JP2006510571A5 - - Google Patents
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- JP2006510571A5 JP2006510571A5 JP2003573017A JP2003573017A JP2006510571A5 JP 2006510571 A5 JP2006510571 A5 JP 2006510571A5 JP 2003573017 A JP2003573017 A JP 2003573017A JP 2003573017 A JP2003573017 A JP 2003573017A JP 2006510571 A5 JP2006510571 A5 JP 2006510571A5
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- JP
- Japan
- Prior art keywords
- tyr
- ser
- lys
- peptide
- pro
- Prior art date
- 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
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- 150000001875 compounds Chemical class 0.000 claims 69
- 238000000034 method Methods 0.000 claims 55
- 108090000765 processed proteins & peptides Proteins 0.000 claims 32
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 28
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 28
- KDXKERNSBIXSRK-RXMQYKEDSA-N D-lysine Chemical compound NCCCC[C@@H](N)C(O)=O KDXKERNSBIXSRK-RXMQYKEDSA-N 0.000 claims 16
- OUYCCCASQSFEME-MRVPVSSYSA-N D-tyrosine Chemical compound OC(=O)[C@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-MRVPVSSYSA-N 0.000 claims 16
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 16
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 15
- MTCFGRXMJLQNBG-UWTATZPHSA-N D-Serine Chemical compound OC[C@@H](N)C(O)=O MTCFGRXMJLQNBG-UWTATZPHSA-N 0.000 claims 15
- DCXYFEDJOCDNAF-UWTATZPHSA-N D-Asparagine Chemical compound OC(=O)[C@H](N)CC(N)=O DCXYFEDJOCDNAF-UWTATZPHSA-N 0.000 claims 12
- ZDXPYRJPNDTMRX-GSVOUGTGSA-N D-glutamine Chemical compound OC(=O)[C@H](N)CCC(N)=O ZDXPYRJPNDTMRX-GSVOUGTGSA-N 0.000 claims 12
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 11
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 11
- CKLJMWTZIZZHCS-UHFFFAOYSA-N D-OH-Asp Natural products OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 claims 10
- CKLJMWTZIZZHCS-UWTATZPHSA-N D-aspartic acid Chemical compound OC(=O)[C@H](N)CC(O)=O CKLJMWTZIZZHCS-UWTATZPHSA-N 0.000 claims 10
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 10
- 229940127089 cytotoxic agent Drugs 0.000 claims 9
- 239000002254 cytotoxic agent Substances 0.000 claims 9
- WHUUTDBJXJRKMK-GSVOUGTGSA-N D-glutamic acid Chemical compound OC(=O)[C@H](N)CCC(O)=O WHUUTDBJXJRKMK-GSVOUGTGSA-N 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 210000004204 blood vessel Anatomy 0.000 claims 8
- 210000004027 cell Anatomy 0.000 claims 8
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- 125000006850 spacer group Chemical group 0.000 claims 7
- 230000008685 targeting Effects 0.000 claims 7
- 230000000975 bioactive effect Effects 0.000 claims 6
- 210000000265 leukocyte Anatomy 0.000 claims 6
- 108010051479 Bombesin Proteins 0.000 claims 5
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 5
- 108010056088 Somatostatin Proteins 0.000 claims 5
- 231100000599 cytotoxic agent Toxicity 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 claims 4
- 101800001288 Atrial natriuretic factor Proteins 0.000 claims 4
- 102400001282 Atrial natriuretic peptide Human genes 0.000 claims 4
- 101800001890 Atrial natriuretic peptide Proteins 0.000 claims 4
- 102000053028 CD36 Antigens Human genes 0.000 claims 4
- 108010045374 CD36 Antigens Proteins 0.000 claims 4
- 101710091342 Chemotactic peptide Proteins 0.000 claims 4
- 101800001982 Cholecystokinin Proteins 0.000 claims 4
- 102100025841 Cholecystokinin Human genes 0.000 claims 4
- 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 4
- 239000000579 Gonadotropin-Releasing Hormone Substances 0.000 claims 4
