US 2009/0269301 A1 · Novel Inhibitors of Glutaminyl Cyclase

Abstract

The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 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)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 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)R5; R4 and R5 independently represent alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl and -alkylheterocyclyl, with the proviso that, when R1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R3 may not be —C(O)R5.

Claims27

Dependent claims

A compound of formula (I),

or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein
R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl;
R2 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)2, -alkylheteroaryl;
-aryl-heteroaryl;
heterocyclyl-aryl-;
-aryl-aryl;
-heteroaryl-aryl;
-heteroaryl-heteroaryl, and —C(O)R4;
R3 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)R5;
R4 and R5 independently represent alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl and -alkylheterocyclyl;
with the proviso that, when R1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R3 may not be —C(O)R5.

26 more elements

A compound selected from the group consisting of examples 1-473 below and the pharmaceutically acceptable salts, solvates and polymorphs of them:

Example 1 5-sec-Butyl-4-fluoro-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 2 4-Fluoro-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-pentyl-1,5-dihydro-pyrrol-2-one,
Example 3 4-Fluoro-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-methyl-1,5-dihydro-pyrrol-2-one,
Example 4 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,
Example 5 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-p-tolyl-1,5-dihydro-pyrrol-2-one,
Example 6 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)-1,5-dihydro-pyrrol-2-one,
Example 7 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 8 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 9 5-(1,2-Dihydroxy-ethyl)-3-hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 10 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but-1-enyl)-1,5-dihydro-pyrrol-2-one,
Example 11 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 12 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-1,5-dihydro-pyrrol-2-one,
Example 13 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 14 3-Hydroxy-5-(2-hydroxy-phenyl)-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 15 5-(3,4-Dimethyl-phenyl)-3-hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 16 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-pentyl-1,5-dihydro-pyrrol-2-one,
Example 17 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 18 3-Hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 19 5-Cyclopropyl-3-hydroxy-4-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 20 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 21 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-p-tolyl-1,5-dihydro-pyrrol-2-one,
Example 22 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 23 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 24 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(3-methyl-but-1-enyl)-1,5-dihydro-pyrrol-2-one,
Example 25 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 26 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 27 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 28 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 29 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 30 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-pentyl-1,5-dihydro-pyrrol-2-one,
Example 31 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4,5-dimethyl-1,5-dihydro-pyrrol-2-one,
Example 32 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 33 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(styryl)-1,5-dihydro-pyrrol-2-one,
Example 34 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-phenyl-1,5-dihydro-pyrrol-2-one,
Example 35 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 36 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 37 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-(6-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 38 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-trifluoromethyl-1,5-dihydro-pyrrol-2-one,
Example 39 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 40 3-Hydroxy-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 41 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 42 3-Hydroxy-5-(2-hydroxy-naphthalen-1-yl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 43 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-pyridin-2-yl-1,5-dihydro-pyrrol-2-one,
Example 44 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-pyridin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 45 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-5-thiophen-2-yl-1,5-dihydro-pyrrol-2-one,
Example 46 5-Cyclopropyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 47 5-(Furan-2-yl-)3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 48 5-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 49 5-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 50 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 51 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 52 3-Hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 53 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 54 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-p-tolyl-1,5-dihydro-pyrrol-2-one,
Example 55 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 56 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 57 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 58 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 59 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-(4-methoxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 60 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 61 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 62 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-pentyl-1,5-dihydro-pyrrol-2-one,
Example 63 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 64 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-(styryl)-1,5-dihydro-pyrrol-2-one,
Example 65 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-phenyl-1,5-dihydro-pyrrol-2-one,
Example 66 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 67 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 68 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 69 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-pyridin-2-yl-1,5-dihydro-pyrrol-2-one,
