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1. WO2021023876 - GNRH ANTAGONISTS FOR THE TREATMENT OF ESTROGEN-DEPENDENT DISORDERS

Publication Number WO/2021/023876
Publication Date 11.02.2021
International Application No. PCT/EP2020/072301
International Filing Date 07.08.2020
IPC
A61K 31/519 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 15/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders; Contraceptives
A61K 31/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
A61P 5/24 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
24of the sex hormones
CPC
A61K 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
A61K 31/519
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 5/24
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
24of the sex hormones
Applicants
  • OBSEVA S.A. [CH]/[CH]
Inventors
  • GOTTELAND, Jean-Pierre
  • BESTEL, Elke
Agents
  • KATZAROV S.A.
Priority Data
62/884,43708.08.2019US
62/914,06411.10.2019US
63/007,63209.04.2020US
63/048,52606.07.2020US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) GNRH ANTAGONISTS FOR THE TREATMENT OF ESTROGEN-DEPENDENT DISORDERS
(FR) ANTAGONISTES DE GNRH POUR LE TRAITEMENT DE TROUBLES DÉPENDANT DES ŒSTROGÈNES
Abstract
(EN) The present disclosure provides compositions and methods for treating estrogen-dependent disorders, such as disorders of the female reproductive system, including uterine fibroids and endometriosis, among others. 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. Using the compositions and methods described herein, GnRH antagonists may be periodically administered to a patient, such as one or more times per day, week, or month, over the course of an extended treatment period, such as a treatment period having a duration of multiple years. Advantageously, using the compositions and methods of the present disclosure, the GnRH antagonist may be administered to a patient over a lengthy treatment period without inducing adverse side effects, such as a loss in bone mineral density, which is otherwise known to be a risk associated with GnRH antagonism.
(FR) La présente invention concerne des compositions et des procédés de traitement de troubles dépendant des œstrogènes, tels que des troubles du système reproducteur féminin, notamment les fibromes utérins et l'endométriose, entre autres. Les composés décrits dans la description qui peuvent être utilisés pour traiter de telles indications comprennent des antagonistes de l'hormone de libération de la gonadotropine (GnRH). Les antagonistes de la GnRH appropriés utiles en association avec les compositions et les procédés décrits dans la description comprennent des dérivés de thiéno[3,4d]pyrimidine, tels que l'acide 3-[2-fluoro-5-(2,3-difluoro-6-méthoxybenzyloxy)4-méthoxyphényl]-2,4-dioxo-1,2,3,4-tétrahydrothiéno [3,4d]pyrimidine-5-carboxylique et son sel de choline, entre autres. Au moyen de l'utilisation des compositions et des procédés décrits dans la description, des antagonistes de la GnRH peuvent être administrés périodiquement à un patient, par exemple une ou plusieurs fois par jour, semaine ou mois, au cours d'une période de traitement étendue, telle qu'une période de traitement ayant une durée de plusieurs années. Avantageusement, au moyen des compositions et des procédés de la présente invention, l'antagoniste de la GnRH peut être administré à un patient sur une longue période de traitement sans induire d'effets secondaires indésirables, tels qu'une perte de densité minérale osseuse, qui est autrement connue comme étant un risque associé à l'antagonisme de la GnRH.
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