Claims for Patent: 8,420,684
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Summary for Patent: 8,420,684
Title: | Inhibitors of glutaminyl cyclase |
Abstract: | The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, ##STR00001## or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R.sup.1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R.sup.2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R.sup.3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and --C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and --C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl).sub.2; -alkyl-heteroaryl; -alkyl(heteroaryl).sub.2; -alkyl(heteroaryl)(aryl); -aryl-O-aryl; aryl; heterocyclyl, -alkyl-C(O)-heterocyclyl, -alkyl-heterocyclyl, -alkyl-C(O)--NR.sup.5-heterocyclyl or -alkyl(heterocyclyl).sub.2 in any of which groups heterocyclyl may be optionally substituted by one or more groups selected from alkyl hydroxy and oxo; -heteroaryl; or -hydroxyalkylaryl; R.sup.4 represents H or C.sub.1-3 alkyl; R.sup.5 represents H or C.sub.1-3 alkyl; and X represents O or S. |
Inventor(s): | Thormann; Michael (Martinsried, DE), Altmstetter; Michael (Martinsried, DE), Treml; Andreas (Martinsried, DE), Heiser; Ulrich (Halle/Saale, DE), Buchholz; Mirko (Halle/Saale, DE), Niestroj; Andre J. (Sennewitz, DE) |
Assignee: | Probiodrug AG (Halle-Salle, DE) |
Application Number: | 11/937,146 |
Patent Claims: | 1. A compound of formula (I) ##STR00379## or a pharmaceutically acceptable salt thereof, including all tautomers and stereoisomers thereof wherein: R.sup.1 represents
heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R.sup.2 represents alkyl, which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and
hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl, oxo and hydroxy; aryl or heteroaryl of R.sup.2 may be optionally
substituted with one or more of alkyl, alkenyl, alkynyl, haloalkyl, -thioalkyl, -thiomethyl, SOalkyl, --SO.sub.2alkyl, SOcycloalkyl, alkoxy-, cycloalkyl, fluoroalkyl, --SO.sub.2cycloalkyl, alkenyloxy-, alkynyloxy-, --C(O)-alkyl, alkoxyalkyl-, nitro,
halogen, cyano, hydroxyl, oxo, --C(O)OH, --C(O)Oalkyl, --NH.sub.2, --NHalkyl, --N(alkyl).sub.2, --C(O)N(alkyl).sub.2, --C(O)NH.sub.2 or --C(O)NH(alkyl); R.sup.3 represents heteroaryl; alkyl, which may optionally be substituted by one of more groups
selected from alkoxy, amine, hydroxy and --C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, alkoxy, amine, hydroxy and --C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl).sub.2; -alkyl-heteroaryl; -alkyl(heteroaryl).sub.2; -alkyl(heteroaryl)(aryl); -aryl-O-aryl; aryl; heterocyclyl, -alkyl-C(O)-heterocyclyl, -alkyl-heterocyclyl, -alkyl-C(O)--NR.sup.5-heterocyclyl or -alkyl(heterocyclyl).sub.2 in any of which groups heterocyclyl may be
optionally substituted by one or more groups selected from alkyl, hydroxy and oxo; -heteroaryl; or -hydroxyalkylaryl; R.sup.4 represents H or C.sub.1-3 alkyl; R.sup.5 represents H or C.sub.1-3 alkyl; and X represents O or S.
2. A compound according to claim 1, wherein the compounds ##STR00380## are excluded from the definition of formula (I). 3. A compound according to claim 1, wherein R.sup.1 represents -alkylheteroaryl. 4. A compound according to claim 3, wherein R.sup.1 represents --C.sub.2-4 alkylheteroaryl. 5. A compound according to claim 3 wherein R.sup.1 represents 3-imidazol-1-yl-propyl. 6. A compound according to claim 1, wherein R.sup.1 represents -heteroaryl. 7. A compound according to claim 6, wherein R.sup.1 represents 1H-benzoimidazol-5-yl. 8. A compound according to claim 1, wherein R.sup.2 represents alkyl, which may optionally be substituted by hydroxy; carbocyclyl which may optionally be substituted by alkyl; aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl; and aryl or heteroaryl of R.sup.2 may be optionally substituted with one or more of alkyl, alkenyl, alkynyl, haloalkyl, -thioalkyl (e.g. -thiomethyl), SOalkyl, --SO.sub.2alkyl, SOcycloalkyl, alkoxy-, cycloalkyl, fluoroalkyl, --SO.sub.2cycloalkyl, alkenyloxy-, alkynyloxy-, --C(O)-alkyl, alkoxyalkyl-, nitro, halogen, cyano, hydroxyl, oxo, --C(O)OH, --C(O)Oalkyl, --NH.sub.2, --NHalkyl, --N(alkyl).sub.2, --C(O)N(alkyl).sub.2, --C(O)NH.sub.2 or --C(O)NH(alkyl). 9. A compound according to claim 8, wherein R.sup.2 represents alkyl, which is substituted by hydroxy; carbocyclyl which may optionally be substituted by alkyl; aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl; and aryl or heteroaryl of R.sup.2 may be optionally substituted with one or more of alkyl, alkenyl, alkynyl, haloalkyl, -thioalkyl (e.g. -thiomethyl), SOalkyl, --SO.sub.2alkyl, SOcycloalkyl, alkoxy-, cycloalkyl, fluoroalkyl, --SO.sub.2cycloalkyl, alkenyloxy-, alkynyloxy-, --C(O)-alkyl, alkoxyalkyl-, nitro, halogen, cyano, hydroxyl, oxo, --C(O)OH, --C(O)Oalkyl, --NH.sub.2, --NHalkyl, --N(alkyl).sub.2, --C(O)N(alkyl).sub.2, --C(O)NH.sub.2 or --C(O)NH(alkyl). 10. A compound according to claim 9, wherein R.sup.2 represents aryl; heteroaryl; -aryl-heterocyclyl; or cycloalkenyl which may optionally be substituted by alkyl; and aryl or heteroaryl of R.sup.2 may be optionally substituted with one or more of alkyl, alkenyl, alkynyl, haloalkyl, -thioalkyl (e.g. -thiomethyl), SOalkyl, --SO.sub.2alkyl, SOcycloalkyl, alkoxy-, cycloalkyl, fluoroalkyl, --SO.sub.2cycloalkyl, alkenyloxy-, alkynyloxy-, --C(O)-alkyl, alkoxyalkyl-, nitro, halogen, cyano, hydroxyl, oxo, --C(O)OH, --C(O)Oalkyl, --NH.sub.2, --NHalkyl, --N(alkyl).sub.2, --C(O)N(alkyl).sub.2, --C(O)NH.sub.2 or --C(O)NH(alkyl). 11. A compound according to claim 10, wherein R.sup.2 represents aryl or heteroaryl, which may be optionally substituted with one or more of alkyl, alkenyl, alkynyl, haloalkyl, -thioalkyl (e.g. -thiomethyl), SOalkyl, --SO.sub.2alkyl, SOcycloalkyl, alkoxy-, cycloalkyl, fluoroalkyl, --SO.sub.2cycloalkyl, alkenyloxy-, alkynyloxy-, --C(O)-alkyl, alkoxyalkyl-, nitro, halogen, cyano, hydroxyl, oxo, --C(O)OH, --C(O)Oalkyl, --NH.sub.2, --NHalkyl, --N(alkyl).sub.2, --C(O)N(alkyl).sub.2, --C(O)NH.sub.2 or --C(O)NH(alkyl). 