JP2008523239A5 - - Google Patents
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- Publication number
- JP2008523239A5 JP2008523239A5 JP2007546901A JP2007546901A JP2008523239A5 JP 2008523239 A5 JP2008523239 A5 JP 2008523239A5 JP 2007546901 A JP2007546901 A JP 2007546901A JP 2007546901 A JP2007546901 A JP 2007546901A JP 2008523239 A5 JP2008523239 A5 JP 2008523239A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- substituted
- alkyl
- independently
- heteroalkyl
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 27
- 229920000642 polymer Polymers 0.000 claims description 5
- FSVCELGFZIQNCK-UHFFFAOYSA-N N,N-bis(2-hydroxyethyl)glycine Chemical compound OCCN(CCO)CC(O)=O FSVCELGFZIQNCK-UHFFFAOYSA-N 0.000 claims description 3
- 125000002947 alkylene group Chemical group 0.000 claims description 3
- 150000001413 amino acids Chemical group 0.000 claims description 3
- 125000000732 arylene group Chemical group 0.000 claims description 3
- 239000007998 bicine buffer Substances 0.000 claims description 3
- 150000004665 fatty acids Chemical group 0.000 claims description 3
- 125000005549 heteroarylene group Chemical group 0.000 claims description 3
- 229920000768 polyamine Chemical group 0.000 claims description 3
- 108090000765 processed proteins & peptides Chemical group 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims 26
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 17
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000004405 heteroalkoxy group Chemical group 0.000 claims 9
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 230000001588 bifunctional effect Effects 0.000 claims 8
- 125000005647 linker group Chemical group 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 7
- 125000000547 substituted alkyl group Chemical group 0.000 claims 7
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 7
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims 6
- 230000008685 targeting Effects 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 229940039227 diagnostic agent Drugs 0.000 claims 4
- 239000000032 diagnostic agent Substances 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 3
- 239000002253 acid Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 238000006116 polymerization reaction Methods 0.000 claims 3
- 230000003213 activating effect Effects 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 229940088623 biologically active substance Drugs 0.000 claims 2
- 230000008878 coupling Effects 0.000 claims 2
- 238000010168 coupling process Methods 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- -1 leaving groups Chemical group 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 230000000975 bioactive effect Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000002131 composite material Substances 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 0 CC(C)(*)*C(C)(C)C(C(C)(*)N(C)C)=I Chemical compound CC(C)(*)*C(C)(C)C(C(C)(*)N(C)C)=I 0.000 description 24
- GXHBGUKUPHAMAY-UHFFFAOYSA-N CC(C)(C)OC(NCCOCCOCCNC(COCC(O)=O)=O)=O Chemical compound CC(C)(C)OC(NCCOCCOCCNC(COCC(O)=O)=O)=O GXHBGUKUPHAMAY-UHFFFAOYSA-N 0.000 description 1
- BJLXRUJPJFQITJ-UHFFFAOYSA-N CC(C)COC(CN(CCO)CCOC(COCC(NCCOCCOCCNC(OC(C)(C)C)=O)=O)=O)=O Chemical compound CC(C)COC(CN(CCO)CCOC(COCC(NCCOCCOCCNC(OC(C)(C)C)=O)=O)=O)=O BJLXRUJPJFQITJ-UHFFFAOYSA-N 0.000 description 1
- FNHJKFIBFQVYGZ-UHFFFAOYSA-N CC(C)COC(CN(CCOC(C)=O)CCOC(COCC(NCCOCCOCCNC(OC(C)(C)C)=O)=O)=O)=O Chemical compound CC(C)COC(CN(CCOC(C)=O)CCOC(COCC(NCCOCCOCCNC(OC(C)(C)C)=O)=O)=O)=O FNHJKFIBFQVYGZ-UHFFFAOYSA-N 0.000 description 1
