Abstract: The invention provides ?-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1?-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as preterm labor at the early gestational stage by the administration of these substances to a patient in need of treatment.
Type:
Grant
Filed:
January 27, 2020
Date of Patent:
December 13, 2022
Assignee:
ObsEva S.A.
Inventors:
Patrick Naxos Page, Matthias Schwarz, Catherine Jorand-Lebrun, Anna Quattropani, Vincent Pomel, Ernest Loumaye, Oliver Pohl, Jean-Pierre Gotteland
Abstract: The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.
Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.
Abstract: Crystalline (3Z,S3)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime is disclosed. A pharmaceutical composition containing the crystalline compound and methods for treating conditions related to the OT-R activity, such as preterm labor, and for increasing embryo implantation rate in a mammal undergoing embryo transfer, comprising administering the crystalline compound are also disclosed.
Abstract: The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. 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-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.
Type:
Application
Filed:
June 5, 2018
Publication date:
June 11, 2020
Applicant:
ObsEva S.A.
Inventors:
Ernest LOUMAYE, Jean-Pierre GOTTELAND, Oliver POHL
Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.
Abstract: The invention provides pharmaceutical compositions comprising a compound of formula (I) or (II) and an additional therapeutic agent Also provided is the HCI salt and crystalline form of the compound of formula (I). The compounds inhibit the prostaglandin F receptor (PGF2alpha) and thus useful in the treatment of disorders such as preterm labor at the early gestational stage.
Type:
Grant
Filed:
January 4, 2017
Date of Patent:
February 11, 2020
Assignee:
ObsEva S.A.
Inventors:
Patrick Naxos Page, Matthias Schwarz, Catherine Jorand-Lebrun, Anna Quattropani, Vincent Pomel, Ernest Loumaye, Oliver Pohl, Jean-Pierre Gotteland
Abstract: The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one-O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.
Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-meth19243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.
Abstract: The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one-O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.
Abstract: Crystalline (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methyloxime is disclosed. A pharmaceutical composition containing the crystalline compound and methods for treating conditions related to the OT-R activity, such as preterm labor, and tor increasing embryo implantation rate in a mammal undergoing embryo transfer, comprising administering the crystalline compound are also disclosed.
Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methy19243-yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.