IP Library Granted Patent US 11,731,974
Granted Patent B2
US 11,731,974 · App. 17/066,086 · Granted Aug 22, 2023

N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists

Inventors: Hamid R. Hoveyda (Brussels, BE); Guillaume Dutheuil (Vedrin, BE); Graeme Fraser (Bousval, BE)
Assignee: Ogeda SA
C07D487/04
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Quick Facts
Patent No.
US 11,731,974
App. No.
17/066,086
Granted
Aug 22, 2023
Kind
B2
Abstract

A method for treating and/or preventing polycystic ovary syndrome (PCOS) including the administration, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.

Claims (10)

1. A method for preventing and/or treating moderate hot flashes or severe hot flashes in a patient, wherein the method comprises administering to the patient in need thereof for at least four weeks a pharmaceutically effective amount of the following compound:

wherein the frequency of moderate hot flashes or severe hot flashes in the patient after at least four weeks of treatment is reduced compared to the frequency of moderate hot flashes or severe hot flashes in the patient before at least four weeks of treatment.

2. The method according to claim 1 , wherein the moderate hot flashes or severe hot flashes are related to a condition selected from the group consisting of a perimenopausal condition, a menopausal condition, and a postmenopausal condition, or a combination thereof.

3. The method according to claim 1 , wherein the moderate hot flashes or severe hot flashes are a consequence of hormone therapy which intentionally lowers the level of sex hormones.

4. The method according to claim 3 , wherein the moderate hot flashes or severe hot flashes are selected from the group consisting of therapy-induced moderate hot flashes in breast cancer, therapy-induced severe hot flashes in breast cancer, therapy-induced moderate hot flashes in uterine cancer, therapy-induced severe hot flashes in uterine cancer, therapy-induced moderate hot flashes in prostate cancer, and therapy-induced sever hot flashes in prostate cancer.

5. A method for preventing and/or treating moderate hot flashes or severe hot flashes in a patient, wherein the method comprises administering to the patient in need thereof for at least four weeks a pharmaceutically effective amount of the following compound:

wherein the severity of moderate hot flashes or severe hot flashes in the patient after at least four weeks of treatment is reduced compared to the severity of moderate hot flashes or severe hot flashes in the patient before at least four weeks of treatment.

6. The method according to claim 5 , wherein the moderate hot flashes or severe hot flashes are related to a condition selected from the group consisting of a perimenopausal condition, a menopausal condition, and a postmenopausal condition, or a combination thereof.

7. The method according to claim 5 , wherein the moderate hot flashes or severe hot flashes are a consequence of hormone therapy which intentionally lowers the level of sex hormones.

8. The method according to claim 7 , wherein the moderate hot flashes or severe hot flashes are selected from the group consisting of therapy-induced moderate hot flashes in breast cancer, therapy-induced severe hot flashes in breast cancer, therapy-induced moderate hot flashes in uterine cancer, therapy-induced severe hot flashes in uterine cancer, therapy-induced moderate hot flashes in prostate cancer, and therapy-induced sever hot flashes in prostate cancer.

Assignments (4)
CHANGE OF NAME Recorded Jul 7, 2026
From: OGEDA SA
To: OGEDA NV
Reel/Frame 075187/0533 →
CHANGE OF NAME Recorded Jul 7, 2026
From: OGEDA NV
To: OGEDA BV
Reel/Frame 075187/0614 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 7, 2026
From: OGEDA BV
To: ASTELLAS PHARMA INC.
Reel/Frame 075187/0656 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2023
From: HOVEYDA, HAMID; DUTHEUIL, GUILLAUME; FRASER, GRAEME
To: OGEDA SA
Reel/Frame 063317/0118 →
Priority Claims (3)
EP 13161863 · Mar 29, 2013 · regional
EP 13193025 · Nov 15, 2013 · regional
EP 14154303 · Feb 7, 2014 · regional
Continuity (7)
Continuation 16204390 · Nov 29, 2018
Continuation 15796028 · Oct 27, 2017
Continuation In Part 15371600 · Dec 7, 2016
Continuation In Part 15205304 · Jul 8, 2016
Continuation 14694228 · Apr 23, 2015
Continuation In Part PCTEP2014056367 · Mar 28, 2014
Related Publication 20210094959A1 · Apr 1, 2021