Claims for Patent: 8,278,345

Summary for Patent: 8,278,345

Title:	Inhibitors of glutaminyl cyclase
Abstract:	The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, ##STR00001## R.sup.1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R.sup.2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, --C(O)OH and --C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, --C(O)OH and --C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl).sub.2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and --C(O)R.sup.4; R.sup.3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, --C(O)OH and --C(O)O-alkyl; aryl; heteroaryl; --C(O)R.sup.5; R.sup.4 and R.sup.5 independently represent alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl and -alkylheterocyclyl, with the proviso that, when R.sup.1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R.sup.3 may not be --C(O)R.sup.5.
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 (Saale), DE)
Application Number:	11/937,149
Patent Claims:	1. A compound of formula (I) ##STR00544## or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein: R.sup.1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl, wherein the heteroaryl of the alkylheteroaryl may be optionally substituted by one or more groups selected from alkyl, alkoxy- and halogen; R.sup.2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, haloalkyl, hydroxyl, alkoxy-, -thioalkyl, --C(O)OH and --C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, --C(O)OH and --C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl optionally substituted by one or more alkyl groups; -alkylaryl; -alkyl(aryl).sub.2; -alkylheteroaryl; -aryl-heteroaryl; heterocyclyl-aryl-; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; or --C(O)R.sup.4; R.sup.3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, --C(O)OH and --C(O)O-alkyl; aryl; heteroaryl; or --C(O)R.sup.5; R.sup.4 represents alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl or -alkylheterocyclyl; and R.sup.5 represents C.sub.2-4 alkyl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl or -alkylheterocyclyl; with the proviso that, when R.sup.1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R.sup.3 is not --C(O)R.sup.5. 2. A compound according to claim 1 wherein the following compound is excluded from the scope of formula (I): ##STR00545## 3. A compound according to claim 1, wherein R.sup.1 represents -alkylheteroaryl, wherein the heteroaryl of the alkylheteroaryl may be optionally substituted by one or more groups selected from alkyl, alkoxy- and halogen. 4. A compound according to claim 3, wherein R.sup.1 represents 3-imidazol-1-yl-propyl. 5. A compound according to claim 1, wherein R.sup.1 represents -heteroaryl. 6. A compound according to claim 5, wherein R.sup.1 represents phenyl ring fused to a 5-membered heteroaryl ring wherein R.sup.1 is linked to the core of formula (I) through the phenyl ring. 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 aryl, heteroaryl, aryl-heteroaryl or heterocyclyl optionally substituted by one or more alkyl groups. 9. A compound according to claim 8, wherein R.sup.2 represents heteroaryl. 10. A compound according to claim 8, wherein R.sup.2 represents aryl. 11. A compound according to claim 10, wherein R.sup.2 represents substituted phenyl. 12. A compound according to claim 1, wherein R.sup.3 represents alkyl, aryl, heteroaryl, or --C(O)R.sup.5. 13. A compound according to claim 12, wherein R.sup.3 represents aryl. 14. A compound according to claim 12, wherein R.sup.3 represents heteroaryl. 15. A compound according to claim 12, wherein R.sup.3 represents --C(O)R.sup.5. 16. A compound according to claim 15, wherein R.sup.5 represents C.sub.2-4 alkyl. 17. A compound according to claim 15, wherein R.sup.5 represents cycloalkyl. 18. A compound selected from the group consisting of: 5-sec-Butyl-4-fluoro-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyr- rol-2-one; 4-Fluoro-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-pentyl-1,5-dihy- dro-pyrrol-2-one; 4-Fluoro-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-methyl-1,5-dihydro-pyrrol- -2-one; 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-4-(3-hydroxy-phenyl)-1- -(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-p-tolyl-1,5-d- ihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)- -1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-propyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-pyrazol-3- -yl)-1,5-dihydro-pyrrol-2-one; 5-(1,2-Dihydroxy-ethyl)-3-hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl- -propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but- -1-enyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-fur- an-2-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-y- l)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-ph- enyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-5-(2-hydroxy-phenyl)-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-pr- opyl)-1,5-dihydro-pyrrol-2-one; 5-(3,4-Dimethyl-phenyl)-3-hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl- -propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-pentyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(3-hydroxy-phenyl)-1-(3-imidaz- ol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-y- l)-1,5-dihydro-pyrrol-2-one; 