Patent ID: 7666901
Filing Date: 2010-02-23
Classification: A61P,C07D,C07J

Abstract:
1. A compound selected from the group consisting of: (1E,4S,4aR,5R,6aS,7S,9aR)-1-[(diethylamino)methylene]-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S,9aR)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1-(Pyrrolidin-1-ylmethylene)-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S,9aR)-1-(anilinomethylene)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-{[tert-butyl(2-hydroxyethyl)amino]methylene}-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-{[[3-(dimethylamino)propyl](methyl)amino]methylene}-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-1-{[methyl(1-methylpyrrolidin-3-yl)amino]methylene}-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-[(4-cyclohexylpiperazin-1-yl)methylene]-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-{([butyl(methyl)amino]methylene}-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-{[cyclohexyl(methyl)amino]methylene}-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-[(4-benzylpiperazin-1-yl)methylene]-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1-(piperidin-1-ylmethylene)-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-(3,4-dihydroisoquinolin-2(1H)-ylmethylene)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1-[(4-phenylpiperazin-1-yl)methylene]-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno [4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-1-[(4-methylpiperazin-1-yl)methylene]-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno [4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1-[(4-phenylpiperidin-1-yl)methylene]-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno [4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-7-(formyloxy)-11-hydroxy-4-(methoxymethyl)-4a,6a -dimethyl-2,10-dioxo-1-(pyrrolidin-1-ylmethylene)-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-[(diethylamino)methylene]-7-(formyloxy)-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-[(diethylamino)methylene]-7-(formyloxy)-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; Acetic acid 4-{[bis-(2-hydroxy-ethyl)-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-[(tert-butyl-methyl-amino)-methylene]-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-{[bis-(3-dimethylamino-propyl)-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; 1-(11-Acetoxy-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,7,10,11,12,13,14,15,16,17-decahydro-2-oxa-cyclopenta[a]phenanthren-4-ylidenemethyl)-piperidine-4-carboxylic acid methyl ester; 1-(11-Acetoxy-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,7,10,11,12,13,14,15,16,17-decahydro-2-oxa-cyclopenta[a]phenanthren-4-ylidenemethyl)-piperidine-4-carboxylic acid; 4-[(11-Acetoxy-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,7,10,11,12,13,14,15,16,17-decahydro-2-oxa-cyclopenta[a]phenanthren-4-ylidenemethyl)-methyl-amino]-2,5-dimethyl-hex-2-enoic acid methyl ester; Acetic acid 6,17-dihydroxy-1-methoxymethyl-4-[({3-[4-(4-methoxy-phenyl)-piperazin-1-yl]-propyl}-methyl-amino)-methylene]-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-4-({methyl-[3-(4-methyl-piperazin-1-yl)-propyl]-amino}-methylene)-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-4-{[methyl-(3-morpholin-4-yl-propyl)-amino]-methylene}-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-{[(2-benzenesulfonyl-ethyl)-(3-diethylamino-propyl)-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-{[(1-aza-bicyclo[3,3,1]non-5-ylmethyl)-benzyl-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-4-[4-(3-morpholin-4-yl-propyl)-piperazin-1-ylmethylene]-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-{[(2-dimethylamino-ethyl)-methyl-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-[4-(3-dimethylamino-propyl)-piperazin-1-ylmethylene]-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-4-[4-(2-morpholin-4-yl-ethyl)-piperazin-1-ylmethylene]-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-4[4-(1-methyl-piperidin-4-yl)-piperazin-1-ylmethylene]-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; [(11-Acetoxy-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,7,10,11,12,13,14,15,16,17-decahydro-2-oxa-cyclopenta[a]phenanthren-4-ylidenemethyl)-methyl-amino]-acetic acid tert-butyl ester; Acetic acid 4{[(2,3-dihydroxy-propyl)-methyl-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; 4-[(11-Acetoxy-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,7,10,11,12,13,14,15,16,17-decahydro-2-oxa-cyclopenta[a]phenanthren-4-ylidenemethyl)-methyl-amino]-butyric acid; 1-(11-Acetoxy-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,7,10,11,12,13,14,15,16,17-decahydro-2-oxa-cyclopenta[a]phenanthren-4-ylidenemethyl)-azetidine-2-carboxylic acid; 1-(11-Acetoxy-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,7,10,11,12,13,14,15,16,17-decahydro-2-oxa-cyclopenta[a]phenanthren-4-ylidenemethyl)-pyrrolidine-2-carboxylic acid methyl ester; Acetic acid 4-{[benzyl-(2-cyano-ethyl)-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-{[(2-diethylamino-ethyl)-methyl-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-{[(2-diethylamino-ethyl)-ethyl-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-{[benzyl-(2-dimethylamino-ethyl)-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-4-(4-oxo-piperidin-1-ylmethylene)-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; 4-{[(2-Dimethylamino-ethyl)-ethyl-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-10,11,12,13,14,15,16,17-octahydro-1H,4H-2-oxa-cyclopenta[a]phenanthrene-3,7-dione; Acetic acid 4-{[(2-dimethylamino-ethyl)-ethyl-amino]methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-[1,4′]bipiperidinyl-1′-ylmethylene-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-4-morpholin-4-ylmethylene-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Propionic acid 4-{[(2-dimethylamino-ethyl)-methyl-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; (1E,4S,4aR,5R,6aS,7S,9aR)-1-[(diethylamino)methylene]-5,7,11-trihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-4a,5,6,6a,7,8,9,9a-octahydroindeno[4,5-h]isochromene-2,10(1H,4H)-dione; Acetic acid 4-butylsulfanylmethylene-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; 7-Pegylated di-(1E,4S,4aR,5R,6aS,7S)-1-{[[3-(dimethylamino)propyl](methyl)amino]methylene}-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1E,4S,4aR,5R,6aS,7S)-1-{[[3-(dimethylamino)propyl](methyl)amino]methylene}-5,7,11-trihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-4a,5,6,6a,7,8,9,9a-octahydroindeno[4,5-h]isochromene-2,10(1H,4H)-dione; (1E,4S,4αR,5R,6αS,7S,9αR)-1-({tert-butyl[2-(dimethylamino)ethyl]amino}methylene)-7,11-dihydroxy-4-(methoxymethyl)-4, α6α-dimethyl-2,10-dioxo-1,2,4,4α,5,6,6α,7,8,9,9α,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; Butanoic acid 4-{[(2-dimethylamino-propyl)-methyl-amino]-methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester; Acetic acid 4-{[(2-dimethylamino-propyl)-ethyl-amino]methylene}-6,17-dihydroxy-1-methoxymethyl-10,13-dimethyl-3,7-dioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta[a]phenanthren-11-yl ester (1E,4S,4aR,5R,6aS,7S,9aR)-1-({4-[2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)ethyl]piperazin-1-yl}methylene)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1Z,4S,4aR,5R,6aS,7S)-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1{12-oxo-16-[(3aR,4R,6aS)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]-5,8-dioxa-2,11-diazahexadec-1-ylidene}-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; 7-Pegylated (1E,4S,4aR,5R,6aS,7S,9aR)-1-[(diethylamino)methylene]-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1Z,4S,4aR,5R,6aS,7S)-1-{[t-butylamino]methylene}-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1Z,4S,4aR,5R,6aS,7S)-7,11-dihydroxy-1-{[(2-mercaptoethyl)amino]methylene}-4-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; (1Z,4S,4aR,5R,6aS,7S,9aR)-1-[(ethylamino)methylene]-7,11-dihydroxy-4-in-(methoxymethyl)-4a,6a-dimethyl-2,10-dioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; and salts, solvates, and hydrates thereof.