JP2005528380A5 - - Google Patents
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- Publication number
- JP2005528380A5 JP2005528380A5 JP2003582125A JP2003582125A JP2005528380A5 JP 2005528380 A5 JP2005528380 A5 JP 2005528380A5 JP 2003582125 A JP2003582125 A JP 2003582125A JP 2003582125 A JP2003582125 A JP 2003582125A JP 2005528380 A5 JP2005528380 A5 JP 2005528380A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- group
- compound
- 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
- 150000001875 compounds Chemical class 0.000 claims 28
- 125000000217 alkyl group Chemical group 0.000 claims 17
- -1 heteroaromatic amine Chemical class 0.000 claims 13
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 229920000642 polymer Polymers 0.000 claims 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000004405 heteroalkoxy group Chemical group 0.000 claims 8
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 8
- 125000000547 substituted alkyl group Chemical group 0.000 claims 8
- 125000003107 substituted aryl group Chemical group 0.000 claims 8
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 7
- 230000001588 bifunctional effect Effects 0.000 claims 5
- 125000004404 heteroalkyl group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000006850 spacer group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 238000000034 method Methods 0.000 claims 3
- 229920001223 polyethylene glycol Polymers 0.000 claims 3
- LDCYZAJDBXYCGN-VIFPVBQESA-N 5-hydroxy-L-tryptophan Chemical compound C1=C(O)C=C2C(C[C@H](N)C(O)=O)=CNC2=C1 LDCYZAJDBXYCGN-VIFPVBQESA-N 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 230000000975 bioactive effect Effects 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000003827 glycol group Chemical group 0.000 claims 2
- SEOVTRFCIGRIMH-UHFFFAOYSA-N indole-3-acetic acid Chemical compound C1=CC=C2C(CC(=O)O)=CNC2=C1 SEOVTRFCIGRIMH-UHFFFAOYSA-N 0.000 claims 2
- TXQAZWIBPGKHOX-UHFFFAOYSA-N 1H-indol-3-amine Chemical compound C1=CC=C2C(N)=CNC2=C1 TXQAZWIBPGKHOX-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- JOAHPSVPXZTVEP-YXJHDRRASA-N Terguride Chemical compound C1=CC([C@H]2C[C@@H](CN(C)[C@@H]2C2)NC(=O)N(CC)CC)=C3C2=CNC3=C1 JOAHPSVPXZTVEP-YXJHDRRASA-N 0.000 claims 1
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 1
- BLGXFZZNTVWLAY-CCZXDCJGSA-N Yohimbine Natural products C1=CC=C2C(CCN3C[C@@H]4CC[C@@H](O)[C@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-CCZXDCJGSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 1
- BLGXFZZNTVWLAY-UHFFFAOYSA-N beta-Yohimbin Natural products C1=CC=C2C(CCN3CC4CCC(O)C(C4CC33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-UHFFFAOYSA-N 0.000 claims 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 1
- QZUDBNBUXVUHMW-UHFFFAOYSA-N clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 claims 1
- 229960004170 clozapine Drugs 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 239000003617 indole-3-acetic acid Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 claims 1
- 229960001597 nifedipine Drugs 0.000 claims 1
- LDCYZAJDBXYCGN-UHFFFAOYSA-N oxitriptan Natural products C1=C(O)C=C2C(CC(N)C(O)=O)=CNC2=C1 LDCYZAJDBXYCGN-UHFFFAOYSA-N 0.000 claims 1
- PHUTUTUABXHXLW-UHFFFAOYSA-N pindolol Chemical compound CC(C)NCC(O)COC1=CC=CC2=NC=C[C]12 PHUTUTUABXHXLW-UHFFFAOYSA-N 0.000 claims 1
- 229960002508 pindolol Drugs 0.000 claims 1
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims 1
- 238000006116 polymerization reaction Methods 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 1
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 1
- 229960004558 terguride Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 229960003048 vinblastine Drugs 0.000 claims 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
- BLGXFZZNTVWLAY-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-SCYLSFHTSA-N 0.000 claims 1
- 229960000317 yohimbine Drugs 0.000 claims 1
- AADVZSXPNRLYLV-UHFFFAOYSA-N yohimbine carboxylic acid Natural products C1=CC=C2C(CCN3CC4CCC(C(C4CC33)C(O)=O)O)=C3NC2=C1 AADVZSXPNRLYLV-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36973202P | 2002-04-04 | 2002-04-04 | |
