JP2010235584A5 - - Google Patents

Info

Publication number

JP2010235584A5

JP2010235584A5 JP2010018324A JP2010018324A JP2010235584A5 JP 2010235584 A5 JP2010235584 A5 JP 2010235584A5 JP 2010018324 A JP2010018324 A JP 2010018324A JP 2010018324 A JP2010018324 A JP 2010018324A JP 2010235584 A5 JP2010235584 A5 JP 2010235584A5

Authority

JP

Japan

Prior art keywords

pharmaceutical formulation

formulation according

bioactive molecule

biodegradable polymer

group

Prior art date

2010-01-29

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
• Discuss

• 239000008194 pharmaceutical composition Substances 0.000 claims 16
• 230000000975 bioactive effect Effects 0.000 claims 10
• 229920002988 biodegradable polymer Polymers 0.000 claims 7
• 239000004621 biodegradable polymer Substances 0.000 claims 7
• NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 6
• 239000002202 Polyethylene glycol Substances 0.000 claims 4
• 229920001477 hydrophilic polymer Polymers 0.000 claims 4
• 229920001223 polyethylene glycol Polymers 0.000 claims 4
• 102000004877 Insulin Human genes 0.000 claims 3
• 108090001061 Insulin Proteins 0.000 claims 3
• 229920000954 Polyglycolide Polymers 0.000 claims 3
• 229920001577 copolymer Polymers 0.000 claims 3
• 229940125396 insulin Drugs 0.000 claims 3
• 229920000747 poly(lactic acid) Polymers 0.000 claims 3
• 239000004633 polyglycolic acid Substances 0.000 claims 3
• 239000004626 polylactic acid Substances 0.000 claims 3
• 229920001273 Polyhydroxy acid Polymers 0.000 claims 2
• 108010033394 biphalin Proteins 0.000 claims 2
• DESSEGDLRYOPTJ-VRANXALZSA-N biphalin Chemical compound C([C@H](N)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)NNC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=C(O)C=C1 DESSEGDLRYOPTJ-VRANXALZSA-N 0.000 claims 2
• 230000002209 hydrophobic effect Effects 0.000 claims 2
• 229920000642 polymer Polymers 0.000 claims 2
• 108090000623 proteins and genes Proteins 0.000 claims 2
• 101710169336 5'-deoxyadenosine deaminase Proteins 0.000 claims 1
• 102000055025 Adenosine deaminases Human genes 0.000 claims 1
• 108010024976 Asparaginase Proteins 0.000 claims 1
• 102000015790 Asparaginase Human genes 0.000 claims 1
• 102000011022 Chorionic Gonadotropin Human genes 0.000 claims 1
• 108010062540 Chorionic Gonadotropin Proteins 0.000 claims 1
• 101800000414 Corticotropin Proteins 0.000 claims 1
• 239000000055 Corticotropin-Releasing Hormone Substances 0.000 claims 1
• 102000009025 Endorphins Human genes 0.000 claims 1
• 108010049140 Endorphins Proteins 0.000 claims 1
• 108010092674 Enkephalins Proteins 0.000 claims 1
• 102000003951 Erythropoietin Human genes 0.000 claims 1
• 108090000394 Erythropoietin Proteins 0.000 claims 1
• 108060003199 Glucagon Proteins 0.000 claims 1
• 102400000321 Glucagon Human genes 0.000 claims 1
• 102000004269 Granulocyte Colony-Stimulating Factor Human genes 0.000 claims 1
• 108010017080 Granulocyte Colony-Stimulating Factor Proteins 0.000 claims 1
• 102000004457 Granulocyte-Macrophage Colony-Stimulating Factor Human genes 0.000 claims 1
• 108010017213 Granulocyte-Macrophage Colony-Stimulating Factor Proteins 0.000 claims 1
• 102000018997 Growth Hormone Human genes 0.000 claims 1
• 108010051696 Growth Hormone Proteins 0.000 claims 1
• HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims 1
• 108090000723 Insulin-Like Growth Factor I Proteins 0.000 claims 1
• 102000006992 Interferon-alpha Human genes 0.000 claims 1
• 108010047761 Interferon-alpha Proteins 0.000 claims 1
• 108090000467 Interferon-beta Proteins 0.000 claims 1
• 102000003996 Interferon-beta Human genes 0.000 claims 1
• 102000008070 Interferon-gamma Human genes 0.000 claims 1
• 108010074328 Interferon-gamma Proteins 0.000 claims 1
• 102000000589 Interleukin-1 Human genes 0.000 claims 1
• 108010002352 Interleukin-1 Proteins 0.000 claims 1
• 102000013462 Interleukin-12 Human genes 0.000 claims 1
• 108010065805 Interleukin-12 Proteins 0.000 claims 1
• 102000000588 Interleukin-2 Human genes 0.000 claims 1
• 108010002350 Interleukin-2 Proteins 0.000 claims 1
• 102000000646 Interleukin-3 Human genes 0.000 claims 1
• 108010002386 Interleukin-3 Proteins 0.000 claims 1
• URLZCHNOLZSCCA-VABKMULXSA-N Leu-enkephalin Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(O)=O)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)C1=CC=CC=C1 URLZCHNOLZSCCA-VABKMULXSA-N 0.000 claims 1
