WO2010014236A3 - Acylhydrazone-based cleavable linkers - Google Patents

Acylhydrazone-based cleavable linkers Download PDF

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Publication number
WO2010014236A3
WO2010014236A3 PCT/US2009/004402 US2009004402W WO2010014236A3 WO 2010014236 A3 WO2010014236 A3 WO 2010014236A3 US 2009004402 W US2009004402 W US 2009004402W WO 2010014236 A3 WO2010014236 A3 WO 2010014236A3
Authority
WO
WIPO (PCT)
Prior art keywords
acylhydrazone
cleavable linkers
based cleavable
cleavable linker
cleavable
Prior art date
Application number
PCT/US2009/004402
Other languages
French (fr)
Other versions
WO2010014236A2 (en
Inventor
Harold L. Kohn
Ki Duk Park
Original Assignee
The University Of North Carolina At Chapel Hill
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
Application filed by The University Of North Carolina At Chapel Hill filed Critical The University Of North Carolina At Chapel Hill
Publication of WO2010014236A2 publication Critical patent/WO2010014236A2/en
Publication of WO2010014236A3 publication Critical patent/WO2010014236A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/13—Labelling of peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

The present invention provides cleavable linker compounds of Formula (I): wherein: X is a cleavable linker comprising an acylhydrazone; and Y and R are each independently selected from the group consisting of covalent coupling groups and members of a specific binding pair. Solid supports having such cleavable linkers coupled thereto, and methods of using the same, are also described.
PCT/US2009/004402 2008-07-30 2009-07-30 Acylhydrazone-based cleavable linkers WO2010014236A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8475608P 2008-07-30 2008-07-30
US61/084,756 2008-07-30

Publications (2)

Publication Number Publication Date
WO2010014236A2 WO2010014236A2 (en) 2010-02-04
WO2010014236A3 true WO2010014236A3 (en) 2010-06-03

Family

ID=41610895

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/004402 WO2010014236A2 (en) 2008-07-30 2009-07-30 Acylhydrazone-based cleavable linkers

Country Status (1)

Country Link
WO (1) WO2010014236A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2509939A4 (en) * 2009-09-23 2013-09-18 Univ North Carolina Novel n-benzylamide substitued derivatives of 2-(acylamido)acetic acid and 2-(acy-lamido) propionic acids: potent neurological agents
EP3473273A1 (en) * 2011-07-29 2019-04-24 Avelas Biosciences, Inc. Selective delivery molecules and methods of use
WO2016176335A1 (en) 2015-04-27 2016-11-03 Concert Pharmaceuticals, Inc. Deuterated otx-015
WO2020010133A1 (en) * 2018-07-03 2020-01-09 Rutgers, The State University Of New Jersey A luminescent layered composition and a method for using the composition

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5122368A (en) * 1988-02-11 1992-06-16 Bristol-Myers Squibb Company Anthracycline conjugates having a novel linker and methods for their production

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5122368A (en) * 1988-02-11 1992-06-16 Bristol-Myers Squibb Company Anthracycline conjugates having a novel linker and methods for their production

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
AISSAOUI, ABDERRAHIM ET AL.: "Novel Cationic Lipids Incorporating an Acid- Sensitive Acylhydrazone Linker: Synthesis and Transfection Properties", J. MED. CHEM., vol. 47, no. 21, 2004, pages 5210 - 5223 *
FELIX KARTZ ET AL.: "Synthesis of New Maleimide Derivatives of Daunorubicin and Biological Activity of Acid Labile Transferrin Conjugates", BIOORG. MED. CHEM. LETT., vol. 7, no. 5, 1997, pages 617 - 622 *
PAULA C. A. RODRIGUES ET AL.: "Acid-Sensitive Polyethylene Glycol Conjugates of Doxorubicin: Preparation, In Vitro Efficacy and Intracellular Distribution", BIOORG. MED. CHEM., vol. 7, 1999, pages 2517 - 2524 *

Also Published As

Publication number Publication date
WO2010014236A2 (en) 2010-02-04

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