JP2013536853A5 - - Google Patents

Info

Publication number

JP2013536853A5

JP2013536853A5 JP2013527248A JP2013527248A JP2013536853A5 JP 2013536853 A5 JP2013536853 A5 JP 2013536853A5 JP 2013527248 A JP2013527248 A JP 2013527248A JP 2013527248 A JP2013527248 A JP 2013527248A JP 2013536853 A5 JP2013536853 A5 JP 2013536853A5

Authority

JP

Japan

Prior art keywords

compound

pharmaceutical composition

composition according

salt

disease

Prior art date

2011-08-31

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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• 150000001875 compounds Chemical class 0.000 claims 21
• 239000008194 pharmaceutical composition Substances 0.000 claims 20
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
• 201000010099 disease Diseases 0.000 claims 7
• 150000003839 salts Chemical class 0.000 claims 6
• 102000042838 JAK family Human genes 0.000 claims 5
• 108091082332 JAK family Proteins 0.000 claims 5
• 208000035475 disorder Diseases 0.000 claims 4
• 230000001404 mediated effect Effects 0.000 claims 4
• 239000000203 mixture Substances 0.000 claims 4
• 230000002062 proliferating effect Effects 0.000 claims 4
• DCRWIATZWHLIPN-QGZVFWFLSA-N (r)-(4-fluorophenyl)-[4-[(5-methyl-1h-pyrazol-3-yl)amino]quinazolin-2-yl]methanol Chemical compound N1C(C)=CC(NC=2C3=CC=CC=C3N=C(N=2)[C@H](O)C=2C=CC(F)=CC=2)=N1 DCRWIATZWHLIPN-QGZVFWFLSA-N 0.000 claims 3
• 230000000155 isotopic effect Effects 0.000 claims 3
• 239000000546 pharmaceutical excipient Substances 0.000 claims 3
• 239000000651 prodrug Substances 0.000 claims 3
• 229940002612 prodrug Drugs 0.000 claims 3
• 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 2
• 206010028980 Neoplasm Diseases 0.000 claims 2
• 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 2
• 201000011510 cancer Diseases 0.000 claims 2
• 239000003054 catalyst Substances 0.000 claims 2
• 208000027866 inflammatory disease Diseases 0.000 claims 2
• 208000032839 leukemia Diseases 0.000 claims 2
• 238000004519 manufacturing process Methods 0.000 claims 2
• 239000012453 solvate Substances 0.000 claims 2
• 208000024891 symptom Diseases 0.000 claims 2
• WDYGPMAMBXJESZ-SFHVURJKSA-N (2s)-1,1-bis(4-methoxyphenyl)-3-methylbutane-1,2-diamine Chemical compound C1=CC(OC)=CC=C1C(N)([C@@H](N)C(C)C)C1=CC=C(OC)C=C1 WDYGPMAMBXJESZ-SFHVURJKSA-N 0.000 claims 1
• DCRWIATZWHLIPN-UHFFFAOYSA-N (4-fluorophenyl)-[4-[(5-methyl-1h-pyrazol-3-yl)amino]quinazolin-2-yl]methanol Chemical compound N1C(C)=CC(NC=2C3=CC=CC=C3N=C(N=2)C(O)C=2C=CC(F)=CC=2)=N1 DCRWIATZWHLIPN-UHFFFAOYSA-N 0.000 claims 1
• OGWVFYOLYMSTEP-UHFFFAOYSA-N (4-fluorophenyl)-[4-[(5-methyl-1h-pyrazol-3-yl)amino]quinazolin-2-yl]methanone Chemical compound N1C(C)=CC(NC=2C3=CC=CC=C3N=C(N=2)C(=O)C=2C=CC(F)=CC=2)=N1 OGWVFYOLYMSTEP-UHFFFAOYSA-N 0.000 claims 1
• 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 group 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
• 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 1
• 108091000080 Phosphotransferase Proteins 0.000 claims 1
• 229920002565 Polyethylene Glycol 400 Polymers 0.000 claims 1
• 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 1
• 239000002775 capsule Substances 0.000 claims 1
• 230000004663 cell proliferation Effects 0.000 claims 1
• 239000002552 dosage form Substances 0.000 claims 1
• 230000000694 effects Effects 0.000 claims 1
• 238000003821 enantio-separation Methods 0.000 claims 1
• CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical group CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
• 230000002401 inhibitory effect Effects 0.000 claims 1
• 238000001990 intravenous administration Methods 0.000 claims 1
• 239000006207 intravenous dosage form Substances 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 239000006186 oral dosage form Substances 0.000 claims 1
• 102000020233 phosphotransferase Human genes 0.000 claims 1
• 230000002685 pulmonary effect Effects 0.000 claims 1
• 230000000241 respiratory effect Effects 0.000 claims 1
• 239000002904 solvent Substances 0.000 claims 1
• 238000011200 topical administration Methods 0.000 claims 1
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1