- 101000851058 Homo sapiens Neutrophil elastase Proteins 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 108090000723 Insulin-Like Growth Factor I Proteins 0.000 claims 4
- 102000014429 Insulin-like growth factor Human genes 0.000 claims 4
- 108010063738 Interleukins Proteins 0.000 claims 4
- 102000015696 Interleukins Human genes 0.000 claims 4
- 239000000637 Melanocyte-Stimulating Hormone Substances 0.000 claims 4
- 108010007013 Melanocyte-Stimulating Hormones Proteins 0.000 claims 4
- 108010035030 Platelet Membrane Glycoprotein IIb Proteins 0.000 claims 4
- 102000004211 Platelet factor 4 Human genes 0.000 claims 4
- 108090000778 Platelet factor 4 Proteins 0.000 claims 4
- 101000857870 Squalus acanthias Gonadoliberin Proteins 0.000 claims 4
- 108010003205 Vasoactive Intestinal Peptide Proteins 0.000 claims 4
- 102400000015 Vasoactive intestinal peptide Human genes 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- NSQLIUXCMFBZME-MPVJKSABSA-N carperitide Chemical compound C([C@H]1C(=O)NCC(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(O)=O)=O)[C@@H](C)CC)C1=CC=CC=C1 NSQLIUXCMFBZME-MPVJKSABSA-N 0.000 claims 4
- PRQROPMIIGLWRP-BZSNNMDCSA-N chemotactic peptide Chemical compound CSCC[C@H](NC=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 PRQROPMIIGLWRP-BZSNNMDCSA-N 0.000 claims 4
- 229940107137 cholecystokinin Drugs 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 231100000433 cytotoxic Toxicity 0.000 claims 4
- 230000001472 cytotoxic effect Effects 0.000 claims 4
- 239000000857 delta opiate receptor antagonist Substances 0.000 claims 4
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 claims 4
- XLXSAKCOAKORKW-AQJXLSMYSA-N gonadorelin Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 XLXSAKCOAKORKW-AQJXLSMYSA-N 0.000 claims 4
- 229940035638 gonadotropin-releasing hormone Drugs 0.000 claims 4
- -1 hSer Chemical compound 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 102000052502 human ELANE Human genes 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 229920001477 hydrophilic polymer Polymers 0.000 claims 4
- VBUWHHLIZKOSMS-RIWXPGAOSA-N invicorp Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)C(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=C(O)C=C1 VBUWHHLIZKOSMS-RIWXPGAOSA-N 0.000 claims 4
- 239000003591 leukocyte elastase inhibitor Substances 0.000 claims 4
- 230000000955 neuroendocrine Effects 0.000 claims 4
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- FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical compound C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 claims 4
- IZTQOLKUZKXIRV-YRVFCXMDSA-N sincalide Chemical compound C([C@@H](C(=O)N[C@@H](CCSC)C(=O)NCC(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](N)CC(O)=O)C1=CC=C(OS(O)(=O)=O)C=C1 IZTQOLKUZKXIRV-YRVFCXMDSA-N 0.000 claims 4
- 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 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
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- 102000013585 Bombesin Human genes 0.000 claims 3
- 102000005157 Somatostatin Human genes 0.000 claims 3
- 125000003277 amino group Chemical group 0.000 claims 3
- RWCCWEUUXYIKHB-UHFFFAOYSA-N benzophenone Chemical compound C=1C=CC=CC=1C(=O)C1=CC=CC=C1 RWCCWEUUXYIKHB-UHFFFAOYSA-N 0.000 claims 3
- 239000012965 benzophenone Substances 0.000 claims 3
- 230000004071 biological effect Effects 0.000 claims 3
- DNDCVAGJPBKION-DOPDSADYSA-N bombesin Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC=1NC2=CC=CC=C2C=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1NC(=O)CC1)C(C)C)C1=CN=CN1 DNDCVAGJPBKION-DOPDSADYSA-N 0.000 claims 3