- PSOACONXHIXHEX-UHFFFAOYSA-N CCCC(C)(N)N=N Chemical compound CCCC(C)(N)N=N PSOACONXHIXHEX-UHFFFAOYSA-N 0.000 description 1
- RGTLAJIDOSPEDH-UHFFFAOYSA-N CN(CCS1)C1=S Chemical compound CN(CCS1)C1=S RGTLAJIDOSPEDH-UHFFFAOYSA-N 0.000 description 1
- JDFXJJLFADUZIY-UHFFFAOYSA-N CON(C(CC1)=O)C1=O Chemical compound CON(C(CC1)=O)C1=O JDFXJJLFADUZIY-UHFFFAOYSA-N 0.000 description 1
- BNUHAJGCKIQFGE-UHFFFAOYSA-N COc(cc1)ccc1[N+]([O-])=O Chemical compound COc(cc1)ccc1[N+]([O-])=O BNUHAJGCKIQFGE-UHFFFAOYSA-N 0.000 description 1
- 230000009056 active transport Effects 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11/011,818 | 2004-12-14 | ||
| US11/011,818 US7413738B2 (en) | 2002-08-13 | 2004-12-14 | Releasable polymeric conjugates based on biodegradable linkers |
| PCT/US2005/045467 WO2006066020A2 (en) | 2004-12-14 | 2005-12-13 | Releasable polymeric conjugates based on aliphatic biodegradable linkers |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008523239A JP2008523239A (ja) | 2008-07-03 |
| JP2008523239A5 true JP2008523239A5 (enExample) | 2013-10-24 |
| JP5405746B2 JP5405746B2 (ja) | 2014-02-05 |
Family
ID=36588567
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007546901A Expired - Fee Related JP5405746B2 (ja) | 2004-12-14 | 2005-12-13 | 脂肪族生物分解性リンカーに基づく放出可能なポリマー複合体 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7413738B2 (enExample) |
| EP (1) | EP1827497A4 (enExample) |
| JP (1) | JP5405746B2 (enExample) |
| KR (1) | KR20070089739A (enExample) |
| CN (1) | CN101076353B (enExample) |
| AU (1) | AU2005316520B2 (enExample) |
| CA (1) | CA2589975C (enExample) |
| IL (1) | IL183582A0 (enExample) |
| MX (1) | MX2007007034A (enExample) |
| RU (1) | RU2007126802A (enExample) |
| TW (1) | TWI375556B (enExample) |
| WO (1) | WO2006066020A2 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7087229B2 (en) * | 2003-05-30 | 2006-08-08 | Enzon Pharmaceuticals, Inc. | Releasable polymeric conjugates based on aliphatic biodegradable linkers |
| US7413738B2 (en) * | 2002-08-13 | 2008-08-19 | Enzon Pharmaceuticals, Inc. | Releasable polymeric conjugates based on biodegradable linkers |
| US7122189B2 (en) * | 2002-08-13 | 2006-10-17 | Enzon, Inc. | Releasable polymeric conjugates based on aliphatic biodegradable linkers |
| US7365127B2 (en) * | 2005-02-04 | 2008-04-29 | Enzon Pharmaceuticals, Inc. | Process for the preparation of polymer conjugates |
| ATE440856T1 (de) * | 2005-05-04 | 2009-09-15 | Lonza Ag | Festphasengebundenes thymosin-alpha1 und dessen synthese |
| GB2427360A (en) * | 2005-06-22 | 2006-12-27 | Complex Biosystems Gmbh | Aliphatic prodrug linker |
| US8133707B2 (en) | 2006-01-17 | 2012-03-13 | Enzon Pharmaceuticals, Inc. | Methods of preparing activated polymers having alpha nitrogen groups |
| JP2009539879A (ja) * | 2006-06-09 | 2009-11-19 | エンゾン ファーマスーティカルズ インコーポレイテッド | インデノイソキノリン放出性ポリマー複合体 |
| US8110559B2 (en) * | 2006-09-15 | 2012-02-07 | Enzon Pharmaceuticals, Inc. | Hindered ester-based biodegradable linkers for oligonucleotide delivery |
| BRPI0716823A2 (pt) * | 2006-09-15 | 2015-05-26 | Enzon Pharmaceuticals Inc | Conjunto poliméricos contendo porções positivamente carregadas |
| EP2063912A4 (en) * | 2006-09-15 | 2010-07-28 | Enzon Pharmaceuticals Inc | POLYALKYLENE OXIDES HAVING BIODEGRADABLE BOND SEGMENTS BASED ON COARSE ESTER |
| BRPI0716808A2 (pt) * | 2006-09-15 | 2013-11-05 | Enzon Pharmaceuticals Inc | Ligantes poliméricos baseados em lisina |
| US20100279408A1 (en) * | 2006-11-27 | 2010-11-04 | Enzon Pharmaceuticals, Inc. | Polymeric short interfering rna conjugates |
