The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Sep. 06, 2016

Filed:

Jul. 10, 2015
Applicant:

Yeda Research and Development Co., Ltd., Rehovot, IL;

Inventors:

Yoram Shechter, Rehovot, IL;

Matityahu Fridkin, Rehovot, IL;

Haim Tsubery, Elad, IL;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 207/404 (2006.01); A61K 47/48 (2006.01); C07D 207/416 (2006.01); C07D 207/452 (2006.01); C07D 403/12 (2006.01); A61K 38/26 (2006.01); A61K 38/28 (2006.01); A61K 38/22 (2006.01); A61K 31/7036 (2006.01); A61K 38/17 (2006.01); A61K 38/21 (2006.01); A61K 38/27 (2006.01);
U.S. Cl.
CPC ...
A61K 47/48023 (2013.01); A61K 31/7036 (2013.01); A61K 38/1709 (2013.01); A61K 38/212 (2013.01); A61K 38/22 (2013.01); A61K 38/26 (2013.01); A61K 38/27 (2013.01); A61K 38/28 (2013.01); A61K 47/48215 (2013.01); C07D 207/404 (2013.01); C07D 207/416 (2013.01); C07D 207/452 (2013.01); C07D 403/12 (2013.01);
Abstract

Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.


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