IP Library › Granted Patent US 12,721,861
Granted Patent B2
US 12,721,861 · App. 17/602,110 · Granted Sep 1, 2026

Delivery and retention of active agents within the skin

Inventors: Samir Mitragotri (Lexington, MA); Eric Spengler (Cambridge, MA); Douglas Levinson (Sherborn, MA); Douglas R. Vogus (Cambridge, MA)
Assignee: Fount Bio, Inc.
A61K31/728A61K8/735A61K47/545A61Q19/00A61K2800/413
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Quick Facts
Patent No.
US 12,721,861
App. No.
17/602,110
Granted
Sep 1, 2026
Kind
B2
Abstract

The present application describes the synthesis, formulation and uses of systems comprising agents capable of penetrating skin.

Claims (21)

1 . A system comprising a penetrating agent having a structure of formula (I-a):

or pharmaceutically acceptable salt thereof,

wherein

A is or comprises a glycosaminoglycan;

L is selected from an optionally substituted C 1-6 alkylene chain wherein one, two, or three methylene units of L are optionally and independently replaced by —NH—, —O—, —S— or —C(O)—, —NH—, —O—, —S—, —S(O)—, —S(O) 2 —, —C(O)—, polyethylene glycol, and a moiety which results from a click reaction, nucleophilic addition, or Michael addition;

R 1 is independently —H, halogen, —CN, optionally substituted C 1-6 aliphatic, optionally substituted 5- to 10-membered heterocyclyl, optionally substituted 6- to 10-membered aryl, or optionally substituted 5- to 10-membered heteroaryl;

R 2 is —H, halogen, —CN, optionally substituted C 1-6 aliphatic, optionally substituted 5- to 10-membered heterocyclyl, optionally substituted 6- to 10-membered aryl, or optionally substituted 5- to 10-membered heteroaryl; and

m is 1-3.

2 . The system of claim 1 , wherein the penetrating agent has the structure of formula (I-b):

or pharmaceutically acceptable salt thereof.

3 . The system of claim 1 , wherein the penetrating agent has the structure of formula (I-d):

or pharmaceutically acceptable salt thereof.

4 . The system of claim 1 , wherein m is greater than 1.

5 . The system of claim 1 , wherein L is degradable under biological conditions.

6 . The system of claim 1 , wherein the penetrating agent has the structure of formula (I-c):

or pharmaceutically acceptable salt thereof.

7 . The system of claim 1 , wherein the glycosaminoglycan is selected from: hyaluronic acid, heparan sulphate, heparin, chondroitin sulphate, dermatan sulphate, and keratan sulphate.

8 . The system of claim 1 , wherein the glycosaminoglycan is or comprises hyaluronic acid.

9 . The system of claim 1 , wherein the glycosaminoglycan is a glycosaminoglycan-based protein glycan.

10 . The system of claim 1 , wherein the glycosaminoglycan is a glycosaminoglycan-based protein glycan selected from versican, perlecan, glypican, syndecan, and decorin.

11 . The system of claim 1 , wherein the penetrating agent is characterized by a particular degree of lipophilicity sufficient to enhance penetration and/or retention of the penetrating agent across skin when applied to a surface thereof, relative to that observed for A alone.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 12, 2022
From: MITRAGOTRI, SAMIR; SPENGLER, ERIC; LEVINSON, DOUGLAS; VOGUS, DOUGLAS R.
To: FOUNT BIO, INC.
Reel/Frame 058630/0412 →
Continuity (2)
Provisional Application 62836402 · Apr 19, 2019
Related Publication 20220175819A1 · Jun 9, 2022
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