JP2006515363A5 - - Google Patents

Info

Publication number

JP2006515363A5

JP2006515363A5 JP2006500425A JP2006500425A JP2006515363A5 JP 2006515363 A5 JP2006515363 A5 JP 2006515363A5 JP 2006500425 A JP2006500425 A JP 2006500425A JP 2006500425 A JP2006500425 A JP 2006500425A JP 2006515363 A5 JP2006515363 A5 JP 2006515363A5

Authority

JP

Japan

Prior art keywords

complex

aprotinin

substance

brain barrier

blood brain

Prior art date

2004-01-05

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

• ZPNFWUPYTFPOJU-LPYSRVMUSA-N iniprol Chemical compound C([C@H]1C(=O)NCC(=O)NCC(=O)N[C@H]2CSSC[C@H]3C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(N[C@H](C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N[C@@H](CC=4C=CC=CC=4)C(=O)N[C@@H](CC=4C=CC(O)=CC=4)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC=4C=CC=CC=4)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC2=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CSSC[C@H](NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H]2N(CCC2)C(=O)[C@@H](N)CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N2[C@@H](CCC2)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)N3)C(=O)NCC(=O)NCC(=O)N[C@@H](C)C(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H](C(=O)N1)C(C)C)[C@@H](C)O)[C@@H](C)CC)=O)[C@@H](C)CC)C1=CC=C(O)C=C1 ZPNFWUPYTFPOJU-LPYSRVMUSA-N 0.000 claims 26
• 239000000126 substance Substances 0.000 claims 26
• 230000008499 blood brain barrier function Effects 0.000 claims 25
• 210000001218 blood-brain barrier Anatomy 0.000 claims 25
• 108010039627 Aprotinin Proteins 0.000 claims 11
• 229960004405 aprotinin Drugs 0.000 claims 11
• 208000012902 Nervous system disease Diseases 0.000 claims 8
• 208000025966 Neurological disease Diseases 0.000 claims 8
• 150000001413 amino acids Chemical class 0.000 claims 7
• 239000003814 drug Substances 0.000 claims 7
• 230000032258 transport Effects 0.000 claims 7
• 208000003174 Brain Neoplasms Diseases 0.000 claims 6
• 235000001014 amino acid Nutrition 0.000 claims 6
• 210000003169 central nervous system Anatomy 0.000 claims 6
• 201000010099 disease Diseases 0.000 claims 6
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
• 239000008194 pharmaceutical composition Substances 0.000 claims 5
• 230000001404 mediated effect Effects 0.000 claims 4
• 239000000546 pharmaceutical excipient Substances 0.000 claims 4
• 235000018102 proteins Nutrition 0.000 claims 4
• 102000004169 proteins and genes Human genes 0.000 claims 4
• 108090000623 proteins and genes Proteins 0.000 claims 4
• 230000031998 transcytosis Effects 0.000 claims 4
• 208000024827 Alzheimer disease Diseases 0.000 claims 3
• 208000023105 Huntington disease Diseases 0.000 claims 3
• 206010059282 Metastases to central nervous system Diseases 0.000 claims 3
• 208000008589 Obesity Diseases 0.000 claims 3
• 208000018737 Parkinson disease Diseases 0.000 claims 3
• 208000006011 Stroke Diseases 0.000 claims 3
• 239000002246 antineoplastic agent Substances 0.000 claims 3
• 206010015037 epilepsy Diseases 0.000 claims 3
• 238000004519 manufacturing process Methods 0.000 claims 3
• 235000020824 obesity Nutrition 0.000 claims 3
• 201000000980 schizophrenia Diseases 0.000 claims 3
• 108090000790 Enzymes Proteins 0.000 claims 2
• 102000004190 Enzymes Human genes 0.000 claims 2
• DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
• 108010043121 Green Fluorescent Proteins Proteins 0.000 claims 2
• 102000004144 Green Fluorescent Proteins Human genes 0.000 claims 2
• 239000003242 anti bacterial agent Substances 0.000 claims 2
• 230000001772 anti-angiogenic effect Effects 0.000 claims 2
• 229940088710 antibiotic agent Drugs 0.000 claims 2
• -1 antibodies Substances 0.000 claims 2
• 108010005774 beta-Galactosidase Proteins 0.000 claims 2
• 102000005936 beta-Galactosidase Human genes 0.000 claims 2
• 239000003795 chemical substances by application Substances 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 231100000599 cytotoxic agent Toxicity 0.000 claims 2
• 239000002619 cytotoxin Substances 0.000 claims 2
• 229940079593 drug Drugs 0.000 claims 2
• 239000005090 green fluorescent protein Substances 0.000 claims 2
• 102000004196 processed proteins & peptides Human genes 0.000 claims 2
• 108090000765 processed proteins & peptides Proteins 0.000 claims 2
• 230000002285 radioactive effect Effects 0.000 claims 2
• 108020003175 receptors Proteins 0.000 claims 2
• 102000005962 receptors Human genes 0.000 claims 2
• 238000001179 sorption measurement Methods 0.000 claims 2
• WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 1
• 239000004471 Glycine Substances 0.000 claims 1
• COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 1
• 229930012538 Paclitaxel Natural products 0.000 claims 1
• AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 1
• 239000004473 Threonine Substances 0.000 claims 1
• 230000004888 barrier function Effects 0.000 claims 1
• 208000015114 central nervous system disease Diseases 0.000 claims 1
• 239000012634 fragment Substances 0.000 claims 1
• 235000013922 glutamic acid Nutrition 0.000 claims 1
• 239000004220 glutamic acid Substances 0.000 claims 1
• 125000005647 linker group Chemical group 0.000 claims 1
• 229960001592 paclitaxel Drugs 0.000 claims 1
• COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 1
• 150000003839 salts Chemical class 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
• OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Chemical group OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
• 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 1