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    SILDENAFIL N-OXIDE AS PRODRUG
    1.
    发明申请
    SILDENAFIL N-OXIDE AS PRODRUG 审中-公开
    SILDENAFIL N-OXIDE作为PRODRUG

    公开(公告)号：WO2009000798A1

    公开(公告)日：2008-12-31

    申请号：PCT/EP2008/057940

    申请日：2008-06-23

    Applicant: SOLVAY PHARMACEUTICALS B.V. ,  TURSKI, Lechoslaw A. ,  STOIT, Axel ,  KRUSE, Cornelis, G. ,  VADER, Sander ,  TULP, Martinus Th., M.

    Inventor： TURSKI, Lechoslaw A. ,  STOIT, Axel ,  KRUSE, Cornelis, G. ,  VADER, Sander ,  TULP, Martinus Th., M.

    IPC: C07D487/04 ,  A61P15/10 ,  A61K31/519 ,  A61P11/00

    CPC classification number: C07D487/04

    Abstract: The invention concerns sildenafil N-oxide as prodrug, to pharmaceutical compositions containing this compound, to methods for preparing it, and methods for preparing compositions. The invention relates to 1-[[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methyl-4-oxido-piperazine having formula (1 A ) and pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to uses of the compound, and compositions containing it, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with sildenafil.

    Abstract translation: 本发明涉及西地那非N-氧化物作为前药，含有该化合物的药物组合物，其制备方法和制备组合物的方法。 本发明涉及1 - [[3-（6,7-二氢-1-甲基-7-氧代-3-丙基-1H-吡唑并[4,3-d]嘧啶-5-基）-4-乙氧基苯基] 磺酰基] -4-甲基-4-氧代 - 哌嗪及其药理学上可接受的盐，水合物和溶剂化物。 本发明还涉及该化合物和含有它的组合物的用途，特别是用于制备可用于治疗感染或有效治疗的疾病的药物 - 尽管有副作用 - 西地那非。

    MUSCARINIC AGONISTS TO TREAT IMPULSE CONTROL DISORDERS
    2.
    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。

    PIPERAZINE OXIME DERIVATIVES HAVING NK-1 RECEPTOR ANTAGONISTIC ACTIVITY
    4.
    发明申请
    PIPERAZINE OXIME DERIVATIVES HAVING NK-1 RECEPTOR ANTAGONISTIC ACTIVITY 审中-公开
    具有NK-1受体拮抗活性的哌嗪衍生物

    公开(公告)号：WO2003006459A1

    公开(公告)日：2003-01-23

    申请号：PCT/EP2002/007472

    申请日：2002-07-03

    Applicant: SOLVAY PHARMACEUTICALS B.V. ,  VAN MAARSEVEEN, Jan, H. ,  VAN SCHARRENBURG, Gustaaf, J., M. ,  TULP, Martinus, Th., M. ,  MCCREARY, Andrew, C. ,  IWEMA BAKKER, Wouter, I. ,  COOLEN, Hein, K., A., C. ,  HERREMANS, Arnoldus, H., J. ,  VAN DEN HOOGENBAND, Adrianus

    Inventor： VAN MAARSEVEEN, Jan, H. ,  VAN SCHARRENBURG, Gustaaf, J., M. ,  TULP, Martinus, Th., M. ,  MCCREARY, Andrew, C. ,  IWEMA BAKKER, Wouter, I. ,  COOLEN, Hein, K., A., C. ,  HERREMANS, Arnoldus, H., J. ,  VAN DEN HOOGENBAND, Adrianus

    IPC: C07D403/06

    CPC classification number: C07D401/14 ,  C07D241/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D471/04

    Abstract: The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein:X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH 3 , CF 3 , OCH 3 , halogen, cyano and 5-CF 3 -tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1-3C); n has the value 0-3; m has the value 0-2; R 1 represents NH 2 , NH-alkyl (1-3C), dialkyl (1-3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH 3 -piperazinyl; R 2 is hydrogen, alkyl (1-4C) or phenyl, or R 2 together with (CH 2 ) m wherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; R 3 and R 4 independently represent hydrogen or methyl, or R 3 and R 4 together are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved.

    Abstract translation: 本发明涉及一组具有有趣的NK-1拮抗活性的新型哌嗪肟衍生物。 本发明涉及通式（1）的化合物，其中：X表示苯基或被1或2个取代基取代的吡啶基，所述取代基为CH 3，CF 3，OCH 3，卤素，氰基和5-CF > 3 < - 四唑-1-基; Y代表2-或3-吲哚基，苯基，7-氮杂 - 吲哚-3-基或3-吲唑基，2-萘基，3-苯并[b]噻吩基，2-苯并呋喃基，它们可以被一个或多个 卤素或烷基（1-3C）; n的值为0-3; m的值为0-2; R 1表示被一个或两个甲基和/或甲氧基甲基取代的二烷基（1-3C）N，吗啉代或吗啉代，硫代吗啉代，1,1-二氧代硫代吗啉代， 2-，3-或4-吡啶基或4- CH 3'-哌嗪基; R 2是氢，烷基（1-4C）或苯基，或R 2与（CH 2）m（其中m是1）一起，中间体碳，氮和氧原子形成异恶唑基或 4,5-二氢异恶唑基; R 3和R 4独立地代表氢或甲基，或R 3和R 4一起是氧。 本发明还涉及一种制备新化合物的方法，以及包含式（1）化合物作为活性成分的药物组合物，以及这些化合物用于治疗涉及神经激肽-1受体的疾病的用途。

    TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES
    8.
    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。

    TETRAHYDROPYRIDIN-4-YL INDOLES WITH A COMBINATION OF AFFINITY FOR DOPAMINE-D2 RECEPTORS AND SEROTONIN REUPTAKE SITES
    9.
    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
    具有多巴胺D2受体和丝氨酸蛋白酶重复位点的亲和力组合的四氢吡啶并[4-YL]吲哚

    公开(公告)号：WO2006061373A2

    公开(公告)日：2006-06-15

    申请号：PCT/EP2005/056501

    申请日：2005-12-06

    Applicant: SOLVAY PHARMACEUTICALS B.V. ,  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.

    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的四氢吡啶-4-基吲哚：5-羟色胺再摄取抑制和对多巴胺-D 2受体的亲和力，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-基吲哚的新型中间体。 本发明还涉及本文公开的化合物在制备产生有益效果的药物中的用途。 本发明涉及式（I）的新型四氢吡啶-4-基吲哚和互变异构体，立体异构体，前药，N-氧化物，其药理学上可接受的盐，水合物和溶剂合物，其中：R 1是 氢，卤素，烷基（C 1-3-3）或烷氧基（C 1-3 - ），CN或CF 3 - ， - > 2是氢或烷基（C 1-3-3），R 3是氢或烷基（C 1-3-3） ， - Z是氢或烷基（C 1-3-3），烷氧基（C 1-3-3）或烷硫基（C 1-3） ， - A是氢或烷基（C 1-3-3），或 - A和Z一起形成饱和或（部分）不饱和的5-或6-元环，其可被卤素，烷基 （C 1-3）或苯基，其中Z表示碳，氮的硫。

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