12. A compound according to claim 11, wherein R.sup.3 represents alkyl, which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy, and --C(O)Oalkyl; carbocyclyl, which may be optionally substituted by hydroxy; -alkyl-aryl; -alkyl(aryl).sub.2; -alkyl-heteroaryl; -aryl-O-aryl; aryl; heteroaryl; -alkyl-heterocyclyl, -alkyl-C(O)--NR.sup.5-heterocyclyl or -alkyl-C(O)-heterocyclyl in any of which groups heterocyclyl may be optionally substituted by one or more groups selected from alkyl, hydroxyl and oxo; or -hydroxyalkylaryl. 13. A compound according to claim 12, wherein R.sup.3 represents alkyl; -alkyl(aryl).sub.2; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-C(O)-heterocyclyl; carbocyclyl, which may optionally be substituted by hydroxy; -aryl; or heteroaryl. 14. A compound according to claim 1, wherein R.sup.4 represents H. 15. A compound according to claim 1, wherein R.sup.5 represents H. 16. A compound according to claim 1, wherein X represents S. 17. A compound according to claim 1, wherein X represents O. 18. A compound selected from the group consisting of: 4-Cyclopropylimino-5-(3,4-dihydro-2H-pyran-2-yl)-1-(3-imidazol-1-yl-propy- l)-imidazolidin-2-one; 4-Cyclohexylimino-5-(3,4-dihydro-2H-pyran-2-yl)-1-(3-imidazol-1-yl-propyl- )-imidazolidin-2-one; 4-Cyclohexylimino-5-(2,3-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imid- azolidin-2-one; 4-Cyclohexylimino-5-(3,5-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imid- azolidin-2-one; 5-(4-Chloro-3-fluoro-phenyl)-4-cyclohexylimino-1-(3-imidazol-1-yl-propyl)- -imidazolidin-2-one; 5-(2-Chloro-phenyl)-4-cyclohexylimino-1-(3-imidazol-1-yl-propyl)-imidazol- idin-2-one; 5-Butyl-4-cyclohexylimino-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 4-Cyclohexylimino-5-(2-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imidazol- idin-2-one; 5-(2,3-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-1-phenyl-ethylimino-- imidazolidin-2-one; 5-(2-Chloro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-1-phenyl-ethylimino-imid- azolidin-2-one; 5-Butyl-1-(3-imidazol-1-yl-propyl)-4-1-phenyl-ethylimino-imidazolidin-2-o- ne; 4-2-(1,3-Dihydro-isoindol-2-yl)-2-oxo-ethylimino-5-(2-hydroxy-3-methyl- -phenyl)-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 5-(4-Chloro-3-fluoro-phenyl)-4-2-(1,3-dihydro-isoindol-2-yl)-2-oxo-ethyli- mino-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 1-(3-Imidazol-1-yl-propyl)-4-methylimino-5-phenyl-imidazolidin-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-1-(3-imidazol-1-yl-propyl)-4-methylimino-im- idazolidin-2-one; 5-Butyl-1-(3-imidazol-1-yl-propyl)-4-methylimino-imidazolidin-2-one; 5-(4-Hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-methylimino-imidazolidi- n-2-one; 4-4-Chloro-benzylimino-1-(3-imidazol-1-yl-propyl)-5-phenyl-imidaz- olidin-2-one; 4-4-Chloro-benzylimino-5-(3,5-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)- -imidazolidin-2-one; 4-4-Chloro-benzylimino-5-(4-chloro-3-fluoro-phenyl)-1-(3-imidazol-1-yl-pr- opyl)-imidazolidin-2-one; 4-4-Chloro-benzylimino-5-(2-chloro-phenyl)-1-(3-imidazol-1-yl-propyl)-imi- dazolidin-2-one; 5-Butyl-4-4-chloro-benzylimino-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-- one; 4-4-Chloro-benzylimino-5-(2-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)- -imidazolidin-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-1-(3-imidazol-1-yl-propyl)-4-3,4,5-trimetho- xy-benzylimino-imidazolidin-2-one; 5-(2,3-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-3,4,5-trimethoxy-ben- zylimino-imidazolidin-2-one; 5-(2-Chloro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-3,4,5-trimethoxy-benzyli- mino-imidazolidin-2-one; 5-Butyl-1-(3-imidazol-1-yl-propyl)-4-3,4,5-trimethoxy-benzylimino-imidazo- lidin-2-one; 5-(2-Fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-3,4,5-trimethoxy-benzyli- mino-imidazolidin-2-one; 4-2,3-Dihydro-benzo1,4dioxin-6-ylimino-1-(3-imidazol-1-yl-propyl)-5-propy- l-imidazolidin-2-one; 4-2,3-Dihydro-benzo1,4dioxin-6-ylimino-5-(3,4-dihydro-2H-pyran-2-yl)-1-(3- -imidazol-1-yl-propyl)-imidazolidin-2-one; 5-(2,3-Difluoro-phenyl)-4-2,3-dihydro-benzo1,4dioxin-6-ylimino-1-(3-imida- zol-1-yl-propyl)-imidazolidin-2-one; 5-(3,5-Difluoro-phenyl)-4-2,3-dihydro-benzo1,4dioxin-6-ylimino-1-(3-imida- zol-1-yl-propyl)-imidazolidin-2-one; 5-(4-Chloro-3-fluoro-phenyl)-4-2,3-dihydro-benzo1,4dioxin-6-ylimino-1-(3-- imidazol-1-yl-propyl)-imidazolidin-2-one; 5-(2-Chloro-phenyl)-4-2,3-dihydro-benzo1,4dioxin-6-ylimino-1-(3-imidazol-- 1-yl-propyl)-imidazolidin-2-one; 5-Butyl-4-2,3-dihydro-benzo1,4dioxin-6-ylimino-1-(3-imidazol-1-yl-propyl)- -imidazolidin-2-one; 4-Butylimino-5-(2,3-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imidazoli- din-2-one; 4-Butylimino-5-(3,5-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)- -imidazolidin-2-one; 1-(3-Imidazol-1-yl-propyl)-5-phenyl-4-2-thiophen-2-yl-ethylimino-imidazol- idin-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-1-(3-imidazol-1-yl-propyl)-4-2-thiophen-2-y- l-ethylimino-imidazolidin-2-one; 5-(2,3-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-thiophen-2-yl-ethy- limino-imidazolidin-2-one; 5-(3,5-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-thiophen-2-yl-ethy- limino-imidazolidin-2-one; 5-(4-Chloro-3-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-thiophen-2-yl- -ethylimino-imidazolidin-2-one; 5-(2-Chloro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-(2-thiophen-2-yl-ethylim- ino)-imidazolidin-2-one; 5-(2-Fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-thiophen-2-yl-ethylimi- no-imidazolidin-2-one; 5-(4-Hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-thiophen-2-yl-ethylim- ino-imidazolidin-2-one; 5-(2-Hydroxy-3-methyl-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-- yl)-ethylimino-imidazolidin-2-one; 1-(3-Imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino-5-thiophen-3-yl- -imidazolidin-2-one; 1-(3-Imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino-5-methyl-imidaz- olidin-2-one; 1-(3-Imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino-5-phenyl-imidaz- olidin-2-one; 