| PCT/US2003/009875 WO2003084926A2 (en) | 2002-04-04 | 2003-03-31 | Polymeric acyl derivatives of indoles |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005528380A JP2005528380A (ja) | 2005-09-22 |
| JP2005528380A5 true JP2005528380A5 (enExample) | 2006-03-02 |
| JP4527404B2 JP4527404B2 (ja) | 2010-08-18 |
Family
ID=28791989
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003582125A Expired - Fee Related JP4527404B2 (ja) | 2002-04-04 | 2003-03-31 | インドールのポリマー性アシル誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7393953B2 (enExample) |
| EP (1) | EP1494757A2 (enExample) |
| JP (1) | JP4527404B2 (enExample) |
| AU (1) | AU2003226166A1 (enExample) |
| CA (1) | CA2479810A1 (enExample) |
| WO (1) | WO2003084926A2 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1757607A1 (en) | 2005-08-24 | 2007-02-28 | Molisa GmbH | N5-substituted benzo¬2,3|azepino¬4,5-b|indol-6-ones for treating tropical diseases |
| US9782488B2 (en) | 2007-03-12 | 2017-10-10 | Nektar Therapeutics | Oligomer-beta blocker conjugates |
| US20100184989A1 (en) * | 2007-03-12 | 2010-07-22 | Nektar Therapeutics | De Novo Synthesis of Conjugates |
| WO2009032286A2 (en) * | 2007-09-06 | 2009-03-12 | Nektar Therapeutics Al, Corporation | Oligomer-calcium channel blocker conjugates |
| KR20120089843A (ko) | 2009-07-31 | 2012-08-14 | 사노피-아벤티스 도이칠란트 게엠베하 | 인슐린 링커 접합체를 포함한 프로드럭 |
| UA108475C2 (uk) | 2009-07-31 | 2015-05-12 | Санофі-Авентіс Дойчланд Гмбх | Композиція інсуліну тривалої дії |
| LT2459220T (lt) | 2009-07-31 | 2020-12-28 | Ascendis Pharma A/S | Biologiškai suyrantys vandenyje netirpūs hidrogeliai polietilenglikolio pagrindu |
| WO2011082368A2 (en) * | 2009-12-31 | 2011-07-07 | Enzon Pharmaceuticals, Inc | Polymeric conjugates of aromatic amine containing compounds including releasable urea linker |
| EP2438930A1 (en) | 2010-09-17 | 2012-04-11 | Sanofi-Aventis Deutschland GmbH | Prodrugs comprising an exendin linker conjugate |
| WO2013024047A1 (en) | 2011-08-12 | 2013-02-21 | Ascendis Pharma A/S | High-loading water-soluble carrier-linked prodrugs |
| AU2012296951B2 (en) | 2011-08-12 | 2016-09-15 | Ascendis Pharma A/S | Protein carrier-linked prodrugs |
| CA2843503C (en) | 2011-08-12 | 2020-12-22 | Ulrich Hersel | Polymeric hyperbranched carrier-linked prodrugs |
| AU2012322917B2 (en) | 2011-10-12 | 2016-11-03 | Ascendis Pharma Ophthalmology Division A/S | Prevention and treatment of ocular conditions |
| HK1208813A1 (en) | 2012-10-11 | 2016-03-18 | Ascendis Pharma A/S | Diagnosis, prevention and treatment of diseases of the joint |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5840900A (en) * | 1993-10-20 | 1998-11-24 | Enzon, Inc. | High molecular weight polymer-based prodrugs |
| DE19636889A1 (de) * | 1996-09-11 | 1998-03-12 | Felix Dr Kratz | Antineoplastisch wirkende Transferrin- und Albuminkonjugate zytostatischer Verbindungen aus der Gruppe der Anthrazykline, Alkylantien, Antimetabolite und Cisplatin-Analoga und diese enthaltende Arzneimittel |
| US6153655A (en) * | 1998-04-17 | 2000-11-28 | Enzon, Inc. | Terminally-branched polymeric linkers and polymeric conjugates containing the same |
| US6251382B1 (en) * | 1998-04-17 | 2001-06-26 | Enzon, Inc. | Biodegradable high molecular weight polymeric linkers and their conjugates |
| AU778735B2 (en) | 1998-06-16 | 2004-12-16 | Centre National De La Recherche Scientifique | Fused azepinone cyclin dependent kinase inhibitors |
| FR2804959B1 (fr) * | 2000-02-15 | 2006-04-28 | Centre Nat Rech Scient | Utilisation de derives de paullones pour la fabrication de medicaments |
-
2003
- 2003-03-31 US US10/403,789 patent/US7393953B2/en not_active Expired - Fee Related
- 2003-03-31 JP JP2003582125A patent/JP4527404B2/ja not_active Expired - Fee Related
- 2003-03-31 WO PCT/US2003/009875 patent/WO2003084926A2/en not_active Ceased
- 2003-03-31 CA CA002479810A patent/CA2479810A1/en not_active Abandoned
- 2003-03-31 EP EP03746088A patent/EP1494757A2/en not_active Withdrawn
- 2003-03-31 AU AU2003226166A patent/AU2003226166A1/en not_active Abandoned
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