IP Library Granted Patent US 8,466,276
Granted Patent B2
US 8,466,276 · App. 12/918,780 · Granted Jun 18, 2013

Oligomer conjugates of heteropentacyclic nucleosides

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Quick Facts
Patent No.
US 8,466,276
App. No.
12/918,780
Granted
Jun 18, 2013
Kind
B2
Abstract

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.

Claims (21)

1. A compound having the following structure:

wherein:

R 2 is hydrogen or hydroxyl;

R 3 is hydroxyl when R 2 is hydrogen and R 3 is hydrogen when R 2 is hydroxyl;

(a) is two;

X is an amide linkage; and

each POLY is independently a water-soluble, non-peptidic oligomer,

and 5′-phosphates and 3′,5′-cyclic phosphates thereof and ammonium and alkali metal salts of each of the 5′-phosphates and 3′,5′-cyclic phosphates.

2. The compound of claim 1 , wherein the weight average molecular weight of each water-soluble, non-peptidic oligomer is less than 400 Daltons.

3. The compound of claim 1 , wherein each water-soluble, non-peptidic oligomer is a poly(alkylene oxide).

4. The compound of claim 3 , wherein each poly(alkylene oxide) is a poly(ethylene oxide).

5. The compound of claim 4 , wherein the water-soluble, non-peptidic oligomer has a number of repeating monomers in the range of from 1 to 30.

6. The compound of claim 5 , wherein the water-soluble, non-peptidic oligomer has a number of repeating monomers in the range of from 1 to 10.

7. The compound of claim 3 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.

8. A composition comprising (i) a compound of claim 1 , and (ii) a pharmaceutically acceptable excipient.

9. A composition of matter comprising a compound of claim 1 present in a dosage form.

10. The compound of claim 1 , wherein the compound is selected from a compound of the formula

wherein for each occurrence, n is an integer from 1 to 15.

11. The compound of claim 10 , wherein for each occurrence, n is an integer from 1 to 10.

12. The compound of claim 11 , wherein for each occurrence, n is 5.

13. A composition comprising (i) a compound of claim 10 , and (ii) a pharmaceutically acceptable excipient.

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 →
GRANT OF SECURITY INTEREST Recorded Jul 17, 2012
From: NEKTAR THERAPEUTICS
To: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 028571/0141 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 27, 2010
From: DENG, BO-LIANG; RILEY, TIMOTHY A.; RIGGS-SAUTHIER, JENNIFER
To: NEKTAR THERAPEUTICS
Reel/Frame 025207/0214 →