1-(3-Imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino-5-(1H-pyrrol-2-- yl)-imidazolidin-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-- yl)-ethylimino-imidazolidin-2-one; 5-(2,3-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-et- hylimino-imidazolidin-2-one; 5-(3,5-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-et- hylimino-imidazolidin-2-one; 5-(4-Chloro-3-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-y- l)-ethylimino-imidazolidin-2-one; 5-(2-Chloro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethyli- mino-imidazolidin-2-one; 5-Hydroxymethyl-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino- -imidazolidin-2-one; 5-Cyclopropyl-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino-i- midazolidin-2-one; 5-Furan-2-yl-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino-im- idazolidin-2-one; 5-Butyl-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino-imidazo- lidin-2-one; 5-Ethyl-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethylimino-imidazo- lidin-2-one; 5-(2-Fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethyli- mino-imidazolidin-2-one; 5-(3-Fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethyli- mino-imidazolidin-2-one; 5-(4-Fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethyli- mino-imidazolidin-2-one; 5-(4-Hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-2-(1H-indol-3-yl)-ethyl- imino-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-1-(3-imidazol-1-yl- -propyl)-5-thiophen-3-yl-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-1-(3-imidazol-1-yl- -propyl)-5-phenyl-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-5-(3,4-dihydro-2H-- pyran-2-yl)-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 5-(2,3-Difluoro-phenyl)-4-2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-ethyl- imino-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 5-(3,5-Difluoro-phenyl)-4-2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-ethyl- imino-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 5-(4-Chloro-3-fluoro-phenyl)-4-2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-- ethylimino-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 5-(2-Chloro-phenyl)-4-2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimin- o-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-5-hydroxymethyl-1-- (3-imidazol-1-yl-propyl)-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-5-furan-2-yl-1-(3-- imidazol-1-yl-propyl)-imidazolidin-2-one; 5-Butyl-4-2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-1-(3-imida- zol-1-yl-propyl)-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-5-ethyl-1-(3-imida- zol-1-yl-propyl)-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-5-(2-fluoro-phenyl- )-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-5-(3-fluoro-phenyl- )-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-5-(4-fluoro-phenyl- )-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 4-2-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-oxo-ethylimino-5-(4-hydroxy-pheny- l)-1-(3-imidazol-1-yl-propyl)-imidazolidin-2-one; 4-Benzhydrylimino-1-(3-imidazol-1-yl-propyl)-5-methyl-imidazolidin-2-one; 4-Benzhydrylimino-1-(3-imidazol-1-yl-propyl)-5-phenyl-imidazolidin-2-one; 4-Benzhydrylimino-5-(3,4-dihydro-2H-pyran-2-yl)-1-(3-imidazol-1-yl-propyl- )-imidazolidin-2-one; 4-Benzhydrylimino-5-(2,3-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imid- azolidin-2-one; 4-Benzhydrylimino-5-(3,5-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imid- azolidin-2-one; 4-Benzhydrylimino-5-hydroxymethyl-1-(3-imidazol-1-yl-propyl)-imidazolidin- -2-one; 4-Benzhydrylimino-5-butyl-1-(3-imidazol-1-yl-propyl)-imidazolidin-- 2-one; 4-Benzhydrylimino-5-(2-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-im- idazolidin-2-one; 4-Benzhydrylimino-5-(3-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imidazol- idin-2-one; 4-Benzhydrylimino-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-imidazo- lidin-2-one; 5-(3,5-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-pyridin-3-ylmethylim- ino-imidazolidin-2-one; 5-(3-Fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-pyridin-3-ylmethylimino-- imidazolidin-2-one; 4-Benzylimino-1-(3-imidazol-1-yl-propyl)-5-phenyl-imidazolidin-2-one; 4-Benzylimino-1-(3-imidazol-1-yl-propyl)-5-(1H-pyrrol-2-yl)-imidazolidin-- 2-one; 4-Benzylimino-5-(2,3-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-im- idazolidin-2-one; 4-Benzylimino-5-(3,5-difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imidazol- idin-2-one; 4-Benzylimino-5-(4-chloro-3-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imi- dazolidin-2-one; 4-Benzylimino-5-(2-chloro-phenyl)-1-(3-imidazol-1-yl-propyl)-imidazolidin- -2-one; 4-Benzylimino-5-(2-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-imida- zolidin-2-one; 4-Benzylimino-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-imidazolidi- n-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-1-(3-imidazol-1-yl-propyl)-4-4-phen- oxy-phenylimino-imidazolidin-2-one; 5-(4-Chloro-3-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-4-phenoxy-pheny- limino-imidazolidin-2-one; 5-Hydroxymethyl-1-(3-imidazol-1-yl-propyl)-4-4-phenoxy-phenylimino-imidaz- olidin-2-one; 5-Butyl-1-(3-imidazol-1-yl-propyl)-4-4-phenoxy-phenylimino-imidazolidin-2- -one; 4-3,3-Diphenyl-propylimino-1-(3-imidazol-1-yl-propyl)-5-propyl-imida- zolidin-2-one; 4-3,3-Diphenyl-propylimino-1-(3-imidazol-1-yl-propyl)-5-phenyl-imidazolid- in-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-4-3,3-diphenyl-propylimino-1-(3-im- idazol-1-yl-propyl)-imidazolidin-2-one; 5-(2,3-Difluoro-phenyl)-4-3,3-diphenyl-propylimino-1-(3-imidazol-1-yl-pro- pyl)-imidazolidin-2-one, 5-(3,5-Difluoro-phenyl)-4-3,3-diphenyl-propylimino-1-(3-imidazol-1-yl-pro- pyl)-imidazolidin-2-one; 5-(4-Chloro-3-fluoro-phenyl)-4-3,3-diphenyl-propylimino-1-(3-imidazol-1-y- l-propyl)-imidazolidin-2-one; 5-(2-Chloro-phenyl)-4-3,3-diphenyl-propylimino-1-(3-imidazol-1-yl-propyl)- -imidazolidin-2-one; 4-3,3-Diphenyl-propylimino-5-hydroxymethyl-1-(3-imidazol-1-yl-propyl)-imi- dazolidin-2-one; 4-3,3-Diphenyl-propylimino-5-(2-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)- -imidazolidin-2-one; 