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    61.
    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.

    63.
    发明专利
    未知

    公开(公告)号：BRPI0410002A

    公开(公告)日：2006-04-25

    申请号：BRPI0410002

    申请日：2004-05-04

    Applicant: SERVIER LAB

    Inventor： GRAINDORGE EMMANUEL ,  FRANCOTTE PIERRE ,  BOVERIE STEPHANE ,  TULLIO PASCAL DE ,  PIROTTE BERNARD ,  LESTAGE PIERRE ,  DANOBER LAURENCE ,  RENARD PIERRE ,  CAIGNARD DANIEL HENRI

    IPC: A61P25/18 ,  C07D513/04 ,  A61K31/549

    Abstract: Compounds of formula (I): wherein: A represents thienyl, furyl, pyrrolyl, oxathiol, thiazole, isothiazole, oxazole or imidazole, represents a single bond or a double bond, R1 represents hydrogen, linear or branched (C1-C6)alkyl optionally substituted by one or more groups selected from halogen or (C1-C6)alkoxy-(C1-C6)alkyl, R2 represents hydrogen or linear or branched (C1-C6)alkyl group optionally substituted by one or more halogen, R3 represents hydrogen or a group selected from linear or branched (C1-C6)alkyl, CONHR' and SO2NHR' wherein R' represents linear or branched (C1-C6)alkyl, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same, which are useful as AMPA inhibitors.

    64.
    发明专利
    未知

    公开(公告)号：BRPI0500235A

    公开(公告)日：2005-09-06

    申请号：BRPI0500235

    申请日：2005-01-26

    Applicant: SERVIER LAB

    Inventor： FRANCOTTE PIERRE ,  FRAIKIN PIERRE ,  TULLIO PASCAL DE ,  PIROTTE BERNARD ,  LESTAGE PIERRE ,  DANOBER LAURENCE ,  CAIGNARD DANIEL HENRI ,  RENARD PIERRE

    IPC: A61K31/5415 ,  A61K31/549 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07B53/00 ,  C07D285/22 ,  C07D285/24 ,  A61K31/54

    Abstract: 4-(Fluorinated alkyl or fluorinated cycloalkylalkyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxide derivatives (I) are new. Benzothiadiazine derivatives of formula (I) (including optical isomers where appropriate) and their acid or base addition salts are new. R fmono- or polyfluoroalkyl or mono- or polyfluoro-cycloalkylalkyl; R 1H, alkylaminocarbonyl or alkyl (optionally substituted by one or more halo); R 2H, halo, cycloalkyl or alkyl (optionally substituted by one or more halo); R 3 - R 6H, halo, NO 2, CN, alkylsulfonyl, OH, alkoxy, alkyl (optionally substituted by one or more halo) or NH 2 (optionally substituted by 1 or 2 alkyl); Alkyl moieties have 1-6C and cycloalkyl moieties 3-7C; provided that R 3 = H when R 6 is other than H. Independent claims are also included for: (A) new benzothiadiazine derivatives of formula (VI); and (B) the preparation of (I). [Image] [Image] ACTIVITY : Nootropic; Tranquilizer; Antidepressant; Neuroprotective; Antiparkinsonian; Anticonvulsant; Neuroleptic. In object recognition tests in 17 month old rats, 7-chloro-4-(2-fluoroethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine-1,1-dioxide (Ia) at oral doses of 0.1 mg/kg significant reduced age-associated loss of memory. MECHANISM OF ACTION : alpha -Amino-5-methyl-4-isoxazole-propionic acid (AMPA) receptor modulator. In tests in Xenopus ovocytes, (Ia) strongly potentiated the excitative effect of AMPA, showing EC2X and EC5X values of 6.7 mu M and 14.5 mu M respectively for increasing the AMPA-inducedionic current.

    65.
    发明专利
    未知

    公开(公告)号：FR2846656B1

    公开(公告)日：2004-12-24

    申请号：FR0213802

    申请日：2002-11-05

    Applicant: SERVIER LAB

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

    IPC: A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/10 ,  C07D471/04 ,  A61K31/437

    Abstract: Imidazopyridine derivatives (I) are new. Imidazopyridine derivatives of formula (I), their enantiomers, diastereoisomers, and their salts with acids and bases are new. R1 = H, halogen, alkyl, polyhaloalkyl, CN, NO2, hydroxycarbonyl, alkoxycarbonyl, aminocarbonyl, or dialkylaminocarbonyl; R2 = H, alkyl, aryl (optionally substituted), heteroaryl (optionally substituted) or a group of formula R20-C(X)-; R20 = alkyl, alkoxy, amino, alkylamino, dialkylamino, aryl (optionally substituted), or heteroaryl (optionally substituted); X = O, S, or NR21; R21, R3 = H or alkyl; n = 1-6; and N = pyrido ring with the N atom in the 1, 2, 3, or 4 positions. Alkyl and alkoxy groups have 1-6 C atoms, aryl is phenyl or naphthyl, polyhaloalkyl groups having 1-3 C atoms and 1-7 halogen atoms, heteroaryl groups may be mono or bicyclic of 5 - 11 ring atoms, at least one ring being aromatic, and having 2 or 3 heteroatoms (O, N, S) and may be substituted by 1-3 alkyl groups. Optional substituents on aryl groups may be 1 or 2 substituents selected from halogens, alkyl, alkoxy, polyhaloalkyl, hydroxy, CN, NO2, amino, alkylamino, dialkylamino, carboxyl, amido, and -COO-alkyl groups, and heteroaryl groups having a non-aromatic ring may be further substituted on this non-aromatic ring by oxo.

    New benzo-oxazino-isoindole derivatives, useful for treating cancers, are inhibitors of the cell cycle
    68.
    发明专利
    New benzo-oxazino-isoindole derivatives, useful for treating cancers, are inhibitors of the cell cycle 未知

    公开(公告)号：FR2845994A1

    公开(公告)日：2004-04-23

    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: A61P35/00 ,  C07D497/04 ,  C07D497/14 ,  C07D487/04 ,  C07D471/04 ,  C07D265/36 ,  C07D265/38 ,  A61K31/538 ,  A61K31/4375

    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.

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