公开(公告)号：US07183288B2

公开(公告)日：2007-02-27

申请号：US10493454

申请日：2002-10-29

申请人： Eddy Jean Edgard Freyne ,  Peter Jacobus Johannes Antonius Buijnsters ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Jean Fernand Armand Lacrampe ,  Herwig Josephus Margareta Janssen, legal representative ,  Paul Peter Maria Janssen, legal representative ,  Graziella Maria Constantina Janssen, legal representative ,  Jasmine Josée Werner Janssen, legal representative ,  Maroussia Godelieve Frank Janssen, legal representative ,  Theodora Joanna Francisca Arts ,  Paulus Joannes Lewi ,  Jan Heeres ,  Marc René de Jonge ,  Lucien Maria Henricus Koymans ,  Frederik Frans Desiré Daeyaert ,  Michael Joseph Kukla ,  Hugo Alfons Gabriel Geerts ,  Rony Maria Nuydens ,  Marc Hubert Mercken ,  Donald William Ludovici

发明人： Paul Adriaan Jan Janssen, deceased

IPC分类号： A61K31/505 ,  C07D239/42

CPC分类号： C07D213/81 ,  C07D213/82 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21—C1-6alkyl; R21—O—; R21—S—; R21—C(═O)—; R21—S(═O)p—; R7—S(═O)p—; R7—S(═O)p—NH—; R21—S(═O)p—NH—; R7—C(═O)—; —NHC(═O)H; —C(═O)NHNH2; R7—C(═O)—NH—; R21—C(═O)—NH—; —C(═NH)R7; —C(═NH)R21; R4a or R4b each independently represent hydrogen, R8, —Y1—NR9—Y2—NR10R11, —Y1—NR9—Y1—R8, —Y1—NR9R10; provided that —X—R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.