JP2015526435A5 - - Google Patents
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- JP2015526435A5 JP2015526435A5 JP2015526846A JP2015526846A JP2015526435A5 JP 2015526435 A5 JP2015526435 A5 JP 2015526435A5 JP 2015526846 A JP2015526846 A JP 2015526846A JP 2015526846 A JP2015526846 A JP 2015526846A JP 2015526435 A5 JP2015526435 A5 JP 2015526435A5
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- JP
- Japan
- Prior art keywords
- polypeptide
- seq
- linked
- xaa
- antibody
- 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.)
- Pending
Links
- 108090000765 processed proteins & peptides Proteins 0.000 description 38
- 229920001184 polypeptide Polymers 0.000 description 37
- 102000004196 processed proteins & peptides Human genes 0.000 description 37
- 239000000306 component Substances 0.000 description 10
- 231100000599 cytotoxic agent Toxicity 0.000 description 10
- 125000000539 amino acid group Chemical group 0.000 description 8
- 229940127089 cytotoxic agent Drugs 0.000 description 7
- 239000002254 cytotoxic agent Substances 0.000 description 7
- 125000003396 thiol group Chemical group [H]S* 0.000 description 6
- 238000000034 method Methods 0.000 description 5
- 235000018102 proteins Nutrition 0.000 description 5
- 108090000623 proteins and genes Proteins 0.000 description 5
- 102000004169 proteins and genes Human genes 0.000 description 5
- 239000012634 fragment Substances 0.000 description 4
- 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 description 4
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 4
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- 239000002619 cytotoxin Substances 0.000 description 3
- JWDFQMWEFLOOED-UHFFFAOYSA-N (2,5-dioxopyrrolidin-1-yl) 3-(pyridin-2-yldisulfanyl)propanoate Chemical compound O=C1CCC(=O)N1OC(=O)CCSSC1=CC=CC=N1 JWDFQMWEFLOOED-UHFFFAOYSA-N 0.000 description 2
- 101710112752 Cytotoxin Proteins 0.000 description 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 2
- 239000004472 Lysine Substances 0.000 description 2
- PEEHTFAAVSWFBL-UHFFFAOYSA-N Maleimide Chemical compound O=C1NC(=O)C=C1 PEEHTFAAVSWFBL-UHFFFAOYSA-N 0.000 description 2
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 description 2
- 125000000217 alkyl group Chemical group 0.000 description 2
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 description 2
- 150000001540 azides Chemical class 0.000 description 2
- 230000021615 conjugation Effects 0.000 description 2
- ZPWOOKQUDFIEIX-UHFFFAOYSA-N cyclooctyne Chemical compound C1CCCC#CCC1 ZPWOOKQUDFIEIX-UHFFFAOYSA-N 0.000 description 2
- 238000010188 recombinant method Methods 0.000 description 2
- 239000004474 valine Substances 0.000 description 2
- KQRHTCDQWJLLME-XUXIUFHCSA-N (2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-aminopropanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-4-methylpentanoic acid Chemical group CC(C)C[C@@H](C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)N KQRHTCDQWJLLME-XUXIUFHCSA-N 0.000 description 1
- WEZDRVHTDXTVLT-GJZGRUSLSA-N 2-[[(2s)-2-[[(2s)-2-[(2-aminoacetyl)amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]acetic acid Chemical compound OC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)CN)CC1=CC=CC=C1 WEZDRVHTDXTVLT-GJZGRUSLSA-N 0.000 description 1
- 229940127149 ANG4043 Drugs 0.000 description 1
- 108010064942 Angiopep-2 Proteins 0.000 description 1
- 108010039627 Aprotinin Proteins 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- 108020004705 Codon Proteins 0.000 description 1
