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Title:
新規なジヒドロフロ〔3,4-b〕キノリン-1-オン化合物、その製造方法及びそれを含有する医薬組成物
Document Type and Number:
Japanese Patent JP3566649
Kind Code:
B2
Abstract:
Tricyclic quinoline derivatives (I) are new. Tricyclic quinoline derivatives of formula (I) and their optical isomers, hydrates, solvates and acid-addition salts are new: R0 = H, OH or 1-6C alkoxy; R1, R2 = H, halogen, 1-6C alkyl, 1-6C alkoxy, OH, 1-6C polyhaloalkyl, NO2, NH2, mono- or di(1-6C alkyl)amino or 3- to 6-membered 1-azacycloalkyl, or together form a 5- to 12-membered mono- or bicyclic group optionally containing 1-2 heteroatoms selected from O, S and N; R3 = H or R4; R4 = aryl, heteroaryl or 3-8C cycloalkyl; 1-6C alkyl optionally substituted by aryl, heteroaryl, OH, 1-6C alkoxy or NR5R6; or COR7; R5, R6 = 1-6C alkyl or 1-6C hydroxyalkyl, or NR5R6 is a 5- to 7-membered saturated ring optionally containing 1-2 additional heteroatoms selected from O, S and N; R7 = aryl; 1-6C alkyl optionally substituted by NR5R6; amino optionally substituted by aryl, heteroaryl or optionally NR5R6-substituted 1-6C alkyl; or OR10; R10 = H, aryl or optionally NR5R6-substituted 1-6C alkyl; X = O, S, CH2 or CH2CH2; Ar = aryl, heteroaryl or aryl(1-6C)alkyl; aryl = phenyl, biphenylyl, naphthyl or tetrahydronaphthyl optionally substituted by halogen, 1-6C alkyl, OH, 1-6C alkoxy, 1-6C polyhaloalkyl, NH2, mono- or di(1-6C alkyl)amino, NO2, 1-6C acyl and/or 1-2C alkylenedioxy; heteroaryl = a 5- to 12-membered mono- or bicyclic aromatic group that contains 1-3 heteroatoms selected from O, S and N and is optionally substituted by halogen, 1-6C alkyl, OH, 1-6C alkoxy, 1-6C polyhaloalkyl, NH2 and/or mono- or di(1-6C alkyl)amino. Independent claims are also included for: (1) the preparation of (I) by reacting a compound of formula (II) with a compound of formula (III) to yield a compound of formula (Ia) which can then be reduced to form (Ib); (2) the one-pot preparation of (I) by reacting a compound of formula (II) with compounds of formulae (VIII) and (IX) to yield (Ia) which can then be reduced to form (Ib).

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Inventors:
Henri-Philip Yousson
Sylvianne Giorgi-Renault
Christoph Tratra
Gurham Atasi
Alan Pierre
Pierre Renard
Bruno Pfeiffer
Application Number:
JP2000355438A
Publication Date:
September 15, 2004
Filing Date:
November 22, 2000
Export Citation:
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Assignee:
Réra Bora Toir Servier
International Classes:
A61K31/47; A61K31/473; A61K31/4741; A61K31/4743; A61K31/4745; A61P35/00; C07D219/06; C07D221/06; C07D221/16; C07D221/18; C07D491/04; C07D491/044; C07D491/048; C07D491/056; C07D215/14; C07D491/14; C07D491/147; C07D491/153; C07D491/16; C07D491/22; C07D495/04; C07D495/14; C07D495/16; (IPC1-7): C07D219/06; A61K31/473; A61K31/4741; A61K31/4743; A61K31/4745; A61P35/00; C07D221/06; C07D221/18; C07D491/044; C07D491/147; C07D491/153; C07D491/22; C07D495/04; C07D495/14
Domestic Patent References:
JP49134685A
Other References:
MATSUO Keizo et al.,SYNTHESIS AND REACTION OF 9-ARYL-1H,3H-THIENO[3,4-b]-QUINOLIN-1-ONES,Chemistry Express,1993年,Vol. 8, No. 6,pp. 389-392
Attorney, Agent or Firm:
Hajime Tsukuni
Fumio Shinoda



 
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