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    82.
    发明专利
    未知

    公开(公告)号：AT348612T

    公开(公告)日：2007-01-15

    申请号：AT04291901

    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: 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 ,  A61K31/428

    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.

    86.
    发明专利
    未知

    公开(公告)号：FR2845994B1

    公开(公告)日：2006-05-19

    申请号：FR0212964

    申请日：2002-10-18

    Applicant: SERVIER LAB

    Inventor： COUDERT GERARD ,  LEPIFRE FRANCK ,  CAIGNARD DANIEL HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  KRAUS BERTHIER LAURENCE

    IPC: C07D487/04 ,  A61K31/4375 ,  A61K31/538 ,  A61P35/00 ,  C07D207/452 ,  C07D213/74 ,  C07D265/00 ,  C07D265/36 ,  C07D265/38 ,  C07D471/04 ,  C07D497/04 ,  C07D497/14

    Abstract: Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. Benzo(e)(1,4)oxazino(3,2-g)isoindole derivatives of formula (I), and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new W1 = atoms that complete phenyl or pyridyl; Z = hydrogen, halo, 1-6C alkyl or alkoxy (both optionally substituted by aryl), aryl, aryloxy or hydroxy; R1 = hydrogen, 1-6C alkyl, optionally substituted by aryl, aryl, COR5 or 1-6C alkylene, substituted by one or more of halo, cyano, OR6, NR6R7, COOR6, COR6 or CONHR6; R2 = hydrogen or -CH2CH2OR8; R3 and R4 = hydrogen, 1-6C alkyl, optionally substituted by aryl, or aryl, or together they complete a 5 or 6-membered, monocyclic heterocycle, optionally including an additional oxygen or nitrogen; n = 1-6; R5 = hydrogen, 1-6C alkyl or alkoxy, hydroxy, aryl, aryl(1-6C)alkyl or aryloxy; R6 and R7 = hydrogen, 1-6C alkyl, aryl(1-6C)alkyl or aryl, or together they complete a heterocycle as above; R8 = hydrogen, 1-6C alkyl, aryl, aryl(1-6C)alkyl, S(O)tR6 or -T1-R9; t = 0-2; T1 = 1-6C alkylene; R9 = halo, cyano, OR6, NR6R7, CHO, COOR6 or CONR6R7; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl, all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy or amino, optionally substituted by 1 or 2 1-6C alkyl. Independent claims are also included for the following:0041658 (1) methods for the preparation of (I); and (2) intermediates of formulae (X), (XI) and (XIV). Boc = tert-butoxycarbonyl; and Pg = Boc or phenoxycarbonyl.

    87.
    发明专利
    未知

    公开(公告)号：BR0312444A

    公开(公告)日：2005-05-10

    申请号：BR0312444

    申请日：2003-06-16

    Applicant: SHANGHAI INST MATERIA MEDICA ,  SERVIER LAB

    Inventor： QIN GUO-WEI ,  TANG XI-CAN ,  LESTAGE PIERRE ,  CAIGNARD DANIEL HENRI ,  RENARD PIERRE

    IPC: A61K31/47 ,  A61P25/28 ,  C07D209/96 ,  C07D217/20

    Abstract: The invention relates to acutumine and compounds thereof and also to compounds of formula (I): wherein R 1 and R 2 each represent hydrogen or together form an additional bond, R 3 represents hydrogen or alkoxy, R 5 represents hydrogen or chlorine, R 6 represents hydrogen or alkyl, alkylcarbonyl or aroyl, R 7 and R 10 each represent alkoxy, R 10 represents alkoxy, R 4 , R 8 , R 9 , R 11 , R 12 , R 13 and R 14 are as defined in the description. and medicinal products containing the same which are useful in treating deficiencies of memory.

    89.
    发明专利
    未知

    公开(公告)号：FR2846657B1

    公开(公告)日：2004-12-24

    申请号：FR0213804

    申请日：2002-11-05

    Applicant: SERVIER LAB

    Inventor： RAULT SYLVAIN ,  LANCELOT JEAN CHARLES ,  KOPP MARINA ,  CAIGNARD DANIEL HENRI ,  PFEIFFER BRUNO ,  RENARD PIERRE

    IPC: A61P3/04 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  A61P19/02 ,  A61P35/00 ,  C07D471/04 ,  A61K31/513

    Abstract: Pyridopyrimidone derivatives (I), their enantiomers, diastereoisomers, tautomers, and their salts with acids and bases are new. Pyridopyrimidone derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and their salts with acids and bases are new. R1, R2 = H or alkyl; R3 = halogen, alkoxy, aryl (optionally substituted by 1-3 R33), or NR'1R'2; R'1, R'2 = H, alkyl, or R'1-N-R'2 is a heterocycle; R4 = H or NR''1R''2; R''1, R''2 = H or alkyl; R1+R2, R'1+R'2, R''1+R''2 = mono or bicyclic of 5 - 11 C heterocycle optionally containing a further 1 or 2 heteroatoms (O, N, S), optionally substituted by 1-3 alkyl groups; R33 = halogens, alkyl, alkoxy, polyhaloalkyl (containing 1 - 3 C atoms and 1 - 7 halogen atoms) and hydroxy; provided that: (1) alkyl and alkoxy groups have 1 - 8 C atoms, aryl is phenyl or naphthyl; and An Independent claim is also included for the preparation of (I).

    90.
    发明专利
    未知

    公开(公告)号：FR2845997B1

    公开(公告)日：2004-12-24

    申请号：FR0212965

    申请日：2002-10-18

    Applicant: SERVIER LAB

    Inventor： COUDERT GERARD ,  AYERBE NATHALIE ,  LEPIFRE FRANCK ,  ROUTIER SYLVAIN ,  CAIGNARD DANIEL HENRI ,  RENARD PIERRE ,  HICKMAN JOHN ,  PIERRE ALAIN ,  LEONCE STEPHANE

    IPC: A61P35/00 ,  C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07D498/14 ,  A61K31/403 ,  A61K31/5383 ,  A61K31/538

    Abstract: 1,4-benzodioxino(2,3-e)isoindole derivatives (I) are new. 1,4-benzodioxino(2,3-e)isoindole derivatives of formula (I) and their enantiomers, diastereoisomers, N-oxides and addition salts with acids and bases are new. A = atoms that complete groups of formula (a) or (b); W1 = atoms that complete a phenyl or pyridyl ring; Z' = H, halogen, 1-6C alkyl or alkoxy (both optionally substituted by aryl), nitro, cyano, hydroxy, aryl, or NR5R6; R5, R6 = H or 1-6C alkyl; R4 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or COOR'5; R'5 = 1-6C alkyl, aryl or aryl(1-6C)alkyl; Y' = oxygen or methylene; R2 = H; and R3 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl or trifluoromethylsulfonyl; or R2+R3 = bond; R1 = H, 1-6C alkyl, aryl, aryl(1-6C)alkyl, or 1-6C alkylene, substituted by one or more of OR5 or NR5R6; Z1, Z2 = H or; Z1+Z2 = fused phenyl; and aryl = phenyl, naphthyl, di- or tetra-hydronaphthyl, indenyl or indanyl (all optionally substituted by one or more of halo, 1-6C (trihalo)alkyl or alkoxy, hydroxy, amino or mono- or di-1-6C alkylamino. Provided that if Z' is H, then R1 is not H. Independent claims are included for preparing (I).

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