5-Cyclopropyl-3-hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1- ,5-dihydro-pyrrol-2-one; 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-- methyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-p-tolyl-1,5-dihydro-pyrro- l-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-propyl-1,5-dihydr- o-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(1H-pyrazol-3-yl)-1,5-dih- ydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(3-methyl-but-1-enyl)-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(5-methyl-furan-2-yl)-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-methyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-4-methyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-di- hydro-pyrrol-2-one; 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-pentyl-1,5-dihydro-pyrrol- -2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4,5-dimethyl-1,5-dihydro-pyrr- ol-2-one; 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-prop- yl)-4-methyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(styryl)-1,5-dihydro-pyrr- ol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-phenyl-1,5-dihyd- ro-pyrrol-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-meth- yl-1,5-dihydro-pyrrol-2-one; 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(6-methyl-1H-indol-3-yl)-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-trifluoromethyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-4-methyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-di- hydro-pyrrol-2-one; 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol- -2-one; 3-Hydroxy-5-(2-hydroxy-naphthalen-1-yl)-1-(3-imidazol-1-yl-propyl)- -4-methyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-pyridin-2-yl-1,5-dihydro-- pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-pyridin-4-yl-1,5-dihydro-- pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-thiophen-2-yl-1,5-dihydro- -pyrrol-2-one; 5-Cyclopropyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-p- yrrol-2-one; 5-(Furan-2-yl-)3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-- pyrrol-2-one; 5-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-- 2-one; 5-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-p- yrrol-2-one; 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dih- ydro-pyrrol-2-one; 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dih- ydro-pyrrol-2-one; 3-Hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-p-tolyl-1,5-dihydro-py- rrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-propyl-1,5-dihydro-pyr- rol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-(1 H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-(5-methyl-furan-2-yl)-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-isopropyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-(4-methoxy-phenyl)-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5- -dihydro-pyrrol-2-one; 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-pentyl-1,5-dihydro-pyr- rol-2-one; 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-pro- pyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-(styryl)-1,5-dihydro-p- yrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-phenyl-1,5-dihydro-pyr- rol-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-prop- yl)-4-isopropyl-1,5-dihydro-pyrrol-2-one; 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-di- hydro-pyrrol-2-one; 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4isopropyl-1,5-dihydro-pyrr- ol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-pyridin-2-yl-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-pyridin-4-yl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-thiophen-2-yl-1,5-dihy- dro-pyrrol-2-one; 5-Furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro- -pyrrol-2-one; 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-- dihydro-pyrrol-2-one; 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-- dihydro-pyrrol-2-one; 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5- -dihydro-pyrrol-2-one; 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-- phenyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-p-tolyl-1,5-dihydro-pyrro- l-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)-4-phenyl-1,5- -dihydro-pyrrol-2-one; 5-sec-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyr- rol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-propyl-1,5-dihy- dro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-(1H-pyrazol-3-yl)-1,5-dih- ydro-pyrrol-2-one; 5-(1,2-Dihydroxy-ethyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but-1-enyl)-4-phenyl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-furan-2-yl)-4-phenyl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-phenyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-4-phenyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-di- hydro-pyrrol-2-one; 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-pentyl-4-phenyl-1,5-dihydro-pyrrol- -2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-methyl-4-phenyl-1,5-dihydro- -pyrrol-2-one; 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-propyl)-4-phe- nyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4,5-diphenyl-1,5-dihydro-pyrrol-2-on- e; 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-ph- enyl-1,5-dihydro-pyrrol-2-one; 