4-3,3-Diphenyl-propylimino-5-(3-fluoro-phenyl)-1-(3-imidazol-1-yl-propyl)- -imidazolidin-2-one; 5-(2,3-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-tetrahydro-furan-2-y- lmethylimino-imidazolidin-2-one; 5-(3,5-Difluoro-phenyl)-1-(3-imidazol-1-yl-propyl)-4-tetrahydro-furan-2-y- lmethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-methylimino-imidazolidin-2-- one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-fluoro-phenyl)-4-cyclopropyli- mino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-1,1,3,3-tetramethyl-butylimino-5-p-tolyl-imid- azolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-thiophen-2-yl)-4-2-oxo-2-piperidin-1- -yl-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(6-methyl-1H-indol-3-yl)-4-3-phenyl-propylimi- no-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-indan-1-ylimino-5-quinolin-4-yl-imidazolidin-- 2-one; 1-(1H-Benzoimidazol-5-yl)-4-2-hydroxy-cyclohexylimino-5-(1H-indol-5- -yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,3-dihydro-benzo1,4dioxin-6-yl)-4-methylimi- no-imidazolidin-2-one; 3-{3-(1H-Benzoimidazol-5-yl)-5-benzylimino-2-thioxo-imidazolidin-4-yl}-ch- romen-4-one; 2-(1-(1H-benzo[d]imidazol-5-yl)-5-(3,5-dibromophenyl)-2-thioxoimidazolidi- n-4-ylideneamino)-1-thiomorpholinoethan-one; 3-(1-(1H-benzo[d]imidazol-5-yl)-5-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2- -thioxoimidazolidin-4-ylideneamino)benzo-nitrile; 1-(1H-Benzoimidazol-5-yl)-4-2-hydroxy-cyclohexylimino-5-(6-methyl-4-oxo-4- H-chromen-3-yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(4-chloro-phen- yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(4-pyrrolidin-1-yl-phenyl)- -imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-cycloheptylimino-5-(2,4,4-trimethyl-pentyl)-i- midazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-dibromo-phenyl)-4-3-phenyl-propylimino-i- midazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(3,5-dibromo-phenyl)-4-1H-indol-5-ylmethylimi- no-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(4-bromo-phenyl)-imidazolidine-- 2-thione; 2-(1-(1H-benzo[d]imidazol-5-yl)-5-(3-chloro-2,6-difluorophenyl)-- 2-thioxoimidazolidin-4-ylideneamino)-1-(3-hydroxypiperidin-1-yl)ethanone; 1-(1H-Benzoimidazol-5-yl)-5-(2-chloro-phenyl)-4-2-oxo-2-thiomorpholin-4-y- l-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2-ethyl-phenyl)-4-1,2,3,4-tetrahydro-naphtha- len-1-ylimino-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-2-thiophen-2-- yl-ethylimino-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(2-trifluoromethyl-phenyl)-4-1,2,2-trimethyl-- propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-1,2-diphenyl-- ethylimino-imidazolidine-2-thione; 3-(1-(1H-benzo[d]imidazol-5-yl)-5-(2,4-dimethylphenyl)-2-thioxoimidazolid- in-4-ylideneamino)benzo-nitrile; 1-(1H-Benzoimidazol-5-yl)-4-methylimino-5-p-tolyl-imidazolidine-2-thione; 3-(1H-Benzoimidazol-5-yl)-5-2-hydroxy-cyclohexylimino-5'-methyl-1,3,4,5-t- etrahydro-3'H-4,4'biimidazolyl-2-one; 2-1-(1H-Benzo[d]imidazol-5-yl)-5-(5-bromobenzo[d][1,3]dioxol-6-yl)-2-thio- xoimidazolidin-4-ylideneamino)-N-(piperidin-1-yl)acetamide; 2-1-(1H-Benzoimidazol-5-yl)-2-thioxo-5-(2-trifluoromethyl-phenyl)-imidazo- lidin-(4Z)-ylideneamino-1-piperidin-1-yl-ethanone; 1-(1H-Benzoimidazol-5-yl)-4-1H-indol-5-ylmethylimino-5-p-tolyl-imidazolid- ine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-indan-1-ylimino-imidazolid- ine-2-thione; 1-{3-1-(3H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-2-thioxo-imidazolidin-(- 4Z)-ylideneamino-propyl}-pyrrolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(3,5-difluoro-- phenyl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-cyclohex-1-enyl-4-2-trifluoromethyl-phenylimi- no-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-1,2,3,4-tetrahydro-naphthalen-1-ylimino-5-(2,- 4,4-trimethyl-pentyl)-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(4-methylsulfa- nyl-phenyl)-imidazolidine-2-thione; 2-(3-(1H-benzo[d]imidazol-5-yl)-5-(3-bromophenyl)-2-thioxoimidazolidin-4-- ylideneamino)-1-thiomorpholinoetha-none; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-difluoro-phenyl)-4-2-hydroxy-2-phenyl-et- hylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-2-(3-hydroxy- -piperidin-1-yl)-2-oxo-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]thiadiazol-5-yl-4-3-(2-oxo-pyr- rolidin-1-yl)-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-phenyl)-4-isopropylimino-imidaz- olidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-3-dimethylamino-propylimino-5-naphthalen-2-yl- -imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropylimino-5-(2-trifluoromethyl-phenyl)- -imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-methylimino-5-naphthalen-2-yl-imidazolidin-2-- one; 1-(1H-Benzoimidazol-5-yl)-5-(2-ethyl-phenyl)-4-1,2,3,4-tetrahydro-nap- hthalen-1-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-1,2,3,4-tetrahydro-naphtha- len-1-ylimino-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(4-chloro-phenyl)-imidazolidin-- 2-one; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-3-morpholin-4-yl-prop- ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-1,2-diphenyl-ethylimino-im- idazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-1,2,2-trimet- hyl-propylimino-imidazolidine-2-thione; 5-Benzobthiophen-2-yl-1-(1H-benzoimidazol-5-yl)-4-3-(2-oxo-pyrrolidin-1-y- l)-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-methylimino-5-p-tolyl-imidazolidin-2-one, 5-Benzo1,3dioxol-5-yl-1-(1H-benzoimidazol-5-yl)-4-3-(2-oxo-pyrrolidin-1-y- l)-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-cyclohex-1-enyl-4-1,2-diphenyl-ethylimino-imi- dazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-1H-indol-5-ylmethylimino-5-p-tolyl-imidazolid- in-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-naphthalen-2-yl-i- midazolidin-2-one; 5-Benzobthiophen-2-yl-1-(1H-benzoimidazol-5-yl)-4-3-phenyl-propylimino-im- idazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(1H-indol-5-yl- )-imidazolidin-2-one; 3-{3-(1H-Benzoimidazol-5-yl)-5-isopropylimino-2-oxo-imidazolidin-4-yl}-be- nzonitrile; 