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    91.
    发明专利
    未知

    公开(公告)号：DE602005003907D1

    公开(公告)日：2008-01-31

    申请号：DE602005003907

    申请日：2005-11-02

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  CORDI ALEXIS ,  LESTAGE PIERRE

    IPC: A61K31/5415 ,  A61P25/00 ,  C07D285/24

    Abstract: Benzothiadiazine compounds (I) and their enantiomers, diastereoisomers and addition salts with an acid or base are new. Benzothiadiazine compounds of formula (I) and their enantiomers, diastereoisomers and addition salts with an acid or base are new. R 11-6C alkyl substituted by halo(s); R 2H, halo or OH; R 3aryl (optionally substituted by 1-6C alkyl(s)), 1-6C polyhaloalkyl, halo, 1-6C alkoxy-carbonyl, 1-6C alkylthio, carboxy, 1-6C acyl, 1-6C (polyhalo)alkoxy, OH, CN, nitro, amidino (optionally substituted by 1 or 2 1-6C alkyl, OH, 1-6C alkoxy or -O-(C(=O))-R 12), amino (optionally substituted by 1 or 2 1-6C alkyl), aminocarbonyl (optionally substituted by 1 or 2 1-6C alkyl), benzyloxy, 1-6C alkylsulfonylamino (optionally substituted on the N by 1-6C alkyl), trifluoromethylsulfonylamino, heterocyclic or 1-6C alkyl (substituted by halo, 1-6C alkyl, NR 4R 5, S(O) nR 6, OR 7, amidino (optionally substituted by 1 or 2 1-6C alkyl, OH, 1-6C alkoxy or -O-(C=O)-R 12) and/or heterocyclic); R 4H, 1-6C alkyl, S(O) pR 8, COR 9 or P(O)(OR 10)(OR 11); and R 5H or 1-6C alkyl; or NR 4R 5heterocyclic; R 6, R 8-R 12H, 1-6C alkyl (optionally substituted by halo(s)), aryl-(1-6C alkyl) or aryl; R 71-6C alkyl or 1-6C acyl; and n, p : 0-2. [Image] ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Neuroprotective; Cerebroprotective; Anticonvulsant; Neuroleptic; Vasotropic. MECHANISM OF ACTION : Alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) modulator. The ability of (I) to modulate AMPA was assessed using rats. The results showed that N-(4-{[4-(2-bromoethyl)-1,1-dioxido-3,4-dihydro-2H-1,2,4-benzothiadiazin-7-yl]oxy}benzyl)methanesulfonamide exhibited an EC2X value of 0.04 mu M.

    93.
    发明专利
    未知

    公开(公告)号：FR2885615B1

    公开(公告)日：2007-06-22

    申请号：FR0504757

    申请日：2005-05-12

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  CORDI ALEXIS ,  LESTAGE PIERRE

    IPC: C07D413/14 ,  A61K31/496 ,  A61P3/04 ,  A61P25/00 ,  A61P29/00 ,  C07D213/74 ,  C07D241/04 ,  C07D295/26 ,  C07D401/04

    Abstract: Phenyl pyridinyl piperazine derivatives (I), their enantiomers and diastereoisomers, acid and base addition salts are new. Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts are new. R 1NR 3SO 2R 4; R 3H or 1-6C alkyl; R 41-6C alkyl, T or NR 5R 6; either R 5, R 6R 3, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl; NR 5R 65-8 membered ring (where C is optionally replaced by S, N, O, SO or SO 2) (optionally bridged by a 1-6C alkyl and/or optionally to be substituted by T 1); T 1halo, 1-6C (polyhalo)alkyl, 1-6C alkoxy, COOH, OH, CN, NO 2, NH 2 (optionally substituted by 1-6C alkyl); R 21-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-1-6C alkyl; and T : aryl e.g. phenyl, naphtyl or biphenyl (all optionally substituted by T 1). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Cerebroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic; CNS-Gen.; Antiparkinsonian. MECHANISM OF ACTION : Central histaminergic H3 receptor antagonist. The antagonistic activity of (I) against central histaminergic H3 receptor antagonist was tested. The results showed that (I) exhibited a significant antagonistic activity against central histaminergic H3 receptor antagonist.

