PATENT CLAIM ANALYSIS

Application Number: 16098244
Application Type: Utility
Filing Date: 2018-11
Publication Date: 2019-05
Patent Classification: ["514", "218000"]

Abstract:
The present invention relates to new compounds of general formula (I) that show great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially α2δ-1 subunit of voltage-gated calcium channels or dual activity towards subunit α2δ of voltage-gated calcium channels (VGCC), especially α2δ-1 subunit of voltage-gated calcium channels, and noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

Claim (Index 25):
The compound according to  claim 18 , which is selected from the following list:\n [1] tert-Butyl methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)carbamate; [2] tert-butyl (R)-methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)carbamate; [3] tert-butyl (S)-methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)carbamate; [4] tert-butyl methyl(2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)carbamate; [5] tert-butyl (2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)carbamate; [6] tert-butyl methyl(2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)carbamate; [7] tert-butyl methyl(3-methyl-2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)butyl)carbamate; [8] tert-butyl methyl(2-(4-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)carbamate; [9] tert-butyl methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamate; [10] tert-butyl (R)-methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamate; [11] tert-butyl (S)-methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamate; [12] tert-butyl methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate; [13] tert-butyl (R)-methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate; [14] tert-butyl (S)-methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate; [15] tert-butyl methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)carbamate; [16] tert-butyl (R)-methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)carbamate; [17] tert-butyl (S)-methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)carbamate; [18] tert-butyl methyl(2-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-1-phenylethyl)carbamate; [19] 2-(trimethylsilyl)ethyl methyl(2-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-2-phenylethyl)carbamate; [20] tert-butyl methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)carbamate; [21] tert-butyl benzyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)carbamate; [22] tert-butyl methyl(2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)ethyl)carbamate; [23] tert-butyl methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)propyl)carbamate; [24] tert-butyl methyl(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenethyl)carbamate; [25] tert-butyl methyl(2-methyl-2-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)propyl)carbamate; [26] tert-butyl methyl(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)carbamate; [27] tert-butyl 3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)pyrrolidine-1-carboxylate; [28] tert-butyl 4-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-4-phenylpiperidine-1-carboxylate; [29] 9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [30] 9-ethyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [31] 9-methyl-6-(3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [32] 6-(3-methoxyphenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [33] 3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzonitrile; [34] 6-(3-((tert-butyldimethylsilyl)oxy)phenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [35] 6-(3-bromophenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [36] 6-(3-(2-hydroxyethyl)phenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [37] 6-(4-methoxyphenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [38] 6-(4-((tert-butyldimethylsilyl)oxy)phenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [39] tert-butyl methyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamate; [40] tert-butyl ((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamate; [41] tert-butyl benzyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamate; [42] 6-(3-(4-(diethoxymethyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [43] tert-butyl methyl(2-(1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)ethyl)carbamate; [44] tert-butyl methyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)-1H-1,2,3-triazol-4-yl)methyl)carbamate; [45] tert-butyl methyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-pyrazol-4-yl)methyl)carbamate; [46] tert-butyl methyl((1-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-imidazol-4-yl)methyl)carbamate; [47] tert-butyl methyl((5-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1,3,4-oxadiazol-2-yl)methyl)carbamate; [48] tert-butyl methyl(3-(2-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl) phenoxy)-3-phenylpropyl)carbamate; [49] tert-butyl methyl(4-methyl-3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)pentyl)carbamate; [50] tert-butyl methyl(3-((3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)butyl)carbamate; [51] 2-(trimethylsilyl)ethyl methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate; [52] tert-butyl methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(pyridin-2-yl)propyl)carbamate; [53] tert-butyl methyl(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(pyridin-3-yl)propyl)carbamate; [54] 8-(ethylamino)-1-methyl-4-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [55] 4-(3-(4-ethyl-5-methyl-4H-1,2,4-triazol-3-yl)phenyl)-8-(ethylamino)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [56] tert-butyl (3-(3-(8-(ethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-phenylpropyl)(methyl)carbamate; [57] tert-butyl (3-((3-(8-(ethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [58] 2-(trimethylsilyl)ethyl (3-(3-(8-(ethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [59] 2-(trimethylsilyl)ethyl (3-(3-(8-(dimethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [60] 2-(trimethylsilyl)ethyl (3-((3-(8-(ethylamino)-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [61] tert-butyl (2-fluoroethyl)(3-(3-(9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate; [62] tert-Butyl methyl(2-(3-((9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)phenoxy)-2-phenylethyl)carbamate; [63] tert-butyl methyl(2-(4-((9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)phenoxy)-2-phenylethyl)carbamate; [64] tert-butyl methyl(4-((9-methyl-2-(methylthio)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)benzyl)carbamate; [65] tert-Butyl (R)-(3-((3-(2-(ethylamino)-9-methyl-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [66] N-ethyl-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-2-amine; [67] N-ethyl-6-(3-methoxybenzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-2-amine; [68] N-ethyl-6-(4-methoxybenzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-2-amine; [69] tert-Butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)(methyl)carbamate; [70] tert-butyl (R)-(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)(methyl)carbamate; [71] tert-butyl (S)-(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)(methyl)carbamate; [72] tert-butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)(methyl)carbamate; [73] tert-butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)carbamate; [74] tert-butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)(methyl)carbamate; [75] tert-butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-methylbutyl)(methyl)carbamate; [76] tert-butyl (2-(4-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-2-phenylethyl)(methyl)carbamate; [77] tert-butyl (3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [78] tert-butyl (R)-(3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [79] tert-butyl (S)-(3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [80] tert-butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [81] tert-butyl (R)-(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [82] tert-butyl (S)-(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [83] tert-butyl (3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [84] tert-butyl (R)-(3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [85] tert-butyl (S)-(3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [86] tert-butyl (2-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-1-phenylethyl)(methyl)carbamate; [87] 2-(trimethylsilyl)ethyl (2-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-2-phenylethyl)(methyl)carbamate; [88] tert-butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)(methyl)carbamate; [89] tert-butyl benzyl(3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)propyl)carbamate; [90] tert-butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)ethyl)(methyl)carbamate; [91] tert-butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)propyl)(methyl)carbamate; [92] tert-butyl (3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenethyl)(methyl)carbamate; [93] tert-butyl (2-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-2-methylpropyl)(methyl)carbamate; [94] tert-butyl (3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)(methyl)carbamate; [95] tert-butyl 3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)pyrrolidine-1-carboxylate; [96] tert-butyl 4-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-4-phenylpipendine-1-carboxylate; [97] 2-(ethylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [98] 2-(isobutylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [99] 2-((2-methoxyethyl)amino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [100] 9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-2-(methylamino)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [101] 2-amino-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]di2-(benzylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one azepin-5-one; [102] 2-(benzylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [103] 2-(cyclohexylamino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [104] 2-(benzyl(methyl)amino)-9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [105] 9-methyl-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-2-(phenethylamino)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [106] 9-methyl-2-(methyl (pyridin-2-ylmethyl)amino)-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [107] 9-ethyl-2-(ethylamino)-6-(3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [108] 2-(ethylamino)-9-methyl-6-(3-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [109] 2-(ethylamino)-6-(3-methoxyphenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [110] 3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzonitrile; [111] 6-(3-((tert-butyldimethylsilyl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [112] 2-(ethylamino)-6-(3-(2-hydroxyethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [113] 2-(ethylamino)-6-(3-(2-hydroxyethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [114] 2-(ethylamino)-6-(4-methoxyphenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [115] 6-(4-((tert-butyldimethylsilyl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [116] tert-butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)(methyl)carbamate; [117] tert-butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamate; [118] tert-butyl benzyl((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)carbamate; [119] 