1-(2-(1-(1H-benzo[d]imidazol-5-yl)-5-(3-bromophenyl)-2-thioxoimidazolidin- -4-ylideneamino)ethyl)pyrrolidin-2-one; 5-Benzo1,3dioxol-5-yl-1-(1H-benzoimidazol-5-yl)-4-benzotriazol-1-ylmethyl- imino-imidazolidine-2-thione; 1-(1H-benzo[d]imidazol-6-yl)-4-(benzylimino)-5-(3-bromophenyl)imidazolidi- n-2-one; 1-(1H-Benzoimidazol-5-yl)-5-isopropyl-4-1 ,1,3,3-tetramethyl-butylimino-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(3,5-dibromo-phenyl)-4-2-oxo-2-thiomorpholin-- 4-yl-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-dimethylamino-phenyl)-4-pyridin-3-ylmethyl- imino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(4-methylsulfa- nyl-phenyl)-imidazolidin-2-one; 2-(1-(1H-benzo[d]imidazol-6-yl)-5-(4-bromothiophen-2-yl)-2-thioxoimidazol- idin-4-ylideneamino)-1-(3,4-dihydroisoquinolin-2(1H)-yl)ethanone; 1-(3H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-1,2,3,4-tetr- ahydro-naphthalen-1-ylimino-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-thiophen-2-yl)-4-cyclohexylimino-imi- dazolidin-2-one; 2-(1-(1H-benzo[d]imidazol-6-yl)-5-(3-chloro-2,6-difluorophenyl)-2-thioxoi- midazolidin-4-ylideneamino)-1-(piperidin-1-yl)ethanone; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(3,5-dibromo-phenyl)-imida- zolidin-2-one; 2-(1-(1H-benzo[d]imidazol-6-yl)-5-(4-bromothiophen-2-yl)-2-thioxoimidazol- idin-4-ylideneamino)-1-(piperidin-1-yl)ethanone; 1-(3H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-2,6-dichloro- -phenylimino-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(6-methyl-pyri- din-2-yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2-chloro-phenyl)-4-1,2,3,4-tetrahydro-naphth- alen-1-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-indan-1-ylimino-5-quinolin-4-yl-imidazolidine- -2-thione; 3-{3-(1H-Benzoimidazol-5-yl)-5-2,5-dichloro-phenylimino-2-thiox- o-imidazolidin-4-yl}-chromen-4-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-indan-1-ylim- ino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-phenyl)-4-2,5-dichloro-phenylimino-- imidazolidine-2-thione; 5-Benzo1,3dioxol-5-yl-1-(1H-benzoimidazol-5-yl)-4-methylimino-imidazolidi- n-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-cyclo- hexylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-1,2,3,4-tetrahydro-naphthalen-1-ylimino-5-(2,- 4,4-trimethyl-pentyl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-indan-1-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-cyclohexylimino-imidazolid- in-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-1,1- ,3,3-tetramethyl-butylimino-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-2-oxo-2-thiom- orpholin-4-yl-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-4-fluoro-phenylimino-5-quinolin-4-yl-imidazol- idine-2-thione; 3-{3-(1H-Benzoimidazol-5-yl)-5-2-hydroxy-cyclohexylimino-2-thioxo-imidazo- lidin-4-yl}-6-methyl-chromen-4-one; 1-(3H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(6-bromo-benzo- 1,3dioxol-5-yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cycloheptylimino-5-(tetrahydro-furan-3-yl)-im- idazolidin-2-one; Methyl 2-(1-(1H-benzo[d]imidazol-5-yl)-5-(2,4-dimethylcyclohex-3-enyl)-2-oxoimid- azolidin-4-ylideneamino)propanoate; 2-(5-(benzo[b]thiophen-2-yl)-1-(1H-benzo[d]imidazol-5-yl)-2-thioxoimidazo- lidin-4-ylideneamino)-1-thiomorpholinoethan-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-2-oxo-2-thiomorpholin-4-yl- -ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-oxo-4H-chromen-3-yl)-4-3-phenyl-propylimin- o-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(4-pyrrolidin-1-yl-phenyl)- -imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-phenyl)-4-cyclopentylimino-imidazol- idin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-3-morpholin-4-yl-propylimino-5-quinolin-4-yl-- imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-indan-1-ylimino-5-(6-methyl-4-oxo-4H-chromen-- 3-yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2,5-dichloro-phenylimino-5-(3-hydroxy-phenyl)- -imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-3-(2-oxo-pyrrolidin-1-yl)-propylimino-5-quino- lin-8-yl-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(4-bromo-phenyl)-imidazolidin-2- -one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(2,3-dihy- dro-benzo1,4dioxin-6-yl)-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-indan-1-ylimino-5-(1H-indol-5-yl)-imidazolidi- n-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-phenyl)-4-2-(1H-indol-3- -yl)-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-cyclohexylim- ino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-naphthalen-2-yl-4-pyridin-3-ylmethylimino-imi- dazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2-(3-hydroxy-pyrrolidin-1-yl)-2-oxo-ethylimin- o-5-(1H-indol-5-yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(5-chloro-1H-indol-3-yl)-4-methylimino-imidaz- olidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-3-phenyl-propylimino-imidaz- olidin-2-one; 2-(1-(1H-Benzo[d]imidazol-5-yl)-5-(2-fluoro-4-methoxyphenyl)-2-thioxoimid- azolidin-4-ylideneamino)-1-thiomorpholinoethanone; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(1H-indol-5-yl)-imidazolid- in-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-difluoro-phenyl)-4-pyridin-3-yl- methylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-1,2,3,4-tetr- ahydro-naphthalen-1-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-difluoro-phenyl)-4-2-hydroxy-2-phenyl-et- hylimino-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(6-methyl-1H-indol-3-yl)-imidaz- olidin-2-one; 1-{3-1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]thiadiazol-5-yl-2-thioxo-- imidazolidin-(4Z)-ylideneamino-propyl}-pyrrolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(6-fluoro-1H-indol-3-yl)-4-3-phenyl-propylimi- no-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2-morpholin-4-yl-ethylimino-5-naphthalen-2-yl- -imidazolidin-2-one; Methyl 2-(1-(1H-benzo[d]imidazol-5-yl)-2-oxo-5-phenylimidazolidin-4-ylideneamino- )propanoate; 