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Title:
HIV阻害性ピリミジン誘導体
Document Type and Number:
Japanese Patent JP2005507380
Kind Code:
A
Abstract:
This invention concerns HIV replication inhibitors of formulathe N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl;n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted Cl-6alkyloxyCl-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S(=O)pR6, -NH-S(=O)pR6, -C(=O)R6, -NHC(=O)H, -C(=O)NHNH2, -NHC(=O)R6, -C(=NH)R6 or a 5-membered heterocycle; X1 is -NR5-, -NH-NH-, -N=N-, -O-, -C(=O)-, C1-4alkanediyl, -CHOH-, -S-, -S(=O)p-, -X2-C1-4alkanediyl- or -C1-4alkanediyl-X2-; R3 is NHR13; NR13R14; -C(=O)-NER13; -C(=O)-NR13R14; -C(=O)-R15; -CH=N-NH-C(=O)-R16; substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl; substituted C2-6alkynyl; C1-6alkyl substituted with hydroxy and a second substituent; -C(=N-O-R8)-C1-4alkyl; R7; or -X3-R7; R4 is halo, hydroxy, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, cyano, nitro, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyl, formyl, amino, mono- or di(C1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

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Inventors:
Guilmon, Jerome Emile Giorgiyu
Parangyan, Patrice
De Jong, Marc Rene
Coymans, Lucien Maria Henrix
Vinkels, Hendrik Marten
Freyalik Franc Desire
Jerez, Jiang
Van Aken, Ken Jeanne Alfon
Levi, Paulus Giouane
Paul Jensen, Paul Adrien Jiang
Application Number:
JP2003521229A
Publication Date:
March 17, 2005
Filing Date:
August 09, 2002
Export Citation:
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Assignee:
JANSSEN PHARMACEUTICA NAAMLOZE VENNOOTSCHAP
International Classes:
A61K31/505; A61K31/506; A61K31/5355; A61K31/541; A61K31/551; A61K45/00; A61P31/18; C07C211/00; C07C255/42; C07C257/12; C07D233/96; C07D239/47; C07D239/48; C07D401/12; C07D401/14; C07D403/12; C07D403/14; C07D405/12; C07D407/12; C07D409/12; C07D413/12; C07D417/12; C07D239/46; A61K; C07C; C07D; (IPC1-7): C07D239/48; A61K31/505; A61K31/506; A61K31/5355; A61K31/541; A61K31/551; A61K45/00; A61P31/18; C07C255/42; C07D239/47; C07D401/12; C07D401/14; C07D403/12; C07D405/12; C07D409/12; C07D413/12; C07D417/12
Domestic Patent References:
JPS63159316A1988-07-02
JP2000035628A2000-02-02
JPS5490121A1979-07-17
JP2004525914A2004-08-26
JP2004532793A2004-10-28
JP2003525277A2003-08-26
JP2003532635A2003-11-05
Foreign References:
WO1999050920A11999-10-07
WO2000027825A12000-05-18
WO2001022938A12001-04-05
WO2001023362A22001-04-05
EP0945443A11999-09-29
US5958935A1999-09-28
WO2000012485A12000-03-09
WO1997019065A11997-05-29
Attorney, Agent or Firm:
Heikichi Odashima



 
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