IP Library Granted Patent US 9,527,793
Granted Patent B2
US 9,527,793 · App. 14/361,993 · Granted Dec 27, 2016

Mandelic acid condensation polymers

Inventors: Robert A. Anderson, Jr. (Chicago, IL); Xiao-Hui Diao (Chicago, IL); Lourens J. D. Zaneveld (Sao Paulo, BR); Calvin J. Chany, II (Dubuque, IA); Aleksej Krunic (Chicago, IL); Donald P. Waller (Oak Brook, IL); Duane L. Venton (Lombard, IL); Sanjay Jain (Pune, IN)
Assignees: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS; RUSH UNIVERSITY MEDICAL CENTER
C07C59/50C07C51/347C07C59/48C07C67/465C07C69/616C07C2101/16
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Quick Facts
Patent No.
US 9,527,793
App. No.
14/361,993
Granted
Dec 27, 2016
Kind
B2
Abstract

Disclosed herein are compounds and compositions useful for reducing the risk of infection. In particular, disclosed herein are mandelic acid condensation polymers, compositions comprising such compounds, processes for producing such compounds, and methods of using such compounds.

Claims (25)

1. A polymer comprising a distribution of compounds of formula (I)

or a pharmaceutically acceptable salt, ester, amide, or prodrug form thereof, wherein R 1 , R 2 , and R 3 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycle, heteroaryl, aryl, and counterion;

R 4 is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycle, heteroaryl, and aryl;

R 5 , R 6 , and R 7 are each independently selected from the group consisting of alkyl, alkoxy, and halogen;

n is an integer greater than zero;

x, y, and z are each an integer independently selected from the group consisting of 0, 1, 2, 3, and 4;

and wherein the polymer is produced by a process comprising:

cooling a strong acid to a temperature below 0° C. in the absence of solvent;

adding mandelic acid or a mandelic acid derivative to the strong acid; and

isolating the polymer.

2. The polymer of claim 1 , wherein the strong acid is cooled to a temperature below −10° C.

3. The polymer of claim 1 , wherein the strong acid is cooled to a temperature below −30° C.

4. The polymer of claim 1 , wherein the mandelic acid or mandelic acid derivative is added over a period of about 30 minutes.

5. The polymer of claim 1 , wherein the reaction mixture is maintained at a temperature ranging from about −35° C. to about −30° C. for a period of about 1 hour.

6. The polymer of claim 1 , wherein the strong acid is concentrated sulfuric acid.

7. The polymer of claim 1 , wherein the process is conducted under neat reaction conditions.

8. The polymer of claim 1 , wherein the compounds have a structure of formula (3a):

and wherein the isolated polymer has a melting point (mp) of 205-206° C. and demonstrates NMR peaks as follows: 1 H NMR (DMSO-d 6 ): δ 7.35-7.02 (m), 5.23 (br, s), 5.15-4.75 (m), 3.41 (br, s), and 13 C NMR (DMSO-d 6 ): δ 174.09, 140.23, 139.72, 138.85, 138.25, 129.38, 127.96, 56.76.

9. The polymer of claim 1 , wherein the compounds have a structure of formula (5a):

and wherein the isolated polymer has a melting point (mp) of 125-126° C. and demonstrates NMR peaks as follows: 1 H NMR (DMSO-d 6 ): δ 7.26-6.96 (m), 5.30 (s), 5.05-4.80 (m), 3.76-3.46 (m).

10. The polymer of claim 1 , wherein the compounds have a structure of formula (7a):

and wherein the isolated polymer has a melting point (mp) of 320-321° C.

11. A method for protecting an individual from contracting a sexually transmitted disease through contact with a bodily fluid, said method comprising applying to the body or portion of the body of the individual an effective amount of a protective agent, wherein the protective agent comprises a compound according to claim 1 .

12. A method of reducing the risk of transmission of a sexually transmitted pathogen to a human subject, comprising contacting the pathogen or cells susceptible to infection by the pathogen with an effective amount of a compound according to claim 1 , thereby reducing the risk of transmission of the pathogen.

13. The method of claim 11 , wherein the sexually transmitted disease is HIV/AIDS.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 9, 2015
From: ANDERSON, ROBERT A., JR.; DIAO, XIAO-HUI; ZANEVELD, LOURENS J.D.; CHANY, CALVIN J., II
To: RUSH UNIVERSITY MEDICAL CENTER
Reel/Frame 036045/0522 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 9, 2015
From: KRUNIC, ALEKSEJ; WALLER, DONALD P.; VENTON, DUANE L.; JAIN, SANJAY
To: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Reel/Frame 036046/0186 →
CONFIRMATORY LICENSE Recorded May 15, 2015
From: UNIVERSITY OF ILLINOIS AT CHICAGO
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 035685/0819 →
Continuity (2)
Provisional Application 61566441 · Dec 2, 2011
Related Publication 20140371310A1 · Dec 18, 2014