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    N-OXIDES OF VENLAFAXINE AND O-DESMETHYLVENLAFAXINE AS PRODRUGS
    26.
    发明专利
    N-OXIDES OF VENLAFAXINE AND O-DESMETHYLVENLAFAXINE AS PRODRUGS 未知

    公开(公告)号：CA2699961A1

    公开(公告)日：2008-12-31

    申请号：CA2699961

    申请日：2008-06-23

    Applicant: SOLVAY PHARM BV

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

    IPC: C07C291/04 ,  A61K31/135 ,  A61P25/24

    Abstract: The invention concerns venlafaxine-N-oxide and O-desmethylvenlafaxine-N-oxide as prodrugs of venlafaxine and its major (active) metabolite O-desmethylvenlafaxine respectively, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxide, having formula (1), wherein R1 is H or CH3, and tautomers, stereoisomers, hydrates and solvates thereof. The invention also relates to the uses of the N-oxides and compositions, particularly for the manufacture of medicaments useful in the treatment of affections or diseases effectively treatable - albeit with side effects - with venlafaxine.

    27.
    发明专利
    未知

    公开(公告)号：BRPI0518465A2

    公开(公告)日：2008-11-18

    申请号：BRPI0518465

    申请日：2005-12-06

    Applicant: SOLVAY PHARM BV

    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

    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 .

    MUSCARINIC AGONISTS TO TREAT IMPULSE CONTROL DISORDERS
    30.
    发明专利
    MUSCARINIC AGONISTS TO TREAT IMPULSE CONTROL DISORDERS 未知

    公开(公告)号：CA2649917A1

    公开(公告)日：2007-11-15

    申请号：CA2649917

    申请日：2007-04-23

    Applicant: SOLVAY PHARM BV

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

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

    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.

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