IP Library › Granted Patent US 11,452,731
Granted Patent B2
US 11,452,731 · App. 16/418,651 · Granted Sep 27, 2022

Method of treating and preventing loss of cognition

Inventor: Fernand Labrie (Québec, CA)
A61K31/5685A61K31/453A61K31/568
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Quick Facts
Patent No.
US 11,452,731
App. No.
16/418,651
Granted
Sep 27, 2022
Kind
B2
Abstract

Novel methods for reduction or elimination the incidence of hot flushes, vasomotor symptoms, and night sweats while decreasing the risk of acquiring breast, uterine or endometrial cancer and furthermore having beneficial effect by inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes type 2, loss of muscle mass, adiposity, Alzheimer's disease, loss of cognition, loss of memory, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of an amount of a sex steroid precursor, particularly dehydroepiandrosterone (DHEA) and an antiestrogen or a selective estrogen receptor modulator, particularly compounds having the general structure: Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

Claims (11)

1. A method of treating loss of cognition, wherein said loss of cognition is memory loss due to menopause, said method comprising administering to a postmenopausal woman in need of said treatment, (i) an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone-sulfate, androst-5-ene-3β,17β-diol and 4-androstene-3,17-dione, in combination with (ii) an amount of a selective estrogen receptor modulator, wherein the modulator is EM-652 or a pharmaceutically acceptable salt thereof, and wherein said amounts are sufficient to achieve said treatment.

2. The method of claim 1 , where said selective estrogen receptor modulator is:

and wherein the selective estrogen receptor modulator is an optically active compound.

3. The method of claim 1 , wherein the selective estrogen receptor modulator is a EM-652 salt of an acid selected from the group consisting of acetic acid, adipic acid, benzenesulfonic acid, benzoic acid, camphorsulfonic acid, citric acid, fumaric acid, hydroiodic acid, hydrobromic acid, hydrochloric acid, hydrochlorothiazide acid, hydroxy-naphthoic acid, lactic acid, maleic acid, methanesulfonic acid, methyl sulfuric acid, 1,5-naphthalenedisulfonic acid, nitric acid, palmitic acid, pivalic acid, phosphoric acid, propionic acid, succinic acid, sulfuric acid, tartaric acid, terephthalic acid, p-toluenesulfonic acid, and valeric acid.

4. The method of claim 1 , wherein said selective estrogen receptor modulator is:

wherein the selective estrogen receptor modulator is an optically active compound; and wherein the sex steroid precursor is dehydroepiandrosterone.

5. The method of claim 1 , wherein said selective estrogen receptor modulator is intravaginally administered.

6. The method of claim 2 , wherein the selective estrogen receptor modulator is intravaginally administered.

7. The method of claim 1 , wherein the selective estrogen receptor modulator is orally administered.

8. The method of claim 1 , wherein the selective estrogen receptor modulator is percutaneously administered.

9. The method of claim 1 , wherein the amount of selective estrogen receptor modulator decreases the risk of breast, uterine and endometrial cancer normally occurring in said postmenopausal women and to prevent bone loss, osteoporosis, hypertension, insulin resistance, diabetes, obesity and atherosclerosis.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 21, 2019
From: LABRIE, FERNAND, DR.
To: ENDORECHERCHE, INC.
Reel/Frame 049246/0059 →
Continuity (4)
Continuation 13875027 · May 1, 2013
Division 12791174 · Jun 1, 2010
Provisional Application 61187549 · Jun 16, 2009
Related Publication 20190269697A1 · Sep 5, 2019