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(6-methyl-1H-indol-3-yl)-4-phenyl-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-trifluoromethyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-4-phenyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-di- hydro-pyrrol-2-one; 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol- -2-one; 3-Hydroxy-5-(2-hydroxy-naphthalen-1-yl)-1-(3-imidazol-1-yl-propyl)- -4-phenyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-pyridin-2-yl-1,5-dihydro-- pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-pyridin-4-yl-1,5-dihydro-- pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-thiophen-2-yl-1,5-dihydro- -pyrrol-2-one; 3-Hydroxy-5-hydroxymethyl-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro- -pyrrol-2-one; 5-Cyclopropyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-p- yrrol-2-one; 5-Furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-py- rrol-2-one; 5-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-- 2-one; 5-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-p- yrrol-2-one; 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dih- ydro-pyrrol-2-one; 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dih- ydro-pyrrol-2-one; 3-Hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-di- hydro-pyrrol-2-one; 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-- (1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-p-tolyl-1,5-dihy- dro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-propyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-(1H-pyrazol-3-yl- )-1,5-dihydro-pyrrol-2-one; 5(1,2-Dihydroxy-ethyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3- -yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-(3-methyl-but-1-- enyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-(5-methyl-furan-- 2-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-(1H-indol-3-yl)-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-(4-methoxy-pheny- l)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-y- l)-1,5-dihydro-pyrrol-2-one; 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-- 3-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-pentyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-methyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-propyl)-4-(1H- -indol-3-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-phenyl-1,5-dihyd- ro-pyrrol-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-- indol-3-yl)-1,5-dihydro-pyrrol-2-one; 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-(6-methyl-1H-ind- ol-3-yl) -1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-trifluoromethyl-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4,5-bis-(1H-indol- 3-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-y- l)-1,5-dihydro-pyrrol-2-one; 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-pyridin-2-yl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-pyridin-4-yl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-thiophen-2-yl-1,- 5-dihydro-pyrrol-2-one; 3-Hydroxy-5-hydroxymethyl-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,- 5-dihydro-pyrrol-2-one; 5-Cyclopropyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-- dihydro-pyrrol-2-one; 5-Furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-d- ihydro-pyrrol-2-one; 5-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydr- o-pyrrol-2-one; 5-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydr- o-pyrrol-2-one; 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl- )-1,5-dihydro-pyrrol-2-one; 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl- )-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-y- l)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-y- l)-1,5-dihydro-pyrrol-2-one; 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imi- dazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-p-tolyl-1,5-d- ihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)- -1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-propyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-pyrazol-3- -yl)-1,5-dihydro-pyrrol-2-one; 5(1,2-Dihydroxy-ethyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-- propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but- -1-enyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-fur- an-2-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-y- l)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-ph- enyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-5-(2-hydroxy-phenyl)-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-pr- opyl)-1,5-dihydro-pyrrol-2-one; 5-(3,4-Dimethyl-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl- -propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-pentyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-methyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(4-hydroxy-phenyl)-1-(3-imidaz- ol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-phenyl-1,5-di- hydro-pyrrol-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazo- l-1-yl-propyl)-1,5-dihydro-pyrrol-2-one; 5-Cyclohex-1-enyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propy- l)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(6-methyl-1H-- indol-3-yl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-trifluorometh- yl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-y- l)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-pr- opyl)-1,5-dihydro-pyrrol-2-one; 