1-(1H-Benzoimidazol-5-yl)-5-(2,3-dihydro-benzo1,4dioxin-6-yl)-4-2,3-dihyd- ro-benzo1,4dioxin-6-ylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(4-bromo-thiophen-2-yl)-4-1,2,3,4-tetrahydro-- naphthalen-1-ylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-2,6-dichloro-phenylimino-5-p-tolyl-imidazolid- ine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]thiadiazol-5-yl-4-2-hydroxy-cy- clohexylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(6-methyl-4-oxo-4H-chromen-3-yl)-4-(3-phenyl-- propylimino)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-cyclohex-1-enyl-4-1,2-diphenyl-ethylimino-imi- dazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-3-(2-oxo-pyrrolidin-1-yl)-- propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-dimethylamino-phenyl)-4-indan-1-ylimino-im- idazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-2-(4-methyl-- 1,4diazepan-1-yl)-2-oxo-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(3,5-difluoro-phenyl)-imid- azolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2-ethyl-phenylimino-5-phenyl-imidazolidin-2-o- ne; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(4-oxo-4H-chromen-3-yl)- -imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-3-(2-oxo-pyrrolidin-1-yl)-propylimino-5-quino- lin-4-yl-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-2-(4-hydroxy-piperidin-1-yl)-2-oxo-ethylimino- -5-(1H-indol-5-yl)-imidazolidin-2-one; Methyl 2-(1-(1H-benzo[d]imidazol-5-yl)-2-thioxo-5-p-tolylimidazolidin-4-ylidenea- mino)propanoate; 1-(3H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-2-oxo-2-pipe- ridin-1-yl-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(4-chloro-phenyl)-imidazolidine- -2-thione; 1-(3-(5-(benzo[b]thiophen-2-yl)-1-(1H-benzo[d]imidazol-5-yl)-2-- thioxoimidazolidin-4-ylideneamino)propyl)pyrrolidin-2-one; 4-(3-(Dimethylamino)propylimino)-1-(1H-benzo[d]imidazol-5-yl)-5-m-tolylim- idazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-isopropylimi- no-imidazolidin-2-one; 1-(3-(5-(benzo[d][1,3]dioxol-5-yl)-1-(1H-benzo[d]imidazol-5-yl)-2-thioxoi- midazolidin-4-ylideneamino)propyl)pyrrolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-naphthalen-2-yl-imidazolid- ine-2-thione; 3-(3H-Benzoimidazol-5-yl)-5-indan-1-ylimino-5'-methyl-1,3,4,5-tetrahydro-- 3'H-4,4'biimidazolyl-2-one; 5-Benzobthiophen-2-yl-1-(1H-benzoimidazol-5-yl)-4-3-phenyl-propylimino-im- idazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-2,3-dihydro-benzo1,4dioxin-6-ylimino-5-(2,4-d- imethyl-cyclohex-3-enyl)-imidazolidin-2-one; 5-Benzobthiophen-2-yl-1-(1H-benzoimidazol-5-yl)-4-2-thiophen-2-yl-ethylim- ino-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(3-bromo-phenyl)-imidazolidine-- 2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-phenyl)-4-1,1,3,3-tetr- amethyl-butylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(6-methyl-4-oxo-4H-chromen-3-yl)-4-3-morpholi- n-4-yl-propylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-2-bromo-phenylimino-5-naphthalen-2-yl-imidazo- lidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-cyclohex-1-enyl-4-2-oxo-2-thiomorpholin-4-yl-- ethylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-cyclohexylimi- no-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(6-methyl-4-oxo-4H-chromen-3-yl)-4-3-(2-oxo-p- yrrolidin-1-yl)-propylimino-imidazolidin-2-one; Methyl 2-(1-(1H-benzo[d]imidazol-5-yl)-5-(3-chloro-2,6-difluorophenyl)-2-thioxoi- midazolidin-4-ylideneamino)propanoate; 1-(1H-Benzoimidazol-5-yl)-4-methylimino-5-(4-pyrrolidin-1-yl-phenyl)-imid- azolidin-2-one; 2-(1-(1H-benzo[d]imidazol-5-yl)-5-(quinolin-4-yl)-2-thioxoimidazolidin-4-- ylideneamino)-1-(4-hydroxypiperidin-1-yl)ethanone; 1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]thiadiazol-5-yl-4-benzotriazol- -1-ylmethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-phenyl)-4-cyclopentylimino-imidazol- idine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-indan-1-ylim- ino-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-1,2,2-trimet- hyl-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-3-(2-oxo-pyr- rolidin-1-yl)-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-1,2,2-trimet- hyl-propylimino-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(6-methyl-pyri- din-2-yl)-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(2-chloro-phenyl)-4-1,2,3,4-tetrahydro-naphth- alen-1-ylimino-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-quinolin-4-yl-- imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(4-dimethylami- no-phenyl)-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-fluoro-phenyl)-4-2-(3-hydroxy-pyr- rolidin-1-yl)-2-oxo-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]thiadiazol-5-yl-4-2-(3-hydroxy- -pyrrolidin-1-yl)-2-oxo-ethylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-cycloheptylimino-5-(2,4-dimethyl-phenyl)-imid- azolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-3-phenyl-propylimino-imidaz- olidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-m-tolyl-imidaz- olidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-4-1 ,1,3,3-tetramethyl-butylimino-imidazolidine-2-thione; 5-Benzo1,3dioxol-5-yl-1-(1H-benzoimidazol-5-yl)-4-2-ethyl-phenylimino-imi- dazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-2-ethyl-phen- ylimino-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-3-(2-oxo-pyrrolidin-1-yl)-p- ropylimino-imidazolidin-2-one; Methyl 2-(1-(1H-benzo[d]imidazol-5-yl)-5-(4-chloro-2,6-difluorophenyl)-2-oxoimid- azolidin-4-ylideneamino)propanoate; 1-(3H-Benzoimidazol-5-yl)-4-2-bromo-phenylimino-5-(1H-indol-5-yl)-imidazo- lidine-2-thione; 5-Benzo1,3dioxol-5-yl-1-(1H-benzoimidazol-5-yl)-4-2,3-dihydro-benzo1,4dio- xin-6-ylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-1 ,1,3,3-tetramethyl-butylimino-5-p-tolyl-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-2-oxo-2-thio- morpholin-4-yl-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]-5-yl-4-2-bromo-phenylimino-im- idazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(3,5-dibromo-phenyl)-4-2-morpholin-4-yl-ethyl- imino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2-hydroxy-cyclohexylimino-5-(4-oxo-4H-chromen- -3-yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-1,3-dimethyl-butylimino-5-(2-trifluoromethyl-- phenyl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2,5-dichloro-phenylimino-5-m-tolyl-imidazolid- ine-2-thione; 