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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).
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公开(公告)号:NO20052373A
公开(公告)日:2005-05-13
申请号:NO20052373
申请日:2005-05-13
Applicant: SERVIER LAB
Inventor: PIERRE ALAIN , RENARD PIERRE , HICKMAN JOHN , KRAUS-BERTHIER LAURENCE , COUDERT GERARD , CAIGNARD DANIEL-HENRI , LEPIFRE FRANK
IPC: A61P35/00 , C07D497/04 , C07D497/14 , C07D498/04 , A61K31/535 , C07D265/38 , C07D498/14
CPC classification number: C07D497/04 , C07D497/14
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公开(公告)号:NO20052373L
公开(公告)日:2005-05-13
申请号:NO20052373
申请日:2005-05-13
Applicant: SERVIER LAB
Inventor: PIERRE ALAIN , RENARD PIERRE , HICKMAN JOHN , KRAUS-BERTHIER LAURENCE , COUDERT GERARD , CAIGNARD DANIEL-HENRI , LEPIFRE FRANK
IPC: A61P35/00 , C07D497/04 , C07D497/14 , C07D498/04 , A61K31/535 , C07D498/14 , C07D265/38
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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