    New benzothiadiazine compounds, a process for their preparation and pharmaceutical compositions containing them
    95.
    发明专利
    New benzothiadiazine compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：NZ543358A

    公开(公告)日：2007-04-27

    申请号：NZ54335805

    申请日：2005-11-02

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  CORDI ALEXIS ,  LESTAGE PIERRE

    IPC: C07D285/24 ,  C07D417/04 ,  C07D513/04 ,  A61K31/54 ,  A61K31/5415 ,  A61K31/549 ,  A61P25/00 ,  A61P25/28

    Abstract: Benzothiadiazine compounds of formula (I), their enantiomers and diastereoisomers, and also addition salts thereof with a pharmaceutically acceptable acid or base are disclosed, wherein: R1 represents a linear or branched (C1-C6)alkyl group substituted by one or more halogen atoms; R2 represents a hydrogen atom, a halogen atom or a hydroxy group; R3 represents an unsubstituted aryl group or an aryl group substituted by one or more identical or different groups selected from the substituents defined in the specification. These benzothiadiazine compounds surprisingly exhibit especially valuable pharmacological activity on the AMPA current, and they are useful as AMPA modulators for the treatment or prevention of disorders of memory and cognition that are associated with age, with syndromes of anxiety or depression, with progressive neurodegenerative diseases, with Alzheimer's disease, with Pick's disease, with Huntington's chorea, with schizophrenia, with the sequelae of acute neurodegenerative diseases, with the sequelae of ischaemia and with the sequelae of epilepsy.

    New phenylpyridinylpiperazine compounds, a processfor their preparation and pharmaceutical composit ions containing them
    96.
    发明专利
    New phenylpyridinylpiperazine compounds, a processfor their preparation and pharmaceutical composit ions containing them 未知

    公开(公告)号：SG127801A1

    公开(公告)日：2006-12-29

    申请号：SG200603045

    申请日：2006-05-05

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  CORDI ALEXIS ,  LESTAGE PIERRE

    Abstract: Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts, are new. Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts. X : C(O) or SO 2; R 1T or NR 3R 4; either R 3, R 4H, 1-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl; or NR 3R 45-8 membered ring (where C is optionally replaced by S, N, O, SO or SO 2) (optionally bridged by a 1-6C alkyl and/or optionally to be substituted by T 1); T 1halo, 3-8C cycloalkyl, 1-6C (polyhalo)alkyl, 1-6C alkoxy, COOH, OH, CN, O, NO 2, NH 2 (optionally substituted by 1-6C alkyl); R 21-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-1-6C alkyl; and T : aryl e.g. phenyl, naphthyl or biphenyl (all optionally substituted by T 1). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Cerebroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic; CNS-Gen.; Antiparkinsonian. MECHANISM OF ACTION : Central histaminergic H3 receptor antagonist. The antagonistic activity of (I) against central histaminergic H3 receptor antagonist was tested. The results showed that (I) exhibited a significant antagonistic activity against central histaminergic H3 receptor antagonist.

    New phenylpyridinylpiperazine compounds, a processfor their preparation and pharmaceuticals composi tions containing them
    97.
    发明专利
    New phenylpyridinylpiperazine compounds, a processfor their preparation and pharmaceuticals composi tions containing them 未知

    公开(公告)号：SG127800A1

    公开(公告)日：2006-12-29

    申请号：SG200603043

    申请日：2006-05-05

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  CORDI ALEXIS ,  LESTAGE PIERRE

