N-MALEIMIDYL POLYMER DERIVATIVES

• US 20190330422A1
• Filed: 07/02/2019
• Published: 10/31/2019
• Est. Priority Date: 02/22/2000
• Status: Active Grant

• Current Assignee: Nektar Therapeutics Incorporated
• Original Assignee: Nektar Therapeutics Incorporated
• Inventors: Shen, Xiaoming
• Granted Patent: US 10,774,181 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/74 Synthetic polymeric materials
• CPC Class Codes: A61K 47/58 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
• CPC Class Codes: A61K 47/60 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
• CPC Class Codes: A61K 47/65 Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
• CPC Class Codes: C08G 65/00 Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
• CPC Class Codes: C08G 65/33337 cyclic
• CPC Class Codes: C08G 65/33396 having oxygen in addition to nitrogen
• CPC Class Codes: C08G 65/48 Polymers modified by chemical after-treatment

Abstract

The invention is directed to multi-functional N-maleimidyl polymer derivatives comprising a water soluble and non-peptidic polymer backbone having a terminal carbon, such as a poly(alkylene glycol), the terminal carbon of the polymer backbone being directly bonded to the nitrogen atom of a N-maleimidyl moiety without a linking group therebetween. The invention also provides two methods of preparing such linkerless N-maleimidyl polymer derivatives.

Claims

1. A multi-functional N-maleimidyl polymer derivative having the formula:

X—

CH₂CH₂O—

(CH₂CH₂O)_n—

CH₂CH₂-L

wherein;

L is the point of bonding to the nitrogen atom of the N-maleimidyl moiety;

X is amine; and

n is about 20 to about 4000.