JP2012532170A5 - - Google Patents

Info

Publication number

JP2012532170A5

JP2012532170A5 JP2012518822A JP2012518822A JP2012532170A5 JP 2012532170 A5 JP2012532170 A5 JP 2012532170A5 JP 2012518822 A JP2012518822 A JP 2012518822A JP 2012518822 A JP2012518822 A JP 2012518822A JP 2012532170 A5 JP2012532170 A5 JP 2012532170A5

Authority

JP

Japan

Prior art keywords

alkylamino

group

alkyl

alkoxy

mono

Prior art date

2010-07-07

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.)

Granted

Links

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• 150000001875 compounds Chemical class 0.000 claims description 139
• -1 bromo, difluoromethyl Chemical group 0.000 claims description 90
• 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 59
• 125000001153 fluoro group Chemical group F* 0.000 claims description 56
• 238000000034 method Methods 0.000 claims description 54
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 51
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 50
• 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 46
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 45
• 229910052739 hydrogen Inorganic materials 0.000 claims description 42
• 239000001257 hydrogen Substances 0.000 claims description 40
• 125000001424 substituent group Chemical group 0.000 claims description 39
• 206010028980 Neoplasm Diseases 0.000 claims description 37
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 31
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 26
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 25
• 201000011510 cancer Diseases 0.000 claims description 25
• 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 25
• 125000004043 oxo group Chemical group O=* 0.000 claims description 23
• 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 22
• 125000001309 chloro group Chemical group Cl* 0.000 claims description 21
• 239000008194 pharmaceutical composition Substances 0.000 claims description 20
• 150000003839 salts Chemical class 0.000 claims description 20
• 239000003814 drug Substances 0.000 claims description 19
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 19
• 230000002062 proliferating effect Effects 0.000 claims description 19
• 238000011282 treatment Methods 0.000 claims description 18
• 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 16
• 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 16
• 125000003282 alkyl amino group Chemical group 0.000 claims description 16
• 239000002904 solvent Substances 0.000 claims description 16
• 201000010099 disease Diseases 0.000 claims description 14
• 125000001072 heteroaryl group Chemical group 0.000 claims description 14
• 150000002431 hydrogen Chemical class 0.000 claims description 14
• 229910052757 nitrogen Inorganic materials 0.000 claims description 14
• 239000002253 acid Substances 0.000 claims description 12
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
• 238000002360 preparation method Methods 0.000 claims description 12
• 239000012453 solvate Substances 0.000 claims description 12
• 229940124597 therapeutic agent Drugs 0.000 claims description 12
• 125000004076 pyridyl group Chemical group 0.000 claims description 10
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 9
• 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 9
• 125000000217 alkyl group Chemical group 0.000 claims description 8
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• 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 8
• 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
• HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 7
• 125000005842 heteroatom Chemical group 0.000 claims description 7
• 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims description 6
• 241000238366 Cephalopoda Species 0.000 claims description 6
• 125000003545 alkoxy group Chemical group 0.000 claims description 5
• 125000001246 bromo group Chemical group Br* 0.000 claims description 5
• 238000004587 chromatography analysis Methods 0.000 claims description 5
• 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 5
• 230000008569 process Effects 0.000 claims description 5
• 229910052717 sulfur Inorganic materials 0.000 claims description 5
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
• 229910052760 oxygen Inorganic materials 0.000 claims description 4
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• 150000004677 hydrates Chemical class 0.000 claims description 3
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• 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
• 210000004556 brain Anatomy 0.000 claims description 2
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 2
• 210000001035 gastrointestinal tract Anatomy 0.000 claims description 2
• 230000009401 metastasis Effects 0.000 claims description 2
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
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• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 13
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• 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
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• 239000000203 mixture Substances 0.000 description 66
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• QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 43
• 210000004027 cell Anatomy 0.000 description 42
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• XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 39
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• WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 34
• 239000000243 solution Substances 0.000 description 34
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• 238000003556 assay Methods 0.000 description 16
• KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 15
• 235000011054 acetic acid Nutrition 0.000 description 14
• BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 14
• 238000010992 reflux Methods 0.000 description 14
• FPGGTKZVZWFYPV-UHFFFAOYSA-M tetrabutylammonium fluoride Chemical compound [F-].CCCC[N+](CCCC)(CCCC)CCCC FPGGTKZVZWFYPV-UHFFFAOYSA-M 0.000 description 14
• 125000004356 hydroxy functional group Chemical group O* 0.000 description 13
• 108091000080 Phosphotransferase Proteins 0.000 description 12
• NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 12
• UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 12
• HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 12
• 239000004480 active ingredient Substances 0.000 description 12
• 102000020233 phosphotransferase Human genes 0.000 description 12
• DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 11
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• RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 10
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• JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 10
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• 238000012360 testing method Methods 0.000 description 10
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• 238000005481 NMR spectroscopy Methods 0.000 description 9
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• 239000003480 eluent Substances 0.000 description 9
• VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 9
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