Example 70 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-pyridin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 71 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-5-thiophen-2-yl-1,5-dihydro-pyrrol-2-one,
Example 72 5-Furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 73 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 74 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 75 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 76 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 77 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-p-tolyl-1,5-dihydro-pyrrol-2-one,
Example 78 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 79 5-sec-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 80 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 81 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 82 5-(1,2-Dihydroxy-ethyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 83 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but-1-enyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 84 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-furan-2-yl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 85 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 86 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 87 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 88 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 89 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-pentyl-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 90 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-methyl-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 91 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 92 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4,5-diphenyl-1,5-dihydro-pyrrol-2-one,
Example 93 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 94 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 95 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(6-methyl-1H-indol-3-yl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 96 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-trifluoromethyl-1,5-dihydro-pyrrol-2-one,
Example 97 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 98 3-Hydroxy-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 99 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 100 3-Hydroxy-5-(2-hydroxy-naphthalen-1-yl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 101 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-pyridin-2-yl-1,5-dihydro-pyrrol-2-one,
Example 102 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-pyridin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 103 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-5-thiophen-2-yl-1,5-dihydro-pyrrol-2-one,
Example 104 3-Hydroxy-5-hydroxymethyl-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 105 5-Cyclopropyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 106 5-Furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 107 5-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 108 5-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 109 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 110 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 111 3-Hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 112 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 113 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,
Example 114 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-p-tolyl-1,5-dihydro-pyrrol-2-one,
Example 115 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 116 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 117 5-(1,2-Dihydroxy-ethyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 118 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,
Example 119 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,
Example 120 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 121 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-(4-methoxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 122 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 123 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 124 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-pentyl-1,5-dihydro-pyrrol-2-one,
Example 125 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-methyl-1,5-dihydro-pyrrol-2-one,
Example 126 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,
Example 127 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-phenyl-1,5-dihydro-pyrrol-2-one,
Example 128 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,
Example 129 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 130 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-(6-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 131 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-trifluoromethyl-1,5-dihydro-pyrrol-2-one,
Example 132 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4,5-bis-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 133 3-Hydroxy-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 134 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 135 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-pyridin-2-yl-1,5-dihydro-pyrrol-2-one,
Example 136 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-pyridin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 137 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-5-thiophen-2-yl-1,5-dihydro-pyrrol-2-one,
Example 138 3-Hydroxy-5-hydroxymethyl-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 139 5-Cyclopropyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 140 5-Furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 141 5-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 142 5-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 143 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 144 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 145 3-Hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 146 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 147 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 148 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-p-tolyl-1,5-dihydro-pyrrol-2-one,
Example 149 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)-1,5-dihydro-pyrrol-2-one,
Example 150 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 151 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 152 5-(1,2-Dihydroxy-ethyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 153 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but-1-enyl)-1,5-dihydro-pyrrol-2-one,
Example 154 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 155 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-1,5-dihydro-pyrrol-2-one,
