Unlock instant, AI-driven research and patent intelligence for your innovation.

Cell penetrating cyanine-coupled antibodies

A cell and antibody technology, applied in antineoplastic drugs, anti-infective drugs, allergic diseases, etc., can solve problems such as labor-consuming, damage to the structural and functional integrity of cells or antibodies

Active Publication Date: 2018-09-28
CITY OF HOPE
View PDF36 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, delivering antibodies into cells is labor-intensive and can also compromise the structural and functional integrity of the cells or the antibodies themselves

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cell penetrating cyanine-coupled antibodies
  • Cell penetrating cyanine-coupled antibodies
  • Cell penetrating cyanine-coupled antibodies

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach P1

[0277] Embodiment P1. A cell penetrating conjugate having the formula:

[0278]

[0279] in

[0280] Ar 1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted fused ring aryl or substituted or unsubstituted fused ring hetero Aryl;

[0281] Ar 2 is a substituted or unsubstituted cycloalkylene, a substituted or unsubstituted heterocycloalkylene, a substituted or unsubstituted arylene, or a substituted or unsubstituted heterocyclene Aryl;

[0282] L 1 is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene;

[0283] P is a non-cell penetrating protein;

[0284] n is 1 or 2; and

[0285] z 1 and z 2 are independently 1 or 2.

[0286] Embodiment P2. The cell penetrating conjugate of embodiment P1, wherein Ar 1 is a substituted or unsubstituted fused ring aryl or a substituted or unsubstituted fused ring heteroaryl; and Ar 2 is a substituted or unsubstituted fused r...

Embodiment approach P3

[0287] Embodiment P3. The cell penetrating conjugate of Embodiment P1 or P2, wherein the cell penetrating conjugate has the formula:

[0288]

[0289] in

[0290] R 1 , R 2 , R 3 and R 4 independently hydrogen, halogen, CX 3 , -CN, -C(O)OH, -CH 2 C(O)OH, -C(O)NH 2 , -OH, -SH, -NO 2 , -NH 2 , -NHNH 2 , -ONH 2 , -NHC=(O)NHNH 2 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; and

[0291] X is -F, -Cl, -Br or -I.

[0292] Embodiment P4. The cell penetrating conjugate of embodiment P3, wherein R 1 , R 2 , R 3 and R 4 are independently hydrogen or substituted or unsubstituted alkyl.

[0293] Embodiment P5. The cell penetrating conjugate of embodiment P3 or P4, wherein R 1 , R 2 , R 3 and R 4 are independently hydrogen or methyl.

Embodiment approach P6

[0294] Embodiment P6. The cell penetrating conjugate of any one of embodiments P3-P5, wherein R 1 , R 2 and R 3 is methyl.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

Described herein are compositions relating to cell-penetrating conjugates of formula (I) or (IV). The compositions are capable of penetrating cells and recognizing intracellular targets (e.g., STAT3)and are, inter alia, useful for diagnostic and therapeutic purposes.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application No. 62 / 265,727, filed December 10, 2015, which is hereby incorporated by reference in its entirety for all purposes. [0003] Statement of Rights to Inventions Resulting from Federally Sponsored Research and Development [0004] This invention was made with government support under Grant Number RO1CA122976 awarded by the National Institutes of Health. The government has certain rights in this invention. Background of the invention [0005] Antibodies have excellent binding specificity and minimal off-target effects, and due to their ease of production and biological persistence, antibodies have been proven to be effective drug forms. However, many important targets for disease therapy and disease diagnosis are intracellular. Furthermore, delivering antibodies into cells is labor-intensive and can also compromise the structural and functional integrity of t...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C09B23/00
CPCA61K47/6891A61K47/545A61K45/06A61P1/04A61P5/00A61P37/02A61P9/00A61P25/00A61P37/00A61P35/00A61P1/16A61P31/00A61P3/00C09B23/0066C09B23/06C09B23/083C07D403/14
Inventor A·赫尔曼H·于C·拉兹
Owner CITY OF HOPE