- 239000004971 Cross linker Substances 0.000 description 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
- 108010009504 Gly-Phe-Leu-Gly Proteins 0.000 description 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 description 1
- 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 description 1
- 108091028043 Nucleic acid sequence Proteins 0.000 description 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 1
- 108010054982 alanyl-leucyl-alanyl-leucine Proteins 0.000 description 1
- HAXFWIACAGNFHA-UHFFFAOYSA-N aldrithiol Chemical group C=1C=CC=NC=1SSC1=CC=CC=N1 HAXFWIACAGNFHA-UHFFFAOYSA-N 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 150000001413 amino acids Chemical group 0.000 description 1
- 229960004405 aprotinin Drugs 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide group Chemical group [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 description 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- 230000000975 bioactive effect Effects 0.000 description 1
- 210000004899 c-terminal region Anatomy 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 238000012650 click reaction Methods 0.000 description 1
- 230000001268 conjugating effect Effects 0.000 description 1
- 239000008358 core component Substances 0.000 description 1
- 238000002784 cytotoxicity assay Methods 0.000 description 1
- 231100000263 cytotoxicity test Toxicity 0.000 description 1
- 239000000412 dendrimer Substances 0.000 description 1
- 229920000736 dendritic polymer Polymers 0.000 description 1
- 125000002228 disulfide group Chemical group 0.000 description 1
- 229960003668 docetaxel Drugs 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 210000003527 eukaryotic cell Anatomy 0.000 description 1
- 125000000291 glutamic acid group Chemical group N[C@@H](CCC(O)=O)C(=O)* 0.000 description 1
- CTRFEEQNDJFNNL-UHFFFAOYSA-N hexanoic acid;pyrrole-2,5-dione Chemical compound O=C1NC(=O)C=C1.CCCCCC(O)=O CTRFEEQNDJFNNL-UHFFFAOYSA-N 0.000 description 1
- -1 maleimidomethyl Chemical group 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 108020004707 nucleic acids Proteins 0.000 description 1
- 102000039446 nucleic acids Human genes 0.000 description 1
- 150000007523 nucleic acids Chemical class 0.000 description 1
- 239000002773 nucleotide Substances 0.000 description 1
- 125000003729 nucleotide group Chemical group 0.000 description 1
- 238000005457 optimization Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 210000001236 prokaryotic cell Anatomy 0.000 description 1
- 230000009257 reactivity Effects 0.000 description 1
- 238000010532 solid phase synthesis reaction Methods 0.000 description 1
- 125000006850 spacer group Chemical group 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- JJAHTWIKCUJRDK-UHFFFAOYSA-N succinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate Chemical compound C1CC(CN2C(C=CC2=O)=O)CCC1C(=O)ON1C(=O)CCC1=O JJAHTWIKCUJRDK-UHFFFAOYSA-N 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 125000002987 valine group Chemical group [H]N([H])C([H])(C(*)=O)C([H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
Images
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261682991P | 2012-08-14 | 2012-08-14 | |
| US61/682,991 | 2012-08-14 | ||
| US201361865071P | 2013-08-12 | 2013-08-12 | |
| US61/865,071 | 2013-08-12 | ||
| PCT/CA2013/050625 WO2014026286A1 (en) | 2012-08-14 | 2013-08-14 | Conjugates including an antibody moiety, a polypeptide that traverses the blood-brain barrier, and a cytotoxin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015526435A JP2015526435A (ja) | 2015-09-10 |