5-Benzyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(2-hydroxy-naphthalen-1-yl)-4-(4-hydroxy-phenyl)-1-(3-imidazo- l-1-yl-propyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-pyridin-2-yl-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-pyridin-4-yl-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-thiophen-2-yl- -1,5-dihydro-pyrrol-2-one; 3-Hydroxy-5-hydroxymethyl-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)- -1,5-dihydro-pyrrol-2-one; 5-Cyclopropyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1- ,5-dihydro-pyrrol-2-one; 5-Furan-2-yl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,- 5-dihydro-pyrrol-2-one; 5-Butyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dih- ydro-pyrrol-2-one; 5-Ethyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dih- ydro-pyrrol-2-one; 5-(3-Chloro-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-pro- pyl)-1,5-dihydro-pyrrol-2-one; 5-(2-Fluoro-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-pro- pyl)-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-4,5-bis-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-5-(3-hydroxy-phenyl)-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-pr- opyl)-1,5-dihydro-pyrrol-2-one; 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-- pentyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-p-tolyl-1,5-dihydro-pyrro- l-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)-4-pentyl-1,5- -dihydro-pyrrol-2-one; 5-sec-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyr- rol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-propyl-1,5-dihy- dro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-(1H-pyrazol-3-yl)-1,5-dih- ydro-pyrrol-2-one; 5(1,2-Dihydroxy-ethyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-- dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but-1-enyl)-4-pentyl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-furan-2-yl)-4-pentyl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-pentyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-4-pentyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-di- hydro-pyrrol-2-one; 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5- -dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4,5-dipentyl-1,5-dihydro-pyrrol-2-on- e; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-methyl-4-pentyl-1,5-dihydro-pyrr- ol-2-one; 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-prop- yl)-4-pentyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-phenyl-1,5-dihydro-pyrrol- -2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)- -4-pentyl-1,5-dihydro-pyrrol-2-one; 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(6-methyl-1H-indol-3-yl)-4-pentyl-- 1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-trifluoromethyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-4-pentyl-1,5-dihyd- ro-pyrrol-2-one; 3-Hydroxy-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-di- hydro-pyrrol-2-one; 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol- -2-one; 3-Hydroxy-5-(2-hydroxy-naphthalen-1-yl)-1-(3-imidazol-1-yl-propyl)- -4-pentyl-1,5-dihydro-pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-pyridin-2-yl-1,5-dihydro-- pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-pyridin-4-yl-1,5-dihydro-- pyrrol-2-one; 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-thiophen-2-yl-1,5-dihydro- -pyrrol-2-one; 3-Hydroxy-5-hydroxymethyl-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro- -pyrrol-2-one; 5-Cyclopropyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-p- yrrol-2-one; 5-Furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-py- rrol-2-one; 5-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-- 2-one; 5-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-p- yrrol-2-one; 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dih- ydro-pyrrol-2-one; 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dih- ydro-pyrrol-2-one; 3-Hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-di- hydro-pyrrol-2-one; 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-di- hydro-pyrrol-2-one; 5-(3,5-Dichloro-2-hydroxy-phenyl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-pr- opyl)-1,5-dihydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-p-tolyl-1,5-dihydro-pyrrol- -2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)-1,5-d- ihydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-propyl-1,5-dihydro-pyrrol-- 2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-pyrazol-3-yl)-1,- 5-dihydro-pyrrol-2-one; 5(1,2-Dihydroxy-ethyl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-d- ihydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but-1-enyl)-1,5-- dihydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-furan-2-yl)-1,5-- dihydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-1,5-dihydr- o-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-1,5-dih- ydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dih- ydro-pyrrol-2-one; 5-(3,4-Dimethyl-phenyl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-- dihydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-pentyl-1,5-dihydro-pyrrol-- 2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-methyl-1,5-dihydro-p- yrrol-2-one; 4-Ethyl-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-propy- l)-1,5-dihydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(styryl)-1,5-dihydro-pyrro- l-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-phenyl-1,5-dihydro- -pyrrol-2-one; 