JP2008511637A5 - - Google Patents

Info

Publication number

JP2008511637A5

JP2008511637A5 JP2007530195A JP2007530195A JP2008511637A5 JP 2008511637 A5 JP2008511637 A5 JP 2008511637A5 JP 2007530195 A JP2007530195 A JP 2007530195A JP 2007530195 A JP2007530195 A JP 2007530195A JP 2008511637 A5 JP2008511637 A5 JP 2008511637A5

Authority

JP

Japan

Prior art keywords

lung

active agent

respirable

active

drug

Prior art date

2005-08-26

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

Links

• Espacenet
• Global Dossier
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• 239000000203 mixture Substances 0.000 claims description 24
• 210000004072 lung Anatomy 0.000 claims description 18
• 229940121375 antifungal agent Drugs 0.000 claims description 12
• 239000003429 antifungal agent Substances 0.000 claims description 12
• VHVPQPYKVGDNFY-DFMJLFEVSA-N 2-[(2r)-butan-2-yl]-4-[4-[4-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one Chemical compound O=C1N([C@H](C)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@@H]3O[C@](CN4N=CN=C4)(OC3)C=3C(=CC(Cl)=CC=3)Cl)=CC=2)C=C1 VHVPQPYKVGDNFY-DFMJLFEVSA-N 0.000 claims description 7
• 229960004130 itraconazole Drugs 0.000 claims description 7
• 229960003483 oxiconazole Drugs 0.000 claims description 7
• QRJJEGAJXVEBNE-MOHJPFBDSA-N oxiconazole Chemical compound ClC1=CC(Cl)=CC=C1CO\N=C(C=1C(=CC(Cl)=CC=1)Cl)\CN1C=NC=C1 QRJJEGAJXVEBNE-MOHJPFBDSA-N 0.000 claims description 7
• XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 claims description 6
• AFNXATANNDIXLG-SFHVURJKSA-N 1-[(2r)-2-[(4-chlorophenyl)methylsulfanyl]-2-(2,4-dichlorophenyl)ethyl]imidazole Chemical compound C1=CC(Cl)=CC=C1CS[C@H](C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 AFNXATANNDIXLG-SFHVURJKSA-N 0.000 claims description 6
• OCAPBUJLXMYKEJ-UHFFFAOYSA-N 1-[biphenyl-4-yl(phenyl)methyl]imidazole Chemical compound C1=NC=CN1C(C=1C=CC(=CC=1)C=1C=CC=CC=1)C1=CC=CC=C1 OCAPBUJLXMYKEJ-UHFFFAOYSA-N 0.000 claims description 6
• LEZWWPYKPKIXLL-UHFFFAOYSA-N 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole Chemical compound C1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 LEZWWPYKPKIXLL-UHFFFAOYSA-N 0.000 claims description 6
• BYBLEWFAAKGYCD-UHFFFAOYSA-N Miconazole Chemical compound ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 BYBLEWFAAKGYCD-UHFFFAOYSA-N 0.000 claims description 6
• 229960002206 bifonazole Drugs 0.000 claims description 6
• 229960004022 clotrimazole Drugs 0.000 claims description 6
• VNFPBHJOKIVQEB-UHFFFAOYSA-N clotrimazole Chemical compound ClC1=CC=CC=C1C(N1C=NC=C1)(C=1C=CC=CC=1)C1=CC=CC=C1 VNFPBHJOKIVQEB-UHFFFAOYSA-N 0.000 claims description 6
• 229960003913 econazole Drugs 0.000 claims description 6
• 229960004884 fluconazole Drugs 0.000 claims description 6
• RFHAOTPXVQNOHP-UHFFFAOYSA-N fluconazole Chemical compound C1=NC=NN1CC(C=1C(=CC(F)=CC=1)F)(O)CN1C=NC=N1 RFHAOTPXVQNOHP-UHFFFAOYSA-N 0.000 claims description 6
• 229960004413 flucytosine Drugs 0.000 claims description 6
• XRECTZIEBJDKEO-UHFFFAOYSA-N flucytosine Chemical compound NC1=NC(=O)NC=C1F XRECTZIEBJDKEO-UHFFFAOYSA-N 0.000 claims description 6
• 229960004125 ketoconazole Drugs 0.000 claims description 6
• 229960002509 miconazole Drugs 0.000 claims description 6
• 229960003255 natamycin Drugs 0.000 claims description 6
• NCXMLFZGDNKEPB-FFPOYIOWSA-N natamycin Chemical compound O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1/C=C/C=C/C=C/C=C/C[C@@H](C)OC(=O)/C=C/[C@H]2O[C@@H]2C[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 NCXMLFZGDNKEPB-FFPOYIOWSA-N 0.000 claims description 6
• 235000010298 natamycin Nutrition 0.000 claims description 6
• 239000004311 natamycin Substances 0.000 claims description 6
• 229960002607 sulconazole Drugs 0.000 claims description 6