• 102000009151 Luteinizing Hormone Human genes 0.000 claims 1
• 108010073521 Luteinizing Hormone Proteins 0.000 claims 1
• 108091034117 Oligonucleotide Proteins 0.000 claims 1
• 102000003982 Parathyroid hormone Human genes 0.000 claims 1
• 108090000445 Parathyroid hormone Proteins 0.000 claims 1
• 229920002732 Polyanhydride Polymers 0.000 claims 1
• 229920001710 Polyorthoester Polymers 0.000 claims 1
• 102100027467 Pro-opiomelanocortin Human genes 0.000 claims 1
• 102000003946 Prolactin Human genes 0.000 claims 1
• 108010057464 Prolactin Proteins 0.000 claims 1
• 102000013275 Somatomedins Human genes 0.000 claims 1
• 102000005157 Somatostatin Human genes 0.000 claims 1
• 108010056088 Somatostatin Proteins 0.000 claims 1
• 102000007501 Thymosin Human genes 0.000 claims 1
• 108010046075 Thymosin Proteins 0.000 claims 1
• 102000011923 Thyrotropin Human genes 0.000 claims 1
• 108010061174 Thyrotropin Proteins 0.000 claims 1
• 102000002852 Vasopressins Human genes 0.000 claims 1
• 108010004977 Vasopressins Proteins 0.000 claims 1
• 239000000074 antisense oligonucleotide Substances 0.000 claims 1
• 238000012230 antisense oligonucleotides Methods 0.000 claims 1
• KBZOIRJILGZLEJ-LGYYRGKSSA-N argipressin Chemical compound C([C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@@H](C(N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N1)=O)N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C1=CC=CC=C1 KBZOIRJILGZLEJ-LGYYRGKSSA-N 0.000 claims 1
• 229960003272 asparaginase Drugs 0.000 claims 1
• DCXYFEDJOCDNAF-UHFFFAOYSA-M asparaginate Chemical compound [O-]C(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-M 0.000 claims 1
• 229940015047 chorionic gonadotropin Drugs 0.000 claims 1
• 238000013270 controlled release Methods 0.000 claims 1
• IDLFZVILOHSSID-OVLDLUHVSA-N corticotropin Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@@H](N)CO)C1=CC=C(O)C=C1 IDLFZVILOHSSID-OVLDLUHVSA-N 0.000 claims 1
• 229960000258 corticotropin Drugs 0.000 claims 1
• 229940105423 erythropoietin Drugs 0.000 claims 1
• 229940044627 gamma-interferon Drugs 0.000 claims 1
• MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 1
• 229960004666 glucagon Drugs 0.000 claims 1
• 150000004676 glycans Chemical class 0.000 claims 1
• 229960002897 heparin Drugs 0.000 claims 1
• 229920000669 heparin Polymers 0.000 claims 1
• 229940088597 hormone Drugs 0.000 claims 1
• 239000005556 hormone Substances 0.000 claims 1
• 230000002267 hypothalamic effect Effects 0.000 claims 1
• 229940117681 interleukin-12 Drugs 0.000 claims 1
• 229940076264 interleukin-3 Drugs 0.000 claims 1
• 239000003055 low molecular weight heparin Substances 0.000 claims 1
• 229940127215 low-molecular weight heparin Drugs 0.000 claims 1
• 229940040129 luteinizing hormone Drugs 0.000 claims 1
• 239000011859 microparticle Substances 0.000 claims 1
• 239000002105 nanoparticle Substances 0.000 claims 1
• 239000000199 parathyroid hormone Substances 0.000 claims 1
• 229960001319 parathyroid hormone Drugs 0.000 claims 1
• 229920001451 polypropylene glycol Polymers 0.000 claims 1
• 229920001282 polysaccharide Polymers 0.000 claims 1
• 239000005017 polysaccharide Substances 0.000 claims 1
• OXCMYAYHXIHQOA-UHFFFAOYSA-N potassium;[2-butyl-5-chloro-3-[[4-[2-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol Chemical compound [K+].CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C2=N[N-]N=N2)C=C1 OXCMYAYHXIHQOA-UHFFFAOYSA-N 0.000 claims 1
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• NHXLMOGPVYXJNR-ATOGVRKGSA-N somatostatin Chemical compound C([C@H]1C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N1)[C@@H](C)O)NC(=O)CNC(=O)[C@H](C)N)C(O)=O)=O)[C@H](O)C)C1=CC=CC=C1 NHXLMOGPVYXJNR-ATOGVRKGSA-N 0.000 claims 1
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• LCJVIYPJPCBWKS-NXPQJCNCSA-N thymosin Chemical compound SC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(C)C)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](C(C)C)C(=O)N[C@H](CO)C(=O)N[C@H](CO)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@H]([C@H](C)O)C(=O)N[C@H](C(C)C)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@H](C(C)C)C(=O)N[C@H](C(C)C)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@@H](C)C(=O)N[C@H](CCC(O)=O)C(O)=O LCJVIYPJPCBWKS-NXPQJCNCSA-N 0.000 claims 1
• 229960003726 vasopressin Drugs 0.000 claims 1