IP Library › Granted Patent US 12,280,052
Granted Patent B2
US 12,280,052 · App. 17/289,418 · Granted Apr 22, 2025

Compositions and methods for the treatment of adenomyosis and rectovaginal endometriosis

Inventors: Jean-Pierre Gotteland (Geneva, CH); Ernest Loumaye (Cologny, CH)
Assignee: Kissei Pharmaceutical Co., Ltd.
A61K31/519A61K31/4184A61K31/4439A61K31/513A61K31/55A61K31/565A61K31/567A61K31/57A61K31/573A61K31/585A61K47/541A61P15/00
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Quick Facts
Patent No.
US 12,280,052
App. No.
17/289,418
Granted
Apr 22, 2025
Kind
B2
Abstract

The present disclosure provides compositions and methods for treating endometrial growth disorders in a patient, such as a human patient, and particularly pre-menopausal female human patients. Exemplary disorders that may be treated using the compounds and therapeutic regimens described herein include adenomyosis and rectovaginal endometriosis. The compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others.

Claims (12)

1. A method of treating adenomyosis in a human patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of a compound, 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid, represented by formula (VI)

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is administered to the patient in the form of a pharmaceutically acceptable salt thereof.

3. The method of claim 2 , wherein the pharmaceutically acceptable salt is a choline salt of (VI), choline 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylate.

4. The method of claim 1 , wherein the compound is administered to the patient orally.

5. The method of claim 1 , wherein the compound is administered to the patient one or more times daily.

6. The method of claim 5 , wherein the compound is administered to the patient once daily.

7. The method of claim 1 , wherein the compound is administered to the patient in an amount of about 100 mg per day.

8. The method of claim 1 , wherein the compound is administered to the patient in an amount of about 200 mg per day.

9. The method of claim 1 , wherein the patient exhibits a reduction in uterine volume following administration of the compound to the patient.

10. The method of claim 9 , wherein the reduction in uterine volume is assessed by way of MRI or transvaginal ultrasound (TVUS).

11. The method of claim 1 , wherein the patient exhibits a reduction in pelvic pain, dysmenorrhea, dyspareunia, and/or dyschezia following administration of the compound to the patient.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 21, 2022
From: OBSEVA S.A.
To: KISSEI PHARMACEUTICAL CO., LTD.
Reel/Frame 061500/0951 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 7, 2021
From: GOTTELAND, JEAN-PIERRE; LOUMAYE, ERNEST
To: OBSEVA S.A.
Reel/Frame 056777/0202 →
Continuity (2)
Provisional Application 62752100 · Oct 29, 2018
Related Publication 20220117969A1 · Apr 21, 2022
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