Title:
置換ベンゾール〔e〕〔1,4〕オキサジノ〔3,2-g〕イソインドール誘導体、それらの製造方法、及びそれらを含有する医薬組成物
Document Type and Number:
Japanese Patent JP2006506375
Kind Code:
A
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.
Inventors:
Gerard, Qudale
Rupiful, frank
Canary, Daniel-Henri
Renard, Pierre
Ikman, John
Alain Pierre
Cross-Bertier, Laurence
Rupiful, frank
Canary, Daniel-Henri
Renard, Pierre
Ikman, John
Alain Pierre
Cross-Bertier, Laurence
Application Number:
JP2004546097A
Publication Date:
February 23, 2006
Filing Date:
October 17, 2003
Export Citation:
Assignee:
Réra Bora Toir Servier
International Classes:
C07D498/04; A61K31/5383; A61P35/00; C07D265/34; C07D497/04; C07D497/14; C07D498/14
Attorney, Agent or Firm:
Hajime Tsukuni
Fumio Shinoda
Fumio Shinoda