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    Heterocyclic oxime compounds, a process for their preparation and pharmaceutical compositions containing them.
    12.
    发明专利
    Heterocyclic oxime compounds, a process for their preparation and pharmaceutical compositions containing them. 未知

    公开(公告)号：ZA200405893B

    公开(公告)日：2005-01-24

    申请号：ZA200405893

    申请日：2004-07-23

    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: 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 ,  A61K ,  A61P ,  C07D

    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.

    New benzothiazolyl derivatives useful for the treatment of diabetes, cardiovascular disorders, psoriasis, dementia, osteoporosis, inflammation, obesity, anorexia, bulimia, hormono-dependent cancers and other disorders
    17.
    发明专利
    New benzothiazolyl derivatives useful for the treatment of diabetes, cardiovascular disorders, psoriasis, dementia, osteoporosis, inflammation, obesity, anorexia, bulimia, hormono-dependent cancers and other disorders 未知

    公开(公告)号：FR2830012A1

    公开(公告)日：2003-03-28

    申请号：FR0112205

    申请日：2001-09-21

    Applicant: SERVIER LAB

    Inventor： LESIEUR DANIEL ,  BLANC DELMAS ELODIE ,  BENNEJEAN CAROLINE ,  CHAVATTE PHILIPPE ,  GUILLAUMET GERALD ,  DACQUET CATHERINE ,  LEVENS NIGEL ,  BOUTIN JEAN ALBERT ,  RENARD PIERRE

    IPC: A61P3/10 ,  A61P9/10 ,  A61P17/06 ,  A61P19/10 ,  A61P35/00 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/428

    Abstract: Benzothiazolyl derivatives (I), their enantiomers, diastereoisomers, and addition salts with acids and bases. Benzothiazolyl derivatives of formula (I), their enantiomers, diastereoisomers, and addition salts with acids and bases. X = O, S, CH2 or is CH linked to R ; Y = O or S; R and R = H, alkyl, aralkyl, aryloxy, arylalkyloxy, alkoxy, OH, amino, mono- and di-alkylamino; or R +R = oxo, thioxo, or imino; A = alkylene in which one methylene group may be replaced by O, S, or NH, N-alkyl, phenylene or naphthylene; B = alkylene, alkenylene, or alkynylene; D and D' = a benzene or pyridine ring, optionally substituted by 1-3 halo, CN, NO2, R, OR, -S(O)n-R, C(Z)R, -CH(OR)-R', C(Z)OR, NRR', C(Z)NRR', -CR=N-OR, -NR-C(Z)R', -NR-C(Z)OR', and OC(Me)2-COOR; R and R' = H, alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl, heteroarylalkyl, cycloalkyl, or cycloalkyl alkyl; Z = O or S; n = 0-2; R and R = H, halo, R, OR, or NRR'; or R +R = 5-6 membered ring that may contain O, N, or S; R = H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, alkylcarbonyl, arylcarbonyl, or heteroaryl carbonyl, all of which may be substituted by one or more R , -CH2CHR R , -CH=CR R , halo, OH, NO2, CN, NH2 or alkoxy; R = -(CH2)t-C(=Z)Z'; t = 0-6; Z' = OR or NRR'; R and R = -C(=Z)Z' Where alkyl, alkoxy, alkylene, alkenyl, alkynyl, alkenylene and alkynylene groups have 1-6 C atoms, cycloalkyl groups have 3-8 C atoms, aryl means phenyl, naphthyl, or biphenyl, optionally partially hydrogenated, heteroaryl groups have one or two rings containing 5-10 members, optionally partially hydrogenated and containing 1-3 O, N and/or S atoms, and the aryl and heteroaryl groups may be substituted by 1-3 groups selected from alkyl, alkoxy, carboxy, formyl, amino, mono- and dialkylamino, ester, amido, NO2, CN, and OC(Me)2COOR.

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