6-(3-(4-(diethoxymethyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [120] tert-butyl (2-(1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)ethyl)(methyl)carbamate; [121] tert-butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)-1H-1,2,3-triazol-4-yl)methyl)(methyl)carbamate; [122] tert-butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-pyrazol-4-yl)methyl)(methyl)carbamate; [123] tert-butyl ((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-imidazol-4-yl)methyl)(methyl)carbamate; [124] tert-butyl ((5-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1,3,4-oxadiazol-2-yl)methyl)(methyl)carbamate; [125] tert-butyl (3-(2-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-phenylpropyl)(methyl)carbamate; [126] tert-butyl (3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-4-methylpentyl)(methyl)carbamate; [127] tert-butyl (3-((3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)butyl)(methyl)carbamate; [128] tert-butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(pyridin-2-yl)propyl)(methyl)carbamate; [129] tert-butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(pyridin-3-yl)propyl)(methyl)carbamate; [130] tert-butyl (R)-(3-((3-(2-amino-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [131] tert-butyl (R)-(3-((3-(2-(dimethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [132] tert-butyl (R)-methyl(3-((3-(9-methyl-2-(methylamino)-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamate; [133] 2-(trimethylsilyl)ethyl (3-(3-(2-(dimethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [134] tert-butyl (3-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(2-fluoroethyl)carbamate; [135] tert-butyl (2-(3-((2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)phenoxy)-2-phenylethyl)(methyl)carbamate; [136] tert-butyl (2-(4-((2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)phenoxy)-2-phenylethyl)(methyl)carbamate; [137] tert-butyl (4-((2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)methyl)benzyl)(methyl)carbamate; [138] tert-Butyl (R)-(3-((3-(2-methoxy-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [139] tert-butyl (3-((3-(2-methoxy-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [140] tert-Butyl (R)-(3-((3-(2-hydroxy-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [141] tert-butyl (3-((3-(2-hydroxy-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [142] tert-Butyl (R)-(3-((3-(2,9-dimethyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [143] tert-butyl (3-((3-(2,9-dimethyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [144] 2-(trimethylsilyl)ethyl (3-(3-(2,9-dimethyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [145] tert-Butyl (R)-methyl(3-((3-(9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-phenylpropyl)carbamate; [146] tert-butyl methyl(3-((3-(9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzyl)oxy)-3-(thiophen-2-yl)propyl)carbamate; [147] 2-(trimethylsilyl)ethyl methyl(3-(3-(9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenoxy)-3-(thiophen-2-yl)propyl)carbamate; [148] 2-(Ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [149] (R)-2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [150] (S)-2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [151] 9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [152] (R)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [153] (S)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [154] 2-(ethylamino)-9-methyl-6-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [155] 9-methyl-6-(3-(2-(methylamino)-1-phenylethoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [156] 6-(3-(2-amino-1-phenylethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [157] 2-(ethylamino)-9-methyl-6-(3-((1-(methylamino)propan-2-yl)oxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [158] 2-(ethylamino)-9-methyl-6-(3-((3-methyl-1-(methylamino)butan-2-yl)oxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [159] 2-(ethylamino)-9-methyl-6-(4-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [160] 2-(ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [161] (R)-2-(ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [162] (S)-2-(ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [163] 9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [164] (R)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [165] (S)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [166] 2-(ethylamino)-9-methyl-6-(3-((2-(methylamino)-2-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [167] 9-methyl-6-(3-((2-(methylamino)-2-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [168] 2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [169] 6-(3-(3-(benzylamino)propoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [170] 2-(ethylamino)-9-methyl-6-(3-(2-(methylamino)ethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [171] 2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)propyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [172] 2-(ethylamino)-9-methyl-6-(3-(2-(methylamino)ethyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [173] 2-(ethylamino)-9-methyl-6-(3-(2-methyl-1-(methylamino)propan-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [174] 2-(ethylamino)-9-methyl-6-(3-((methylamino)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [175] 2-(ethylamino)-9-methyl-6-(3-(pyrrolidin-3-yloxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [176] 2-(ethylamino)-9-methyl-6-(3-(((4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [177] 2-(ethylamino)-6-(3-hydroxyphenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [178] 2-(ethylamino)-6-(4-hydroxyphenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [179] 