Example 156 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 157 3-Hydroxy-5-(2-hydroxy-phenyl)-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 158 5-(3,4-Dimethyl-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 159 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-pentyl-1,5-dihydro-pyrrol-2-one,
Example 160 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-methyl-1,5-dihydro-pyrrol-2-one,
Example 161 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 162 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-phenyl-1,5-dihydro-pyrrol-2-one,
Example 163 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 164 5-Cyclohex-1-enyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 165 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,
Example 166 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-trifluoromethyl-1,5-dihydro-pyrrol-2-one,
Example 167 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 168 3-Hydroxy-4-(4-hydroxy-phenyl)-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 169 5-Benzyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 170 3-Hydroxy-5-(2-hydroxy-naphthalen-1-yl)-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 171 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-pyridin-2-yl-1,5-dihydro-pyrrol-2-one,
Example 172 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-pyridin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 173 3-Hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-5-thiophen-2-yl-1,5-dihydro-pyrrol-2-one,
Example 174 3-Hydroxy-5-hydroxymethyl-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 175 5-Cyclopropyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 176 5-Furan-2-yl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 177 5-Butyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 178 5-Ethyl-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 179 5-(3-Chloro-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 180 5-(2-Fluoro-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 181 3-Hydroxy-4,5-bis-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 182 3-Hydroxy-5-(3-hydroxy-phenyl)-4-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 183 5-(3,5-Dichloro-2-hydroxy-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 184 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-p-tolyl-1,5-dihydro-pyrrol-2-one,
Example 185 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 186 5-sec-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 187 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 188 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 189 5-(1,2-Dihydroxy-ethyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 190 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but-1-enyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 191 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-furan-2-yl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 192 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 193 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 194 3-Hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 195 5-(3,4-Dimethyl-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 196 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4,5-dipentyl-1,5-dihydro-pyrrol-2-one,
Example 197 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-methyl-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 198 3-Hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 199 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-phenyl-1,5-dihydro-pyrrol-2-one,
Example 200 5-(3,4-Dihydro-2H-pyran-2-yl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 201 5-Cyclohex-1-enyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 202 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(6-methyl-1H-indol-3-yl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 203 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-trifluoromethyl-1,5-dihydro-pyrrol-2-one,
Example 204 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 205 3-Hydroxy-5-(1H-imidazol-2-yl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 206 5-Benzyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 207 3-Hydroxy-5-(2-hydroxy-naphthalen-1-yl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 208 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-pyridin-2-yl-1,5-dihydro-pyrrol-2-one,
Example 209 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-pyridin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 210 3-Hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-5-thiophen-2-yl-1,5-dihydro-pyrrol-2-one,
Example 211 3-Hydroxy-5-hydroxymethyl-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 212 5-Cyclopropyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 213 5-Furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 214 5-Butyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 215 5-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 216 5-(3-Chloro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 217 5-(2-Fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 218 3-Hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 219 3-Hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 220 5-(3,5-Dichloro-2-hydroxy-phenyl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 221 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-p-tolyl-1,5-dihydro-pyrrol-2-one,
Example 222 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(pent-1-enyl)-1,5-dihydro-pyrrol-2-one,
Example 223 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 224 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 225 5-(1,2-Dihydroxy-ethyl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 226 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(3-methyl-but-1-enyl)-1,5-dihydro-pyrrol-2-one,
Example 227 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 228 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-5-yl)-1,5-dihydro-pyrrol-2-one,
Example 229 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(4-methoxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 230 4-Ethyl-3-hydroxy-5-(2-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 231 5-(3,4-Dimethyl-phenyl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 232 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-pentyl-1,5-dihydro-pyrrol-2-one,
Example 233 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-methyl-1,5-dihydro-pyrrol-2-one,
Example 234 4-Ethyl-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 235 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(styryl)-1,5-dihydro-pyrrol-2-one,
