WO2002043663A3 - Tetrapartate prodrugs - Google Patents

Tetrapartate prodrugs Download PDF

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Publication number
WO2002043663A3
WO2002043663A3 PCT/US2001/045127 US0145127W WO0243663A3 WO 2002043663 A3 WO2002043663 A3 WO 2002043663A3 US 0145127 W US0145127 W US 0145127W WO 0243663 A3 WO0243663 A3 WO 0243663A3
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
alkyls
moiety
group
cycloalkyls
Prior art date
Application number
PCT/US2001/045127
Other languages
French (fr)
Other versions
WO2002043663A2 (en
Inventor
Richard B Greenwald
Hong Zhao
Original Assignee
Enzon Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from US09/758,993 external-priority patent/US6720306B2/en
Application filed by Enzon Inc filed Critical Enzon Inc
Priority to AU2002239405A priority Critical patent/AU2002239405A1/en
Priority to JP2002545642A priority patent/JP2004518776A/en
Priority to CA002428018A priority patent/CA2428018A1/en
Priority to EP01987164A priority patent/EP1343494A4/en
Publication of WO2002043663A2 publication Critical patent/WO2002043663A2/en
Publication of WO2002043663A3 publication Critical patent/WO2002043663A3/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

A compound of Formula I, providing a tetrapartate prodrugs is provided, wherein L1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be delivered into a cell; Z is covalently linked to [D]y, wherein Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Y1, Y2, Y3 and Y4 are each independently O, S, or NR12; R11 is a mono- or divalent polymer residue; R1, R4, R9, R10 and R12 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls and substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, halo-, nitro- and cyano-, carboxy-, C1-6 carboxyalkyls and C1-6 alkylcarbonyls; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; (m), (r), (s), (t), and (u) are independently zero or one; (p) is zero or a positive integer; and (y) is 1 or 2; together with methods of preparing and using these new tetrapartate prodrugs.
PCT/US2001/045127 2000-12-01 2001-11-30 Tetrapartate prodrugs WO2002043663A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU2002239405A AU2002239405A1 (en) 2000-12-01 2001-11-30 Tetrapartate prodrugs
JP2002545642A JP2004518776A (en) 2000-12-01 2001-11-30 Tetrapartate prodrug
CA002428018A CA2428018A1 (en) 2000-12-01 2001-11-30 Tetrapartate prodrugs
EP01987164A EP1343494A4 (en) 2000-12-01 2001-11-30 Tetrapartate prodrugs

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US72851200A 2000-12-01 2000-12-01
US09/728,512 2000-12-01
US09/758,993 2001-01-12
US09/758,993 US6720306B2 (en) 1997-12-17 2001-01-12 Tetrapartate prodrugs

Publications (2)

Publication Number Publication Date
WO2002043663A2 WO2002043663A2 (en) 2002-06-06
WO2002043663A3 true WO2002043663A3 (en) 2002-07-25

Family

ID=27111706

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/045127 WO2002043663A2 (en) 2000-12-01 2001-11-30 Tetrapartate prodrugs

Country Status (5)

Country Link
EP (1) EP1343494A4 (en)
JP (1) JP2004518776A (en)
AU (1) AU2002239405A1 (en)
CA (1) CA2428018A1 (en)
WO (1) WO2002043663A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9913827B2 (en) 2012-11-12 2018-03-13 Ignyta, Inc. Bendamustine derivatives and methods of using same

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6624142B2 (en) * 1997-12-30 2003-09-23 Enzon, Inc. Trimethyl lock based tetrapartate prodrugs
WO2003095496A1 (en) * 2002-05-08 2003-11-20 Medical Enzymes Ag Active carbohydrate containing protecting reagents for chemical modifications, their production and use
JP4723380B2 (en) * 2003-09-25 2011-07-13 テルモ株式会社 Polyethylene glycol derivative and drug carrier comprising this as a membrane constituent
CN100415801C (en) * 2003-10-28 2008-09-03 北京键凯科技有限公司 Polyethylene glycol amino acid N-internal ring carbonyl anhydride active derivatives, and medicinal bonding compound and gel thereof
CN100543063C (en) * 2006-04-03 2009-09-23 中国科学院过程工程研究所 Polyethyleneglycol of end group of amino acid and preparation method thereof
CN101534861B (en) 2006-09-15 2013-10-02 安佐制药股份有限公司 Polyalkylene oxides having hindered ester-based biodegradable linkers
CA2662978A1 (en) * 2006-09-15 2008-03-20 Enzon Pharmaceuticals, Inc. Hindered ester-based biodegradable linkers for oligonucleotide delivery
DE102011118029A1 (en) 2011-06-20 2012-12-20 Universität Leipzig Modified antibiotic peptides with variable systemic release
US10040850B2 (en) 2013-10-08 2018-08-07 Ascendis Pharma A/S Protecting group comprising a purification tag

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5710135A (en) * 1995-06-27 1998-01-20 Pharmachemie B.V. Anthracycline prodrugs, method for preparation as well as their use in selective chemotherapy
WO1999030727A1 (en) * 1997-12-17 1999-06-24 Enzon, Inc. Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents
US6005002A (en) * 1995-01-19 1999-12-21 Cancer Research Campaign Technology Limited Nitrogen mustard prodrugs with novel lipophilic protecting groups, and processes for their production

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6005002A (en) * 1995-01-19 1999-12-21 Cancer Research Campaign Technology Limited Nitrogen mustard prodrugs with novel lipophilic protecting groups, and processes for their production
US5710135A (en) * 1995-06-27 1998-01-20 Pharmachemie B.V. Anthracycline prodrugs, method for preparation as well as their use in selective chemotherapy
WO1999030727A1 (en) * 1997-12-17 1999-06-24 Enzon, Inc. Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
GREENWALD ET AL.: "Drug delivery systems employing 1,4- or 1,6-elimination: poly(ethylene glycol)prodrugs of amine-containing compounds", JOURNAL OF MEDICINAL CHEMISTRY, vol. 42, no. 18, 1999, pages 3657 - 3667, XP002184836 *
See also references of EP1343494A4 *
ZIER, ET AL.: "Polyethylene glycol bound benzyl- and fluorenyl derivatives as solubilizing side-chain protecting groups in peptide synthesis", TETRAHEDRON LETTERS, vol. 35, no. 7, 1994, pages 1039 - 1042, XP002950143 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9913827B2 (en) 2012-11-12 2018-03-13 Ignyta, Inc. Bendamustine derivatives and methods of using same

Also Published As

Publication number Publication date
EP1343494A2 (en) 2003-09-17
EP1343494A4 (en) 2005-08-03
CA2428018A1 (en) 2002-06-06
JP2004518776A (en) 2004-06-24
WO2002043663A2 (en) 2002-06-06
AU2002239405A1 (en) 2002-06-11

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