9-methyl-2-(methylthio)-6-(3-(((4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [180] 2-(ethylamino)-9-methyl-6-(3-(4-((methylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [181] 6-(3-(4-(aminomethyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [182] 6-(3-(4-((benzylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [183] 2-(ethylamino)-9-methyl-6-(3-(4-(2-(methylamino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [184] 2-(ethylamino)-9-methyl-6-(3-((4-((methylamino)methyl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [185] 2-(ethylamino)-9-methyl-6-(3-(4-((methylamino)methyl)-1H-pyrazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [186] 2-(ethylamino)-9-methyl-6-(3-(4-((methylamino)methyl)-1H-imidazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [187] 2-(ethylamino)-9-methyl-6-(3-(5-((methylamino)methyl)-1,3,4-oxadiazol-2-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [188] 2-(ethylamino)-9-methyl-6-(2-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [189] 2-(ethylamino)-9-methyl-6-(3-(((4-methyl-1-(methylamino)pentan-3-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [190] 9-methyl-6-(3-(((4-methyl-1-(methylamino)pentan-3-yl)oxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [191] 2-(ethylamino)-9-methyl-6-(3-(((4-(methylamino)butan-2-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [192] 9-methyl-6-(3-(((4-(methylamino)butan-2-yl)oxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [193] 2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(pyridin-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [194] 2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(pyridin-3-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [195] (R)-2-amino-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [196] (R)-2-(dimethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [197] (R)-9-methyl-2-(methylamino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [198] 8-(ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-phenylpropoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [199] 8-(ethylamino)-1-methyl-4-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [200] 2-(ethylamino)-9-methyl-6-(3-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [201] 2-(ethylamino)-9-methyl-6-(4-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [202] 2-(ethylamino)-9-methyl-6-(4-((methylamino)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [203] (R)\u2014N-ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-2-amine; [204] (R)-2-methoxy-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [205] (R)-2-hydroxy-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [206] (R)-2,9-dimethyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [207] (R)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [208] 9-Methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [209] (R)-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [210] (S)-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [211] 2-(ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [212] (R)-2-(ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [213] 2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [214] 2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [215] (R)-2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [216] (S)-2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [217] 9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [218] (R)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [219] (S)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [220] 2-(ethylamino)-6-(3-(3-((2-fluoroethyl)amino)-1-(thiophen-2-yl)propoxy)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [221] 2-methoxy-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2H)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [222] 2-hydroxy-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [223] 2,9-dimethyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [224] 9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [225] 2-(Ethylamino)-9-methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [226] 9-methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [227] 8-(ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [228] 8-(ethylamino)-1-methyl-4-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [229] 8-(dimethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [230] 2-(dimethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [231] 2,9-dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [232] 9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [233] tert-Butyl 4-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-3,6-dihydropyridine-1(2H)-carboxylate; [234] tert-Butyl 4-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)piperidine-1-carboxylate; [235] 2-(Ethylamino)-9-methyl-6-(3-(piperidin-4-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [236] (R)-6-(3-((3-(Dimethylamino)-1-phenylpropoxy)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [237] (S)-6-(3-((3-(dimethylamino)-1-phenylpropoxy)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [238] 6-(3-(3-(dimethylamino)-1-phenylpropoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [239] 6-(3-(2-(dimethylamino)-1-phenylethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [240] 6-(3-(3-(benzyl(methyl)amino)propyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [241] 6-(3-(3-(dimethylamino)propyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [242] 6-(3-(4-((dimethylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [243] 6-(3-(4-((benzyl(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [244] 2-(ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [245] 6-(3-(4-((bis(cyclopropylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [246] 