IP Library Granted Patent US 9,750,749
Granted Patent B2
US 9,750,749 · App. 15/061,727 · Granted Sep 5, 2017

Methods of treating thyroid eye disease

Inventors: Richard P. Phipps (Pittsford, NY); Naxin Guo (Rochester, NY); Steven Feldon (Rochester, NY)
Assignee: University of Rochester
A61K31/557A61K31/166A61K31/201A61K31/403A61K31/4439A61K31/506A61K31/519A61K31/5575A61K31/713A61K31/7105C12N15/1137A61K9/0048C12N2310/14C12N2320/31Y10S514/912
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Quick Facts
Patent No.
US 9,750,749
App. No.
15/061,727
Granted
Sep 5, 2017
Kind
B2
Abstract

The present invention relates to a methods and compositions for the treatment of and management of symptoms for thyroid eye disease. The methods include administering to a patient having thyroid eye disease an agent that interferes with hyaluronan synthesis in an amount that is effective to inhibit hyaluronan synthesis in a retro-ocular space. The pharmaceutical compositions that includes a carrier suitable for ophthalmic delivery and an agent that interferes with hyaluronan synthesis. Combination therapies are also disclosed.

Claims (7)

1. A method of treating thyroid eye disease comprising:

selecting a patient having thyroid eye disease and

administering to the selected patient a composition comprising an agent that interferes with hyaluronan synthesis in an amount that is effective to inhibit hyaluronan synthesis in a retro-ocular space, wherein the agent is 4-benzhydryloxy-1-[3-(1H-tetrazol-5-yl)-propyl]-piperidine (HQL-79), ethyl 3-(2-(3-fluorophenyl)pyrimidine-5-carboxamido)pyrrolidine-1-carboxylate, N-(1-(7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)pyrrolidin-3-yl)-2-(3-fluorophenyl)pyrimidine-5-carboxamide, 2-(3-fluorophenyl)-N-{1-[(methylamino)carbonyl]piperidin-4-yl}pyrimidine-5-carboxamide, 2-(3-fluorophenyl)-N-[1-(6-methyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-yl)pyrrolidin-3-yl]pyrimidine-5-carboxamide, or 2-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyrimidine-5-carboxamide.

2. The method according to claim 1 , wherein the composition comprises a PPARγ ligand, wherein the PPARγ ligand is 15-deoxy-Δ12,14-Prostaglandin J2 or a thiazolidinedione.

3. The method according to claim 1 , wherein said administering is carried out by injecting the agent into the retro-ocular space or application of a composition comprising the agent onto a surface of the patient's eye.

4. The method according to claim 1 , wherein the composition is a pharmaceutical composition further comprising a carrier selected from the group consisting of a liquid, suspension, polymeric delivery vehicle, mucoadhesive substance, and nanosphere.

5. The method according to claim 1 , wherein the agent that interferes with hyaluronan synthesis is 4-benzhydryloxy-1-[3-(1H-tetrazol-5-yl)-propyl]-piperidine (HQL-79).

Assignments (1)
CONFIRMATORY LICENSE Recorded Oct 13, 2016
From: UNIVERSITY OF ROCHESTER
To: NATIONAL INSTITUTES OF HEALTH - DIRECTOR DEITR
Reel/Frame 040337/0965 →
Continuity (3)
Division 13099991 · May 3, 2011
Provisional Application 61330742 · May 3, 2010
Related Publication 20160199386A1 · Jul 14, 2016