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    16.
    发明专利
    未知

    公开(公告)号：BRPI0804073A2

    公开(公告)日：2009-06-16

    申请号：BRPI0804073

    申请日：2008-09-22

    Applicant: SERVIER LAB

    Inventor： DE NANTEUIL GUILLAUME ,  PORTEVIN BERNARD ,  GLOANEC PHILIPPE ,  PARMENTIER JEAN-GILLES ,  BENOIST ALAIN ,  VERBEUREN TONY ,  RUPIN ALAIN ,  COURCHAY CHRISTINE ,  SIMONET SERGE

    IPC: C07F9/38 ,  A61K31/40 ,  A61K31/404 ,  A61K31/421 ,  A61K31/472 ,  C07D207/12 ,  C07D209/08 ,  C07D215/48 ,  C07D271/04 ,  C07D339/06 ,  C07D495/10

    Abstract: Compounds e.g. perindopril-ethoxycarbonyl-butyl-amino-propionyl-octahydro-indole-2-carboxylic acid (I) are new. Compounds e.g. perindopril-ethoxycarbonyl-butyl-amino-propionyl-octahydro-indole-2-carboxylic acid of formula (A) m(B1) n(I) are new. A : angiotensin converting enzyme inhibitor moiety comprising at least one basic functional group; B1 : a moiety comprising at least one acid functional group and at least one NO donor group; m : number of acid functional group of B1; and n : number of basic functional groups of A, where A and B1 are ionic type. Independent claims are included for: (1) alkyl compounds of formula X-(AK 1) x-(Y 1) y-(Ak 2) z-Z (III); and (2) preparation of (I). X : CO 2H, SO 3H or P(O)(OH) 2; Ak 1, Ak 2 : 1-8C alkylene (optionally branched and optionally saturated, where one or more C atom is replaced by O, S, N or SO 2, and optionally substituted by carboxy, OH or amino); x, y, z : 0 or 1; Y 1 : CO or CONH; Z : 4-benzenesulfonyl-5-oxy-furazan-3-oxo moiety of formula (a) or (b); and R 4, R1a 4 : H, halo, 1-6C alkyl, CF 3or -OCF 3. [Image] ACTIVITY : Cardiovascular-Gen.; Hypotensive; Nephrotropic; Vasotropic; Cardiant; Antiarteriosclerotic; Prevention: Anticoagulant; Thrombolytic; Antimicrobial; Cerebroprotective; Antidiabetic; Antiinflammatory; Tranquilizer; Metabolic; Anorectic. MECHANISM OF ACTION : Angiotensin converting enzyme inhibitor. The effect of (I) to inhibit angiotensin converting enzyme was tested in rats. The result showed that (2S)-2-[(3-{[5-oxido-4-(phenylsulfonyl)-1,2,5-oxadiazol-3-yl]-oxy}-propionyl)-amino]-succinic acid-(2S,3as,7aS)-1-[(2S)-2-{[(1S)-1-(ethoxycarbonyl)-butyl]-amino}-propionyl]-octahydro-1H-indole-2-carboxylic acid exhibited 80-85% of inhibition.

    INDANYL-PIPERAZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    18.
    发明专利
    INDANYL-PIPERAZINE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知

    公开(公告)号：HK1096386A1

    公开(公告)日：2007-06-01

    申请号：HK07101184

    申请日：2007-02-01

    Applicant: SERVIER LAB

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

    IPC: A61K20090101 ,  A61P20090101 ,  C07D20090101

    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.

    Indany-piperazine compounds, a process for their preparation and pharmaceutical compositions containing them
    20.
    发明专利
    Indany-piperazine compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：SG126113A1

    公开(公告)日：2006-10-30

    申请号：SG200602026

    申请日：2006-03-28

    Applicant: SERVIER LAB

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

    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.

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