6-(3-(4-(((cyclopropylmethyl)(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [247] 6-(3-(4-(2-(benzyl(methyl)amino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [248] 6-(3-(4-(2-(dimethylamino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [249] 2-(ethylamino)-9-methyl-6-(3-(4-(2-(methyl(phenethyl)amino)ethyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [250] 6-(3-((4-((benzyl(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [251] 6-(3-(4-((benzyl(methyl)amino)methyl)-1H-pyrazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [252] 2-(ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-pyrazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [253] 6-(3-(4-((benzyl(methyl)amino)methyl)-1H-imidazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [254] 2-(ethylamino)-9-methyl-6-(3-(4-((methyl(phenethyl)amino)methyl)-1H-imidazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [255] 6-(3-(5-((benzyl(methyl)amino)methyl)-1,3,4-oxadiazol-2-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [256] 6-(3-(3-(benzyl(methyl)amino)propoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [257] 6-(3-(3-(dimethylamino)propoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [258] 2-(ethylamino)-9-methyl-6-(3-(3-(methyl(phenethyl)amino)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [259] 6-(3-(1-benzylpiperidin-4-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [260] 2-(ethylamino)-9-methyl-6-(3-(1-methylpiperidin-4-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [261] 2-(ethylamino)-9-methyl-6-(3-(1-phenethylpiperidin-4-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [262] 6-(3-((1-(benzyl(methyl)amino)propan-2-yl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [263] 2-(ethylamino)-9-methyl-6-(3-((1-(methyl(phenethyl)amino)propan-2-yl)oxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [264] 6-(3-(2-(benzyl(methyl)amino)ethoxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [265] 2-(ethylamino)-9-methyl-6-(3-(2-(methyl(phenethyl)amino)ethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [266] 6-(3-((1-benzylpyrrolidin-3-yl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [267] 6-(3-((1-(benzyl(methyl)amino)-3-methylbutan-2-yl)oxy)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [268] 2-(ethylamino)-9-methyl-6-(3-((3-methyl-1-(methyl(phenethyl)amino)butan-2-yl)oxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [269] 6-(3-(2-(benzyl(methyl)amino)ethyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [270] 2-(ethylamino)-9-methyl-6-(3-(2-(methyl(phenethyl)amino)ethyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [271] 9-methyl-6-(3-(((1-methyl-4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [272] 2-(ethylamino)-9-methyl-6-(3-(((1-methyl-4-phenylpiperidin-4-yl)oxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [273] 2-(ethylamino)-6-(3-(4-(((2-(2-hydroxyethoxy)ethyl)(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [274] 3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenethyl 4-methylbenzenesulfonate; [275] 2-(Ethylamino)-6-(3-(2-(4-(3-hydroxyphenyl)piperidin-1-yl)ethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [276] (R)-9-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenethyl)-4-isopropyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one; [277] 1-(3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazole-4-carbaldehyde; [278] 2-(Ethylamino)-9-methyl-6-(3-(4-((4-phenylpiperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [279] 2-(ethylamino)-6-(3-(4-((4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [280] 2-(ethylamino)-9-methyl-6-(3-(4-((4-phenylpiperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [281] 2-(ethylamino)-9-methyl-6-(3-(4-(piperidin-1-ylmethyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [282] 6-(3-(4-((3,4-dihydroisoquinolin-2(1H)-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [283] 6-(3-(4-((3,4-dihydro-2H-spiro[isoquinoline-1,4\u2032-piperidin]-1\u2032-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [284] (R)-9-((1-(3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)-4-isopropyl-2-methyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one; [285] 6-(3-(4-(((cyclopropylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [286] 2-(ethylamino)-6-(3-(4-((ethylamino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [287] 2-(ethylamino)-6-(3-(4-(((4-fluorobenzyl)(methyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [288] 2-(ethylamino)-9-methyl-6-(3-(4-((methyl(pyridin-2-ylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [289] 2-(ethylamino)-9-methyl-6-(3-(4-((methyl(pyridin-3-ylmethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [290] 2-(ethylamino)-6-(3-(4-(((2-(2-hydroxyethoxy)ethyl)amino)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [291] 6-(3-(4-((4-(dimethylamino)-4-phenylpiperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [292] 6-(3-((4-(dimethylamino)-4-phenylpiperidin-1-yl)methyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [293] 6-(3-(4-((4-(dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [294] 6-(3-(4-((4-(dimethylamino)-4-phenylpiperidin-1-yl)methyl)-1H-pyrazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [295] 6-(3-(4-((4-(dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-pyrazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [296] 6-(3-(4-((4-(dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1H-imidazol-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [297] 2-(trimethylsilyl)ethyl (3-(3-(8-chloro-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [298] 2-(trimethylsilyl)ethyl (S)-(3-(3-(8-chloro-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [299] 2-(trimethylsilyl)ethyl (S)-(3-(4-((8-chloro-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)methyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [300] tert-butyl (3-((3-(8-chloro-1-methyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [301] 2-(Trimethylsilyl)ethyl (S)-(3-(4-((1,8-dimethyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)methyl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [302] 2-(trimethylsilyl)ethyl (3-(3-(1,8-dimethyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)phenoxy)-3-(thiophen-2-yl)propyl)(methyl)carbamate; [303] tert-butyl (3-((3-(1,8-dimethyl-5-oxo-1,2,3,5-tetrahydro-4H-pyrido[4,3-e][1,4]diazepin-4-yl)benzyl)oxy)-3-phenylpropyl)(methyl)carbamate; [304] (S)-8-Amino-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [305] (S)-8-amino-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [306] 1,8-dimethyl-4-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [307] 1,8-dimethyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [308] (S)-1,8-dimethyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [309] methyl 3-(2-(ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzoate; [310] 2-(ethylamino)-6-(3-(2-hydroxyethyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [311] 6-(3-bromophenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [312] 6-(3-(4-(Dimethylamino)-4-phenylpiperidin-1-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [313] 3-(2-(Ethylamino)-9-methyl-5-oxo-5,7,8,9-tetrahydro-6H-pyrimido[4,5-e][1,4]diazepin-6-yl)benzoic acid; [314] 6-(3-(4-(Dimethylamino)-4-phenylpiperidine-1-carbonyl)-phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]-diazepin-5-one; [315] 9-methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [316] 9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [317] 1-methyl-4-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [318] 9-methyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [319] 9-methyl-6-(2-(2-(methylamino)-1-phenylethoxy)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [320] 9-methyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [321] 9-methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [322] 9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-(trifluoromethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [323] 1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [324] (R)-8-(ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [325] (S)-8-(ethylamino)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [326] (S)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [327] (R)-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [328] 9-methyl-6-(4-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [329] 9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-2-(trifluoromethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [330] 9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2H)propoxy)methyl)phenyl)-2-(trifluoromethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [331] (S)-8-methoxy-1-methyl-4-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [332] (S)-2-amino-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [333] 2-(ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [334] 2-(ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [335] 2-(benzylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [336] 9-methyl-2-(methyl(pyridin-2-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [337] 2-(ethylamino)-9-methyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [338] 2-(ethylamino)-9-methyl-6-(2-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [339] 2-(ethylamino)-9-methyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [340] 2-(ethylamino)-9-methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [341] (R)-9-methyl-2-(methyl(pyridin-2-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [342] (R)-9-methyl-2-(methyl(pyridin-3-ylmethyl)amino)-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [343] (R)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-2-((pyridin-2-ylmethyl)amino)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [344] (R)-2-(((5-fluoropyridin-2-yl)methyl)(methyl)amino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [345] 2-(ethylamino)-6-(3-((3-((2-fluoroethyl)amino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [346] (S)-2-amino-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [347] (R)-2-amino-9-methyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [348] 2-(ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [349] 2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [350] (S)-2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one [351] (R)-2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-3-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [352] (S)-2-amino-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [353] 2,9-dimethyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [354] 2-ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [355] 2,9-dimethyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [356] (R)-2-ethyl-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [357] (R)-2,9-dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [358] (S)-2,9-dimethyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [359] (S)-2,9-dimethyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [360] (R)-2,9-dimethyl-6-(3-((3-(methylamino)-1-(thiophen-2-yl)propoxy)methyl)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [361] 9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [362] 9-methyl-6-(2-(2-(methylamino)-1-phenylethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [363] (R)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [364] (S)-9-methyl-6-(3-(3-(methylamino)-1-(thiophen-2-yl)propoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [365] 