Compound ID |
Compound Name |
Compound Formula |
CP0124222
|
(2S,3R)-3-methyl-1-N-[8-(1,1,1-trifluoro-2-methylpropan-2-yl)-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C20H23F3N6O2S
|
1
|
1 |
IC50 = 4 nM
|
|
|
CP0144577
|
(2S,3R)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide
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|
C20H26N6O2S
|
1
|
1 |
IC50 = 4 nM
|
|
|
CP0176371
|
(2S)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-2-methylpyrrolidine-1,2-dicarboxamide
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|
C20H26N6O2S
|
1
|
1 |
IC50 = 4 nM
|
|
|
CP0120405
|
(2S,3R)-3-methyl-1-N-[7-(1,1,1-trifluoro-2-methylpropan-2-yl)-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C19H22F3N5O2S2
|
1
|
1 |
IC50 = 5 nM
|
|
|
CP0014715
|
US9260439, 213
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|
C21H28N8O3
|
1
|
1 |
IC50 = 5 nM
|
|
|
CP0055472
|
(2S)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)pyrrolidine-1,2-dicarboxamide
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|
C19H24N6O2S
|
1
|
1 |
IC50 = 6 nM
|
|
|
CP0014684
|
US9260439, 194
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|
C24H34N8O3
|
1
|
1 |
IC50 = 6.8 nM
|
|
|
CP0014552
|
US9260439, 262
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|
C23H32N8O2
|
1
|
1 |
IC50 = 6.9 nM
|
|
|
CP0095462
|
(2S,3R)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide
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|
C19H25N5O2S2
|
1
|
1 |
IC50 = 10 nM
|
|
|
CP0099118
|
(2S,3S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-3-methylpyrrolidine-1,2-dicarboxamide
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|
C19H25N5O2S2
|
1
|
1 |
IC50 = 10 nM
|
|
|
CP0176375
|
(1S,5R)-2-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-2-azabicyclo[3.1.0]hexane-1,2-dicarboxamide
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|
C19H23N5O2S2
|
1
|
1 |
IC50 = 11 nM
|
|
|
CP0099116
|
(1S,5R)-2-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-2-azabicyclo[3.1.0]hexane-1,2-dicarboxamide
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|
C20H24N6O2S
|
1
|
1 |
IC50 = 13 nM
|
|
|
CP0215337
|
(2S,3S)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-3-[(dimethylamino)methyl]pyrrolidine-1,2-dicarboxamide
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|
C22H31N7O2S
|
1
|
1 |
IC50 = 15 nM
|
|
|
CP0013602
|
(Scheme A): Preparation of 2,2-difluoroethyl (3S)-3-{[2′-amino-5-fluoro-2-(morpholin-4-yl)-4,5′-bipyrimidin-6-yl]amino}-3-(hydroxymethyl)pyrrolidine-1-carboxylate
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|
C20H25F3N8O4
|
1
|
1 |
IC50 = 18 nM
|
|
|
CP0055470
|
(2S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)pyrrolidine-1,2-dicarboxamide
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|
C18H23N5O2S2
|
1
|
1 |
IC50 = 19 nM
|
|
|
CP0055471
|
(2S,3S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-3-[(dimethylamino)methyl]pyrrolidine-1,2-dicarboxamide
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|
C21H30N6O2S2
|
1
|
1 |
IC50 = 25 nM
|
|
|
CP0099117
|
(2R)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-2-[(dimethylamino)methyl]pyrrolidine-1,2-dicarboxamide
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|
C22H31N7O2S
|
1
|
1 |
IC50 = 25 nM
|
|
|
CP0013339
|
US9260439, 10
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|
C23H33N9O2
|
1
|
1 |
IC50 = 25 nM
|
|
|
CP0013862
|
US9260439, 173
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|
C20H29N9O3S
|
1
|
1 |
IC50 = 27 nM
|
|
|
CP0059183
|
(2S)-1-N-(7-tert-butyl-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl)-2-methylpyrrolidine-1,2-dicarboxamide
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|
C19H25N5O2S2
|
1
|
1 |
IC50 = 28 nM
|
|
|
CP0013601
|
US9260439, 149
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|
C20H28N8O3S
|
1
|
1 |
IC50 = 34 nM
|
|
|
CP0015292
|
US9260439, 211
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|
