Composition comprising a polymeric reagent

Patent metadata

Field	Value
Publication number	US-9775911-B2
Application number	US-201615170827-A
Country	US
Kind code	B2
Filing date	Jun 1, 2016
Priority date	Jun 16, 2005
Publication date	Oct 3, 2017
Grant date	Oct 3, 2017

Abstract

The present invention provides among other things a composition of a polymeric reagent and an antioxidant, such as butylated hydroxyl toluene.

First claim

What is claimed is:

1. A composition, comprising
(a) a polymeric reagent having the following structure:

wherein
POLY 1 is a first poly(alkylene glycol),
POLY 2 is a second poly(alkylene glycol),
X 1 is a first spacer moiety, and
X 2 is a second spacer moiety, and
(b) an antioxidant.

2. The composition of claim 1 , wherein each of POLY′ and POLY is a poly(ethylene glycol).

3. The composition of claim 2 , wherein each poly(ethylene glycol) has a weight-average molecular weight in the range of from about 120 Daltons to about 6,000 Daltons.

4. The composition of claim 2 , wherein each poly(ethylene glycol) has a weight-average molecular weight in the range of from about 6,000 Daltons to about 100,000 Daltons.

5. The composition of claim 1 , wherein the first spacer moiety is selected from the group consisting of —NH—C(O)—, —NH—C(O)—CH 2 —, —NH—C(O)—CH 2 —CH 2 —, —NH—C(O)—CH 2 —CH 2 —CH 2 —, —NH—C(O)—CH 2 —CH 2 —CH 2 —CH 2 —, —NH—C(O)—CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —, —NH—C(O)—CH 2 —CH 2 —C(O)—, —NH—C(O)—CH 2 —CH 2 —CH 2 —C(O)—, —NH—C(O)—CH 2 —CH 2 —CH 2 —CH 2 —C(O)—, —NH—C(O)—CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —C(O)—, —NH—CH 2 —CH 2 —(OCH 2 CH 2 ) 1-3 —NH—C(O)—, —NH—C(O)—CH 2 —O—, —NH—C(O)—CH 2 —CH 2 —CH 2 —C(O)—NH—CH 2 —CH 2 —, and —NH—C(O)—CH 2 —CH 2 —CH 2 —C(O)—NH—CH 2 —CH 2 —O—, and the second spacer moiety is selected from the group consisting of —NH—C(O)—, —NH—C(O)—CH 2 —, —NH—C(O)—CH 2 —CH 2 —, —NH—C(O)—CH 2 —CH 2 —CH 2 —, —NH—C(O)—CH 2 —CH 2 —CH 2 —CH 2 —, —NH—C(O)—CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —, —NH—C(O)—CH 2 —CH 2 —C(O)—, —NH—C(O)—CH 2 —CH 2 —CH 2 —C(O)—, —NH—C(O)—CH 2 —CH 2 —CH 2 —CH 2 —C(O)—, —NH—C(O)—CH 2 —CH 2 —CH 2 —CH 2 —CH 2 —C(O)—, —NH—CH 2 —CH 2 —(OCH 2 CH 2 ) 1-3 —NH—C(O)—, —NH—C(O)—CH 2 —O—, —NH—C(O)—CH 2 —CH 2 —CH 2 —C(O)—NH—CH 2 —CH 2 —, and —NH—C(O)—CH 2 —CH 2 —CH 2 —C(O)—NH—CH 2 —CH 2 —O—.

6. The composition of claim 1 , wherein the polymeric reagent corresponds to the following formula:

wherein each (n) is from 4 to 1500.

7. The composition of claim 1 , wherein the polymeric reagent corresponds to the following formula:

wherein each (n) is from 4 to 1500.

8. The composition of claim 1 , wherein the antioxidant is butylated hydroxyl toluene.

Assignees

• Nektar Therapeutics

Inventors

• Bentley Michael D
• Culbertson Sean M
• Mcmanus Samuel P

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• C08G65/3348

  containing nitrogen in addition to sulfur · CPC title

• C08G65/33396

  having oxygen in addition to nitrogen · CPC title

• C08G65/48

  Polymers modified by chemical after-treatment · CPC title

• A61K47/50 Primary

  the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates · CPC title