9-methyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [366] 9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [367] 9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [368] 9-methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [369] 9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [370] 9-methyl-6-(2-(3-(methylamino)-1-phenylpropoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [371] 9-methyl-6-(2-(2-(methylamino)-1-phenylethoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [372] 9-methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [373] 9-methyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [374] 9-methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [375] (S)-2-methoxy-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [376] 6-(4-(1-(2-fluorophenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [377] (S)-1-methyl-4-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [378] 9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2H)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [379] (S)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [380] (R)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2H)propoxy)benzyl)-2-(methylthio)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [381] 1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [382] (S)-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [383] (S)-8-(ethylamino)-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [384] (S)-8-(dimethylamino)-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [385] (S)-8-methoxy-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [386] (S)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-(trifluoromethyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [387] 2-methoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-311)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [388] 2-methoxy-9-methyl-6-(4-(3-(methylamino)-1-(3-methylthiophen-2H)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [389] (S)-1-ethyl-8-methoxy-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [390] 2-methoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiazol-2H)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [391] (S)-1-ethyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [392] 2-methoxy-9-methyl-6-(4-(3-(methylamino)-1-(5-methylthiophen-2H)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [393] (S)-2-methoxy-9-methyl-6-(3-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [394] (S)-6-(3-fluoro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [395] (S)-9-ethyl-2-methoxy-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [396] 2-methoxy-9-methyl-6-(4-(3-(methylamino)-1-(4-methylthiophen-2H)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [397] (S)-2-methoxy-9-methyl-6-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [398] (S)-9-ethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [399] (S)-9-fluoro-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [400] (S)-9-chloro-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [401] (S)-6-(2-fluoro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [402] (S)-2-methoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [403] (S)-6-(4-fluoro-2-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [404] 2-(ethylamino)-9-methyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [405] 2-(ethylamino)-9-methyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [406] 2-(ethylamino)-9-methyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [407] 2-(ethylamino)-9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [408] 2-(ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [409] 2-(ethylamino)-9-methyl-6-(2-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [410] 2-(ethylamino)-9-methyl-6-(2-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [411] 2-(ethylamino)-9-methyl-6-(3-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [412] 2-(ethylamino)-9-methyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [413] 2-(ethylamino)-9-methyl-6-(4-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [414] (S)-2-(ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [415] (R)-2-(ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [416] 2-(ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [417] (S)-2-(ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [418] (R)-2-(ethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [419] (S)-2-(dimethylamino)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [420] (S)-2-amino-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [421] 2,9-dimethyl-6-(2-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [422] 2,9-dimethyl-6-(4-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [423] 2,9-dimethyl-6-(3-((3-(methylamino)-1-phenylpropoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [424] 2,9-dimethyl-6-(2-((2-(methylamino)-1-phenylethoxy)methyl)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [425] 2,9-dimethyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [426] 2-ethyl-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [427] (R)-2,9-dimethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [428] (S)-2,9-dimethyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [429] 9-methyl-6-(3-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [430] 9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [431] 9-methyl-6-(2-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [432] 9-methyl-6-(2-(2-(methylamino)-1-phenylethoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [433] (S)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [434] (R)-9-methyl-6-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [435] 