    Abstract: Phenyl pyridinyl piperazine derivatives (I), their enantiomers and diastereoisomers, acid and base addition salts are new. Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts are new. R 1NR 3SO 2R 4; R 3H or 1-6C alkyl; R 41-6C alkyl, T or NR 5R 6; either R 5, R 6R 3, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl; NR 5R 65-8 membered ring (where C is optionally replaced by S, N, O, SO or SO 2) (optionally bridged by a 1-6C alkyl and/or optionally to be substituted by T 1); T 1halo, 1-6C (polyhalo)alkyl, 1-6C alkoxy, COOH, OH, CN, NO 2, NH 2 (optionally substituted by 1-6C alkyl); R 21-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-1-6C alkyl; and T : aryl e.g. phenyl, naphtyl or biphenyl (all optionally substituted by T 1). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Cerebroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic; CNS-Gen.; Antiparkinsonian. MECHANISM OF ACTION : Central histaminergic H3 receptor antagonist. The antagonistic activity of (I) against central histaminergic H3 receptor antagonist was tested. The results showed that (I) exhibited a significant antagonistic activity against central histaminergic H3 receptor antagonist.

    New phenylpridinylpiperazine compounds, a process for their preparation and pharmaceutical compositions containing them
    98.
    发明专利
    New phenylpridinylpiperazine compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU2006201993A1

    公开(公告)日：2006-11-30

    申请号：AU2006201993

    申请日：2006-05-12

    Applicant: SERVIER LAB

    Inventor： LESTAGE PIERRE ,  DESOS PATRICE ,  CORDI ALEXIS

    IPC: C07D213/74 ,  A61K31/496 ,  A61P3/04 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00

    Abstract: Phenyl pyridinyl piperazine derivatives (I), their enantiomers and diastereoisomers, acid and base addition salts are new. Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts are new. R 1NR 3SO 2R 4; R 3H or 1-6C alkyl; R 41-6C alkyl, T or NR 5R 6; either R 5, R 6R 3, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl; NR 5R 65-8 membered ring (where C is optionally replaced by S, N, O, SO or SO 2) (optionally bridged by a 1-6C alkyl and/or optionally to be substituted by T 1); T 1halo, 1-6C (polyhalo)alkyl, 1-6C alkoxy, COOH, OH, CN, NO 2, NH 2 (optionally substituted by 1-6C alkyl); R 21-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-1-6C alkyl; and T : aryl e.g. phenyl, naphtyl or biphenyl (all optionally substituted by T 1). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Cerebroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic; CNS-Gen.; Antiparkinsonian. MECHANISM OF ACTION : Central histaminergic H3 receptor antagonist. The antagonistic activity of (I) against central histaminergic H3 receptor antagonist was tested. The results showed that (I) exhibited a significant antagonistic activity against central histaminergic H3 receptor antagonist.

    99.
    发明专利
    未知

    公开(公告)号：NO20062100L

    公开(公告)日：2006-11-13

    申请号：NO20062100

    申请日：2006-05-10

    Applicant: SERVIER LAB

    Inventor： DESOS PATRICE ,  LESTAGE PIERRE ,  CORDI ALEXIS

    IPC: C07D295/04

    Abstract: Phenyl pyridinyl piperazine derivatives (I), their enantiomers and diastereoisomers, acid and base addition salts are new. Phenyl pyridinyl piperazine derivatives of formula (I), their enantiomers and diastereoisomers, acid and base addition salts are new. R 1NR 3SO 2R 4; R 3H or 1-6C alkyl; R 41-6C alkyl, T or NR 5R 6; either R 5, R 6R 3, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl; NR 5R 65-8 membered ring (where C is optionally replaced by S, N, O, SO or SO 2) (optionally bridged by a 1-6C alkyl and/or optionally to be substituted by T 1); T 1halo, 1-6C (polyhalo)alkyl, 1-6C alkoxy, COOH, OH, CN, NO 2, NH 2 (optionally substituted by 1-6C alkyl); R 21-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkyl-1-6C alkyl; and T : aryl e.g. phenyl, naphtyl or biphenyl (all optionally substituted by T 1). An independent claim is included for the preparation of (I). [Image] ACTIVITY : Nootropic; Neuroprotective; Cerebroprotective; Anticonvulsant; Tranquilizer; Anorectic; Analgesic; CNS-Gen.; Antiparkinsonian. MECHANISM OF ACTION : Central histaminergic H3 receptor antagonist. The antagonistic activity of (I) against central histaminergic H3 receptor antagonist was tested. The results showed that (I) exhibited a significant antagonistic activity against central histaminergic H3 receptor antagonist.

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