compound of formula I or a pharmaceutically acceptable salt thereof for the treatment of diseases, related to this 15 receptor.

    Abstract translation: 本发明涉及下式的化合物：其中R 1是氢或卤素; R 2是低级烷基; R 3是氢，低级烷基， - （CH 2 SUB）n - 环烷基， - （CH 2 SUB） 任选被卤素取代的苯基或被卤素取代的低级烷基，或为 - （CH 2）n - 杂环基， - （（C 1 -C 4） （CH 2）n C（O） - （CH 2）n C（O） - （CH 2） 低级烷基，金刚烷基或 - （CH 2）n -O-低级烷基; n是0,1,2或3; 及其药学上可接受的酸加成盐和互变异构体。 已经发现式I化合物对5-HT 5A受体具有良好的活性。 因此，本发明提供了式I化合物或其药学上可接受的盐在治疗与该受体有关的疾病中的用途。

    DUAL MODULATORS OF 5-HT2A AND D3 RECEPTORS
    3.
    发明申请
    DUAL MODULATORS OF 5-HT2A AND D3 RECEPTORS 审中-公开
    5-HT2A和D3受体的双重调节剂

    公开(公告)号：WO2009013212A3

    公开(公告)日：2009-06-11

    申请号：PCT/EP2008059356

    申请日：2008-07-17

    Applicant: HOFFMANN LA ROCHE ,  GOBBI LUCA ,  JAESCHKE GEORG ,  ROCHE OLIVIER ,  RODRIGUEZ SARMIENTO ROSA MARIA ,  STEWARD LUCINDA

    Inventor： GOBBI LUCA ,  JAESCHKE GEORG ,  ROCHE OLIVIER ,  RODRIGUEZ SARMIENTO ROSA MARIA ,  STEWARD LUCINDA

    IPC: C07D413/04 ,  A61K31/454 ,  C07D413/14

    CPC classification number: C07D413/04 ,  C07D413/14

    Abstract: The present invention relates to compounds of the general formula (I), wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.

    Abstract translation: 本发明涉及通式（I）的化合物，其中R 1，R 2，X和n如说明书中所定义，作为血清素5-HT 2a和多巴胺D 3受体的双重调节剂，它们的制造方法，含有它们的药物组合物和 他们作为药物的用途。 通式（I）的化合物对多巴胺D3和5-羟色胺（5-羟色胺; 5-HT）5-HT 2A受体具有高亲和力，并且在治疗精神障碍以及其他疾病例如抑郁和焦虑方面是有效的， 药物依赖，痴呆和记忆障碍。

    DERIVADOS DE QUINOLINA CON PROPIEDADES DE ENLACE A 5-HT.
    10.
    发明专利
    DERIVADOS DE QUINOLINA CON PROPIEDADES DE ENLACE A 5-HT. 未知

    公开(公告)号：ES2347193T3

    公开(公告)日：2010-10-26

    申请号：ES07803542

    申请日：2007-09-18

    Applicant: HOFFMANN LA ROCHE

    Inventor： KOLCZEWSKI SABINE ,  RIEMER CLAUS ,  STEWARD LUCINDA ,  WICHMANN JUERGEN ,  WOLTERING THOMAS

    IPC: C07D215/38 ,  A61K31/4725 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

    Abstract: Compuestos de la fórmula general (I) **(Ver fórmula)** en la que X es un enlace, -CH2CH2-, -CH=CH-, -CH2O-, -CH2NR-, -CH2S(O)-, -CH2S(O)2-, -O-, -OCH2CH2-, -S-, -SCH2-, -OCH2CH2S(O)-, -OCH2CH2S(O)2-, -CH2NRCO-, -CH2NRCH2-, **(Ver fórmula)** -NRS(O) 2NR-, -NHCHR-, -NR- o -NRS(O)2-; y en la que X puede insertarse en ambas direcciones dentro de la fórmula (I); Y es un enlace, -CHR- o -OCH2CH2-; R es hidrógeno o alquilo inferior; Ar1/Ar2 con independencia entre sí son arilo o heteroarilo de 5 a 10 eslabones, opcionalmente sustituido por alquilo inferior, alcoxi inferior, haloalcoxi inferior, halógeno, -CF3, -CH2OH, -CH2O-alquilo inferior, cicloalquilo de 3 a 10 eslabones, heterocicloalquilo de 5 a 10 eslabones, -CH2O(CH2)2O-alquilo inferior, -S(O)2-alquilo inferior o -S(O)2NHR; en donde "radical arilo" puede comprender uno o mas anillos no-aromático(s) fusionados que puede(n) contener heteroátomos elegidos entre N,O o S, y en donde "alquilo inferior" denota un grupo de cadena que contiene de 1 a 7 átomos de carbono y "haloalcoxi inferior" denota un grupo alcoxi C1-6 que está unido vía un átomo de oxígeno y sustituido por uno o mas halógenos; o sus sales de adición de ácido farmacéuticamente aceptables.

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