JP2016527275A5 - - Google Patents

Info

Publication number

JP2016527275A5

JP2016527275A5 JP2016531918A JP2016531918A JP2016527275A5 JP 2016527275 A5 JP2016527275 A5 JP 2016527275A5 JP 2016531918 A JP2016531918 A JP 2016531918A JP 2016531918 A JP2016531918 A JP 2016531918A JP 2016527275 A5 JP2016527275 A5 JP 2016527275A5

Authority

JP

Japan

Prior art keywords

theta

salt

aqueous solution

imatinib

crystalline

Prior art date

2014-07-31

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

• Espacenet
• Global Dossier
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• 150000003839 salts Chemical class 0.000 claims 24
• 239000007864 aqueous solution Substances 0.000 claims 23
• 238000000634 powder X-ray diffraction Methods 0.000 claims 20
• 239000005517 L01XE01 - Imatinib Substances 0.000 claims 18
• KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 18
• 229960002411 imatinib Drugs 0.000 claims 18
• 239000007788 liquid Substances 0.000 claims 7
• 229940112141 dry powder inhaler Drugs 0.000 claims 6
• 239000000243 solution Substances 0.000 claims 5
• TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 claims 4
• 241000124008 Mammalia Species 0.000 claims 4
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 4
• 239000000872 buffer Substances 0.000 claims 4
• 239000003795 chemical substances by application Substances 0.000 claims 4
• 239000000203 mixture Substances 0.000 claims 4
• 239000006199 nebulizer Substances 0.000 claims 4
• 239000000843 powder Substances 0.000 claims 4
• JHJLBTNAGRQEKS-UHFFFAOYSA-M sodium bromide Chemical compound [Na+].[Br-] JHJLBTNAGRQEKS-UHFFFAOYSA-M 0.000 claims 4
• 239000007979 citrate buffer Substances 0.000 claims 3
• 239000002245 particle Substances 0.000 claims 3
• VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical class OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 2
• 229910019142 PO4 Inorganic materials 0.000 claims 2
• NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
• 239000003963 antioxidant agent Substances 0.000 claims 2
• 239000002738 chelating agent Substances 0.000 claims 2
• 235000003599 food sweetener Nutrition 0.000 claims 2
• 229910017053 inorganic salt Inorganic materials 0.000 claims 2
• 210000004072 lung Anatomy 0.000 claims 2
• 229910001629 magnesium chloride Inorganic materials 0.000 claims 2
• NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 2
• 239000010452 phosphate Substances 0.000 claims 2
• 239000008363 phosphate buffer Substances 0.000 claims 2
• CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims 2
• 239000011780 sodium chloride Substances 0.000 claims 2
• 239000002904 solvent Substances 0.000 claims 2
• 239000004094 surface-active agent Substances 0.000 claims 2
• 239000003765 sweetening agent Substances 0.000 claims 2
• 239000000080 wetting agent Substances 0.000 claims 2
• QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
• GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
• UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims 1
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
• VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
• GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
• 229930195725 Mannitol Natural products 0.000 claims 1
• 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
• 229910001622 calcium bromide Inorganic materials 0.000 claims 1
• 239000001110 calcium chloride Substances 0.000 claims 1
• 229910001628 calcium chloride Inorganic materials 0.000 claims 1
• WGEFECGEFUFIQW-UHFFFAOYSA-L calcium dibromide Chemical compound [Ca+2].[Br-].[Br-] WGEFECGEFUFIQW-UHFFFAOYSA-L 0.000 claims 1
• 239000013078 crystal Substances 0.000 claims 1
• 230000008021 deposition Effects 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 239000010419 fine particle Substances 0.000 claims 1
• 239000008101 lactose Substances 0.000 claims 1
• OTCKOJUMXQWKQG-UHFFFAOYSA-L magnesium bromide Chemical compound [Mg+2].[Br-].[Br-] OTCKOJUMXQWKQG-UHFFFAOYSA-L 0.000 claims 1
• 229910001623 magnesium bromide Inorganic materials 0.000 claims 1
• 239000000594 mannitol Substances 0.000 claims 1
• 235000010355 mannitol Nutrition 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 239000012528 membrane Substances 0.000 claims 1
• 229940071648 metered dose inhaler Drugs 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• XGXNTJHZPBRBHJ-UHFFFAOYSA-N n-phenylpyrimidin-2-amine Chemical class N=1C=CC=NC=1NC1=CC=CC=C1 XGXNTJHZPBRBHJ-UHFFFAOYSA-N 0.000 claims 1
• 238000002663 nebulization Methods 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 150000003013 phosphoric acid derivatives Chemical class 0.000 claims 1
• 230000002685 pulmonary effect Effects 0.000 claims 1
• 230000000541 pulsatile effect Effects 0.000 claims 1
• 210000002345 respiratory system Anatomy 0.000 claims 1
• 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
• 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
• 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims 1