C21H28N8O2
|
1
|
1 |
IC50 = 35 nM
|
|
|
CP0109038
|
(2S)-1-N-[5-(2-tert-butylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C18H24N6O2S
|
1
|
1 |
IC50 = 39 nM
|
|
|
CP0014085
|
US9758538, Example 24
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|
C22H32N8O4
|
1
|
1 |
IC50 = 46 nM
|
|
|
CP0013340
|
US9758538, Example 72
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|
C19H25FN8O4
|
1
|
1 |
IC50 = 47 nM
|
|
|
CP0014086
|
US9758538, Example 79
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|
C20H26F2N8O4
|
1
|
1 |
IC50 = 52 nM
|
|
|
CP0010990
|
US9260439, 275
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|
C23H32N8O3
|
1
|
1 |
IC50 = 53 nM
|
|
|
CP0107865
|
(2S)-1-N-[5-(2-tert-butylpyridin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C19H25N5O2S
|
1
|
1 |
IC50 = 61 nM
|
|
|
CP0015003
|
US9260439, 216
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|
C21H29N9O2
|
1
|
1 |
IC50 = 73 nM
|
|
|
CP0008405
|
(2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C19H22F3N5O2S
|
2
|
1 |
IC50 = 74 nM
|
|
|
2 |
IC50 = 200 nM
|
|
|
CP0010991
|
US9758538, Example 34
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|
C19H26N8O4
|
1
|
1 |
IC50 = 91 nM
|
|
|
CP0102057
|
(2S)-1-N-[4-methyl-5-(2-propan-2-ylpyrimidin-4-yl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C17H22N6O2S
|
1
|
1 |
IC50 = 100 nM
|
|
|
CP0013863
|
US9758538, Example 40
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|
C22H32N8O3
|
1
|
1 |
IC50 = 110 nM
|
|
|
CP0047685
|
(2S)-1-N-[4-methyl-5-(4-pyrazol-1-ylphenyl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C19H20N6O2S
|
1
|
1 |
IC50 = 130 nM
|
|
|
CP0014723
|
US9260439, 38
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|
C19H27N9O3S
|
1
|
1 |
IC50 = 130 nM
|
|
|
CP0157490
|
(2S)-1-N-[5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C18H20F3N5O2S
|
1
|
1 |
IC50 = 140 nM
|
|
|
CP0102055
|
(2S)-1-N-[4-methyl-5-[2-(1-methylcyclopropyl)pyrimidin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C18H22N6O2S
|
1
|
1 |
IC50 = 150 nM
|
|
|
CP0107860
|
(2S)-1-N-[5-[2-(diethylamino)pyrimidin-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C18H25N7O2S
|
1
|
1 |
IC50 = 170 nM
|
|
|
CP0124221
|
(2S)-1-N-[7-(cyclopropylmethyl)-4,5-dihydro-[1,3]thiazolo[5,4-e][1,3]benzothiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C18H21N5O2S2
|
1
|
1 |
IC50 = 190 nM
|
|
|
CP0054682
|
(2S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C17H23N5O2S2
|
1
|
1 |
IC50 = 200 nM
|
|
|
CP0419316
|
1-[(3S)-3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]oxypyrrolidin-1-yl]ethanone
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|
C22H23N3O4
|
1
|
1 |
IC50 = 210 nM
|
|
|
CP0116057
|
(2S)-1-N-[5-(2-tert-butylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]azetidine-1,2-dicarboxamide
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|
C17H22N6O2S
|
1
|
1 |
IC50 = 230 nM
|
|
|
CP0055473
|
(2S,4R)-1-N-(8-tert-butyl-4,5-dihydro-[1,3]thiazolo[4,5-h]quinazolin-2-yl)-4-(dimethylamino)pyrrolidine-1,2-dicarboxamide
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|
C21H29N7O2S
|
1
|
1 |
IC50 = 260 nM
|
|
|
CP0085980
|
tert-butyl (3S)-3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]oxypyrrolidine-1-carboxylate
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|
C25H29N3O5
|
1
|
1 |
IC50 = 262 nM
|
|
|
CP0051959
|
(2S)-1-N-[4-chloro-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C18H19ClF3N5O2S
|
1
|
1 |
IC50 = 340 nM
|
|
|
CP0057012
|
(2S)-1-N-[5-(2-cyclobutylpyrimidin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C18H22N6O2S
|
1
|
1 |
IC50 = 440 nM
|
|
|
CP0214687
|
1-[(3S)-3-[6-(6-methoxypyridin-3-yl)quinolin-4-yl]oxypyrrolidin-1-yl]propan-1-one
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|
C22H23N3O3
|
1
|
1 |
IC50 = 606 nM
|
|
|
CP0107861
|
(2S)-1-N-[5-[2-(1-cyanocyclopropyl)pyridin-4-yl]-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
