JP2019006815A5 - - Google Patents

Info

Publication number

JP2019006815A5

JP2019006815A5 JP2018173770A JP2018173770A JP2019006815A5 JP 2019006815 A5 JP2019006815 A5 JP 2019006815A5 JP 2018173770 A JP2018173770 A JP 2018173770A JP 2018173770 A JP2018173770 A JP 2018173770A JP 2019006815 A5 JP2019006815 A5 JP 2019006815A5

Authority

JP

Japan

Prior art keywords

lipid

mole

peg

chol

liposome

Prior art date

2018-09-18

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
• -1 phosphatidyl choline lipid Chemical class 0.000 claims 19
• HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 18
• 229940123237 Taxane Drugs 0.000 claims 12
• 239000002502 liposome Substances 0.000 claims 12
• DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims 12
• 239000000203 mixture Substances 0.000 claims 11
• NRJAVPSFFCBXDT-HUESYALOSA-N 1,2-distearoyl-sn-glycero-3-phosphocholine Chemical group CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCCCC NRJAVPSFFCBXDT-HUESYALOSA-N 0.000 claims 10
• 235000012000 cholesterol Nutrition 0.000 claims 9
• 229930182558 Sterol Natural products 0.000 claims 8
• 150000003432 sterols Chemical class 0.000 claims 8
• 235000003702 sterols Nutrition 0.000 claims 8
• 150000002632 lipids Chemical class 0.000 claims 7
• WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims 7
• KILNVBDSWZSGLL-KXQOOQHDSA-N 1,2-dihexadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCC KILNVBDSWZSGLL-KXQOOQHDSA-N 0.000 claims 6
• 229920001223 polyethylene glycol Polymers 0.000 claims 6
• 239000002202 Polyethylene glycol Substances 0.000 claims 5
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 5
• 239000000232 Lipid Bilayer Substances 0.000 claims 4
• 125000001589 carboacyl group Chemical group 0.000 claims 3
• SNKAWJBJQDLSFF-NVKMUCNASA-N 1,2-dioleoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/CCCCCCCC SNKAWJBJQDLSFF-NVKMUCNASA-N 0.000 claims 2
• LVNGJLRDBYCPGB-UHFFFAOYSA-N 1,2-distearoylphosphatidylethanolamine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(COP([O-])(=O)OCC[NH3+])OC(=O)CCCCCCCCCCCCCCCCC LVNGJLRDBYCPGB-UHFFFAOYSA-N 0.000 claims 2
• ATHVAWFAEPLPPQ-VRDBWYNSSA-N 1-stearoyl-2-oleoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/CCCCCCCC ATHVAWFAEPLPPQ-VRDBWYNSSA-N 0.000 claims 2
• ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 2
• 239000002253 acid Substances 0.000 claims 2
• 239000007864 aqueous solution Substances 0.000 claims 2
• 229960003668 docetaxel Drugs 0.000 claims 2
• 229940079593 drug Drugs 0.000 claims 2
• 239000003814 drug Substances 0.000 claims 2
• 238000003780 insertion Methods 0.000 claims 2
• 230000037431 insertion Effects 0.000 claims 2
• 150000003839 salts Chemical class 0.000 claims 2
• JCXZKUZXVQKENT-UHFFFAOYSA-N 2-(4-methylpiperazin-1-ium-1-yl)acetate Chemical compound CN1CCN(CC(O)=O)CC1 JCXZKUZXVQKENT-UHFFFAOYSA-N 0.000 claims 1
• VRDBIJCCXDEZJN-UHFFFAOYSA-N 2-piperidin-1-ylacetic acid Chemical compound OC(=O)CN1CCCCC1 VRDBIJCCXDEZJN-UHFFFAOYSA-N 0.000 claims 1
• JSHLMMUXJIDENZ-UHFFFAOYSA-N 3-(4-methylpiperazin-1-ium-1-yl)propanoate Chemical compound CN1CCN(CCC(O)=O)CC1 JSHLMMUXJIDENZ-UHFFFAOYSA-N 0.000 claims 1
• YUYHRSGXZZVNMS-UHFFFAOYSA-N 3-morpholin-4-ylpropanoic acid Chemical compound OC(=O)CCN1CCOCC1 YUYHRSGXZZVNMS-UHFFFAOYSA-N 0.000 claims 1
• LPDGWMLCUHULJF-UHFFFAOYSA-N 3-piperidin-1-ylpropanoic acid Chemical compound OC(=O)CCN1CCCCC1 LPDGWMLCUHULJF-UHFFFAOYSA-N 0.000 claims 1
• ATSKLAVSYMLSEX-UHFFFAOYSA-N 4-(4-methylpiperazin-1-ium-1-yl)butanoate Chemical compound CN1CCN(CCCC(O)=O)CC1 ATSKLAVSYMLSEX-UHFFFAOYSA-N 0.000 claims 1
• PNHMBKXVXNJADT-UHFFFAOYSA-N 4-morpholin-4-ium-4-ylbutanoate Chemical compound OC(=O)CCCN1CCOCC1 PNHMBKXVXNJADT-UHFFFAOYSA-N 0.000 claims 1
• BGAVZPPPWLEAKZ-UHFFFAOYSA-N 4-piperidin-1-ylbutanoic acid Chemical compound OC(=O)CCCN1CCCCC1 BGAVZPPPWLEAKZ-UHFFFAOYSA-N 0.000 claims 1
• AROMGYXEPCNUQL-UHFFFAOYSA-N 5-(4-methylpiperazin-1-ium-1-yl)pentanoate Chemical compound CN1CCN(CCCCC(O)=O)CC1 AROMGYXEPCNUQL-UHFFFAOYSA-N 0.000 claims 1
• BSVYXFWQDRWOFH-UHFFFAOYSA-N 5-morpholin-4-ylpentanoic acid Chemical compound OC(=O)CCCCN1CCOCC1 BSVYXFWQDRWOFH-UHFFFAOYSA-N 0.000 claims 1
• GZDFHIJNHHMENY-UHFFFAOYSA-N Dimethyl dicarbonate Chemical compound COC(=O)OC(=O)OC GZDFHIJNHHMENY-UHFFFAOYSA-N 0.000 claims 1
• VIWZVFVJPXTXPA-UHFFFAOYSA-N N-(2-Carboxymethyl)-morpholine Chemical compound OC(=O)CN1CCOCC1 VIWZVFVJPXTXPA-UHFFFAOYSA-N 0.000 claims 1
• 206010028980 Neoplasm Diseases 0.000 claims 1
• NQPDZGIKBAWPEJ-UHFFFAOYSA-N Valeric acid Natural products CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 claims 1
• BFNBIHQBYMNNAN-UHFFFAOYSA-N ammonium sulfate Chemical compound N.N.OS(O)(=O)=O BFNBIHQBYMNNAN-UHFFFAOYSA-N 0.000 claims 1
• 229910052921 ammonium sulfate Inorganic materials 0.000 claims 1
• 235000011130 ammonium sulphate Nutrition 0.000 claims 1
• 201000011510 cancer Diseases 0.000 claims 1
• 238000010438 heat treatment Methods 0.000 claims 1
• 150000008105 phosphatidylcholines Chemical class 0.000 claims 1