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    12.
    发明专利
    未知

    公开(公告)号：BR0315801A

    公开(公告)日：2005-09-20

    申请号：BR0315801

    申请日：2003-11-04

    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 ,  A61K31/505

    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).

    13.
    发明专利
    未知

    公开(公告)号：BR0315800A

    公开(公告)日：2005-09-20

    申请号：BR0315800

    申请日：2003-11-04

    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 ,  A61K31/44

    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.

    14.
    发明专利
    未知

    公开(公告)号：BR0314878A

    公开(公告)日：2005-08-02

    申请号：BR0314878

    申请日：2003-10-17

    Applicant: SERVIER LAB

    Inventor： COUDERT GERARD ,  AYERBE NATHALIE ,  LEPIFRE FRANK ,  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 ,  C07D498/22 ,  A61K31/5365

    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).

    15.
    发明专利
    未知

    公开(公告)号：FR2865474A1

    公开(公告)日：2005-07-29

    申请号：FR0400689

    申请日：2004-01-26

    Applicant: SERVIER LAB

    Inventor： FRANCOTTE PIERRE ,  FRAIKIN PIERRE ,  DE TULLIO PASCAL ,  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 ,  A61P25/18

    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.

    16.
    发明专利
    未知

    公开(公告)号：FR2854634B1

    公开(公告)日：2005-07-08

    申请号：FR0305448

    申请日：2003-05-05

    Applicant: SERVIER LAB

    Inventor： GRAINDORGE EMMANUEL ,  FRANCOTTE PIERRE ,  BOVERIE STEPHANE ,  DE TULLIO PASCAL ,  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.

    18.
    发明专利
    未知

    公开(公告)号：FR2846328A1

    公开(公告)日：2004-04-30

    申请号：FR0213194

    申请日：2002-10-23

    Applicant: SERVIER LAB

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

    IPC: A61K31/381 ,  A61K31/402 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06 ,  A61K31/4025 ,  A61K31/4402

    Abstract: Imidazoline derivatives (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new. Imidazoline derivatives of formula (I), their enantiomers, diastereoisomers, tautomers, and salts with acids and bases, are new: R1 = heteroaryl optionally substituted by T1; R2 = cycloalkyl optionally substituted by T1; T1 = halogen, alkyl, alkoxy, OH, CN, NO2, (di)(alkyl)amino, COOH, COO-alkyl or CONH2-C(O)Rd; Rd = OH, alkoxy or amino; R4 , R5 = H, halogen, (polyhalo)alkyl, R10-C(X)-R11-, R10-Y-C(X)-R11-, R11-Y-R11-, or R10-S-(O)n-R11-; R11 = a bond, alkylene, alkenylene or alkynylene; X = O, S, or NR12; R3, R10, R12 = H or alkyl; Y = O, S or (alkyl)amino; and n = 1 or 2. Alkyl, alkoxy and alkylene have 1-6C, alkenylene have 2-6C and 1-3 double bonds, alkynylene have 2-6C and 1-3 triple bonds, polyhaloalkyl have 1-3C and 1-7 halogens, heteroaryl has 5 - 11 members and is mono or bicyclic with at least one aromatic ring and with 1-3 heteroatoms selected from O, N and S and may be substituted by an oxo group on a non-aromatic part of the structure, cycloalkyl has 3-10C, is mono or bicyclic and may have 1 or 2 unsaturations. An Independent claim is also included for the preparation of (I).

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