• FUSNMLFNXJSCDI-UHFFFAOYSA-N tolnaftate Chemical compound C=1C=C2C=CC=CC2=CC=1OC(=S)N(C)C1=CC=CC(C)=C1 FUSNMLFNXJSCDI-UHFFFAOYSA-N 0.000 claims description 6
• 229960004880 tolnaftate Drugs 0.000 claims description 6
• 208000031888 Mycoses Diseases 0.000 claims description 4
• 239000002184 metal Chemical class 0.000 claims description 4
• 238000000034 method Methods 0.000 claims description 4
• 150000003839 salts Chemical class 0.000 claims description 4
• 239000013543 active substance Substances 0.000 claims 16
• 229940079593 drug Drugs 0.000 claims 12
• 239000003814 drug Substances 0.000 claims 12
• -1 rubconazole Chemical compound 0.000 claims 10
• 239000002245 particle Substances 0.000 claims 7
• BLSQLHNBWJLIBQ-OZXSUGGESA-N (2R,4S)-terconazole Chemical compound C1CN(C(C)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2N=CN=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 BLSQLHNBWJLIBQ-OZXSUGGESA-N 0.000 claims 5
• 239000003960 organic solvent Substances 0.000 claims 5
• 229960000580 terconazole Drugs 0.000 claims 5
• 239000007864 aqueous solution Substances 0.000 claims 4
• 239000000243 solution Substances 0.000 claims 4
• 238000004519 manufacturing process Methods 0.000 claims 3
• 239000008186 active pharmaceutical agent Substances 0.000 claims 2
• 239000012296 anti-solvent Substances 0.000 claims 2
• 150000004696 coordination complex Chemical class 0.000 claims 2
• 229940088679 drug related substance Drugs 0.000 claims 2
• 229910017053 inorganic salt Inorganic materials 0.000 claims 2
• 239000007788 liquid Substances 0.000 claims 2
• 238000004064 recycling Methods 0.000 claims 2
• 239000002002 slurry Substances 0.000 claims 2
• 239000002904 solvent Substances 0.000 claims 2
• 238000005507 spraying Methods 0.000 claims 2
• 239000003381 stabilizer Substances 0.000 claims 2
• 239000004480 active ingredient Substances 0.000 claims 1
• 239000007900 aqueous suspension Substances 0.000 claims 1
• 150000003851 azoles Chemical class 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 229960001589 posaconazole Drugs 0.000 claims 1
• RAGOYPUPXAKGKH-XAKZXMRKSA-N posaconazole Chemical compound O=C1N([C@H]([C@H](C)O)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@H]3C[C@@](CN4N=CN=C4)(OC3)C=3C(=CC(F)=CC=3)F)=CC=2)C=C1 RAGOYPUPXAKGKH-XAKZXMRKSA-N 0.000 claims 1
• 230000002685 pulmonary effect Effects 0.000 claims 1
• 230000000717 retained effect Effects 0.000 claims 1
• 208000024891 symptom Diseases 0.000 claims 1
• MQHLMHIZUIDKOO-OKZBNKHCSA-N (2R,6S)-2,6-dimethyl-4-[(2S)-2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl]morpholine Chemical compound C1=CC(C(C)(C)CC)=CC=C1C[C@H](C)CN1C[C@@H](C)O[C@@H](C)C1 MQHLMHIZUIDKOO-OKZBNKHCSA-N 0.000 description 1
• MPIPASJGOJYODL-SFHVURJKSA-N (R)-isoconazole Chemical compound ClC1=CC(Cl)=CC=C1[C@@H](OCC=1C(=CC=CC=1Cl)Cl)CN1C=NC=C1 MPIPASJGOJYODL-SFHVURJKSA-N 0.000 description 1
• ZCJYUTQZBAIHBS-UHFFFAOYSA-N 1-[2-(2,4-dichlorophenyl)-2-{[4-(phenylsulfanyl)benzyl]oxy}ethyl]imidazole Chemical compound ClC1=CC(Cl)=CC=C1C(OCC=1C=CC(SC=2C=CC=CC=2)=CC=1)CN1C=NC=C1 ZCJYUTQZBAIHBS-UHFFFAOYSA-N 0.000 description 1
• 229960003204 amorolfine Drugs 0.000 description 1
• 239000003085 diluting agent Substances 0.000 description 1
• 229960001274 fenticonazole Drugs 0.000 description 1
• 229960004849 isoconazole Drugs 0.000 description 1
• DOMXUEMWDBAQBQ-WEVVVXLNSA-N terbinafine Chemical compound C1=CC=C2C(CN(C\C=C\C#CC(C)(C)C)C)=CC=CC2=C1 DOMXUEMWDBAQBQ-WEVVVXLNSA-N 0.000 description 1
• 229960002722 terbinafine Drugs 0.000 description 1
• 229960004740 voriconazole Drugs 0.000 description 1
• BCEHBSKCWLPMDN-MGPLVRAMSA-N voriconazole Chemical compound C1([C@H](C)[C@](O)(CN2N=CN=C2)C=2C(=CC(F)=CC=2)F)=NC=NC=C1F BCEHBSKCWLPMDN-MGPLVRAMSA-N 0.000 description 1