IP Library Granted Patent US 10,251,870
Granted Patent B2
US 10,251,870 · App. 15/556,055 · Granted Apr 9, 2019

Method for treating obesity, diabetes, cardiovascular and kidney diseases by regulating GPR30/GPER activity

Inventors: Eric R. Prossnitz (Albuquerque, NM); Matthias Barton (Zurich, CH); Matthias R. Meyer (Stallikon, CH)
Assignee: STC.UNM
A61K31/436A61K31/16A61K31/435A61K31/437A61K31/4355A61K31/7088A61K38/28G01N2800/042
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Quick Facts
Patent No.
US 10,251,870
App. No.
15/556,055
Granted
Apr 9, 2019
Kind
B2
Abstract

The current invention is in the field of molecular biology/pharmacology and provides methods of using compounds that modulate the effects of GPR30/GPER for treating obesity and diabetes (preferably agonists) as well as disease states and/or conditions that result from excessive formation of reactive oxygen species (preferably antagonists). These compounds may function as agonists and/or antagonists of the disclosed estrogen receptor and/or modulate the expression/upregulation of nox and nox-associated reactive oxygen species (ROS).

Claims (12)

1. A method of treating or reducing the likelihood of a disease state or condition in a patient in which excessive production or formation of Nox (NADPH oxidase) isoforms leads to excessive ROS production or formation that mediates said disease state or condition comprising administering to said patient a compound which inhibits and/or reduces the production and/or formation of said Nox (NADPH oxidase) isoforms in said patient, wherein said disease state or condition is a cardiovascular disease state or condition, said cardiovascular disease state or condition is atherosclerosis, myocardial infarction, stroke, arterial hypertension, coronary artery disease, restenosis after balloon angioplasty, ischemia/reperfusion injury after myocardial or cerebral infraction, hypertrophic cardiomyopathy, heart failure or heart failure associated with aging and said compound is according to the chemical structure:

Where R is H or an isopropyl group, or

a pharmaceutically acceptable salt or mixture thereof.

2. The method according to claim 1 wherein R is an isopropyl group.

3. The method according to claim 1 wherein said compound is a pharmaceutically acceptable salt.

4. The method according to claim 1 wherein R is H.

5. The method according to claim 4 wherein said compound is a pharmaceutically acceptable salt.

6. The method according to claim 1 wherein said disease state or condition is heart failure.

7. The method according to claim 2 wherein said disease state or condition is heart failure.

8. The method according to claim 3 wherein said disease state or condition is heart failure.

9. The method according to claim 4 wherein said disease state or condition is heart failure.

10. The method according to claim 5 wherein said disease state or condition is heart failure.

Assignments (2)
CHANGE OF NAME Recorded Nov 18, 2020
From: STC.UNM
To: UNM RAINFOREST INNOVATIONS
Reel/Frame 054403/0714 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 4, 2019
From: BARTON, MATTHIAS; MEYER, MATTHIAS R.
To: REGENTS OF THE UNIVERSITY OF NEW MEXICO
Reel/Frame 048232/0709 →
Continuity (4)
Provisional Application 62217434 · Sep 11, 2015
Provisional Application 62136820 · Mar 23, 2015
Provisional Application 62129224 · Mar 6, 2015
Related Publication 20180055826A1 · Mar 1, 2018
Cited By (1)
US 12,378,243