5-(3,4-Dihydro-2H-pyran-2-yl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl- )-1,5-dihydro-pyrrol-2-one; 5-Cyclohex-1-enyl-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydr- o-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(6-methyl-1H-indol-3-yl)-1- ,5-dihydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-trifluoromethyl-1,5-dihydr- o-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-1,5-dihydr- o-pyrrol-2-one; 5-Benzyl-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-- 2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-pyridin-2-yl-1,5-dih- ydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-pyridin-4-yl-1,5-dihydro-p- yrrol-2-one; 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-thiophen-2-yl-1,5-dihydro-- pyrrol-2-one; 5-Cyclopropyl-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-py- rrol-2-one; 4-Ethyl-5-furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyr- rol-2-one; 5-Butyl-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1 ,5-dihydro-pyrrol-2-one; 5-(3-Chloro-phenyl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihy- dro-pyrrol-2-one; 4-Ethyl-5-(2-fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihy- dro-pyrrol-2-one; 4-Ethyl-3-hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dih- ydro-pyrrol-2-one; 4-Ethyl-3-hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dih- ydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-5-(2,3,5-trifluoro-phenyl- )-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-thiazol-2-yl-1,5-dihydro-- pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(1H-imidazol-- 4-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(5-methyl-furan-2-yl)-1,5- -dihydro-pyrrol-2-one; 4-(Benzo[b]thiophene-2-carbonyl)-1-(1H-benzoimidazol-5-yl)-5-(4-chloro-3-- trifluoromethyl-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-hexanoyl-3-hydroxy-5-(5-methyl-furan-2-yl)-1,- 5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,3-difluoro-phenyl)-3-hydroxy-4-methyl-1,5-- dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-m-tolyl-1,5-- dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(6-methyl-4-oxo-4H-chromen-3-yl)-4-- phenyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(thi- ophene-3-carbonyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,4-dichloro-phenyl)-3-hydroxy-4-phenyl-1,5-- dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dihydroxy-phenyl)-3-hydroxy-4-methyl-1,5- -dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-quinolin-8-yl-1,5-dihydro-- pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(1H-indol-3-yl)-1,5-dihyd- ro-pyrrol-2-one; 5-(Benzo[c][1,2,5]thiadiazol-5-yl)-1-(1H-benzo[d]imidazol-5-yl)-3-hydroxy- -4-(3-hydroxyphenyl)-1H-pyrrol-2(5H)-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-quinolin-4-yl-1,5-dihydro-- pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-(4-hydr- oxy-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(pyr- idine-4-carbonyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(5-methyl-fur- an-2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-hexanoyl-3-hydroxy-5-(tetrahydro-furan-3-yl)-- 1,5-dihydro-pyrrol-2-one; 5-Benzo[b]thiophen-3-yl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(5-chloro-2-hydroxy-phenyl)-4-ethyl-3-hydroxy- -1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(1-methyl-1H-i- ndol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-(tetrahydro-fu- ran-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-(6-methyl-4-ox- o-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-quinolin-8-yl-1,5- -dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(2-hydroxy-5-methyl-phenyl)- -1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(2-hydroxy-5-methyl-phenyl)-4-(4-hy- droxy-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(2-methyl-1H-indo- l-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-(4-oxo-4H-chro- men-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]thiadiazol-5-yl)-4-cyclopropa- necarbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-dibromo-4-hydroxy-phenyl)-4-ethyl-3-hydr- oxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(5-methyl-fura- n-2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-ethyl-3-hydr- oxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(tetrahydro-fu- ran-3-yl)-1,5-dihydro-pyrrol-2-one; 5-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-5-oxo-3-propyl-2,5-dihydro-1H-pyrr- ol-2-yl]-furan-2-carboxylic acid; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-quinolin-4-yl- -1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-3-hydroxy-4-(3-hyd- roxy-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-quinolin-4-y- l-1,5-dihydro-pyrrol-2-one; [1-(1H-Benzoimidazol-5-yl)-4-hydroxy-5-oxo-2-quinolin-4-yl-2,5-dihydro-1H- -pyrrol-3-yl]-acetic acid; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(2-methyl-1H- -indol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-fluoro-phenyl)-3-hydroxy-4-methylsulfanylm- ethyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,2-dimethyl-[1,3]dioxolan-4-yl)-3-hydroxy-4- -isopropyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-quinolin-4-yl-1,5-dihydro-p- yrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(5-hydroxymet- hyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-hydroxy-phenyl)-5-(8-hydroxy-qui- nolin-2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-trifluoromethyl-phenyl)-3-hydroxy- -4-phenyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(6-methyl-pyridin-2-yl)-4-(thiophen- e-3-carbonyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-(3-hydr- oxy-phenyl)-1,5-dihydro-pyrrol-2-one; 