US2015079658A1PendingUtilityA1

Activated Polyoxazolines and Conjugates and Compositions Comprising the Same

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Assignee: SERINA THERAPEUTICS INCPriority: Feb 28, 2007Filed: Nov 21, 2014Published: Mar 19, 2015
Est. expiryFeb 28, 2027(~0.6 yrs left)· nominal 20-yr term from priority
Inventors:J Milton HarrisMichael D. BentleyKunsang YoonZhihao FangFrancesco Maria VeroneseTacey X. ViegasAnna Mero
C07K 14/62C07K 7/08C07K 14/47C12N 9/96C07K 14/505C07K 14/535A61K 38/193A61K 38/1816A61K 38/10C08G 69/48A61K 47/59A61K 31/728A61K 38/33A61K 31/727C12Y 302/01017A61K 38/1719A61K 38/42A61K 38/27A61K 38/47
66
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Claims

Abstract

The present disclosure provides POZ derivatives having a range of active functional groups allowing conjugation of POZ derivatives to a variety of target molecules under a wide range of reaction conditions to produce a hydrolytically stable target molecule-POZ conjugate. Furthermore, the present disclosure provides novel methods of synthesis for the disclosed POZ derivatives and hydrolytically stable target molecule-POZ conjugates created using the disclosed terminally activated monofunctional POZ derivatives. In one embodiment, the POZ derivative is a terminally activated monofunctional POZ derivative.

Claims

exact text as granted — not AI-modified
What is claimed: 
     
         1 . A hydrolytically stable target molecule-POZ conjugate of the general formula POZ-B-TM, wherein,
 POZ is a mono-functional POZ compound;   B is a hydrolytically stable linkage formed between the POZ compound and the target molecule; and   TM is a polypeptide target molecule.   
     
     
         2 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein the mono-functional POZ compound is a POZ polymer having a single active functional group on a terminal end thereof, minus any leaving groups eliminated during the reaction of the active functional group on the POZ compound with a binding partner on TM. 
     
     
         3 . The hydrolytically stable target molecule-POZ conjugate of  claim 2 , wherein the POZ polymer has the structure R 1 -[N(COR 7 )CH 2 CH 2 ] n , wherein R 1  is hydrogen, an unsubstituted or substituted alkyl, alkenyl or aralkyl group and R 7  is independently selected for each repeating unit from an unsubstituted or substituted alkyl, alkenyl or aralkyl group and n is an integer from 3 to 1000. 
     
     
         4 . The hydrolytically stable target molecule-POZ conjugate of  claim 1  wherein the polypeptide contains an available amino group. 
     
     
         5 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein the polypeptide contains an available thiol group. 
     
     
         6 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein B is an amide linkage. 
     
     
         7 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein B is a thioether linkage. 
     
     
         8 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein B is an amine linkage. 
     
     
         9 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein the polypeptide is Dynorphin A 
     
     
         10 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein the polypeptide is lysozyme. 
     
     
         11 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein the polypeptide is insulin. 
     
     
         12 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein the polypeptide is granulocyte macrophage colony stimulating factor. 
     
     
         13 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein the polypeptide is apomyoglobin. 
     
     
         14 . The hydrolytically stable target molecule-POZ conjugate of  claim 1 , wherein the polypeptide is erythropoietin.

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