JP2016525600A5 - - Google Patents

Info

Publication number

JP2016525600A5

JP2016525600A5 JP2016526700A JP2016526700A JP2016525600A5 JP 2016525600 A5 JP2016525600 A5 JP 2016525600A5 JP 2016526700 A JP2016526700 A JP 2016526700A JP 2016526700 A JP2016526700 A JP 2016526700A JP 2016525600 A5 JP2016525600 A5 JP 2016525600A5

Authority

JP

Japan

Prior art keywords

cyclodextrin

ether

sulfoalkyl ether

composition

reaction

Prior art date

2014-07-16

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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• 238000000034 method Methods 0.000 claims 22
• 229920000858 Cyclodextrin Polymers 0.000 claims 17
• RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 13
• 239000001116 FEMA 4028 Substances 0.000 claims 12
• 229960004853 betadex Drugs 0.000 claims 12
• 125000004964 sulfoalkyl group Chemical group 0.000 claims 10
• HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 9
• 238000006243 chemical reaction Methods 0.000 claims 9
• HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims 9
• -1 alkyl sultone Chemical class 0.000 claims 7
• WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 claims 6
• 235000011175 beta-cyclodextrine Nutrition 0.000 claims 6
• 239000000203 mixture Substances 0.000 claims 6
• 239000000546 pharmaceutical excipient Substances 0.000 claims 5
• 238000006467 substitution reaction Methods 0.000 claims 5
• 230000004913 activation Effects 0.000 claims 4
• 239000008186 active pharmaceutical agent Substances 0.000 claims 4
• 239000002585 base Substances 0.000 claims 4
• WMFOQBRAJBCJND-UHFFFAOYSA-M Lithium hydroxide Chemical compound [Li+].[OH-] WMFOQBRAJBCJND-UHFFFAOYSA-M 0.000 claims 3
• KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims 3
• 229940097346 sulfobutylether-beta-cyclodextrin Drugs 0.000 claims 3
• NZAQRZWBQUIBSF-UHFFFAOYSA-N 4-(4-sulfobutoxy)butane-1-sulfonic acid Chemical compound OS(=O)(=O)CCCCOCCCCS(O)(=O)=O NZAQRZWBQUIBSF-UHFFFAOYSA-N 0.000 claims 2
• 238000012377 drug delivery Methods 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 229940124531 pharmaceutical excipient Drugs 0.000 claims 2
• 150000003839 salts Chemical group 0.000 claims 2
• 150000008053 sultones Chemical class 0.000 claims 2
• ITPDYQOUSLNIHG-UHFFFAOYSA-N Amiodarone hydrochloride Chemical compound [Cl-].CCCCC=1OC2=CC=CC=C2C=1C(=O)C1=CC(I)=C(OCC[NH+](CC)CC)C(I)=C1 ITPDYQOUSLNIHG-UHFFFAOYSA-N 0.000 claims 1
• CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 claims 1
• 150000008044 alkali metal hydroxides Chemical class 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 claims 1
• 238000005804 alkylation reaction Methods 0.000 claims 1
• 229960005260 amiodarone Drugs 0.000 claims 1
• 229960004372 aripiprazole Drugs 0.000 claims 1
• 238000010923 batch production Methods 0.000 claims 1
• BLMPQMFVWMYDKT-NZTKNTHTSA-N carfilzomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)[C@]1(C)OC1)NC(=O)CN1CCOCC1)CC1=CC=CC=C1 BLMPQMFVWMYDKT-NZTKNTHTSA-N 0.000 claims 1
• 229960002438 carfilzomib Drugs 0.000 claims 1
• 108010021331 carfilzomib Proteins 0.000 claims 1
• 239000013078 crystal Substances 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 231100000957 no side effect Toxicity 0.000 claims 1
• MHYFEEDKONKGEB-UHFFFAOYSA-N oxathiane 2,2-dioxide Chemical compound O=S1(=O)CCCCO1 MHYFEEDKONKGEB-UHFFFAOYSA-N 0.000 claims 1
• 230000008663 renal system process Effects 0.000 claims 1
• 239000012453 solvate Substances 0.000 claims 1
• 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 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 claims 1
• 229960004740 voriconazole Drugs 0.000 claims 1
• 229960000607 ziprasidone Drugs 0.000 claims 1
• MVWVFYHBGMAFLY-UHFFFAOYSA-N ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 claims 1