Example 236 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-phenyl-1,5-dihydro-pyrrol-2-one,
Example 237 5-(3,4-Dihydro-2H-pyran-2-yl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 238 5-Cyclohex-1-enyl-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 239 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(6-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 240 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-trifluoromethyl-1,5-dihydro-pyrrol-2-one,
Example 241 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 242 5-Benzyl-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 243 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-pyridin-2-yl-1,5-dihydro-pyrrol-2-one,
Example 244 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-pyridin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 245 4-Ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-5-thiophen-2-yl-1,5-dihydro-pyrrol-2-one,
Example 246 5-Cyclopropyl-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 247 4-Ethyl-5-furan-2-yl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 248 5-Butyl-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 249 5-(3-Chloro-phenyl)-4-ethyl-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 250 4-Ethyl-5-(2-fluoro-phenyl)-3-hydroxy-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 251 4-Ethyl-3-hydroxy-5-(4-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 252 4-Ethyl-3-hydroxy-5-(3-hydroxy-phenyl)-1-(3-imidazol-1-yl-propyl)-1,5-dihydro-pyrrol-2-one,
Example 253 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-5-(2,3,5-trifluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 254 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-thiazol-2-yl-1,5-dihydro-pyrrol-2-one,
Example 255 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(1H-imidazol-4-yl)-1,5-dihydro-pyrrol-2-one,
Example 256 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 257 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,
Example 258 1-(1H-Benzoimidazol-5-yl)-4-hexanoyl-3-hydroxy-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 259 1-(1H-Benzoimidazol-5-yl)-5-(2,3-difluoro-phenyl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 260 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-m-tolyl-1,5-dihydro-pyrrol-2-one,
Example 261 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(2,3,5-trifluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 262 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(6-methyl-4-oxo-4H-chromen-3-yl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 263 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(thiophene-3-carbonyl)-1,5-dihydro-pyrrol-2-one,
Example 264 1-(1H-Benzoimidazol-5-yl)-5-(3,4-dichloro-phenyl)-3-hydroxy-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 265 1-(1H-Benzoimidazol-5-yl)-5-(2,4-dihydroxy-phenyl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 266 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-cyclopropyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 267 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-quinolin-8-yl-1,5-dihydro-pyrrol-2-one,
Example 268 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 269 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,
Example 270 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-quinolin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 271 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 272 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(pyridine-4-carbonyl)-1,5-dihydro-pyrrol-2-one,
Example 273 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 274 1-(1H-Benzoimidazol-5-yl)-4-hexanoyl-3-hydroxy-5-(tetrahydro-furan-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 275 5-Benzo[b]thiophen-3-yl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 276 1-(1H-Benzoimidazol-5-yl)-5-(5-chloro-2-hydroxy-phenyl)-4-ethyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 277 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 278 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(1-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 279 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-(tetrahydro-furan-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 280 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-(6-methyl-4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 281 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-quinolin-8-yl-1,5-dihydro-pyrrol-2-one,
Example 282 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(2-hydroxy-5-methyl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 283 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-m-tolyl-1,5-dihydro-pyrrol-2-one,
Example 284 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(2-hydroxy-5-methyl-phenyl)-4-(4-hydroxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 285 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(2-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 286 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-(4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 287 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]thiadiazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 288 1-(1H-Benzoimidazol-5-yl)-5-(3,5-dibromo-4-hydroxy-phenyl)-4-ethyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 289 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 290 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-4-ethyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 291 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(tetrahydro-furan-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 292 5-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-5-oxo-3-propyl-2,5-dihydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid,
Example 293 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-quinolin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 294 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-3-hydroxy-4-(3-hydroxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 295 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(2,2-dimethyl-[1,3]dioxolan-4-yl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 296 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-quinolin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 297 [1-(1H-Benzoimidazol-5-yl)-4-hydroxy-5-oxo-2-quinolin-4-yl-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid,
Example 298 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(2-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 299 1-(1H-Benzoimidazol-5-yl)-5-(3-fluoro-phenyl)-3-hydroxy-4-methylsulfanylmethyl-1,5-dihydro-pyrrol-2-one,
