GEORGE HYND,JOHN GARY MONTANA,HARRY FINCH,ROSA ARIENZO,BARBARA AVITABILE-WOO,MATHIAS DOMOSTOJ
申请号:
HRP20120554
公开号:
HRP20120554T1
申请日:
2012.07.06
申请国别(地区):
HR
年份:
2012
代理人:
摘要:
Compound of formula (I) are are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is -SO2- or *-SO2NR3- wherein the bond marked with an asterisk is attached to Ar1; R1 is hydrogen, fluoro, chloro, CN or CF3; R2 is hydrogen, fluoro or chloro; R3 is hydrogen, C1C8alkyl or C3-C7cycloalkyl; Ar1 is phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3- C7cycloalkyl, -O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Ar2 is phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C3- C3- C7cycloalkyl, -O(C1-C4alkyl) or C1C6alkyl, the latter two groups being optionally substituted by one or more fluoro atoms.Spoj koji je derivat indola formule I ili njegova farmaceutski prihvatljiva sol gdje X je SOili SO NR gdje je veza označena zvjezdicom spojena na Ar R je vodik fluor klor CN ili CF R je vodik fluor ili klor R je vodik C C alkil ili C C cikloalkil Ar je ili eročlana heteroarilna skupina izabrana između furanil tienil oksazolil tiazolil imidazolil pirazolil izoksazolil izotiazolil piridinil piridazinil pirimidinil i pirazinil gdje su fenil ili heteroarilne skupine po izboru supstituirane jednim ili višesupstituenata nezavisno izabranih između fluor klor CN C C cikloalkil O C C alkil ili C C alkil zadnje dvije skupine su po izboru supstituirane jednim ili više atoma fluora iAr je ili eroč