公开(公告)号：US20060063789A1

公开(公告)日：2006-03-23

申请号：US10493446

申请日：2002-10-29

申请人： Eddy Jean Freyne ,  Peter Antonius ,  Marc Willems ,  Werner Johan ,  Paul Janssen ,  Paulus Joannes ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Michael Kukla ,  Hugo Gabriel ,  Bony Nuydens ,  Marc Mercken ,  Donald Ludovici ,  Herwig Janssen ,  Paul Maria ,  Graziella Janssen ,  Jasmine Werner ,  Maroussia Janssen ,  Theodora Arts

发明人： Eddy Jean Freyne ,  Peter Antonius ,  Marc Willems ,  Werner Johan ,  Paul Janssen ,  Paulus Joannes ,  Jan Heeres ,  Marc de Jonge ,  Lucien Koymans ,  Frederik Daeyaert ,  Michael Kukla ,  Hugo Gabriel ,  Bony Nuydens ,  Marc Mercken ,  Donald Ludovici ,  Herwig Janssen ,  Paul Maria ,  Graziella Janssen ,  Jasmine Werner ,  Maroussia Janssen ,  Theodora Arts

IPC分类号： A61K31/655 ,  A61K31/50 ,  A61K31/4965 ,  A61K31/513 ,  C07D241/18 ,  C07D239/47

CPC分类号： C07D239/42 ,  A61K31/506 ,  C07D239/47 ,  C07D239/48 ,  C07D239/50 ,  C07D403/12

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.

摘要翻译： 本发明涉及式的化合物