中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

120 records (took 0.022 seconds)

    5.
    发明专利
    未知

    公开(公告)号：FR2883876B1

    公开(公告)日：2007-05-04

    申请号：FR0503071

    申请日：2005-03-30

    Applicant: SERVIER LAB

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

    IPC: C07D295/10 ,  A61K31/495 ,  A61P1/00 ,  A61P1/08 ,  A61P3/04 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00

    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.

    6.
    发明专利
    未知

    公开(公告)号：FR2859723B1

    公开(公告)日：2005-10-21

    申请号：FR0310828

    申请日：2003-09-16

    Applicant: SERVIER LAB

    Inventor： LAVIELLE GILBERT ,  MULLER OLIVIER ,  MILLAN MARK ,  GOBERT ALAIN ,  DI CARA BENJAMIN

    IPC: A61K31/496 ,  A61P15/00 ,  A61P15/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D209/60 ,  C07D401/12 ,  C07D403/12

    Abstract: N-(N-(4-Methoxy-3-(4-methyl-1-piperazinyl)-phenyl)-aminocarbonyl)-benz-(e, f or g)-indoline derivatives (I) are new. Benzindoline derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. [Image] R 1> + R 2>, R 2> + R 3> or R 3> + R 4>fused benzo ring (optionally substituted by halo, alkyl, alkoxy, CN, NO 2, OH, NH 2, mono- or dialkylamino or CF 3); and R 1> - R 4>H. An independent claim is included for the preparation of (I). ACTIVITY : Antidepressant; Tranquilizer; Neuroleptic; Antiparkinsonian; Nootropic; Vasotropic; Endocrine-Gen.; Hypnotic. In tests in rats, the hydrochloride of N-(4-methoxy-3-(4-methyl-1-piperazinyl)-phenyl)-1,2-dihydro-3H-benz-(e)-indole-3-carboxamide (Ia) at a dose of 10 mg/kg s.c. caused significant increases in the extracellular concentrations of the neurotransmitters noradrenaline, dopamine and acetylcholine, whereas 6-chloro-5-fluoro-N-(4-methoxy-3-(4-methyl-1-piperazinyl)-phenyl)-1-indoline-carboxamide (A) (described in ) at the same dosage caused only slight increases in the noradrenaline and dopamine levels and no increase in the acetylcholine level. MECHANISM OF ACTION : alpha 2-Adrenoceptor/5-HT(2C) receptor double antagonist. The hydrochloride of (Ia) had pK i values of 7.4 and 8.2 in alpha -2 adrenergic receptor and 5-HT(2C) receptor binding assays respectively, compared with 6.4 and 7.4 respectively for (A).

    7.
    发明专利
    未知

    公开(公告)号：FR2859723A1

    公开(公告)日：2005-03-18

    申请号：FR0310828

    申请日：2003-09-16

    Applicant: SERVIER LAB

    Inventor： LAVIELLE GILBERT ,  MULLER OLIVIER ,  MILLAN MARK ,  GOBERT ALAIN ,  DI CARA BENJAMIN

    IPC: A61K31/496 ,  A61P15/00 ,  A61P15/10 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D209/60 ,  C07D401/12 ,  C07D403/12

    Abstract: N-(N-(4-Methoxy-3-(4-methyl-1-piperazinyl)-phenyl)-aminocarbonyl)-benz-(e, f or g)-indoline derivatives (I) are new. Benzindoline derivatives of formula (I) and their enantiomers, diastereomers and acid or base addition salts are new. [Image] R 1> + R 2>, R 2> + R 3> or R 3> + R 4>fused benzo ring (optionally substituted by halo, alkyl, alkoxy, CN, NO 2, OH, NH 2, mono- or dialkylamino or CF 3); and R 1> - R 4>H. An independent claim is included for the preparation of (I). ACTIVITY : Antidepressant; Tranquilizer; Neuroleptic; Antiparkinsonian; Nootropic; Vasotropic; Endocrine-Gen.; Hypnotic. In tests in rats, the hydrochloride of N-(4-methoxy-3-(4-methyl-1-piperazinyl)-phenyl)-1,2-dihydro-3H-benz-(e)-indole-3-carboxamide (Ia) at a dose of 10 mg/kg s.c. caused significant increases in the extracellular concentrations of the neurotransmitters noradrenaline, dopamine and acetylcholine, whereas 6-chloro-5-fluoro-N-(4-methoxy-3-(4-methyl-1-piperazinyl)-phenyl)-1-indoline-carboxamide (A) (described in ) at the same dosage caused only slight increases in the noradrenaline and dopamine levels and no increase in the acetylcholine level. MECHANISM OF ACTION : alpha 2-Adrenoceptor/5-HT(2C) receptor double antagonist. The hydrochloride of (Ia) had pK i values of 7.4 and 8.2 in alpha -2 adrenergic receptor and 5-HT(2C) receptor binding assays respectively, compared with 6.4 and 7.4 respectively for (A).

Patent Agency Ranking