Example 300 1-(1H-Benzoimidazol-5-yl)-5-(2,2-dimethyl-[1,3]dioxolan-4-yl)-3-hydroxy-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 301 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(3-chloro-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 302 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-quinolin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 303 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 304 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-hydroxy-phenyl)-5-(8-hydroxy-quinolin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 305 1-(H-Benzoimidazol-5-yl)-5-(4-chloro-3-trifluoromethyl-phenyl)-3-hydroxy-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 306 1-(H-Benzoimidazol-5-yl)-3-hydroxy-5-(6-methyl-pyridin-2-yl)-4-(thiophene-3-carbonyl)-1,5-dihydro-pyrrol-2-one,
Example 307 1-(H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-(3-hydroxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 308 5-[1-(1H-Benzoimidazol-5-yl)-3-cyclopropanecarbonyl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid,
Example 309 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-(4-pyrrolidin-1-yl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 310 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 311 [1-(H-Benzoimidazol-5-yl)-2-(3-fluoro-phenyl)-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid,
Example 312 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-cyclohex-1-enyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 313 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-propyl-1,5-dihydro-pyrrol-2-one,
Example 314 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(tetrahydro-furan-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 315 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(2,3,5-trifluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 316 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(6-methyl-pyridin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 317 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(tetrahydro-furan-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 318 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-quinolin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 319 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 320 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(6-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 321 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-methyl-furan-2-yl)-4-(thiophene-2-carbonyl)-1,5-dihydro-pyrrol-2-one,
Example 322 [1-(1H-Benzoimidazol-5-yl)-4-hydroxy-2-(1-methyl-1H-indol-3-yl)-5-oxo-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid,
Example 323 1-(1H-Benzoimidazol-5-yl)-5-(3-fluoro-phenyl)-3-hydroxy-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 324 3-[1-(1H-Benzoimidazol-5-yl)-3-butyryl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-propionic acid,
Example 325 1-(1H-Benzoimidazol-5-yl)-5-(2-fluoro-phenyl)-3-hydroxy-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 326 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-thiazol-2-yl-1,5-dihydro-pyrrol-2-one,
Example 327 1-(H-Benzoimidazol-5-yl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-4-(3-methyl-butyryl)-1,5-dihydro-pyrrol-2-one,
Example 328 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(6-methyl-4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 329 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(1-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 330 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(6-methyl-pyridin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 331 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-5-(6-methyl-4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 332 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(2-hydroxy-5-methyl-phenyl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 333 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 334 1-(H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(6-methyl-pyridin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 335 1-(1H-Benzoimidazol-5-yl)-5-(3,5-bis-trifluoromethyl-phenyl)-4-butyryl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 336 1-(1H-Benzoimidazol-5-yl)-5-(5-chloro-2-hydroxy-phenyl)-3-hydroxy-4-methylsulfanylmethyl-1,5-dihydro-pyrrol-2-one,
Example 337 1-(1H-Benzoimidazol-5-yl)-5-(5-chloro-2-hydroxy-phenyl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 338 [1-(1H-Benzoimidazol-5-yl)-2-(5-bromo-2-fluoro-phenyl)-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid,
Example 339 1-(H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-3-hydroxy-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 340 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-4-ethyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 341 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(2,3,5-trifluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 342 1-(H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(4-hydroxy-3,5-dimethyl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 343 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(2-hydroxy-5-methyl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 344 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-4-butyryl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 345 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(4-pyrrolidin-1-yl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 346 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(6-methyl-4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 347 5-Benzo[b]thiophen-3-yl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 348 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-5-thiophen-3-yl-1,5-dihydro-pyrrol-2-one,
Example 349 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-thiazol-2-yl-1,5-dihydro-pyrrol-2-one,
Example 350 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(2,3-difluoro-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 351 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]oxadiazol-5-yl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 352 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 353 1-(1H-Benzoimidazol-5-yl)-4-butyryl-5-furan-2-yl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 354 [1-(1H-Benzoimidazol-5-yl)-4-hydroxy-5-oxo-2-quinolin-8-yl-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid,
Example 355 1-(1H-Benzoimidazol-5-yl)-3-butyryl-4-hydroxy-1,2-dihydro-1′H-[2,2′]bipyrrolyl-5-one,
