Title:
HIV阻害性ピリミジン誘導体
Document Type and Number:
Japanese Patent JP5539927
Kind Code:
B2
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.
Inventors:
The Jerome Emile Giorgiyu Guilmon
Patrice Palangian
Marc Rene de Yong
Lucien Maria Henrix Coymans
Hendrik Marten Vinkels
Frederik Fran Desiree Deyaard
Jiang Jerez
Ken Jeanne Alfon van Aken
Paulus Jioane Levi
Paul Adrian Jiang Jiansen
Patrice Palangian
Marc Rene de Yong
Lucien Maria Henrix Coymans
Hendrik Marten Vinkels
Frederik Fran Desiree Deyaard
Jiang Jerez
Ken Jeanne Alfon van Aken
Paulus Jioane Levi
Paul Adrian Jiang Jiansen
Application Number:
JP2011135468A
Publication Date:
July 02, 2014
Filing Date:
June 17, 2011
Export Citation:
Assignee:
JANSSEN PHARMACEUTICA NAAMLOZE VENNOOTSCHAP
International Classes:
C07D239/47; A61K9/10; A61K31/505; A61K31/506; A61K31/513; A61K31/5355; A61K31/5377; A61K31/541; A61K31/551; A61K31/675; A61K31/7072; A61K31/7076; A61K31/708; A61K45/00; A61K47/32; A61K47/34; A61K47/36; A61K47/38; A61K47/40; A61P31/14; A61P31/18; A61P43/00; C07C211/00; C07C255/42; C07C257/12; C07D233/96; 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
Domestic Patent References:
| JP54090121A | ||||
| JP2003525277A |
Foreign References:
| WO1999050250A1 | ||||
| EP0945443A1 | ||||
| WO2000012485A1 | ||||
| WO1997019065A1 |
Other References:
GHOSH,D.,2,4-Bis(arylamino)pyrimidines as antimicrobial agents,Journal of Medicinal Chemistry,1966年,Vol.9, No.3,p.423-4
Attorney, Agent or Firm:
Patent business corporation Odashima patent office