IP Library Granted Patent US 9,132,200
Granted Patent B2
US 9,132,200 · App. 14/266,317 · Granted Sep 15, 2015

Oligomer-calcium channel blocker conjugates

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Quick Facts
Patent No.
US 9,132,200
App. No.
14/266,317
Granted
Sep 15, 2015
Kind
B2
Abstract

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.

Claims (17)

1. A compound having the structure:

wherein:

R is hydrogen or lower alkyl;

R 1 is selected from the group consisting of hydrogen, substituted lower alkyl, unsubstituted lower alkyl and —YOYNR 6 R 7 , where each Y is independently lower alkylene and R 6 and R 7 are each independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, cycloalkyl, aryl and alkylaryl;

each Y is independently lower alkylene;

R 3 and R 4 are independently selected from the group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, and —YNR 6 R 7 , where Y is lower alkylene and R 6 and R 7 are each independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, cycloalkyl, aryl and alkylaryl;

R 5 is independently selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, chloro, fluoro and nitro;

R 6 is selected from group consisting of hydrogen, unsubstituted lower alkyl, substituted lower alkyl, cycloalkyl, aryl and alkylaryl;

X is a spacer moiety; and

POLY is a water-soluble oligomer wherein the number of monomers has a number between 2 and 30.

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

3. The compound of claim 2 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).

4. The compound of claim 2 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.

5. The compound of claim 1 , having the structure:

wherein n is an integer of from 2 to 10.

6. The compound of claim 1 , having the structure:

wherein n is an integer of from 2 to 10.

Assignments (4)
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 33105, FRAME 0898 Recorded Oct 14, 2015
From: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
To: NEKTAR THERAPEUTICS
Reel/Frame 036855/0524 →
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 →
SECURITY INTEREST Recorded Jun 9, 2014
From: NEKTAR THERAPEUTICS
To: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 033105/0898 →