IP Library Granted Patent US 8,889,638
Granted Patent B2
US 8,889,638 · App. 13/166,796 · Granted Nov 18, 2014

Stimulus-triggered prodrugs

Inventors: Seth M. Cohen (San Marcos, CA); Jody L. Major Jourden (Atlanta, GA)
Assignee: The Regents of the University of California
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Quick Facts
Patent No.
US 8,889,638
App. No.
13/166,796
Granted
Nov 18, 2014
Kind
B2
Abstract

Set forth herein, inter alia, are compositions and methods for treating diseases with prodrugs. Provided herein are prodrug compositions for inhibiting the function of proteins, compositions and methods for treating diseases associated with oxidative compounds, oxidatively-sensitive prodrugs of inhibitors of metalloproteases. and methods of inhibiting metalloproteases using oxidatively-sensitive prodrugs.

Claims (23)

1. A compound of the formula:

wherein,

A is an anticancer drug moiety;

R 1 is —B(OH) 2 or an ROS-reactive boronic ester; and

z is an integer from 1 to 5.

2. The compound of claim 1 , comprising a metal binding moiety.

3. The compound of claim 2 , wherein said metal binding moiety is a zinc binding moiety.

4. The compound of claim 1 , wherein said ROS-reactive boronic ester is capable of reacting with hydrogen peroxide.

5. The compound of claim 1 of formula (I) or (Ia), wherein A is

wherein

R 3 is independently halogen, —CN, —N(O) m , —NR 7 R 8 , —C(O)R 9 , —C(O)—OR 10 , —C(O)NR 11 R 12 , —OR 13 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

m is an integer from 1 to 2;

R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , and R 13 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R 4 is independently hydrogen, or substituted or unsubstituted alkyl;

R 5 is independently hydrogen, or substituted or unsubstituted alkyl;

a, e, and f are independently an integer from 0 to 4;

b and d are independently an integer from 0 to 3;

c is an integer from 0 to 5;

g is an integer from 0 to 6;

and

X is ═O or ═S.

6. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient.

7. The compound of claim 1 , wherein A is not covalently bound to —B(OH) 2 or an ROS-reactive boronic ester or salts thereof.

Assignments (1)
CONFIRMATORY LICENSE Recorded Mar 10, 2015
From: UNIVERSITY OF CALIFORNIA SAN DIEGO
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 035177/0982 →
Continuity (2)
Provisional Application 61357477 · Jun 22, 2010
Related Publication 20110312905A1 · Dec 22, 2011