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|
C19H20N6O2S
|
1
|
1 |
IC50 = 640 nM
|
|
|
CP0237222
|
1-[(3S)-3-[6-(6-methoxypyridin-3-yl)quinazolin-4-yl]oxypyrrolidin-1-yl]propan-1-one
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|
C21H22N4O3
|
1
|
1 |
IC50 = 1030 nM
|
|
|
CP0014685
|
US9758538, Example 35
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|
C21H30N8O3
|
1
|
1 |
IC50 = 1100 nM
|
|
|
CP0014553
|
US9758538, Example 33
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|
C18H26N8O4S
|
1
|
1 |
IC50 = 1300 nM
|
|
|
CP0345063
|
1-[4-[3-[6-(3,4-dimethoxyphenyl)quinazolin-4-yl]benzoyl]piperazin-1-yl]ethanone
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|
C29H28N4O4
|
1
|
1 |
IC50 = 1320 nM
|
|
|
CP0140106
|
2-methoxy-5-[4-[(3S)-1-propanoylpyrrolidin-3-yl]oxyquinazolin-6-yl]pyridine-3-carbonitrile
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|
C22H21N5O3
|
1
|
1 |
IC50 = 1380 nM
|
|
|
CP0068001
|
US8653092, 67
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|
C21H25F3N6O2
|
1
|
1 |
IC50 = 1670 nM
|
|
|
CP0140107
|
1-[(3R)-3-[7-(3,4-dimethoxyphenyl)quinoxalin-2-yl]oxypyrrolidin-1-yl]propan-1-one
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|
C23H25N3O4
|
1
|
1 |
IC50 = 1860 nM
|
|
|
CP0131435
|
1-[4-[3-[6-(6-methoxypyridin-3-yl)quinazolin-4-yl]benzoyl]piperazin-1-yl]ethanone
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|
C27H25N5O3
|
1
|
1 |
IC50 = 2120 nM
|
|
|
CP0330198
|
US8653092, 68
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|
C24H29F3N6O3
|
1
|
1 |
IC50 = 2150 nM
|
|
|
CP0140243
|
1-[(3S)-3-[[6-(6-methoxypyridin-3-yl)-1,5-naphthyridin-4-yl]oxy]pyrrolidin-1-yl]propan-1-one
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|
C21H22N4O3
|
1
|
1 |
IC50 = 2360 nM
|
|
|
CP0107863
|
N-[5-(2-tert-butylpyridin-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1-carboxamide
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|
C18H24N4OS
|
1
|
1 |
IC50 = 2500 nM
|
|
|
CP0066459
|
US8653092, 63
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|
C21H24F3N5O3
|
1
|
1 |
IC50 = 2600 nM
|
|
|
CP0140244
|
5-[4-[3-(4-acetylpiperazine-1-carbonyl)phenyl]quinazolin-6-yl]-2-methoxypyridine-3-carbonitrile
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|
C28H24N6O3
|
1
|
1 |
IC50 = 3440 nM
|
|
|
CP0068002
|
US8653092, 61
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|
C24H28F3N5O4
|
1
|
1 |
IC50 = 3550 nM
|
|
|
CP0102054
|
(2S)-1-N-[4-methyl-5-(6-propan-2-ylpyrimidin-4-yl)-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
Show/Hide
|
C17H22N6O2S
|
1
|
1 |
IC50 = 4600 nM
|
|
|
CP0303600
|
US8653092, 83
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|
C24H32N6O3
|
1
|
1 |
IC50 = 6190 nM
|
|
|
CP0043078
|
US8653092, 1
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|
C24H31N5O4
|
1
|
1 |
IC50 = 6490 nM
|
|
|
CP0067930
|
US8653092, 81
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|
C21H28N6O2
|
1
|
1 |
IC50 = 7410 nM
|
|
|
CP0249954
|
1-[4-[3-[6-(6-methoxypyridin-3-yl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]phenoxy]piperidin-1-yl]ethanone
Show/Hide
|
C26H29N5O3
|
1
|
1 |
IC50 = 9030 nM
|
|
|
CP0051973
|
(2S)-1-N-[5-(2-tert-butylpyridin-4-yl)-4-methyl-1,3-thiazol-2-yl]-2-N-methylpyrrolidine-1,2-dicarboxamide
Show/Hide
|
C20H27N5O2S
|
1
|
1 |
IC50 > 10000 nM
|
|
|
CP0231955
|
1-[(3S)-3-[6-(6-methoxypyridin-3-yl)cinnolin-4-yl]oxypyrrolidin-1-yl]propan-1-one
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|
C21H22N4O3
|
1
|
1 |
IC50 > 10000 nM
|
|
|
CP0067931
|
1-[4-[3-[6-(6-methoxypyridin-3-yl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]benzoyl]piperazin-1-yl]ethanone
Show/Hide
|
C26H28N6O3
|
1
|
1 |
IC50 > 10000 nM
|
|
|
CP0241717
|
1-[(3S)-3-[[6-(6-methoxypyridin-3-yl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]oxy]pyrrolidin-1-yl]propan-1-one
Show/Hide
|
C20H25N5O3
|
1
|
1 |
IC50 > 10000 nM
|
|
|