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    New heterocyclic oxime compounds, a process for their preparation and pharmaceutical compositions containing them
    42.
    发明专利
    New heterocyclic oxime compounds, a process for their preparation and pharmaceutical compositions containing them 未知

    公开(公告)号：AU2004203454B2

    公开(公告)日：2010-05-27

    申请号：AU2004203454

    申请日：2004-07-28

    Applicant: SERVIER LAB

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

    IPC: 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.

    47.
    发明专利
    未知

    公开(公告)号：AT414066T

    公开(公告)日：2008-11-15

    申请号：AT06709172

    申请日：2006-01-26

    Applicant: SERVIER LAB

    Inventor： HURTEVENT AURELIE ,  L HELGOUAL CH JEAN-MARTIAL ,  CARATO PASCAL ,  LEBEGUE NICOLAS ,  LECLERC VERONIQUE ,  BERTHELOT PASCAL ,  DACQUET CATHERINE ,  KTORZA ALAIN ,  CAIGNARD DANIEL-HENRI

    IPC: C07D279/16 ,  A61K31/538 ,  A61K31/5415 ,  A61P3/06 ,  A61P3/10 ,  C07D265/36

    Abstract: Heterocyclic oxime derivatives (I), their enantiomers, diastereomers and their acid or basic addition salts are new. Heterocyclic oxime derivatives of formula (I), their enantiomers, diastereomers and their acid or basic addition salts are new. X : O or S; A : 1-6C alkyl (where CH 2 can be replaced by heteroatom (O or S), NR a or a phenyl or naphthyl group); R aH or 1-6C alkyl; R 1>, R 2>, R, R1 : H, 1-6C ((hetero)aryl)alkyl, 2-6C ((hetero)aryl)alkenyl, 2-6C ((hetero)aryl)alkynyl, (hetero)aryl, 3-8C cycloalkyl-1-6C alkyl or polyhalo-1-6C alkyl; either R 3>, R 4>H, halo, R, OR or NRR1; or -C-R 3>-R 4>-C- : 5-6 membered ring (containing heteroatom (O, S or N); B 1>1-6C alkyl, 2-6C alkenyl (both optionally substituted by -CHR 5>R 6> or R 7>), -CHR 5>R 6> or R 7>; R 5>-C(=Z)-OR, -C(=Z)-NRR1, -N(R)-C(=Z)-R1 or -N(R)-C(=Z)-OR1; Z : O or S; R 6>(hetero)aryl, (hetero)aryl-1-6C alkyl, CN, tetrazole, OR, NRR1, -N(R)-C(=Z)-R1, -N(R)-C(=Z)-OR1 or -N(R)-C(=Z)-R; R 7>CN, tetrazole, -N(R)-C(=Z)-R1, -N(R)-C(=Z)-OR1 or -O-(CH 2) n-C(R 8>R 9>)-COOR; n : 1-6; and R 8>, R 9>H or 1-6C alkyl. Provided that both R 8> and R 9> are not simultaneously H. Provided that: the oxime R 1>-C(=N-OR 2>)- can be the Z or E configuration; the aryl are phenyl, naphthyl or biphenyl, which can be partially hydrogenated; the heteroaryl are 5-10 membered mono or bicylic aromatic, where the bicyclics can partially be hydrogenated, and containing 1-3 heteroatom (O, N or S); the (hetero)aryl are optionally substituted by 1-3 of 1-6C (polyhalo)alkyl, 1-6C alkoxy, OH, carboxy, 1-6C alkoxycarbonyl, 1-6C acyloxy, formyl, 1-6C acyl, aryl, NR bR c, amido, nitro, CN or halo, where R b, R c are H, 1-6C alkyl or (hetero)aryl. Independent claims are included for: (1) the preparations of (I); (2) a composition (X) comprising (I) an antioxidant agent. [Image] ACTIVITY : Antidiabetic; Antilipemic; Analgesic; Antianginal; Cardiant; Vasotropic; Cardiovascular-Gen.; Nephrotropic; Ophthalmological; Antipsoriatic; Gynecological; Osteopathic; Gastrointestinal-Gen.; Antiinflammatory; Antiarteriosclerotic; Anorectic; Anabolic; Eating-Disorders-Gen.; Neuroprotective; Cytostatic; Endocrine-Gen.; Neuroleptic. The antidiabetic and hypolipidemic effect of (I) was tested in female mouse. The results showed that (I) exhibited a very good capacity to reduce the glycemia compared with the effects obtained with Rosiglitazone. MECHANISM OF ACTION : Angiogenesis inhibitor.

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