IP Library Granted Patent US 8,741,858
Granted Patent B2
US 8,741,858 · App. 12/676,128 · Granted Jun 3, 2014

Oligomer-nucleoside phosphate conjugates

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Quick Facts
Patent No.
US 8,741,858
App. No.
12/676,128
Granted
Jun 3, 2014
Kind
B2
Abstract

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble, non-peptidic oligomer. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.

Claims (16)

1. A compound having the following structure:

wherein:

X is a linker when present; and

POLY is a poly(ethylene oxide) oligomer having an end capping group selected from hydroxyl and methoxy end-capping groups.

2. The compound of claim 1 , wherein the poly(ethylene oxide) oligomer is made of between 2 and 30 monomers.

3. The compound of claim 2 , wherein the poly(ethylene oxide) oligomer is made of between 2 and 10 monomers.

4. The compound of claim 1 , wherein the poly(ethylene oxide) oligomer is capped with a methoxy end-capping group.

5. The compound of claim 1 , wherein X is an ether linker.

6. The compound of claim 1 , wherein X is an ester or a phosphoester linker.

7. A composition comprising a compound of claim 1 , and optionally, a pharmaceutically acceptable excipient.

8. A composition of matter comprising a compound of claim 1 , wherein the compound is present in a dosage form.

9. A method of treating cancer, comprising administering a compound of claim 1 to a subject in need thereof.

10. The compound of claim 1 , having the following structure

wherein n is selected from an integer from 2 to 10.

11. The compound of claim 10 , wherein n is selected from 3 and 7.

12. The method of claim 9 , wherein the cancer is selected from breast cancer, colon cancer, pancreatic cancer, lung cancer, and ovarian cancer.

Assignments (5)
RELEASE OF SECURITY INTEREST Recorded Apr 17, 2020
From: TC LENDING, LLC, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 053180/0009 →
RELEASE OF SECURITY INTEREST RECORDED AT REEL 28571, FRAME 0141 Recorded Oct 14, 2015
From: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 036866/0700 →
GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded Oct 6, 2015
From: NEKTAR THERAPEUTICS
To: TC LENDING, LLC, AS COLLATERAL AGENT
Reel/Frame 036796/0562 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 18, 2012
From: REN, ZHONGXU; RIGGS-SAUTHIER, JENNIFER; RILEY, TIMOTHY A.; VANDERVEEN, LAURIE A.; HAMMONS, AARON S.
To: NEKTAR THERAPEUTICS
Reel/Frame 028579/0001 →
GRANT OF SECURITY INTEREST Recorded Jul 17, 2012
From: NEKTAR THERAPEUTICS
To: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 028571/0141 →