1-(1H-Benzoimidazol-5-yl)-4-2-bromo-phenylimino-5-(2,4-dimethyl-cyclohex-- 3-enyl)-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-4-cycloheptylimino-5-(3,5-dibromo-phenyl)-imida- zolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-fluoro-phenyl)-4-2-oxo-2-piperidi- n-1-yl-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-dibromo-phenyl)-4-3-phenyl-propylimino-i- midazolidin-2-one; Methyl 2-(1-(1H-benzo[d]imidazol-5-yl)-5-phenyl-2-thioxoimidazolidin-4-ylideneam- ino)propanoate; 1-(3H-Benzoimidazol-5-yl)-5-(3,5-dibromo-phenyl)-4-1H-indol-5-ylmethylimi- no-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,3-dihydro-benzo1,4dioxin-6-yl)-4-2-(4-meth- yl-1,4diazepan-1-yl)-2-oxo-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-2-(4-methyl-1,4diazepan-1-y- l)-2-oxo-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2-methoxy-ethylimino-5-p-tolyl-imidazolidin-2- -one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-naphthale- n-2-yl-imidazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-cyclopropylimino-imidazoli- din-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(4-bromo-thiophen-2-yl)-4-1,2,3,4-t- etrahydro-naphthalen-1-ylimino-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]thiadiazol-5-yl-4-2-hydroxy-cy- clohexylimino-imidazolidine-2-thione; 3-{3-(1H-Benzoimidazol-5-yl)-5-3-phenyl-propylimino-2-thioxo-imidazolidin- -4-yl}-6-methyl-chromen-4-one; 1-(3H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-2-thiophen-2-- yl-ethylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-cycloheptylimino-5-(2,4,4-trimethyl-pentyl)-i- midazolidine-2-thione; 1-(3H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-2-(4-hydroxy- -piperidin-1-yl)-2-oxo-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2-ethyl-phenylimino-5-phenyl-imidazolidine-2-- thione; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-fluoro-phenyl)-4-cyclopent- ylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-1,2,2-trimet- hyl-propylimino-imidazolidin-2-one; Methyl 2-(1-(1H-benzo[d]imidazol-5-yl)-2-thioxo-5-p-tolylimidazolidin-4-ylidenea- mino)propanoate; 1-(3H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-3-(2-oxo-pyrrolidin-1-yl)-- propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(4-dimethylami- no-phenyl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-fluoro-phenyl)-4-3-(2-oxo-pyrroli- din-1-yl)-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-m-tolyl-imidaz- olidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-imidazolidin-2-o- ne; 1-(1H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-1,2-diphen- yl-ethylimino-imidazolidin-2-one; 4-(2-Oxo-2-(piperidin-1-yl)ethylimino)-1-(1H-benzo[d]imidazol-5-yl)-5-(5-- bromobenzo[d][1,3]dioxol-6-yl)imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-methylimino-5-(6-methyl-4-oxo-4H-chromen-3-yl- )-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-phenyl)-4-2-hydroxy-cyclohexyli- mino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2,3-dihydro-benzo1,4dioxin-6-ylimino-5-(2,4-d- imethyl-cyclohex-3-enyl)-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-2,3-dihydro-benzo1,4dioxin- -6-ylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-phenyl)-4-1,1,3,3-tetramethyl-b- utylimino-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-indan-1-ylimino-imidazolid- in-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-2,3-dihydro-benzo- 1,4dioxin-6-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-difluoro-phenyl)-4-3-(2-oxo-pyrrolidin-1- -yl)-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-1,2,3,4-tetrahydro-naphtha- len-1-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(2-fluoro-phen- yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-1,2-diphenyl-ethylimino-im- idazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-fluoro-phenyl)-4-methylimino-imid- azolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-phenyl)-4-2-(3-hydroxy-pyrrolidin-1- -yl)-2-oxo-ethylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-2-morpholin-4-yl-ethylimin- o-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-2-oxo-2-thiomorpholin-4-yl- -ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-2-(4-hydroxy-piperidin-1-yl)-2-oxo-ethylimino- -5-quinolin-4-yl-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-cycloheptylimino-5-(2,4-dimethyl-phenyl)-imid- azolidine-2-thione; and 1-(1H-Benzoimidazol-5-yl)-5-(6-fluoro-1H-indol-3-yl)-4-2-pyridin-2-yl-eth- ylimino-imidazolidin-2-one; or a pharmaceutically acceptable salt thereof. 19. The compound according to claim 18, wherein said compound or pharmaceutically acceptable salt is selected from the group consisting of: 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-methylimino-imidazolidi- n-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(4-pyrrolidin-1-yl- -phenyl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(4-methylsulfa- nyl-phenyl)-imidazolidine-2-thione; 1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]thiadiazol-5-yl-4-3-(2-oxo-pyr- rolidin-1-yl)-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-methylimino-5-naphthalen-2-yl-imidazolidin-2-- one; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(4-chloro-phenyl)-imidazoli- din-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-3-morpholin-4-yl-- propylimino-imidazolidin-2-one; 5-Benzo1,3dioxol-5-yl-1-(1H-benzoimidazol-5-yl)-4-3-(2-oxo-pyrrolidin-1-y- l)-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-1H-indol-5-ylmethylimino-5-p-tolyl-imidazolid- in-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-naphthalen-2-yl-i- midazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzotriazol-1-ylmethylimino-5-(1H-indol-5-yl- )-imidazolidin-2-one; 1-(1H-benzo[d]imidazol-6-yl)-4-(benzylimino)-5-(3-bromophenyl)imidazolidi- n-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(3,5-dibromo-pheny- l)-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-cyclohexylimi- no-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-cyclohexylimino-imidazolid- in-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-phenyl)-4-cyclopentylimino- -imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-indan-1-ylimino-5-(6-methyl-4-oxo-4H-chromen-- 