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- ZJWGCWJEDARXKV-HWMGBOQISA-N (2s)-2,6-diaminohexanoic acid;(2s)-2-[[(2s)-2-[[(2s)-2-formamido-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoic acid Chemical group NCCCC[C@H](N)C(O)=O.CSCC[C@H](NC=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 ZJWGCWJEDARXKV-HWMGBOQISA-N 0.000 claims 2
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- DEQANNDTNATYII-OULOTJBUSA-N (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa Chemical compound C([C@@H](N)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC=2C3=CC=CC=C3NC=2)NC(=O)[C@H](CC=2C=CC=CC=2)NC1=O)C(=O)N[C@H](CO)[C@H](O)C)C1=CC=CC=C1 DEQANNDTNATYII-OULOTJBUSA-N 0.000 claims 2
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- OERILMBTPCSYNG-UHFFFAOYSA-N 6-amino-2-[[2-[[2-[(2-formamido-4-methylsulfanylbutanoyl)amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]hexanoic acid Chemical compound CSCCC(NC=O)C(=O)NC(CC(C)C)C(=O)NC(C(=O)NC(CCCCN)C(O)=O)CC1=CC=CC=C1 OERILMBTPCSYNG-UHFFFAOYSA-N 0.000 claims 2
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| KR20090009241A (ko) * | 2006-05-18 | 2009-01-22 | 니폰 가야꾸 가부시끼가이샤 | 포도필로톡신류의 고분자 결합체 |
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| ES2584840T3 (es) * | 2006-10-03 | 2016-09-29 | Nippon Kayaku Kabushiki Kaisha | Compuesto de un derivado de resorcinol con un polímero |
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| USRE46190E1 (en) | 2007-09-28 | 2016-11-01 | Nippon Kayaku Kabushiki Kaisha | High-molecular weight conjugate of steroids |
| USRE48468E1 (en) | 2007-10-26 | 2021-03-16 | Biomarin Technologies B.V. | Means and methods for counteracting muscle disorders |
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| KR101483715B1 (ko) | 2008-01-31 | 2015-01-19 | 큐어백 게엠바하 | 면역증강제／애주번트인 화학식（ＮｕＧｌＸｍＧｎＮｖ）ａ를 포함하는 핵산 및 이의 유도체 |
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| JP5687899B2 (ja) * | 2008-03-18 | 2015-03-25 | 日本化薬株式会社 | 生理活性物質の高分子結合体 |
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- 2003-03-03 JP JP2003573017A patent/JP4477881B2/ja not_active Expired - Lifetime
- 2003-03-03 US US10/506,223 patent/US7771727B2/en not_active Expired - Fee Related
- 2003-03-03 DK DK03716299.7T patent/DK1487493T3/da active
- 2003-03-03 CN CNA038099276A patent/CN1649625A/zh active Pending
- 2003-03-03 AU AU2003220011A patent/AU2003220011B2/en not_active Ceased
- 2003-03-03 WO PCT/US2003/006657 patent/WO2003074551A2/en not_active Ceased
- 2003-03-03 IL IL16357303A patent/IL163573A0/xx unknown
- 2003-03-03 CA CA002476182A patent/CA2476182A1/en not_active Abandoned
- 2003-03-03 MX MXPA04008419A patent/MXPA04008419A/es active IP Right Grant
- 2003-03-03 CN CN2010106215969A patent/CN102133407A/zh active Pending
- 2003-03-03 ES ES03716299T patent/ES2339934T3/es not_active Expired - Lifetime
- 2003-03-03 EP EP03716299A patent/EP1487493B1/en not_active Expired - Lifetime
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- 2003-03-03 AT AT03716299T patent/ATE455561T1/de active
- 2003-03-03 BR BRPI0308090-0A patent/BR0308090A/pt not_active IP Right Cessation
- 2003-03-03 PL PL03373567A patent/PL373567A1/xx not_active Application Discontinuation
- 2003-03-03 NZ NZ534719A patent/NZ534719A/en not_active IP Right Cessation
- 2003-03-03 KR KR1020047013597A patent/KR101003622B1/ko not_active Expired - Fee Related
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2004
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- 2004-09-24 NO NO20044039A patent/NO20044039L/no not_active Application Discontinuation
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2009
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