Example 356 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 357 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,
Example 358 [1-(1H-Benzoimidazol-5-yl)-2-(3-chloro-2,6-difluoro-phenyl)-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid,
Example 359 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(1H-imidazol-4-yl)-1,5-dihydro-pyrrol-2-one,
Example 360 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-quinolin-3-yl-1,5-dihydro-pyrrol-2-one,
Example 361 3-[1-(1H-Benzoimidazol-5-yl)-3-cyclohexanecarbonyl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-propionic acid,
Example 362 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 363 1-(H-Benzoimidazol-5-yl)-5-(3-fluoro-phenyl)-3-hydroxy-4-(4-hydroxy-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 364 1-(H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-quinolin-8-yl-1,5-dihydro-pyrrol-2-one,
Example 365 1-(1H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-3-hydroxy-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 366 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 367 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-thiophen-3-yl-1,5-dihydro-pyrrol-2-one,
Example 368 1-(H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 369 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(thiophene-2-carbonyl)-1,5-dihydro-pyrrol-2-one,
Example 370 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-5-(3-fluoro-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 371 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 372 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-5-(3,4-dichloro-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 373 1-(1H-Benzoimidazol-5-yl)-5-(2-chloro-quinolin-3-yl)-3-hydroxy-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 374 5-[1-(1H-Benzoimidazol-5-yl)-3-cyclohexanecarbonyl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid,
Example 375 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-cyclohex-3-enyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 376 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(benzo[c][1,2,5]thiadiazol-5-yl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 377 1-(H-Benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-3-hydroxy-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 378 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 379 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 380 1-(1H-Benzoimidazol-5-yl)-5- benzo[c][1,2,5]thiadiazol-5-yl-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 381 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(6-methyl-pyridin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 382 1-(H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(6-methyl-4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 383 1-(H-Benzoimidazol-5-yl)-5-(2,3-difluoro-phenyl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 384 1-(1H-Benzoimidazol-5-yl)-5-(5-bromo-2-fluoro-phenyl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 385 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-(6-methyl-pyridin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 386 1-(1H-Benzoimidazol-5-yl)-5-(2-fluoro-phenyl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 387 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(4-pyridin-2-yl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 388 1-(H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-isopropyl-1,5-dihydro-pyrrol-2-one,
Example 389 5-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-3-(4-hydroxy-phenyl)-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid,
Example 390 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,
Example 391 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-(8-hydroxy-quinolin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 392 1-(1H-Benzoimidazol-5-yl)-5-(2-chloro-quinolin-3-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 393 1-(H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(2,3,5,6-tetrafluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 394 1-(H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 395 1-(1H-Benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 396 1-(1H-Benzoimidazol-5-yl)-5-(5-bromo-2-fluoro-phenyl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 397 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(1-oxy-pyridin-4-yl)-1,5-dihydro-pyrrol-2-one,
Example 398 1-(H-Benzoimidazol-5-yl)-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-4-phenyl-1,5-dihydro-pyrrol-2-one,
Example 399 5-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-3-methyl-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid,
Example 400 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(2,3,5,6-tetrafluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 401 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(4-pyridin-2-yl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 402 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-thiazol-2-yl-1,5-dihydro-pyrrol-2-one,
Example 403 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(benzo[c][1,2,5]oxadiazol-5-yl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 404 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-quinolin-4-yl-1,5-dihydro-pyrrol-2-one,
Example 405 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 406 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(4-pyrrolidin-1-yl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 407 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(2,3,5-trifluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 408 [2-Benzo[b]thiophen-3-yl-1-(1H-benzoimidazol-5-yl)-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-3-yl]-acetic acid,
Example 409 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 410 5-[3-Acetyl-1-(1H-benzoimidazol-5-yl)-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid,
Example 411 1-(1H-Benzoimidazol-5-yl)-4-hexanoyl-3-hydroxy-5-m-tolyl-1,5-dihydro-pyrrol-2-one,
Example 412 1-(H-Benzoimidazol-5-yl)-5-(3-chloro-2,6-difluoro-phenyl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 413 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-(3-methyl-butyryl)-1,5-dihydro-pyrrol-2-one,
Example 414 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(3,5-dibromo-4-hydroxy-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 415 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 416 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-m-tolyl-1,5-dihydro-pyrrol-2-one,