5-[1-(1H-Benzoimidazol-5-yl)-3-cyclopropanecarbonyl-4-hydroxy-5-oxo-2,5-d- ihydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-(4-pyrrolidin-1-yl-phenyl)- -1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(8-hydro- xy-quinolin-2-yl)-1,5-dihydro-pyrrol-2-one; [1-(1H-Benzoimidazol-5-yl)-2-(3-fluoro-phenyl)-4-hydroxy-5-oxo-2,5-dihydr- o-1H-pyrrol-3-yl]-acetic acid; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-propyl-1,5-dihydro-pyrrol- -2-one; 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(2,3,5-trifluoro-phe- nyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(6-methyl-py- ridin-2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(tetrahydro-- furan-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-4-methyl-- 1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(6-methyl-1H-indo- l-3-yl) -1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-methyl-furan-2-yl)-4-(thiophene-- 2-carbonyl)-1,5-dihydro-pyrrol-2-one; [1-(1H-Benzoimidazol-5-yl)-4-hydroxy-2-(1-methyl-1 H-indol-3-yl)-5-oxo-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid; 1-(1H-Benzoimidazol-5-yl)-5-(3-fluoro-phenyl)-3-hydroxy-4-pentyl-1,5-dihy- dro-pyrrol-2-one; 3-[1-(1H-Benzoimidazol-5-yl)-3-butyryl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyr- rol-2-yl]-propionic acid; 1-(1H-Benzoimidazol-5-yl)-5-(2-fluoro-phenyl)-3-hydroxy-4-pentyl-1,5-dihy- dro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-thiazol-2-yl-1,5-dihydro-p- yrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-4-(3-meth- yl-butyryl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(6-methyl-4-oxo-4H-chromen- -3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(1-methyl-1H-indo- l-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-5-(6-methyl-4-oxo-4H-chro- men-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(2-hydroxy-5-methyl-phenyl)-4-(1H-i- ndol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(6-methyl-pyridin-2-yl)-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3,5-bis-trifluoromethyl-phenyl)-4-butyryl-3-- hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(5-chloro-2-hydroxy-phenyl)-3-hydroxy-4-methy- lsulfanylmethyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(5-chloro-2-hydroxy-phenyl)-3-hydroxy-4-methy- l-1,5-dihydro-pyrrol-2-one; [1-(1H-Benzoimidazol-5-yl)-2-(5-bromo-2-fluoro-phenyl)-4-hydroxy-5-oxo-2,- 5-dihydro-1H-pyrrol-3-yl]-acetic acid; 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-3-hydroxy-4-ph- enyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-4-ethyl-3-hydroxy-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(2,3,5-t- rifluoro-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(4-hydroxy-3- ,5-dimethyl-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(2-hydroxy-5- -methyl-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-4-butyryl-3-hydrox- y-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(6-methyl-4-oxo-4- H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one; 5-Benzo[b]thiophen-3-yl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-4-methyl-1,5-- dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-5-thiophen-3-yl-1,5-dihyd- ro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]oxadiazol-5-yl)-3-hydroxy-4-m- ethyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-5-furan-2-yl-3-hydroxy-1,5-dihydro-py- rrol-2-one; [1-(1H-Benzoimidazol-5-yl)-4-hydroxy-5-oxo-2-quinolin-8-yl-2,5-dihydro-1H- -pyrrol-3-yl]-acetic acid; 1-(1H-Benzoimidazol-5-yl)-3-butyryl-4-hydroxy-1,2-dihydro-1'H-[2,2']bipyr- rolyl-5-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(4-oxo-4H-chromen-3-yl)-1,- 5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(4-oxo-4H-chromen- -3-yl)-1,5-dihydro-pyrrol-2-one; [1-(1H-Benzoimidazol-5-yl)-2-(3-chloro-2,6-difluoro-phenyl)-4-hydroxy-5-o- xo-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(1H-imidazol-4-yl)-1,5-di- hydro-pyrrol-2-one; 3-[1-(1H-Benzoimidazol-5-yl)-3-cyclohexanecarbonyl-4-hydroxy-5-oxo-2,5-di- hydro-1H-pyrrol-2-yl]-propionic acid; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-fluoro-phenyl)-3-hydroxy-4-(4-hydroxy-phen- yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-quinolin-8-yl-- 1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-3-hydroxy-4-is- opropyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)- -1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(thi- ophene-2-carbonyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-5-(3-fluoro-phenyl)-3-hy- droxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-isopropyl-1,5-dihydro-- pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-5-(3,4-dichloro-phenyl)-3- -hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2-chloro-quinolin-3-yl)-3-hydroxy-4-phenyl-1- ,5-dihydro-pyrrol-2-one; 5-[1-(1H-Benzoimidazol-5-yl)-3-cyclohexanecarbonyl-4-hydroxy-5-oxo-2,5-di- hydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid; 