| 主权项 |
1. A compound having the structure of Formula I: or a pharmaceutically acceptable salt thereof or tautomer thereof, wherein: R1 is aryl, heteroaryl, or heterocyclyl, each optionally substituted with one or more R1A with the proviso that R1 is not furanyl or furanyl substituted with optionally substituted aryl;
each R1A is independently selected from the group consisting of hydroxy, halo, cyano, nitro, —SO2OH, O-carbamyl, N-carbamyl, O-thiocarbamyl, N-thiocarbamyl, C-amido, N-amido, S-sulfonamido, N-sulfonamido, C-carboxy, O-carboxy, isocyanato, thiocyanato, isothiocyanato, amino, optionally substituted C3-7 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, C1-6 alkyl optionally substituted with up to 5 R1B, and C1-6 alkoxy optionally substituted with up to 5 R1B;
each R1B is independently selected from the group consisting of OR1C, C-carboxy, O-carboxy, aryl, and heteroaryl, said aryl or heteroaryl each optionally substituted with one or more R1D;each R1C is independently selected from the group consisting of aryl, and heteroaryl, said aryl or heteroaryl each optionally substituted with one or more R1E;each R1D is independently selected from the group consisting of hydroxy, halo, cyano, nitro, O-carbamyl, N-carbamyl, O-thiocarbamyl, N-thiocarbamyl, C-amido, N-amido, S-sulfonamido, N-sulfonamido, C-carboxy, O-carboxy, isocyanato, thiocyanato, isothiocyanato, amino, optionally substituted C3-7 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, C1-6 alkyl optionally substituted with up to 5 fluoro, and C1-6 alkoxy optionally substituted with up to 5 fluoro;
each R1E is independently selected from the group consisting of hydroxy, halo, cyano, nitro, O-carbamyl, N-carbamyl, O-thiocarbamyl, N-thiocarbamyl, C-amido, N-amido, S-sulfonamido, N-sulfonamido, C-carboxy, O-carboxy, isocyanato, thiocyanato, isothiocyanato, amino, optionally substituted C3-7 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, C1-6 alkyl optionally substituted with up to 5 fluoro, and C1-6 alkoxy optionally substituted with up to 5 fluoro; R2 is H (hydrogen), aryl, or heteroaryl, said aryl or heteroaryl each optionally substituted with one or more R2A;
each R2A is independently selected from the group consisting of hydroxy, halo, cyano, nitro, O-carbamyl, N-carbamyl, C-amido, N-amido, C-carboxy, O-carboxy, amino, optionally substituted C3-7 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, C1-6 alkyl optionally substituted with up to 5 fluoro, and C1-6 alkoxy optionally substituted with up to 5 fluoro; R3 is H (hydrogen), aryl, or heteroaryl, said aryl or heteroaryl each optionally substituted with one or more R3A, provided that one of R2 and R3 is H (hydrogen) and one of R2 and R3 is not H (hydrogen);
each R3A is independently selected from the group consisting of hydroxy, halo, cyano, nitro, O-carbamyl, N-carbamyl, C-amido, N-amido, C-carboxy, O-carboxy, amino, optionally substituted C3-7 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, C1-6 alkyl optionally substituted with up to 5 fluoro, and C1-6 alkoxy optionally substituted with up to 5 fluoro;R4 is H (hydrogen), or C1-6 alkyl; andR5 is H (hydrogen), or C1-6 alkyl, or optionally R4 and R5 together are oxo, with the proviso that the compound is not: 4-(4-Iodo-benzylidene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,
4-(Dimethyl-furan-2-ylmethylene)-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,Acetic acid 5-[1-(4-iodo-phenyl)-3,5-dioxo-pyrazolidin-4-ylidenemethyl]-furan-2-ylmethyl ester,4-(4-Bromo-furan-2-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(5-methyl-furan-2-ylmethylene)-pyrazolidine-3,5-dione,4-(5-Bromo-furan-2-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-[5-(2-methoxy-phenyl)-thiophen-2-ylmethylene]-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-thiophen-3-ylmethylene-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(5-phenyl-thiophen-2-ylmethylene)-pyrazolidine-3,5-dione,4-(5-Methyl-furan-2-ylmethylene)-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,4-Thiophen-2-ylmethylene-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,4-(4-Bromo-furan-2-ylmethylene)-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,Acetic acid 5-[3,5-dioxo-1-(3-trifluoromethyl-phenyl)-pyrazolidin-4-ylidenemethyl]-furan-2-ylmethyl