3-yl)-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(4-bromo-phenyl)-imidazolidin-2- -one; 1-(1H-Benzoimidazol-5-yl)-4-indan-1-ylimino-5-(1H-indol-5-yl)-imidaz- olidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-phenyl)-4-2-(1H-indol-3-yl)-eth- ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-cyclohexylim- ino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-3-phenyl-propylimino-imidaz- olidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopentylimino-5-(1H-indol-5-yl)-imidazolid- in-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-1,2- ,3,4-tetrahydro-naphthalen-1-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-4-benzylimino-5-(6-methyl-1H-indol-3-yl)-imidaz- olidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,3-dihydro-benzo1,4dioxin-6-yl)-4-2,3-dihyd- ro-benzo1,4dioxin-6-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-benzo[c][1,2,5]thiadiazol-5-yl-4-2-hydroxy-cy- clohexylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-3-(2-oxo-pyrrolidin-1-yl)-- propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-dimethylamino-phenyl)-4-indan-1-ylimino-im- idazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dimethyl-cyclohex-3-enyl)-4-isopropylimi- no-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-1,2,2-trimet- hyl-propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(1H-indol-5-yl)-4-3-(2-oxo-pyrrolidin-1-yl)-p- ropylimino-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-4-cycloheptylimino-5-(3,5-dibromo-phenyl)-imida- zolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-dibromo-phenyl)-4-3-phenyl-propylimino-i- midazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(3,5-dibromo-phenyl)-4-1H-indol-5-ylmethylimi- no-imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-2-thiophen-2-- yl-ethylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-fluoro-phenyl)-4-cyclopentylimino- -imidazolidin-2-one; 1-(3H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-3-(2-oxo-pyrrolidin-1-yl)-- propylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(6-bromo-benzo1,3dioxol-5-yl)-4-1,2-diphenyl-- ethylimino-imidazolidin-2-one; 4-(2-Oxo-2-(piperidin-1-yl)ethylimino)-1-(1H-benzo[d]imidazol-5-yl)-5-(5-- bromobenzo[d][1,3]dioxol-6-yl)imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-2,3-dihydro-benzo1,4dioxin- -6-ylimino-imidazolidin-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-bromo-phenyl)-4-indan-1-ylimino-imidazolid- in-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-1,2,3,4-tetrahydr- o-naphthalen-1-ylimino-imidazolidin-2-one; and 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-phenyl)-4-1,2-diphenyl-ethylimino-im- idazolidin-2-one; or a pharmaceutically acceptable salt thereof. 20. A pharmaceutical composition comprising a compound according to claim 1 optionally in combination with one or more therapeutically acceptable diluents or carriers. 21. The pharmaceutical composition of claim 20, which comprises additionally at least one compound, selected from the group consisting of neuroprotectants, antiparkinsonian drugs, amyloid protein deposition inhibitors, beta amyloid synthesis inhibitors, antidepressants, anxiolytic drugs, antipsychotic drugs and anti-multiple sclerosis drugs. 22. The pharmaceutical composition of claim 21, which comprises additionally at least one compound, selected from the group consisting of PEP-inhibitors, LiCl, inhibitors of DP IV or DP IV-like enzymes, acetylcholinesterase (ACE) inhibitors, PIMT enhancers, inhibitors of beta secretases, inhibitors of gamma secretases, inhibitors of neutral endopeptidase, inhibitors of Phosphodiesterase-4 (PDE-4), TNFalpha inhibitors, muscarinic M1 receptor antagonists, NMDA receptor antagonists, sigma-1 receptor inhibitors, histamine H3 antagonists, beta-amyloid antibodies, cysteine protease inhibitors, MCP-1 antagonists or an agent selected from the group consisting of natalizumab, fampridine-SR, alemtuzumab, IR 208, NBI 5788/MSP 771 (tiplimotide), paclitaxel, AG 284, SH636, adapalene, an interleukin-4, a matrix-metalloproteinase-inhibitors, interferon-tau (trophoblastin) and laquinimod. 23. A process for preparation of a compound selected from the group consisting of the compounds in any one of claims 1 to 19 or a protected derivative thereof (a) wherein X represents O, which comprises reaction of a compound of formula (II) ##STR00381## or a protected derivative thereof, wherein R.sup.1, R.sup.2 and R.sup.4 are as defined in any one of claims 1 to 19, with a compound of formula (III) ##STR00382## or a protected derivative thereof wherein R.sup.3 in any one of claims 1 to 19, and a cyanate in the presence of an acid catalyst; or (b) wherein X represents sulphur, comprises reaction of a compound of formula (II) or a protected derivative thereof, wherein R.sup.1, R.sup.2 and R.sup.4 are as defined in any one of claims 1 to 19, with a compound of formula (III) or a protected derivative thereof wherein R.sup.3 is as defined in any one of claims 1 to 19, and a thiocyanate in the presence of an acid catalyst. |
Details for Patent 8,420,684
Applicant | Tradename | Biologic Ingredient | Dosage Form | BLA | Approval Date | Patent No. | Expiredate |
---|---|---|---|---|---|---|---|
Jubilant Hollisterstier Llc | N/A | positive skin test control-histamine | Injection | 103891 | 03/13/1924 | ⤷ Try a Trial | 2039-02-26 |
Genzyme Corporation | CAMPATH | alemtuzumab | Injection | 103948 | 05/07/2001 | ⤷ Try a Trial | 2039-02-26 |
Genzyme Corporation | LEMTRADA | alemtuzumab | Injection | 103948 | 11/14/2014 | ⤷ Try a Trial | 2039-02-26 |
Genzyme Corporation | CAMPATH | alemtuzumab | Injection | 103948 | 10/12/2004 | ⤷ Try a Trial | 2039-02-26 |
Biogen Inc. | TYSABRI | natalizumab | Injection | 125104 | 11/23/2004 | ⤷ Try a Trial | 2039-02-26 |
>Applicant | >Tradename | >Biologic Ingredient | >Dosage Form | >BLA | >Approval Date | >Patent No. | >Expiredate |
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