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(benzo[c][1,2,5]thiadiazol-5-yl)-3-h- ydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-3-hydroxy-4-isopro- pyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(1H-pyrazol-3-yl)-1,5-dih- ydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(1H-pyrazol-3- -yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5- benzo[c][1,2,5]thiadiazol-5-yl-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-on- e; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(6-methyl-p- yridin-2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(6-methy- l-4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,3-difluoro-phenyl)-4-(2,2-dimethyl-propion- yl)-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(5-bromo-2-fluoro-phenyl)-3-hydroxy-4-methyl-- 1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(6-methyl-pyridin- -2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2-fluoro-phenyl)-3-hydroxy-4-methyl-1,5-dihy- dro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(4-pyridin-2-yl-phenyl)-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-isoprop- yl-1,5-dihydro-pyrrol-2-one; 5-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-3-(4-hydroxy-phenyl)-5-oxo-2,5-dih- ydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid; 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]oxadiazol-5-yl)-3-hydroxy-4-(- 1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-(8-hydroxy-qui- nolin-2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2-chloro-quinolin-3-yl)-4-(2,2-dimethyl-prop- ionyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(2,3,5,6-tetrafluoro-pheny- l)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-methyl-- 1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-phenyl-- 1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(5-bromo-2-fluoro-phenyl)-4-(2,2-dimethyl-pro- pionyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-4-phenyl-- 1,5-dihydro-pyrrol-2-one; 5-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-3-methyl-5-oxo-2,5-dihydro-1H-pyrr- ol-2-yl]-furan-2-carboxylic acid; 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(2,3,5,6-tetrafluoro-phenyl- )-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(4-pyrid- in-2-yl-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-thiazol-- 2-yl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-quinolin-4-yl-1,5-dihydro- -pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(1H-pyra- zol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(4-pyrrolidin-1-yl-phenyl)-- 1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(2,3,5-trifluoro-phenyl)-1- ,5-dihydro-pyrrol-2-one; [2-Benzo[b]thiophen-3-yl-1-(1H-benzoimidazol-5-yl)-4-hydroxy-5-oxo-2,5-di- hydro-1H-pyrrol-3-yl]-acetic acid; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(1H-- indol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-hexanoyl-3-hydroxy-5-m-tolyl-1,5-dihydro-pyrr- ol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-3-hyd- roxy-4-methyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-(3-methyl-butyryl)-1,5- -dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-m-tolyl-1,5-dihydro-pyrrol- -2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,5-dimethyl-phenyl)-3-hydroxy-4-meth- yl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(5-hydroxyme- thyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-5-furan-2-yl-3-hydro- xy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-quinolin-3-yl-1,5-dihydro-- pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-benzo[c][1,2,5]oxadiazol-5-yl)4-butyryl-3-hydro- xy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-quinolin-3-yl-1,5- -dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(2,3,5,6-tetra- fluoro-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-thiophen-3-yl-1,5-dihydro- -pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(tetrahydro-furan-3-yl)-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-methyl-1,5-dihydro-pyr- rol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(1H-- pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(6-methyl-4-oxo-4H-chromen-- 3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-m-tolyl-1,5-di- hydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-5-(6-methyl-pyridin-2-yl)- -1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]oxadiazol-5-yl)-4-ethyl-3-hyd- roxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(5-hydroxymethyl-furan-2-- yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-hydroxy-phenyl)-5-m-tolyl-1,5-di- hydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(1H-imidazol-- 2-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(6-methyl-1H-indol-3-yl)-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-3-hydroxy-4-(1H-in- dol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl-(benzo[c][1,2,5]thiadiazol-5-yl)-4-cyclopropanec- arbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-1 ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(2,3,5,6- -tetrafluoro-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-quinolin-8-y- l-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-(2,3,5-trifluoro-phenyl)-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(8-hydroxy-q- uinolin-2-yl)-1,5-dihydro-pyrrol-2-one; 3-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-3-(3-methyl-butyryl)-5-oxo-2,5-dih- ydro-1H-pyrrol-2-yl]-propionic acid; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-quinolin-3-yl-1,5-dihydro-- pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-5-cyclopropyl-3-hydroxy-1,5-dihydro-p- yrrol-2-one; 