JP2012509983A5 - - Google Patents

Info

Publication number

JP2012509983A5

JP2012509983A5 JP2011538669A JP2011538669A JP2012509983A5 JP 2012509983 A5 JP2012509983 A5 JP 2012509983A5 JP 2011538669 A JP2011538669 A JP 2011538669A JP 2011538669 A JP2011538669 A JP 2011538669A JP 2012509983 A5 JP2012509983 A5 JP 2012509983A5

Authority

JP

Japan

Prior art keywords

poly

block

hydrophobic

hydrophilic

block copolymer

Prior art date

2009-11-24

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
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• 229920001400 block copolymer Polymers 0.000 claims 25
• 230000002209 hydrophobic effect Effects 0.000 claims 23
• 239000000693 micelle Substances 0.000 claims 17
• 229920001184 polypeptide Polymers 0.000 claims 13
• 108090000765 processed proteins & peptides Proteins 0.000 claims 13
• 102000004196 processed proteins & peptides Human genes 0.000 claims 13
• 229920001223 polyethylene glycol Polymers 0.000 claims 12
• 229920002125 Sokalan® Polymers 0.000 claims 10
• 229940079593 drug Drugs 0.000 claims 8
• 239000003814 drug Substances 0.000 claims 8
• 229920002873 Polyethylenimine Polymers 0.000 claims 7
• 239000000203 mixture Substances 0.000 claims 7
• KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 5
• NYEZZYQZRQDLEH-UHFFFAOYSA-N 2-ethyl-4,5-dihydro-1,3-oxazole Chemical compound CCC1=NCCO1 NYEZZYQZRQDLEH-UHFFFAOYSA-N 0.000 claims 5
• 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 5
• 229920000805 Polyaspartic acid Polymers 0.000 claims 5
• 229920001577 copolymer Polymers 0.000 claims 5
• 150000004676 glycans Chemical class 0.000 claims 5
• 229920002674 hyaluronan Polymers 0.000 claims 5
• 229960003160 hyaluronic acid Drugs 0.000 claims 5
• 108020004707 nucleic acids Proteins 0.000 claims 5
• 150000007523 nucleic acids Chemical class 0.000 claims 5
• 102000039446 nucleic acids Human genes 0.000 claims 5
• 229920001603 poly (alkyl acrylates) Polymers 0.000 claims 5
• 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 claims 5
• 229920002401 polyacrylamide Polymers 0.000 claims 5
• 229920002643 polyglutamic acid Polymers 0.000 claims 5
• 229920001451 polypropylene glycol Polymers 0.000 claims 5
• 229920001282 polysaccharide Polymers 0.000 claims 5
• 239000005017 polysaccharide Substances 0.000 claims 5
• 229920002451 polyvinyl alcohol Polymers 0.000 claims 5
• XLPJNCYCZORXHG-UHFFFAOYSA-N 1-morpholin-4-ylprop-2-en-1-one Chemical compound C=CC(=O)N1CCOCC1 XLPJNCYCZORXHG-UHFFFAOYSA-N 0.000 claims 4
• GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical group C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 claims 4
• 239000000654 additive Substances 0.000 claims 4
• 229920000359 diblock copolymer Polymers 0.000 claims 4
• 238000009472 formulation Methods 0.000 claims 4
• 238000000034 method Methods 0.000 claims 4
• 229920006030 multiblock copolymer Polymers 0.000 claims 4
• 229920001713 poly(ethylene-co-vinyl alcohol) Polymers 0.000 claims 4
• 229920000917 poly(propylene sulfide) Polymers 0.000 claims 4
• 239000000126 substance Substances 0.000 claims 4
• DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 3
• 230000000996 additive effect Effects 0.000 claims 3
• 239000003085 diluting agent Substances 0.000 claims 3
• 229910052708 sodium Inorganic materials 0.000 claims 3
• 239000011734 sodium Substances 0.000 claims 3
• HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 claims 2
• AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 2
• 210000004027 cell Anatomy 0.000 claims 2
• 239000003795 chemical substances by application Substances 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
• OQXNUCOGMMHHNA-UHFFFAOYSA-N 4-methyl-1,3,2-dioxathiolane 2,2-dioxide Chemical compound CC1COS(=O)(=O)O1 OQXNUCOGMMHHNA-UHFFFAOYSA-N 0.000 claims 1
• APKFDSVGJQXUKY-KKGHZKTASA-N Amphotericin-B Natural products O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1C=CC=CC=CC=CC=CC=CC=C[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 APKFDSVGJQXUKY-KKGHZKTASA-N 0.000 claims 1
• 108091023037 Aptamer Proteins 0.000 claims 1
• 229930105110 Cyclosporin A Natural products 0.000 claims 1
• PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 claims 1
• 108010036949 Cyclosporine Proteins 0.000 claims 1
• HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 1
• 108091034117 Oligonucleotide Proteins 0.000 claims 1
• 229930012538 Paclitaxel Natural products 0.000 claims 1
• 108020004459 Small interfering RNA Proteins 0.000 claims 1
• QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
• QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims 1
• QYKIQEUNHZKYBP-UHFFFAOYSA-N Vinyl ether Chemical compound C=COC=C QYKIQEUNHZKYBP-UHFFFAOYSA-N 0.000 claims 1
• -1 acyl hydrazone Chemical class 0.000 claims 1
• 229940009456 adriamycin Drugs 0.000 claims 1
• 150000001408 amides Chemical class 0.000 claims 1
• APKFDSVGJQXUKY-INPOYWNPSA-N amphotericin B 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/C=C/C=C/[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 APKFDSVGJQXUKY-INPOYWNPSA-N 0.000 claims 1
• 229960003942 amphotericin b Drugs 0.000 claims 1
• 150000008064 anhydrides Chemical class 0.000 claims 1
• 239000003242 anti bacterial agent Substances 0.000 claims 1
• 229940088710 antibiotic agent Drugs 0.000 claims 1
• 239000000427 antigen Substances 0.000 claims 1
• 108091007433 antigens Proteins 0.000 claims 1
• 102000036639 antigens Human genes 0.000 claims 1
• 239000002246 antineoplastic agent Substances 0.000 claims 1
• 239000007864 aqueous solution Substances 0.000 claims 1
• 230000003115 biocidal effect Effects 0.000 claims 1
• 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
• 229960001265 ciclosporin Drugs 0.000 claims 1
• 229940127089 cytotoxic agent Drugs 0.000 claims 1
• UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 1
• 229960003957 dexamethasone Drugs 0.000 claims 1
• 238000007865 diluting Methods 0.000 claims 1
• 210000001163 endosome Anatomy 0.000 claims 1
• 150000002148 esters Chemical class 0.000 claims 1
• 229920001038 ethylene copolymer Polymers 0.000 claims 1
• 229960005167 everolimus Drugs 0.000 claims 1
• 239000012634 fragment Substances 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 150000002905 orthoesters Chemical class 0.000 claims 1
• 229960001592 paclitaxel Drugs 0.000 claims 1
• 239000013612 plasmid Substances 0.000 claims 1
• 229920000962 poly(amidoamine) Polymers 0.000 claims 1
• ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 1
• 229960002930 sirolimus Drugs 0.000 claims 1
• QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 1
• 239000004055 small Interfering RNA Substances 0.000 claims 1
• 239000000243 solution Substances 0.000 claims 1
• 150000003457 sulfones Chemical class 0.000 claims 1
• 229960001967 tacrolimus Drugs 0.000 claims 1
• QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 claims 1
• RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
• 150000007970 thio esters Chemical class 0.000 claims 1