| JP2015526435A5 true JP2015526435A5 (enExample) | 2016-03-31 |
Family
ID=50101159
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015526846A Pending JP2015526435A (ja) | 2012-08-14 | 2013-08-14 | 抗体成分と血液脳関門を通過するポリペプチドと細胞毒とを含むコンジュゲート |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US20160106856A1 (enExample) |
| EP (1) | EP2885321A4 (enExample) |
| JP (1) | JP2015526435A (enExample) |
| CN (1) | CN104781281A (enExample) |
| AU (1) | AU2013302273A1 (enExample) |
| CA (1) | CA2880342A1 (enExample) |
| WO (1) | WO2014026286A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2233156T3 (pl) | 2005-07-15 | 2013-09-30 | Angiochem Inc | Zastosowanie polipeptydów aprotyninowych jako nośników w koniugatach farmaceutycznych |
| WO2010043047A1 (en) | 2008-10-15 | 2010-04-22 | Angiochem Inc. | Conjugates of glp-1 agonists and uses thereof |
| WO2010063122A1 (en) | 2008-12-05 | 2010-06-10 | Angiochem Inc. | Conjugates of neurotensin or neurotensin analogs and uses thereof |
| CN104781276A (zh) | 2012-08-14 | 2015-07-15 | 安吉奥开米公司 | 肽-树枝状聚合物结合物及其用途 |
| MA39909B1 (fr) | 2014-04-25 | 2019-05-31 | Pf Medicament | Conjugué anticorps de l'igf-1r-médicament et son utilisation pour le traitement du cancer |
| MX378281B (es) | 2014-04-25 | 2025-03-10 | Pf Medicament | Conjugado farmaco-anticuerpo y su uso para el tratamiento contra el cancer. |
| EP3218414A1 (en) * | 2014-11-14 | 2017-09-20 | Angiochem Inc. | Conjugates including an antibody moiety, a polypeptide that traverses the blood-brain barrier, and a cytotoxin |
| EP3307326B9 (en) | 2015-06-15 | 2021-02-24 | Angiochem Inc. | Methods for the treatment of leptomeningeal carcinomatosis |
| WO2019190293A1 (ko) * | 2018-03-30 | 2019-10-03 | 한미약품 주식회사 | 뇌 표적 지속성 단백질 결합체, 이의 제조 방법, 및 이를 포함하는 조성물 |
| WO2020069488A1 (en) * | 2018-09-28 | 2020-04-02 | North Carolina State University | Compositions and methods for drug delivery |
| EP4021511A4 (en) * | 2019-08-28 | 2023-10-04 | Starpharma Pty Ltd | TARGETED DENDRIMER CONJUGATES |
| AU2021284918A1 (en) * | 2020-06-03 | 2023-01-05 | Starpharma Pty Ltd | Therapeutic conjugates |
| CN114478772B (zh) * | 2021-12-31 | 2023-08-22 | 苏州怡然生物科技有限公司 | 工程化免疫细胞、纳米凝胶及其制备方法和应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2688344C (en) * | 2007-05-29 | 2019-09-03 | Angiochem, Inc. | Aprotinin-like polypeptides for delivering agents conjugated thereto to tissues |
| RU2011146654A (ru) * | 2009-04-20 | 2013-05-27 | Ангиокем Инк. | Способы лечения рака яичников с применением конъюгированного средства |
| KR101806323B1 (ko) * | 2009-11-13 | 2017-12-07 | 다이이치 산쿄 유럽 게엠베하 | Ｈｅｒ-３ 관련 질병을 치료하거나 예방하기 위한 물질 및 방법 |
| EP2588490B1 (en) * | 2010-07-02 | 2017-02-22 | Angiochem Inc. | Short and d-amino acid-containing polypeptides for therapeutic conjugates and uses thereof |
| WO2012037687A1 (en) * | 2010-09-23 | 2012-03-29 | Angiochem Inc. | Therapeutic polypeptides and uses thereof |
-
2013
- 2013-08-14 US US14/421,213 patent/US20160106856A1/en not_active Abandoned
- 2013-08-14 JP JP2015526846A patent/JP2015526435A/ja active Pending
- 2013-08-14 WO PCT/CA2013/050625 patent/WO2014026286A1/en not_active Ceased
- 2013-08-14 CN CN201380043328.5A patent/CN104781281A/zh active Pending
- 2013-08-14 CA CA2880342A patent/CA2880342A1/en not_active Abandoned
- 2013-08-14 AU AU2013302273A patent/AU2013302273A1/en not_active Abandoned
- 2013-08-14 EP EP13829923.5A patent/EP2885321A4/en not_active Withdrawn
-
2016
- 2016-11-11 US US15/349,166 patent/US20170281787A1/en not_active Abandoned
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