| CA2671209A1 (en) * | 2006-12-29 | 2008-07-10 | Enzon Pharmaceuticals, Inc. | Use of adenosine deaminase for treating pulmonary disease |
| PL2147116T3 (pl) * | 2007-04-20 | 2016-08-31 | Leadiant Biosciences Ltd | Stabilna rekombinowana dezaminaza adenozynowa |
| TWI486169B (zh) * | 2007-04-20 | 2015-06-01 | Sigma Tau Rare Diseases S A | 酵素性抗癌療法 |
| JP2010536986A (ja) * | 2007-08-20 | 2010-12-02 | エンゾン ファーマシューティカルズ，インコーポレーテッド | ピリジルジスルフィド部分を含有するポリマーリンカー |
| NZ758050A (en) | 2013-10-15 | 2024-03-22 | Seagen Inc | Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics |
| JP7073266B2 (ja) | 2016-03-25 | 2022-05-23 | シージェン インコーポレイテッド | Ｐｅｇ化薬物リンカー及びその中間体を調製するためのプロセス |
| KR102648564B1 (ko) | 2017-03-24 | 2024-03-19 | 씨젠 인크. | 글루쿠로니드 약물-링커의 제조 공정 및 그 중간물 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3888797A (en) | 1970-08-04 | 1975-06-10 | Carapus Company Limited | Detergent composition |
| US4179337A (en) | 1973-07-20 | 1979-12-18 | Davis Frank F | Non-immunogenic polypeptides |
| DE4135115A1 (de) | 1991-10-24 | 1993-04-29 | Trigon Chemie Gmbh | Kationaktive tenside |
| US5679711A (en) | 1993-10-08 | 1997-10-21 | Fhj Scientific, Inc. | Hydroxyl ions as novel therapeutic agents and compounds that modulate these ions, compositions employing these agents, therapeutic methods for using such agents |
| US5919455A (en) | 1993-10-27 | 1999-07-06 | Enzon, Inc. | Non-antigenic branched polymer conjugates |
| US5643575A (en) | 1993-10-27 | 1997-07-01 | Enzon, Inc. | Non-antigenic branched polymer conjugates |
| EP2174939A1 (en) | 2002-02-25 | 2010-04-14 | Kudos Pharmaceuticals Limited | Pyranones useful as ATM inhibitors |
| US7122189B2 (en) * | 2002-08-13 | 2006-10-17 | Enzon, Inc. | Releasable polymeric conjugates based on aliphatic biodegradable linkers |
| US7413738B2 (en) | 2002-08-13 | 2008-08-19 | Enzon Pharmaceuticals, Inc. | Releasable polymeric conjugates based on biodegradable linkers |
| US7087229B2 (en) | 2003-05-30 | 2006-08-08 | Enzon Pharmaceuticals, Inc. | Releasable polymeric conjugates based on aliphatic biodegradable linkers |
| US7273845B2 (en) | 2002-11-12 | 2007-09-25 | Enzon Pharmaceuticals, Inc. | Polymeric prodrugs of vancomycin |
| US7332164B2 (en) | 2003-03-21 | 2008-02-19 | Enzon Pharmaceuticals, Inc. | Heterobifunctional polymeric bioconjugates |
| KR20060015505A (ko) | 2003-04-13 | 2006-02-17 | 엔존 파마슈티컬즈, 인코포레이티드 | 올리고뉴클레오타이드 전구약물 |
-
2004
- 2004-12-14 US US11/011,818 patent/US7413738B2/en not_active Expired - Fee Related
-
2005
- 2005-11-29 TW TW094141400A patent/TWI375556B/zh not_active IP Right Cessation
- 2005-12-13 JP JP2007546901A patent/JP5405746B2/ja not_active Expired - Fee Related
- 2005-12-13 AU AU2005316520A patent/AU2005316520B2/en not_active Ceased
- 2005-12-13 CA CA2589975A patent/CA2589975C/en not_active Expired - Fee Related
- 2005-12-13 CN CN200580042661XA patent/CN101076353B/zh not_active Expired - Fee Related
- 2005-12-13 KR KR1020077015937A patent/KR20070089739A/ko not_active Withdrawn
- 2005-12-13 RU RU2007126802/04A patent/RU2007126802A/ru not_active Application Discontinuation
- 2005-12-13 EP EP05854230A patent/EP1827497A4/en not_active Withdrawn
- 2005-12-13 WO PCT/US2005/045467 patent/WO2006066020A2/en not_active Ceased
- 2005-12-13 MX MX2007007034A patent/MX2007007034A/es active IP Right Grant
-
2007
- 2007-05-31 IL IL183582A patent/IL183582A0/en unknown
-
2008
- 2008-07-25 US US12/180,187 patent/US8192743B2/en not_active Expired - Fee Related
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