CN104761585A - Substituted aminopyrimidine working as inhibitor of EGFR epidermal growth factor receptor - Google Patents
Substituted aminopyrimidine working as inhibitor of EGFR epidermal growth factor receptor Download PDFInfo
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- CN104761585A CN104761585A CN201410448325.6A CN201410448325A CN104761585A CN 104761585 A CN104761585 A CN 104761585A CN 201410448325 A CN201410448325 A CN 201410448325A CN 104761585 A CN104761585 A CN 104761585A
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Abstract
Description
No | Structure | Measure 1, single mutant, IC 50 (nM) | Measure 2, double mutant, IC 50 (nM) | Measure 3, wild-type, IC 50 (nM) |
Embodiment 42 | (E)-N-(5-{ [the chloro-4-of 5-(1H-indol-3-yl) pyrimidine-2-base] amino }-2-[4-(dimethylin) butyl-2-alkene-2-base]-4-p-methoxy-phenyl) acrylamide hydrochloride | 3.6 | 4.1 | 7.4 |
Embodiment 43 | N-(5-((the chloro-4-of 5-(1H-3-indyl)-2-pyrimidyl) is amino)-2-((2-dimethylin) ethyl) alkylsulfonyl)-4-p-methoxy-phenyl) acrylamide | 9.1 | 5.3 | 135.8 |
Embodiment 9 | N-(5-((the chloro-4-of 5-(1H-3-indyl)-2-pyrimidyl) is amino)-2-(2-(dimethylin)-N-methyl vinyl amido)-4-p-methoxy-phenyl) acrylamide | 1.1 | 1.6 | 3.2 |
Embodiment 45 | (E)-N-(5{ [4-(1H-indol-3-yl) pyrimidine-2-base] amino }-2-[4-(dimethylin) butyl-2-alkene-2-base]-4-p-methoxy-phenyl) acrylamide hydrochloride | 5.3 | 3.3 | 11 |
Embodiment 46 | (E)-N-(5{ [4-(1H-indol-3-yl) pyrimidine-2-base] amino }-2-[(E)-4-(dimethylin) butyl-2-alkene-2-base]-4-p-methoxy-phenyl)-4-(dimethylin) butyl-2-alkene amide hydrochloride | 14.9 | 9.7 | 99.4 |
Embodiment 47 | (E)-N-(2-[4-(dimethylin) butyl-2-alkene-2-base]-4-methoxyl group-5-{ [4-(pyrazoles [1,5-a] pyridin-3-yl) pyrimidine-2-base] amino } phenyl) acrylamide hydrochloride | 32 | 5.7 | 79 |
Embodiment 48 | (E)-N-(2-[4-(dimethylin) butyl-2-alkene-2-base]-4-methoxyl group-5-{ [4-(1-Methyl-1H-indole-3-base) pyrimidine-2-base] amino } phenyl) acrylamide hydrochloride | 13 | 2.5 | 34 |
Embodiment 49 | N-((5-((4-(1H-3-indoles)-2-pyrimidine) is amino)-2-(2-(dimethylin)-N-methyl vinyl amido)-4-p-methoxy-phenyl) acrylamide | 5 | 3.2 | 11 |
Embodiment 8 | N-(2-(2-(dimethylin)-N-methyl vinyl amido)-4-methoxyl group-5-((4-(1-methyl isophthalic acid H-3-indoles)-2-pyrimidine) is amino) phenyl) acrylamide | 25 | 4.5 | 64 |
Embodiment 50 | N-(2-(2-(dimethylin)-N-methyl vinyl amido)-4-methoxyl group-5-((4-(pyrazolo [1,5]-3-pyridyl)-2-pyrimidine) is amino) phenyl) acrylamide | 62.3 | 10.8 | 294.0 |
Embodiment 44 | N-(5-((the chloro-4-of 5-(1H-3-indyl)-2-pyrimidyl) is amino)-2-((2-dimethylin) ethyl) sulfinyl)-4-p-methoxy-phenyl) acrylamide | 4.1 | 4.9 | 10.1 |
Claims (24)
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CN104761544A (en) | 2015-07-08 |
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