Title:
HIV阻害性ピリミジン誘導体
Document Type and Number:
Japanese Patent JP4838396
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:
JP2011134088A
Publication Date:
December 14, 2011
Filing Date:
June 16, 2011
Export Citation:
Assignee:
JANSSEN PHARMACEUTICA NAAMLOZE VENNOOTSCHAP
International Classes:
C07D239/48; A61K9/14; A61K31/505; A61K31/506; A61K31/5355; A61K31/541; A61K31/551; A61K31/7052; A61K45/00; A61K47/32; A61K47/36; A61K47/38; A61P31/18; C07C211/00; C07C255/42; C07C257/12; C07D233/96; C07D239/47; C07D401/12; C07D401/14; C07D403/12; C07D403/14; C07D405/12; C07D407/12; C07D409/12; C07D413/12; C07D417/12; C07D239/46; A61K; C07C; C07D
Foreign References:
| WO1999050250A1 |
Attorney, Agent or Firm:
Patent business corporation Odashima patent office