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    Piperazine compounds, a process for their preparaion and pharmaceutical compositions containing them
    52.
    发明专利
    Piperazine compounds, a process for their preparaion and pharmaceutical compositions containing them 未知

    公开(公告)号：SG126847A1

    公开(公告)日：2006-11-29

    申请号：SG200602029

    申请日：2006-03-28

    Applicant: SERVIER LAB

    Inventor： PEGLION JEAN-LOUIS ,  DESSINGES AIMEE ,  GOUMENT BERTRAND ,  MILLAN MARK ,  LA COUR CLOTILDE MANNOURY

    IPC: A61P25/00 ,  C07D239/02

    Abstract: Piperazine derivatives (I) and their optical isomers, and acid addition salts are new. Piperazine derivatives of formula (I) and their optical isomers, and acid addition salts are new. R 1-R 4H, halo, 1-6C alkyl, 1-6C alkoxy, phenyl or CN; X : a bond, O, -(CH 2) m-, -OCH 2- or -NR 5-; R 5H, 1-6C alkyl, COR 6 or CO 2R 6; R 61-6C alkyl; R 7H, COR 9 or 1-6C alkyl (optionally substituted 5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl or 2,3-dihydro-1,4-benzodioxin-2-yl); R 91-6C alkyl or (hetero)aryl; R 8H or amino (optionally substituted by 1-2 groups of 1-6C alkyl); Z : N or CH; m, n : 1-2; Ak : 1-6C alkylene; Ar 1(hetero)aryl; and (MK12) Y = O, NR 7 or CHR 8. Aryl is phenyl, biphenyl or naphthyl, each of which is optionally substituted by halo, 1-6C (trihalo)alkyl, 1-6C (trihalo)alkoxy, OH or CN. Heteroaryl is 5-12 membered mono or bicyclic aromatic group, containing 1-2 O, N or S, and the heteroaryl is optionally substituted by halo, 1-6C (trihalo)alkyl, 1-6C alkoxy, OH or CN. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Antidepressant; Tranquilizer; Antiaddictive; Anorectic; Eating-Disorders-Gen.; Analgesic; Antiinflammatory; Neuroleptic; Antiemetic; Gastrointestinal-Gen; Nootropic. MECHANISM OF ACTION : Serotonin receptor inhibitor; Neurokinine antagonist. The affinity of (I) for serotonin receptor was tested in frontal cortex membranes of rat. Trans-1-{2 [(3,5-dibromobenzyl)oxy]-2,3-dihydro-1H-inden-1yl}piperazine (IA) dihydrochloride exhibted a negative logarithm of inhibition constant value of 8.35.

    Indanyl-piperazine compounds, a process for their preparation and pharmaceutical compositions containing them
    53.
    发明专利
    Indanyl-piperazine compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU2006201326A1

    公开(公告)日：2006-10-19

    申请号：AU2006201326

    申请日：2006-03-30

    Applicant: SERVIER LAB

    Inventor： ORTUNO JEAN-CLAUDE ,  GLOANEC PHILLIPPE ,  NANTEUIL GUILLAUME DE ,  COUR CLOTILDE MANNOURY LA ,  MILLAN MARK ,  GOBERT ALAIN ,  PORTEVIN BERNARD

    IPC: C07D295/092 ,  A61K31/495 ,  A61P25/18 ,  A61P25/24 ,  C07D295/104 ,  C07D401/12 ,  C07D419/12

    Abstract: Indanyl-piperazine derivatives (I) are new. Indanyl-piperazine derivatives of formula (I) and their optical isomers, salts, enantiomers or diastereoisomers are new. R 3 = H and R 1+R 2 = benzene, naphthalene or quinoline (optionally substituted by H, halo or 1-6C alkyl (optionally substituted by halo)); or R 1 = H; and R 2+R 3 = benzene, naphthalene or quinoline (optionally substituted by H, halo or 1-6C alkyl (optionally substituted by halo)); n = 1-2; X = (CH 2) m-OT, (CH 2) m-NR 4T, C(O)NR 4T or (CH 2) mNR 4C(O); m = 1-6; T = 1-6C alkyl optionally substituted by OH; R 4 = H or 1-6C alkyl; A = (hetero)aryl; aryl = phenyl, biphenyl or naphthyl (optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, CN or 1-6C trihaloalkyl); and heteroaryl = 5-12 membered aromatic mono- or bicyclic rings containing O, N or S heteroatoms and optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH or 1-6C trihaloalkyl. An independent claim is also included for preparation of (I). [Image] ACTIVITY : Antidepressant; Tranquilizer; Anorectic; Analgesic; Antiinflammatory; Neuroleptic; Antiemetic; Gastrointestinal-Gen. MECHANISM OF ACTION : Serotonin receptor inhibitor; Neurokinin-1 antagonist. The ability of (1RS)-1-[1-(3,5-difluorobenzyloxymethyl)indan-1-yl]piperazine dihydrochloride to inhibit serotonin receptor in rats was tested using biological assays. The result showed that (1RS)-1-[1-(3,5-difluoro-benzyloxymethyl)-indan-1-yl]-piperazine dichlorhydrate exhibits a pK i (negative log of inhibitory constant) value of 8.49.

    57.
    发明专利
    未知

    公开(公告)号：DE60105219T2

    公开(公告)日：2005-09-15

    申请号：DE60105219

    申请日：2001-04-12

    Applicant: SERVIER LAB

    Inventor： PEGLION JEAN-LOUIS ,  GOUMENT BERTRAND ,  MILLAN MARK ,  LEJEUNE FRANCOISE ,  CUSSAC DIDIER

    IPC: A61K31/4427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  C07D401/12 ,  C07D401/14

    Abstract: Cyclobuta-indole derivatives (I), their isomers and salts are new. The new compounds are of formula (I): n = 0 - 6; R1 = H, OH, CN, alkoxy, alkoxycarbonyl, carboxy, amino carbonyl (optionally substituted by one or two alkyl, aryl, or aralkyl groups), or NR4R5; R2 = H, alkyl, CH2OH, a croup -(OH)(T), or -U'-V'-W'; T = 3-12C mono- or polycyclic cycloalkyl that may have one C atom replaced by O, Se, S, SO, SO2, or SiR6R7; R3 = H, alkyl, aryl, or heteroaryl; R4 and R5 = alkyl, aryl, aralkyl, heteroaryl, heteroaryl alkyl, cycloalkyl, cycloalkyl alkyl, alkenyl or alkynyl; R6 and R7 = alkyl; U' = methylene or a bond; V' = a bond, O, S, SO, or SO2; and W' = aryl aralkyl, cycloalkyl, or cycloalkyl alkyl. All alkyl, alkoxy, alkenyl and alkynyl groups having up to 6 C atoms, aryl, heteroaryl and cycloalkyl groups may be mono or polycyclic, aryl and heteroaryl groups may be mono or polysubstituted and cycloalkyl groups may contain unsaturation.

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