JP2020517618A5 - - Google Patents

Info

Publication number

JP2020517618A5

JP2020517618A5 JP2019556647A JP2019556647A JP2020517618A5 JP 2020517618 A5 JP2020517618 A5 JP 2020517618A5 JP 2019556647 A JP2019556647 A JP 2019556647A JP 2019556647 A JP2019556647 A JP 2019556647A JP 2020517618 A5 JP2020517618 A5 JP 2020517618A5

Authority

JP

Japan

Prior art keywords

inhibitor

halo

alkyl

optionally substituted

independently

Prior art date

2018-04-20

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Withdrawn

Links

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• 125000005843 halogen group Chemical group 0.000 claims description 232
• 238000000034 method Methods 0.000 claims description 204
• 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 185
• -1 photemstin Chemical compound 0.000 claims description 160
• 125000000217 alkyl group Chemical group 0.000 claims description 139
• 125000005842 heteroatom Chemical group 0.000 claims description 115
• 229910052760 oxygen Inorganic materials 0.000 claims description 112
• 229910052717 sulfur Inorganic materials 0.000 claims description 112
• 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 93
• 125000003118 aryl group Chemical group 0.000 claims description 93
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• 101000877312 Homo sapiens Histone-lysine N-methyltransferase EHMT2 Proteins 0.000 claims description 91
• 229910052799 carbon Inorganic materials 0.000 claims description 91
• 125000004093 cyano group Chemical group *C#N 0.000 claims description 90
• 229910052739 hydrogen Inorganic materials 0.000 claims description 90
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 86
• 125000003545 alkoxy group Chemical group 0.000 claims description 81
• 125000004043 oxo group Chemical group O=* 0.000 claims description 80
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 65
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 65
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 59
• 206010028980 Neoplasm Diseases 0.000 claims description 57
• 229910052757 nitrogen Inorganic materials 0.000 claims description 56
• 150000003839 salts Chemical class 0.000 claims description 55
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• 150000001875 compounds Chemical class 0.000 claims description 52
• 229940124597 therapeutic agent Drugs 0.000 claims description 48
• 125000005647 linker group Chemical group 0.000 claims description 46
• 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 43
• GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims description 43
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 36
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• 125000004663 dialkyl amino group Chemical group 0.000 claims description 32
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• ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 7
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