Example 417 1-(1H-Benzoimidazol-5-yl)-5-(2,5-dimethyl-phenyl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 418 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 419 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-5-furan-2-yl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 420 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-quinolin-3-yl-1,5-dihydro-pyrrol-2-one,
Example 421 1-(1H-Benzoimidazol-5-yl)-benzo[c][1,2,5]oxadiazol-5-yl)4-butyryl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 422 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(1H-indol-3-yl)-5-quinolin-3-yl-1,5-dihydro-pyrrol-2-one,
Example 423 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(2,3,5,6-tetrafluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 424 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-thiophen-3-yl-1,5-dihydro-pyrrol-2-one,
Example 425 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(tetrahydro-furan-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 426 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 427 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 428 1-(1H-Benzoimidazol-5-yl)-4-ethyl-3-hydroxy-5-(6-methyl-4-oxo-4H-chromen-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 429 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(4-hydroxy-phenyl)-5-m-tolyl-1,5-dihydro-pyrrol-2-one,
Example 430 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-isopropyl-5-(6-methyl-pyridin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 431 1-(1H-Benzoimidazol-5-yl)-5-(benzo[c][1,2,5]oxadiazol-5-yl)-4-ethyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 432 1-(1H-Benzoimidazol-5-yl)-4-butyryl-3-hydroxy-5-(5-hydroxymethyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 433 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(4,5-dimethyl-furan-2-yl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 434 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-hydroxy-phenyl)-5-m-tolyl-1,5-dihydro-pyrrol-2-one,
Example 435 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-5-(1H-imidazol-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 436 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-(6-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 437 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-(5-bromo-2-fluoro-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 438 1-(1H-Benzoimidazol-5-yl)-5-(3-bromo-4-hydroxy-phenyl)-3-hydroxy-4-(1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 439 4-Acetyl-1-(1H-benzoimidazol-5-yl)-5-ethyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 440 1-(1H-Benzoimidazol-5-yl-(benzo[c][1,2,5]thiadiazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 441 1-(1H-Benzoimidazol-5-yl)-4-cyclohexanecarbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one
Example 442 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,
Example 443 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-quinolin-8-yl-1,5-dihydro-pyrrol-2-one,
Example 444 4-Acetyl-1-(1H-benzoimidazol-5-yl)-3-hydroxy-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 445 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-phenyl-5-(2,3,5-trifluoro-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 446 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(8-hydroxy-quinolin-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 447 3-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-3-(3-methyl-butyryl)-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-propionic acid,
Example 448 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-methyl-5-quinolin-3-yl-1,5-dihydro-pyrrol-2-one,
Example 449 1-(1H-Benzoimidazol-5-yl)-4-butyryl-5-cyclopropyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 450 3-[3-Acetyl-1-(1H-benzoimidazol-5-yl)-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-propionic acid,
Example 451 5-[1-(1H-Benzoimidazol-5-yl)-4-hydroxy-3-(1H-indol-3-yl)-5-oxo-2,5-dihydro-1H-pyrrol-2-yl]-furan-2-carboxylic acid,
Example 452 1-(1H-Benzoimidazol-5-yl)-3-cyclohexanecarbonyl-4-hydroxy-1,2-dihydro-1′H-[2,2′]bipyrrolyl-5-one,
Example 453 1-(1H-Benzoimidazol-5-yl)-4-cyclopropanecarbonyl-3-hydroxy-5-(6-methyl-1H-indol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 454 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-trifluoromethyl-phenyl)-4-cyclohexanecarbonyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 455 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-(4-pyridin-2-yl-phenyl)-1,5-dihydro-pyrrol-2-one,
Example 456 1-(1H-Benzoimidazol-5-yl)-5-furan-2-yl-3-hydroxy-4-pentyl-1,5-dihydro-pyrrol-2-one,
Example 457 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,
Example 458 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-methyl-butyryl)-5-m-tolyl-1,5-dihydro-pyrrol-2-one,
Example 459 1-(1H-Benzoimidazol-5-yl)-4-(4-chloro-benzoyl)-3-hydroxy-5-(5-methyl-furan-2-yl)-1,5-dihydro-pyrrol-2-one,
Example 460 1-(1H-Benzoimidazol-5-yl)-5-(4-chloro-3-trifluoromethyl-phenyl)-3-hydroxy-4-methyl-1,5-dihydro-pyrrol-2-one,
Example 461 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-5-(1H-imidazol-4-yl)-4-(3-methyl-butyryl)-1,5-dihydro-pyrrol-2-one,
Example 462 1-(1H-Benzoimidazol-5-yl)-4-fluoro-5-(2-fluoro-phenyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 463 1-(1H-Benzoimidazol-5-yl)-5-ethyl-4-hexanoyl-3-hydroxy-1,5-dihydro-pyrrol-2-one,
Example 464 1-(1H-Benzoimidazol-5-yl)-3-hydroxy-4-(3-hydroxy-phenyl)-5-(1H-pyrazol-3-yl)-1,5-dihydro-pyrrol-2-one,
Example 465 1-(1H-Benzoimidazol-5-yl)-4-(2,2-dimethyl-propionyl)-3-hydroxy-1,5-dihydro-pyrrol-2-one.
Example 466 1-(1H-benzo[d]imidazol-5-yl)-4-benzoyl-5-(2,3-difluorophenyl)-3-hydroxy-1H-pyrrol-2(5H)-one
Example 467 1-(1H-benzo[d]imidazol-6-yl)-5-(2,3-difluorophenyl)-3-hydroxy-4-methyl-1H-pyrrol-2(5H)-one
Example 468 1-(1H-benzo[d]imidazol-5-yl)-5-(2,3-dichlorophenyl)-3-hydroxy-4-methyl-1H-pyrrol-2(5H)-one
Example 469 1-(1H-benzo[d]imidazol-5-yl)-5-(2,4,5-trifluorophenyl)-3-hydroxy-4-methyl-1H-pyrrol-2(5H)-one
Example 470 1-(1H-benzo[d]imidazol-5-yl)-5-(2,4-dichlorophenyl)-3-hydroxy-4-methyl-1H-pyrrol-2(5H)-one
Example 471 1-(1H-benzo[d]imidazol-6-yl)-5-(5-bromo-2-fluorophenyl)-3-hydroxy-4-methyl-1H-pyrrol-2(5H)-one
Example 472 1-(1H-benzo[d]imidazol-6-yl)-5-(2-chloro-3,6-difluorophenyl)-3-hydroxy-4-methyl-1H-pyrrol-2(5H)-one
Example 473 1-(1H-benzo[d]imidazol-6-yl)-5-(2,6-difluorophenyl)-3-hydroxy-4-methyl-1H-pyrrol-2(5H)-one

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Novel Inhibitors of Glutaminyl Cyclase

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Novel Inhibitors of Glutaminyl Cyclase

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Abstract

Claims27