JP2013545749A - 複素環化合物及びその使用 - Google Patents

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Publication number

JP2013545749A

JP2013545749A JP2013538894A JP2013538894A JP2013545749A JP 2013545749 A JP2013545749 A JP 2013545749A JP 2013538894 A JP2013538894 A JP 2013538894A JP 2013538894 A JP2013538894 A JP 2013538894A JP 2013545749 A JP2013545749 A JP 2013545749A

Authority

JP

Japan

Prior art keywords

alkyl

compound

heteroaryl

aryl

heterocycloalkyl

Prior art date

2010-11-10

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.)

Pending

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• 150000002391 heterocyclic compounds Chemical class 0.000 title 1
• 150000001875 compounds Chemical class 0.000 claims abstract description 316
• 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims abstract description 102
• 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims abstract description 102
• 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 67
• 238000000034 method Methods 0.000 claims abstract description 52
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 45
• 238000011282 treatment Methods 0.000 claims abstract description 15
• -1 heterocycloalkyloxy Chemical class 0.000 claims description 418
• 125000000217 alkyl group Chemical group 0.000 claims description 265
• 125000001072 heteroaryl group Chemical group 0.000 claims description 209
• 125000003118 aryl group Chemical group 0.000 claims description 186
• 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 177
• 229910052757 nitrogen Inorganic materials 0.000 claims description 169
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 156
• 229910052739 hydrogen Inorganic materials 0.000 claims description 142
• 239000001257 hydrogen Substances 0.000 claims description 142
• 125000005843 halogen group Chemical group 0.000 claims description 130
• 125000004404 heteroalkyl group Chemical group 0.000 claims description 117
• XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 108
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 107
• 125000003710 aryl alkyl group Chemical group 0.000 claims description 100
• 125000003342 alkenyl group Chemical group 0.000 claims description 98
• 125000000304 alkynyl group Chemical group 0.000 claims description 96
• 125000001424 substituent group Chemical group 0.000 claims description 92
• 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 89
• PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims description 87
• 125000003545 alkoxy group Chemical group 0.000 claims description 85
• 150000001408 amides Chemical class 0.000 claims description 77
• 125000004423 acyloxy group Chemical group 0.000 claims description 76
• 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 73
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 73
• XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 69
• 125000002252 acyl group Chemical group 0.000 claims description 64
• 229910019142 PO4 Inorganic materials 0.000 claims description 61
• 239000010452 phosphate Substances 0.000 claims description 60
• BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims description 59
• 239000004202 carbamide Substances 0.000 claims description 59
• NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 59
• CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 56
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 55
• QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 42
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 39
• 229910052721 tungsten Inorganic materials 0.000 claims description 39
• 125000001188 haloalkyl group Chemical group 0.000 claims description 38
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• 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 29
• 108091007960 PI3Ks Proteins 0.000 claims description 28
• 125000002950 monocyclic group Chemical group 0.000 claims description 28
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 27
• 125000002947 alkylene group Chemical group 0.000 claims description 24
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• 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims description 22
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• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 14
• 239000000546 pharmaceutical excipient Substances 0.000 claims description 14
• GTVCVBGHHUYLMO-UHFFFAOYSA-N trithiazetidine 1,1,2-trioxide Chemical compound S1(=O)(=O)NSS1=O GTVCVBGHHUYLMO-UHFFFAOYSA-N 0.000 claims description 12
• KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 claims description 10
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• 125000004474 heteroalkylene group Chemical group 0.000 claims description 9
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 9
• VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims description 7
• 239000005977 Ethylene Substances 0.000 claims description 7
• OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims description 7
• 125000001153 fluoro group Chemical group F* 0.000 claims description 7
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• LOTBYPQQWICYBB-UHFFFAOYSA-N methyl n-hexyl-n-[2-(hexylamino)ethyl]carbamate Chemical compound CCCCCCNCCN(C(=O)OC)CCCCCC LOTBYPQQWICYBB-UHFFFAOYSA-N 0.000 claims description 4
• 229940124597 therapeutic agent Drugs 0.000 claims description 4
• OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical compound C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 claims description 3
• CDGFEINVQHEUQV-UHFFFAOYSA-N [1,3]thiazolo[5,4-d]pyrimidine Chemical compound N1=CN=C2SC=NC2=C1 CDGFEINVQHEUQV-UHFFFAOYSA-N 0.000 claims description 2
• VTVRXITWWZGKHV-UHFFFAOYSA-N imidazo[1,2-b]pyridazine Chemical compound N1=CC=CC2=NC=CN21 VTVRXITWWZGKHV-UHFFFAOYSA-N 0.000 claims description 2
• LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical compound N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 claims description 2
• BWESROVQGZSBRX-UHFFFAOYSA-N pyrido[3,2-d]pyrimidine Chemical compound C1=NC=NC2=CC=CN=C21 BWESROVQGZSBRX-UHFFFAOYSA-N 0.000 claims description 2
• JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims description 2
• JKZWPSHYNAEPAA-UHFFFAOYSA-N cyanocarbamic acid Chemical compound OC(=O)NC#N JKZWPSHYNAEPAA-UHFFFAOYSA-N 0.000 claims 1
• 125000004475 heteroaralkyl group Chemical group 0.000 claims 1
• 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
• 201000010099 disease Diseases 0.000 abstract description 23
• 230000000694 effects Effects 0.000 abstract description 17
• 108091000080 Phosphotransferase Proteins 0.000 abstract description 15
• 102000020233 phosphotransferase Human genes 0.000 abstract description 15
• 150000002431 hydrogen Chemical class 0.000 description 97
• 239000000203 mixture Substances 0.000 description 78
• 125000005842 heteroatom Chemical group 0.000 description 53
• 235000021317 phosphate Nutrition 0.000 description 52
• 125000000623 heterocyclic group Chemical group 0.000 description 44
• 229910052799 carbon Inorganic materials 0.000 description 41
• 125000004432 carbon atom Chemical group C* 0.000 description 39
• 229940002612 prodrug Drugs 0.000 description 32
• 239000000651 prodrug Substances 0.000 description 32
• 150000003839 salts Chemical class 0.000 description 30
• 229910052760 oxygen Inorganic materials 0.000 description 29
• 150000003254 radicals Chemical class 0.000 description 27
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 26
• 125000006413 ring segment Chemical group 0.000 description 26
• 125000004429 atom Chemical group 0.000 description 25
• 125000003386 piperidinyl group Chemical group 0.000 description 25
• 229910052717 sulfur Inorganic materials 0.000 description 25
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 24
• 125000002757 morpholinyl group Chemical group 0.000 description 24
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 23
• 125000004193 piperazinyl group Chemical group 0.000 description 23
• 125000000168 pyrrolyl group Chemical group 0.000 description 23
• 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 22
• 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 22
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• 125000004452 carbocyclyl group Chemical group 0.000 description 21
• 239000001301 oxygen Substances 0.000 description 21
• 125000000719 pyrrolidinyl group Chemical group 0.000 description 20
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• 125000002883 imidazolyl group Chemical group 0.000 description 18
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• 125000000335 thiazolyl group Chemical group 0.000 description 18
• 125000001309 chloro group Chemical group Cl* 0.000 description 17
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