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    MUSCARINIC AGONISTS TO TREAT IMPULSE CONTROL DISORDERS
    1.
    发明申请
    MUSCARINIC AGONISTS TO TREAT IMPULSE CONTROL DISORDERS 审中-公开
    治疗肿瘤控制障碍的药物治疗

    公开(公告)号：WO2007128674A2

    公开(公告)日：2007-11-15

    申请号：PCT/EP2007053934

    申请日：2007-04-23

    Applicant: SOLVAY PHARM BV ,  DE BRUIN NATASJA M W J ,  VAN DRIMMELEN MARLIES L ,  HERREMANS ARNOLDUS H J ,  TULP MARTINUS TH M ,  KRUSE CORNELIS G

    Inventor： DE BRUIN NATASJA M W J ,  VAN DRIMMELEN MARLIES L ,  HERREMANS ARNOLDUS H J ,  TULP MARTINUS TH M ,  KRUSE CORNELIS G

    IPC: A61K31/00 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/551 ,  A61P25/18

    CPC classification number: A61K31/439 ,  A61K31/00 ,  A61K31/4439 ,  A61K31/551 ,  A61K31/5513

    Abstract: The invention relates to a novel use of compounds and pharmaceutically acceptable salts thereof, which are muscarinic, in particular muscarine-1 (M 1 ) agonists. These compounds are useful for the preparation of medicaments for treatment, amelioration or prevention of impulse control disorders. These include impulse control disorders 'Not Elsewhere Classified' such as intermittent explosive disorder, pyromania, kleptomania, pathological gambling and trichotillomania; and impulse control disorders 'Not Otherwise Specified' such as: compulsive buying disorder, binge eating and binge drinking disorder, impulsive self-injurious behaviour such as pathological skin picking, nail-biting and nose-picking, gouging, head banging and self- biting; paraphilic sexual addictions, including exhibitionism, fetishism, frotteurism, pedophilia, masochism, sadism, transvestic fetishism and voyeurism; compulsive Internet use and excessive mobile phone use.

    Abstract translation: 本发明涉及毒蕈碱型化合物及其药学上可接受的盐，特别是毒蕈碱-1（M 1 H 1）激动剂的新用途。 这些化合物可用于制备用于治疗，改善或预防冲动控制障碍的药物。 这些包括脉冲控制障碍“非其他分类”，如间歇性爆发性疾病，pyromania，kleptomania，病态赌博和拔毛病; 和冲动控制障碍“无其他指定”，如：强迫性购买障碍，暴饮暴食饮酒障碍，脉冲性自我伤害行为，如病理性皮肤采摘，咬咬和鼻子抽搐，气刨，头部撞击和自咬 ; 淫秽性成瘾，包括露胸主义，拜物教，愚蠢主义，恋童癖，受虐狂，虐待狂，变性拜拜教和窥视主义; 强制上网使用和手机使用过多。

    TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES
    6.
    发明申请
    TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES 审中-公开
    四氢吡啶-4-基吲哚类化合物对多巴胺D2受体和5-羟色胺再灌注位点的亲和力组合

    公开(公告)号：WO2006061373A3

    公开(公告)日：2006-09-21

    申请号：PCT/EP2005056501

    申请日：2005-12-06

    Applicant: SOLVAY PHARM BV ,  VAN HES ROELOF ,  SMID PIETER ,  KRUSE CORNELIS G ,  TULP MARTINUS TH M

    Inventor： VAN HES ROELOF ,  SMID PIETER ,  KRUSE CORNELIS G ,  TULP MARTINUS TH M

    IPC: C07D401/14 ,  A61K31/519 ,  A61P25/00 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

    CPC classification number: C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

    Abstract: The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine -D 2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin -4-yl indoles of the formula (I) and tautomers, stereoisomers, prodrugs, N -oxides, pharmacologically acceptable salts, hydrates and solvates thereof , wherein: - R 1 is hydrogen, halogen, alkyl (C 1-3 ) or alkoxy(C 1-3 ), CN or CF 3 , - R 2 is hydrogen or alkyl (C 1-3 ), R 3 is hydrogen or alkyl (C 1-3 ), - Z is hydrogen or alkyl (C 1-3 ), alkoxy(C 1-3 ) or alkylthio(C 1-3 ), - A is hydrogen or alkyl (C 1-3 ), or - A and Z together form a saturated or (partly) unsaturated 5 - or 6- membered ring which may be substituted with halogen, alkyl (C 1-3 ) or phenyl, in which ring Z represents carbon, sulfur of nitrogen .

    Abstract translation: 本发明涉及一组具有双重作用模式的新四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D受体的亲和力，涉及制备这些化合物的方法和 涉及可用于合成所述四氢吡啶-4-基吲哚的新颖中间体。 本发明还涉及本文公开的化合物用于制造产生有益效果的药物的用途。 本发明涉及式（I）的新型四氢吡啶-4-基吲哚及其互变异构体，立体异构体，前药，N-氧化物，药理学上可接受的盐，水合物和溶剂化物，其中：-R 1是 氢，卤素，烷基（C 1-3 1-3）或烷氧基（C 1-3 1-3），CN或CF 3，-R 2是氢或烷基（C 1-3 1-3），R 3是氢或烷基（C 1-3 1-3） ，-Z是氢或烷基（C 1-3 1-3），烷氧基（C 1-3 1-3）或烷硫基（C 1-3 1-3） ，-A是氢或烷基（C 1-3 1-3），或者-A和Z一起形成可以被卤素，烷基（例如甲基），乙基 （C 1-3）或苯基，其中环Z表示碳，氮的硫。

    N-OXIDO DE SILDENAFIL COMO PRODROGA
    8.
    发明专利
    N-OXIDO DE SILDENAFIL COMO PRODROGA 未知

    公开(公告)号：AR067128A1

    公开(公告)日：2009-09-30

    申请号：ARP080102686

    申请日：2008-06-23

    Applicant: SOLVAY PHARM BV

    Inventor： STOIT AXEL ,  KRUSE CORNELIS G ,  TULP MARTINUS TH M ,  TURSKI LECHOSLAW A ,  VADER SANDER

    IPC: C07D487/04 ,  A61K31/519 ,  A61P9/12 ,  A61P15/10

    Abstract: La presente se refiere a N-oxido de sildenafil como prodroga, a composiciones farmacéuticas que contienen este compuesto, a métodos para prepararlo, y a métodos para preparar composiciones. Se refiere a 1-[[3-(6,7-dihidro-1-metil-7-oxo-3-propil-1H-pirazolo[4,3-d]pirimidin-5-il)-4-etoxifenil]sulfonil]-4-metil-4-oxido-piperazina que tiene la formula (1) y sales, hidratos y solvatos farmacologicamente aceptables del mismo. También se refiere a usos del compuesto, y composiciones que lo contienen, particularmente para la fabricacion de medicamentos utiles en el tratamiento de disfuncion eréctil o hipertension arterial.

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