IP Library Granted Patent US 10,858,354
Granted Patent B2
US 10,858,354 · App. 15/972,863 · Granted Dec 8, 2020

HPTP-Beta inhibitors

Inventors: John Janusz (West Chester, OH); James Copp (Silverthrone, CO); Kevin Peters (Cincinnati, OH)
Assignee: Aerpio Pharmaceuticals, Inc.
C07D417/04
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Quick Facts
Patent No.
US 10,858,354
App. No.
15/972,863
Granted
Dec 8, 2020
Kind
B2
Abstract

Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed.

Claims (21)

1. A compound of formula:

wherein:

Aryl 1 is 4-phenylsulfamic acid;

Aryl 2 is

wherein:

R e is H;

R f heteroaryl that is substituted or unsubstituted;

X is methylene;

L is alkylene, alkenylene, or alkynylene, any of which is substituted or unsubstituted, or together with the nitrogen atom to which L is bound forms an amide linkage, a carbamate linkage, a ureido linkage, or a sulfonamide linkage, or a chemical bond;

R a is alkyl, alkenyl, alkynyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl, any of which is substituted or unsubstituted, or H;

R b is alkyl, alkenyl, alkynyl, aryl, arylalkyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl, any of which is substituted or unsubstituted, or H;

R c is alkyl which is substituted or unsubstituted, or H; and

R d is alkyl which is substituted or unsubstituted, or H,

or a pharmaceutically-acceptable salt, tautomer, or zwitterion thereof.

2. The compound of claim 1 , wherein:

L together with the nitrogen atom to which L is bound forms a carbamate linkage;

R a is alkyl, which is substituted or unsubstituted;

R b is arylalkyl, which is substituted or unsubstituted;

R c is H; and

R d is H.

3. The compound of claim 1 , wherein the compound is:

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 9, 2021
From: AERPIO PHARMACEUTICALS, INC.
To: EYEPOINT PHARMACEUTICALS, INC.
Reel/Frame 057448/0033 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 17, 2020
From: AERPIO THERAPEUTICS LLC
To: AERPIO PHARMACEUTICALS, INC.
Reel/Frame 052432/0789 →
CHANGE OF NAME Recorded Jul 31, 2019
From: AERPIO THERAPEUTICS, INC.
To: AERPIO THERAPEUTICS LLC
Reel/Frame 049924/0450 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 22, 2018
From: JANUSZ, JOHN; COPP, JAMES; PETERS, KEVIN GENE
To: AERPIO THERAPEUTICS, INC.
Reel/Frame 045872/0713 →