TW202227411A - Myc家族原癌基因蛋白之調節劑 - Google Patents

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Publication number

TW202227411A

TW202227411A TW110131640A TW110131640A TW202227411A TW 202227411 A TW202227411 A TW 202227411A TW 110131640 A TW110131640 A TW 110131640A TW 110131640 A TW110131640 A TW 110131640A TW 202227411 A TW202227411 A TW 202227411A

Authority

TW

Taiwan

Prior art keywords

group

alkyl

compound

heterocyclyl

methyl

Prior art date

2020-08-26

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• 108091057508 Myc family Proteins 0.000 title abstract description 15
• 102000052575 Proto-Oncogene Human genes 0.000 title 1
• 108700020978 Proto-Oncogene Proteins 0.000 title 1
• 150000001875 compounds Chemical class 0.000 claims abstract description 280
• 239000000203 mixture Substances 0.000 claims abstract description 67
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 28
• 201000010099 disease Diseases 0.000 claims abstract description 25
• 206010028980 Neoplasm Diseases 0.000 claims abstract description 21
• 201000011510 cancer Diseases 0.000 claims abstract description 14
• 230000002062 proliferating effect Effects 0.000 claims abstract description 7
• 150000003839 salts Chemical class 0.000 claims description 213
• 125000000623 heterocyclic group Chemical group 0.000 claims description 206
• -1 -C(O)-heteroaryl Chemical group 0.000 claims description 170
• 125000000217 alkyl group Chemical group 0.000 claims description 169
• 125000005843 halogen group Chemical group 0.000 claims description 157
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 145
• 125000001424 substituent group Chemical group 0.000 claims description 98
• 150000001204 N-oxides Chemical class 0.000 claims description 92
• 125000001072 heteroaryl group Chemical group 0.000 claims description 89
• 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 72
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 67
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 64
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 61
• 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 61
• 229910052739 hydrogen Inorganic materials 0.000 claims description 57
• 125000004093 cyano group Chemical group *C#N 0.000 claims description 54
• 125000003545 alkoxy group Chemical group 0.000 claims description 51
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 41
• 229910052757 nitrogen Inorganic materials 0.000 claims description 41
• SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 39
• 229910052799 carbon Inorganic materials 0.000 claims description 37
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 37
• 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims description 37
• 229910052760 oxygen Inorganic materials 0.000 claims description 32
• 150000001602 bicycloalkyls Chemical group 0.000 claims description 30
• 229910052736 halogen Inorganic materials 0.000 claims description 29
• 150000002367 halogens Chemical class 0.000 claims description 29
• 229910052717 sulfur Inorganic materials 0.000 claims description 29
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 27
• 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 27
• 238000006467 substitution reaction Methods 0.000 claims description 25
• 125000003003 spiro group Chemical group 0.000 claims description 24
• 239000008194 pharmaceutical composition Substances 0.000 claims description 22
• 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 21
• QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 20
• 125000001153 fluoro group Chemical group F* 0.000 claims description 19
• 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 16
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 15
• 229910052731 fluorine Inorganic materials 0.000 claims description 14
• 239000000651 prodrug Substances 0.000 claims description 14
• 229940002612 prodrug Drugs 0.000 claims description 14
• 239000002253 acid Substances 0.000 claims description 12
• 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 12
• 238000002560 therapeutic procedure Methods 0.000 claims description 12
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 11
• 239000003112 inhibitor Substances 0.000 claims description 10
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• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 9
• 125000002950 monocyclic group Chemical group 0.000 claims description 9
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• DWRXFEITVBNRMK-UHFFFAOYSA-N Beta-D-1-Arabinofuranosylthymine Natural products O=C1NC(=O)C(C)=CN1C1C(O)C(O)C(CO)O1 DWRXFEITVBNRMK-UHFFFAOYSA-N 0.000 claims 1
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• 238000000034 method Methods 0.000 abstract description 79
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