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1. WO2021023877 - COMPOSITIONS AND METHODS FOR THE TREATMENT OF ESTROGEN-DEPENDENT DISORDERS

Publication Number WO/2021/023877
Publication Date 11.02.2021
International Application No. PCT/EP2020/072302
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
A61K 31/565 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
565not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 31/57 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
57substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
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
CPC
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
A61K 31/565
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
565not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
A61K 31/57
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
57substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
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
Applicants
  • OBSEVA S.A. [CH]/[CH]
Inventors
  • GOTTELAND, Jean-Pierre
  • BESTEL, Elke
Agents
  • KATZAROV S.A.
Priority Data
62/884,42608.08.2019US
63/047,03801.07.2020US
63/048,42706.07.2020US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) COMPOSITIONS AND METHODS FOR THE TREATMENT OF ESTROGEN-DEPENDENT DISORDERS
(FR) COMPOSITIONS ET MÉTHODES DE 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-methoxyphenyI]-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. Advantageously, using the dosing schedules of the present disclosure, the periodic administration the GnRH antagonist may be temporarily halted, allowing a patient to recover any lost bone mineral density, without an accompanying return in the patient's symptoms.
(FR) La présente invention concerne des compositions et des méthodes de traitement de troubles dépendant des œstrogènes, tels que des troubles du système reproducteur féminin comprenant, entre autres, les fibromes utérins et l'endométriose. Les composés de la présente invention 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. À l'aide des compositions et des procédés de la présente invention, des antagonistes de GnRH peuvent être administrés périodiquement à un patient, tel qu'une ou plusieurs fois par jour, par semaine ou par mois. Avantageusement, à l'aide des programmes de dosage de la présente invention, l'administration périodique de l'antagoniste de GnRH peut être temporairement arrêtée, permettant à un patient de récupérer toute densité minérale osseuse perdue, sans retour d'accompagnement dans les symptômes du patient.
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