Patents Assigned to ESTETRA S.A.
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Patent number: 11053274Abstract: The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of: a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wherein P1 and P2 are each independently a protecting group selected from R2—Si—R3R4, or R1CO—, wherein R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I).Type: GrantFiled: June 1, 2012Date of Patent: July 6, 2021Assignee: ESTETRA S.P.R.L.Inventor: Jean-Claude Pascal
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Patent number: 11053273Abstract: The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P1 is a protecting group selected from R2—Si—R3R4 or R1CO—, R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R5, and R5 is a group selected from C6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C1-4alkyl; c) dehalogenation or desulfinylation of tType: GrantFiled: June 1, 2012Date of Patent: July 6, 2021Assignee: ESTETRA S.P.R.L.Inventor: Jean-Claude Pascal
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Patent number: 9579329Abstract: The present invention relates to a new use of tetrahydroxylated estrogens such as estetrol (1,3,5(10)-estratrien-3, 15?, 16?, 17?-tetrol), namely in a method of emergency contraception. The method of emergency contraception according to the invention comprises the oral administration of estetrol in a single dose within 120 hours of sexual intercourse.Type: GrantFiled: August 9, 2012Date of Patent: February 28, 2017Assignee: Estetra S.P.R.L.Inventors: Wout Wouters, Herman Jan Tijmen Coelingh Bennink, Ludivine Petit, Jean-Michel Foidart
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Patent number: 8987484Abstract: The present invention relates to a process for the preparation of a compound of formula (I), hydrates or solvates thereof.Type: GrantFiled: October 5, 2012Date of Patent: March 24, 2015Assignee: Estetra S.P.R.L.Inventor: Jean-Claude Pascal
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Publication number: 20140243539Abstract: The present invention relates to a process for the preparation of a compound of formula (I), hydrates or solvates thereof.Type: ApplicationFiled: October 5, 2012Publication date: August 28, 2014Applicant: Estetra S.P.R.L.Inventor: Jean-Claude Pascal
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Publication number: 20140200202Abstract: The present invention relates to a new use of tetrahydroxylated estrogens such as estetrol (1,3,5(10)-estratrien-3,15?,16?,17?-tetrol), namely in a method of emergency contraception. The method of emergency contraception according to the invention comprises the oral administration of estetrol in a single dose within 120 hours of sexual intercourse.Type: ApplicationFiled: August 9, 2012Publication date: July 17, 2014Applicant: Estetra S.P.R.L.Inventors: Wout Wouters, Herman Jan Tijmen Coelingh Bennink, Ludivine Petit, Jean-Michel Foidart
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Publication number: 20140107091Abstract: The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P1 is a protecting group selected from R2Si—R3R4 or R1CO—, R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R5, and R5 is a group selected from C6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C1-4alkyl; c) dehalogenation or desulfinylation of thType: ApplicationFiled: June 1, 2012Publication date: April 17, 2014Applicant: ESTETRA S.A.Inventor: Jean-Claude Pascal
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Publication number: 20140107358Abstract: The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of: a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wherein P1 and P2 are each independently a protecting group selected from R2?Si—R3R4, or R1CO—, wherein R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I).Type: ApplicationFiled: June 1, 2012Publication date: April 17, 2014Applicant: ESTETRA S.A.Inventor: Jean-Claude Pascal