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    23.
    发明专利
    未知

    公开(公告)号：NO20091794L

    公开(公告)日：2009-05-06

    申请号：NO20091794

    申请日：2009-05-06

    Applicant: SERVIER LAB

    Inventor： AUDINOT VALERIE ,  BOUTIN JEAN ALBERT ,  CAIGNARD DANIEL-HENRI ,  MARCHAND PASCAL ,  PIESSARD SYLVIE ,  DUFLOS MURIEL ,  DELAGRANGE PHILIPPE ,  BABONNEAU VINCENT

    IPC: C07D209/42

    Abstract: Indole derivatives (I), their enantiomers, diastereomers and their acid/base addition salts are new. Indole derivatives of formula (I), their enantiomers, diastereomers and their acid/base addition salts are new. R 11-6C alkyl, 3-8C cycloalkyl or 3-8C cycloalkyl-1-6C alkyl, preferably methyl; R 21-6C alkyl, preferably methyl, ethyl or propyl; and n : 1-6, preferably 2. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Hypnotic; Tranquilizer; Antidepressant; Cardiovascular-Gen; Gastrointestinal-Gen; Neuroleptic; Anorectic; Anticonvulsant; Antidiabetic; Antiparkinsonian; Nootropic; Antimigraine; Neuroprotective; Endocrine-Gen; Contraceptive; Immunomodulator; Cytostatic. MECHANISM OF ACTION : Melatonin receptor binder. The affinity of (I) to bind with melatonin receptors MT1 and MT2 was tested using 2-[ 1> 2> 5>I]-iodomelatonin as reference radioligand. The results showed that (I) exhibited an inhibition constant value of less than 1 mu M.

    29.
    发明专利
    未知

    公开(公告)号：DE602004003751D1

    公开(公告)日：2007-02-01

    申请号：DE602004003751

    申请日：2004-07-27

    Applicant: SERVIER LAB

    Inventor： LECLERC VERONIQUE ,  PAILLOUX SYLVIE ,  CARATO PASCAL ,  INTROVIGNE CARINE ,  LEBEGUE NICOLAS ,  BERTHELOT PASCAL ,  DACQUET CATHERINE ,  BOUTIN JEAN ALBERT ,  CAIGNARD DANIEL HENRI ,  RENARD PIERRE

    IPC: A61K31/428 ,  C07D235/26 ,  A61K31/426 ,  A61K31/427 ,  A61P1/04 ,  A61P1/18 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P13/04 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/10 ,  A61P21/04 ,  A61P25/28 ,  A61P27/02 ,  A61P35/00 ,  C07D235/12 ,  C07D277/68 ,  C07D417/10 ,  C07D417/12

    Abstract: Benzoxazole, benzothiazole or indole oxime derivatives (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine) are new. Benzoxazole, benzothiazole or indole oxime derivatives of formula (I) (including analogs with the benzo ring replaced by pyridine, pyrazine, pyrimidine or pyridazine), and their enantiomers, diastereomers and salts are new. [Image] X : O, S, CH 2 or CHR' 2>; R 1>, R 2>H, alkyl, aryl, aralkyl, aryloxy, aralkoxy, alkoxy, OH, NH 2 or mono- or dialkylamino; or R 1> + R 2>=O, =S or =NH; R' 2>group forming an additional bond with R 2>; A : 1-6C alkylene (optionally having one CH 2 replaced by O, S, NRa', phenylene or naphthylene); Ra' : H or alkyl; R 3>, R 4>H, halo, R, OR or NRR'; or R 3> + R 4>group forming an ortho-fused 5- or 6-membered ring (optionally containing an O, S or N heteroatom); R, R', R 5>, R 6>H, alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl, heteroaralkynyl, cycloalkyl, cycloalkylalkyl or polyhaloalkyl; D : benzene ring (in which case X is other than CHR' 2>); or a pyridine, pyrazine, pyrimidine or pyridazine ring; B : alkyl or alkenyl, both substituted by -CHR 7>R 8> or by R 9>; or -CHR 7>R 8> or R 9>; R 7>-C(Z)OR, -C(Z)NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; Z : O or S; R 8>aryl, aralkyl, heteroaryl, heteroaralkyl, CN, tetrazole, OR, NRR', -N(R)C(Z)R' or -N(R)C(Z)OR'; R 9>CN, tetrazole, -N(R)C(Z)R', -N(R)C(Z)OR' or -O(CH 2) n-CR 1> 0>R 1> 1>-COOR; n : 0-6; R 1> 0>, R 1> 1>H or alkyl, but not both H; aryl moieties : phenyl, naphthyl or biphenyl (all optionally partially hydrogenated and optionally substituted by 1-3 alkyl, polyhaloalkyl, alkoxy, OH, COOH, CHO, NRaRb, ester, amido, NO 2, CN or halo groups); heteroaryl moieties : 5-10 membered mono- or bicyclic aryl (where one ring is optionally partially hydrogenated in the case of bicyclic systems) containing 1-3 O, S and/or N heteroatom(s) and optionally substituted as for aryl; Rb, Rc : H, alkyl, aryl or heteroaryl; the oxime group -C(R 6>)=NOR 5> has E- or Z-configuration; alkyl moieties have 1-6C, alkenyl or alkynyl moieties 2-6C and cycloalkyl moieties 3-8C. Independent claims are included for: (1) preparation method of (I); and (2) new ketone intermediates of formula (V). [Image] ACTIVITY : Antidiabetic; Antilipemic; Cardiant; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Nootropic; Osteopathic; Antiinflammatory; Antiarteriosclerotic; Anorectic; Cytostatic. In tests in ob/ob mice, oral administration of 10 mg/kg of methyl 3-(4-(2-(6-((methoxyimino)-(phenyl)-methyl)-2-oxo-1,3-benzothiazol-3(2H)-yl)-ethoxy)-phenyl)-2-(2,2,2-trifluoroethoxy)-propanoate (Ia) twice per day for 4 days reduced blood sugar levels by 51% and reduced the weight gain by 80% in comparison with controls, whereas analogous administration of rosiglitazone reduced blood sugar levels by 61% but increased the weight gain by 33% in comparison with controls. MECHANISM OF ACTION : Aldose Reductase Inhibitor; Angiogenesis Inhibitor.

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