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Conjugates containing hydrophilic spacer linkers

a technology of hydrophilic spacer linkers and conjugates, which is applied in the direction of drug compositions, peptides/protein ingredients, antibacterial agents, etc., can solve the problems of complex approaches and adverse side effects of the currently available chemotherapeutic agents and radiation therapy regimens

Pending Publication Date: 2014-03-13
ENDOCTYE INC
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

These conjugates enable targeted delivery of therapeutic agents to pathogenic cells, reducing toxicity to normal cells by utilizing hydrophilic spacer linkers that favor renal clearance over hepatic uptake, thereby enhancing the therapeutic index and minimizing adverse side effects.

Problems solved by technology

However, many of the currently available chemotherapeutic agents and radiation therapy regimens have adverse side effects because they work not only to destroy pathogenic cells, but they also affect normal host cells, such as cells of the hematopoietic system.
However, these approaches have been complicated by the difficulties in defining tumor-specific antigens.

Method used

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  • Conjugates containing hydrophilic spacer linkers
  • Conjugates containing hydrophilic spacer linkers
  • Conjugates containing hydrophilic spacer linkers

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[0315]General Method 2 for Preparing Conjugates having a hydrophilic spacer linker (one-pot). Illustrated with preparation of EC0543. DIPEA (7.8 μL) and isobutyl chloroformate (3.1 μL) were added with the help of a syringe in tandem into a solution of tubulysin A (18 mg) in anhydrous EtOAc (0.50 mL) at −15° C. After stirring for 35 minutes at −15° C. under argon, to the reaction mixture was added a solution of EC0311 (5.8 mg) in anhydrous EtOAc (0.50 mL). The cooling was removed and the reaction mixture was stirred under argon for an additional 45 minutes, concentrated, vacuumed, and the residue was dissolved in THF (2.0 mL). Meanwhile, EC0488 (40 mg) was dissolved in deionized water (bubbled with argon for 10 minutes prior to use) and the pH of the aqueous solution was adjusted to 6.9 by saturated NaHCO3. Additional deionized water was added to the EC0488 solution to make a total volume of 2.0 mL and to which was added immediately the THF solution containing the activated tubulysin...

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Abstract

Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and / or treating diseases and disease states caused by pathogenic cell populations.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of priority under 35 U.S.C. §119(e) of U.S. provisional patent application Ser. Nos. 60 / 946,092 and 61 / 036,186, filed Jun. 25, 2007 and Mar. 13, 2008, respectively; the disclosures of which are incorporated herein in their entirety by reference.TECHNICAL FIELD[0002]The present invention relates to compositions and methods for use in targeted drug delivery. More particularly, the invention is directed to cell-surface receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations and to methods and pharmaceutical compositions that use and include such conjugates.BACKGROUND[0003]The mammalian immune system provides a means for the recognition and elimination of tumor cells, other pathogenic cells, and invading foreign pathogens. While the immune system normally provides a strong line of defense, there are many instanc...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/48
CPCA61K47/4813A61K47/48338A61K47/65A61K47/60A61K47/545C07H15/24C07K9/003A61P31/00A61P31/04A61P31/10A61P31/12A61P33/00A61P33/02A61P33/04A61P33/10A61P35/00A61P35/02
Inventor LEAMON, CHRISTOPHER P.VLAHOV, IONTCHO R.SANTHAPURAM, HARI KRISHNA R.KLEINDL, PAUL J.WANG, KEVIN YUYOU, FEI
Owner ENDOCTYE INC
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