9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [436] (S)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [437] (R)-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2H)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [438] 6-(3-(2-(4-(dimethylamino)-4-phenylpiperidin-1-yl)ethyl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [439] 2-(ethylamino)-9-methyl-6-(3-(2-(piperidin-1-yl)ethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [440] 2-(ethylamino)-9-methyl-6-(3-(2-morpholinoethoxy)phenyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [441] 6-(3-(5-((4-(dimethylamino)-4-phenylpiperidin-1-yl)methyl)-1,3,4-oxadiazol-2-yl)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [442] 6-(3-(5-((4-(dimethylamino)-4-(3-hydroxyphenyl)piperidin-1-yl)methyl)-1,3,4-oxadiazol-211)phenyl)-2-(ethylamino)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [443] 6-(4-(1-(2-fluorophenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [444] 4-(4-(1-(2-fluorophenyl)-3-(methylamino)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [445] 4-(4-(1-(2-fluorophenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [446] 6-(4-(1-(3-fluorophenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [447] 6-(4-(1-(3-fluorophenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [448] 4-(4-(1-(3-fluorophenyl)-3-(methylamino)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [449] 4-(4-(1-(3-fluorophenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [450] 6-(4-(1-(4-fluorophenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [451] 6-(4-(1-(4-fluorophenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [452] 4-(4-(1-(4-fluorophenyl)-3-(methylamino)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [453] 4-(4-(1-(4-fluorophenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [454] 6-(4-(1-(2-chlorophenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [455] 6-(4-(1-(2-chlorophenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [456] 4-(4-(1-(2-chlorophenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [457] 6-(4-(1-(3-chlorophenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [458] 6-(4-(1-(3-chlorophenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [459] 4-(4-(1-(3-chlorophenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [460] 6-(4-(1-(4-chlorophenyl)-3-(methylamino)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [461] 6-(4-(1-(4-chlorophenyl)-3-(methylamino)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [462] 4-(4-(1-(4-chlorophenyl)-3-(methylamino)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [463] (S)-8-methoxy-1-methyl-4-(4-(3-(methylamino)-1-phenylpropoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [464] 1-methyl-4-(4-(3-(methylamino)-1-(5-methylthiophen-2H)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [465] 9-methyl-6-(4-(3-(methylamino)-1-(5-methylthiophen-2H)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [466] 8-methoxy-1-methyl-4-(4-(3-(methylamino)-1-(5-methylthiophen-2H)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [467] 8-methoxy-1-methyl-4-(4-(3-(methylamino)-1-(thiophen-311)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [468] 1-methyl-4-(4-(3-(methylamino)-1-(thiophen-3-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [469] 9-methyl-6-(4-(3-(methylamino)-1-(thiophen-3-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [470] (S)-4-(3-fluoro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [471] (S)-4-(3-fluoro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [472] (S)-6-(3-fluoro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [473] (S)-6-(2-fluoro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [474] (S)-4-(2-fluoro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-8-methoxy-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [475] (S)-4-(2-fluoro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [476] (S)-8-methoxy-1-methyl-4-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [477] (S)-1-methyl-4-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [478] (S)-9-methyl-6-(2-methyl-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [479] (S)-6-(3-chloro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [480] (S)-6-(3-chloro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [481] (S)-4-(3-chloro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [482] (S)-6-(2-chloro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-2-methoxy-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [483] (S)-6-(2-chloro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-9-methyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [484] (S)-4-(2-chloro-4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [485] (S)-2-ethoxy-9-methyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one; [486] (S)-8-methoxy-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; [487] (S)-1-isopropyl-4-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-1,2,3,4-tetrahydro-5H-pyrido[4,3-e][1,4]diazepin-5-one; and [488] (S)-9-isopropyl-6-(4-(3-(methylamino)-1-(thiophen-2-yl)propoxy)benzyl)-6,7,8,9-tetrahydro-5H-pyrimido[4,5-e][1,4]diazepin-5-one.

Metadata:
- Claim Count in Document: 44.0
- Percentile: 98.0
- Lexical Diversity: 1.88235
- Patent Class: 514.0
- Transitional Phrase Type: none
- Component Type: 0
- Foreign Priority: True
- Related Applications: ['14820711', '12680353', '12485108', '13910349', '11828457']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.7924769667867286
- 35 USC 102 Novelty (BERT): 0.5387007464282353
- Combined Prediction Score: 0.7670993447508794
- Mean Citation Score: 342.51614000000006
- Max Citation Score: 362.67856
- Similarity Product: 285.03495904088976

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 1

Dataset: test