5-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-3-(1H-indol-3-yl)-5-oxo-2,5-dihydr- o-1H-pyrrol-2-yl]-furan-2-carboxylic acid; 1-(1H-Benzoimidazol-5-yl)-3-cyclohexanecarbonyl-4-hydroxy-1 ,2-dihydro-1'H-[2,2']bipyrrolyl-5-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(6-methyl-1H- -indol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-trifluoromethyl-phenyl)-4-cyclohe- xanecarbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(4-pyridin-2-y- l-phenyl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-pentyl-1,5-dihydro-pyr- rol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]thiadiazol-5-yl-3-h- ydroxy-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-m-tolyl-1,5-di- hydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-trifluoromethyl-phenyl)-3-hydroxy- -4-methyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(1H-imidazol-4-yl)-4-(3-methyl-buty- ryl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-fluoro-5-(2-fluoro-phenyl)-3-hydroxy-1,5-dihy- dro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-ethyl-4-hexanoyl-3-hydroxy-1,5-dihydro-pyrrol- -2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-hydroxy-phenyl)-5-(1H-pyr- azol-3-yl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-1,5-dihydr- o-pyrrol-2-one; 1-(1H-benzo[d]imidazol-6-yl)-5-(2,3-difluorophenyl)-3-hydroxy-4-methyl-1H- -pyrrol-2(5H)-one; 1-(1H-benzo[d]imidazol-5-yl)-5-(2,3-dichlorophenyl)-3-hydroxy-4-methyl-1H- -pyrrol-2(5H)-one; 1-(1H-benzo[d]imidazol-5-yl)-5-(2,4,5-trifluorophenyl)-3-hydroxy-4-methyl- -1H-pyrrol-2(5H)-one; 1-(1H-benzo[d]imidazol-5-yl)-5-(2,4-dichlorophenyl)-3-hydroxy-4-methyl-1H- -pyrrol-2(5H)-one; 1-(1H-benzo[d]imidazol-6-yl)-5-(5-bromo-2-fluorophenyl)-3-hydroxy-4-methy- l-1H-pyrrol-2(5H)-one; 1-(1H-benzo[d]imidazol-6-yl)-5-(2-chloro-3,6-difluorophenyl)-3-hydroxy-4-- methyl-1H-pyrrol-2(5H)-one; and 1-(1H-benzo[d]imidazol-6-yl)-5-(2,6-difluorophenyl)-3-hydroxy-4-methyl-1H- -pyrrol-2(5H)-one; or a pharmaceutically acceptable salt thereof. 19. The compound according to claim 18, wherein said compound or a pharmaceutically acceptable salt thereof is selected from the group consisting of: 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(5-methyl-furan-2-yl)-1,5- -dihydro-pyrrol-2-one; 5-(Benzo[c][1,2,5]thiadiazol-5-yl)-1-(1H-benzo[d]imidazol-5-yl)-3-hydroxy- -4-(3-hydroxyphenyl)-1H-pyrrol-2(5H)-one; 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]thiadiazol-5-yl)-4-cyclopropa- necarbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-(2,2-dimethyl-[1,3]dioxolan-4-yl)-3-hydroxy-4- -isopropyl-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-4-(3-meth- yl-butyryl)-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)- -1,5-dihydro-pyrrol-2-one; 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(benzo[c][1,2,5]thiadiazol-5-yl)-3-h- ydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(4-pyridin-2-yl-phenyl)-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-quinolin-3-yl-1,5-dihydro-- pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-benzo[c][1,2,5]oxadiazol-5-yl)4-butyryl-3-hydro- xy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-quinolin-3-yl-1,5- -dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-methyl-1,5-dihydro-pyr- rol-2-one; 1-(1H-Benzoimidazol-5-yl-(benzo[c][1,2,5]thiadiazol-5-yl)-4-cyc- lopropanecarbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-(2,3,5-trifluoro-phenyl)-1- ,5-dihydro-pyrrol-2-one; 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(8-hydroxy-q- uinolin-2-yl)-1,5-dihydro-pyrrol-2-one; and 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]thiadiazol-5-yl-3-hydroxy-4-(- 1H-indol-3-yl)-1,5-dihydro-pyrrol-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, LiCI, inhibitors of dipeptidyl aminopeptidases, preferably 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), TNF alpha inhibitors, muscarinic M1 receptor antagonists, NMDA receptor antagonists, sigma-1 receptor inhibitors, histamine H3 antagonists, immunomodulatory agents, immunosuppressive agents, beta-amyloid antibodies, cysteine protease inhibitors, MCP-1 antagonists or an agent selected from the group consisting of antegren (natalizumab), Neurelan (fampridine-SR), campath (alemtuzumab), IR 208, NBI 5788/MSP 771 (tiplimotide), paclitaxel, Anergix.MS (AG 284), SH636, Differin (CD 271, adapalene), BAY 361677 (interleukin-4), matrix-metalloproteinase-inhibitors (e.g. BB 76163), interferon-tau (trophoblastin) and SAIK-MS. 23. A process for preparation of a compound selected from the group consisting of the compounds in claims 1 to 19, which comprises: reaction of a compound of formula (II) ##STR00546## or a protected derivative thereof, wherein R.sup.1 and R.sup.2 is as defined in any one of claims 1 to 11, 18 and 19, with a compound of formula (III) ##STR00547## or a protected derivative thereof wherein R.sup.3 is as defined in any one of claims 1 and 12 to 19 and L is a leaving group.

Details for Patent 8,278,345

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		2026-11-09
Genzyme Corporation	CAMPATH	alemtuzumab	Injection	103948	05/07/2001		2026-11-09
Genzyme Corporation	LEMTRADA	alemtuzumab	Injection	103948	11/14/2014		2026-11-09
Genzyme Corporation	CAMPATH	alemtuzumab	Injection	103948	10/12/2004		2026-11-09