ester,4-(7-Bromo-8-hydroxy-quinolin-5-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-[5-(4-nitro-phenyl)-furan-2-ylmethylene]-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-[5-(2-nitro-phenyl)-furan-2-ylmethylene]-pyrazolidine-3,5-dione,4-(5-Hydroxymethyl-furan-2-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(5-nitro-thiophen-2-ylmethylene)-pyrazolidine-3,5-dione,4-(5-Hydroxymethyl-furan-2-ylmethylene)-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,4-(5-Nitro-thiophen-2-ylmethylene)-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(5-nitro-furan-2-ylmethylene)-pyrazolidine-3,5-dione,4-(4, 5-Dimethyl-furan-2-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,5-[1-(4-Iodo-phenyl)-3,5-dioxo-pyrazolidin-4-ylidenemethyl]-furan-2-sulfonic acid,4-[1-(4-Iodo-phenyl)-3,5-dioxo-pyrazolidin-4-ylidenemethyl]-benzonitrile,1-(4-Iodo-phenyl)-4-(3-methyl-thiophen-2-ylmethylene)-pyrazolidine-3,5-dione,4-(4-Bromo-thiophen-2-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(5-methyl-thiophen-2-ylmethylene)-pyrazolidine-3,5-dione,4-Benzo[b]thiophen-2-ylmethylene-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(4-nitro-thiophen-2-ylmethylene)-pyrazolidine-3,5-dione,5-[1-(4-Iodo-phenyl)-3,5-dioxo-pyrazolidin-4-ylidenemethyl]-thiophene-3-carboxylic acid,4-[1-(4-Iodo-phenyl)-3,5-dioxo-pyrazolidin-4-ylidenemethyl]-thiophene-3-carboxylic acid,2-[3,5-Dioxo-1-(3-trifluoromethyl-phenyl)-pyrazolidin-4-ylidenemethyl]-thiophene-3-carboxylic acid,4-(4-Nitro-thiophen-2-ylmethylene)-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,4-[3,5-Dioxo-1-(3-trifluoromethyl-phenyl)-pyrazolidin-4-ylidenemethyl]-thiophene-3-carboxylic acid,{3-[3,5-Dioxo-1-(3-trifluoromethyl-phenyl)-pyrazolidin-4-ylidenemethyl]-thiophen-2-ylsulfanyl-acetic acid,2-[1-(4-Iodo-phenyl)-3,5-dioxo-pyrazolidin-4-ylidenemethyl]-thiophene-3-carboxylic acid,4-(4-Hydroxymethyl-furan-3-ylmethylene)-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,4-benzo[b]thiophen-2-ylmethylene-1-(3-trifluoromethyl-phenyl)-pyrazolidine-3,5-dione,5-[3,5-Dioxo-1-(3-trifluoromethyl-phenyl)-pyrazolidin-4-ylidenemethyl]-thiophene-3-carboxylic acid,5-[1-(4-Iodo-phenyl)-3,5-dioxo-pyrazolidin-4-ylidenemethyl]-furan-2-carboxylic acid,5-(1-Biphenyl-4-yl-3,5-dioxo-pyrazolidin-4-ylidenemethyl)-furan-2-carboxylic acid,4-(4-Hydroxy-naphthalen-1-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(1-oxy-pyridin-4-ylmethylene)-pyrazolidine-3,5-dione,4-(1H-Indol-5-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,4-(4-Hydroxymethyl-furan-3-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodophenyl)-4-(1H-pyrrol-2-ylmethylene)-pyrazolidine-3,5-dione,1-(4-Iodophenyl)-4-(1-methyl-1H-pyrrol-2-ylmethylene)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-[1-(2-nitro-benzyl)-1H-pyrrol-2-ylmethylene]-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl-4-(1H-pyrazol-3-ylmethylene)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl-4-(1H-pyrazol-3-ylmethylene)-pyrazolidine-3,5-dione,4-(2, 3-Dihydro-benzofuran-5-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-quinolin-2-ylmethylene-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-quinolin-4-ylmethylene-pyrazolidine-3,5-dione,4-[3-(2-Hydroxy-ethoxy)-benzylidene]-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(5-naphthalen-2-yl-thiophen-2-ylmethylene)-pyrazolidine-3,5-dione,3-{5-[1-(4-Iodo-phenyl)-3,5-dioxo-pyrazolidin-4-ylidenemethyl]-furan-2-yl}-thiophene-2-carboxylic acid methyl ester,4-(5-Chloro-thiophen-2-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,[1-(4-Iodo-phenyl)-4-thiazol-2-ylmethylene-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-(1-methyl-1H-imidazol-2-ylmethylene)-pyrazolidine-3,5-dione,4-(2-Diethylamino-thiazol-5-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,4-[2-(4-Benzyl-piperazin-1-yl)-thiazol-5-ylmethylene]-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,1-(4-Iodo-phenyl)-4-[2-(4-methoxy-phenoxy)-thiazol-5-ylmethylene]-pyrazolidine-3,5-dione,4-(9-Ethyl-9H-carbazol-3-ylmethylene)-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione, or 4-Benzo[b]thiophen-3-ylmethylene-1-(4-iodo-phenyl)-pyrazolidine-3,5-dione,or a pharmaceutically acceptable salt thereof or tautomer thereof. |
