EA200802385A1 - КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 11β-(4-АЦЕТИЛФЕНИЛ)-20,20,21,21,21-ПЕНТАФТОР-17-ГИДРОКСИ-19-НОР-17A-ПРЕГНА-4,9-ДИЕН-3-ОНА - Google Patents

КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 11β-(4-АЦЕТИЛФЕНИЛ)-20,20,21,21,21-ПЕНТАФТОР-17-ГИДРОКСИ-19-НОР-17A-ПРЕГНА-4,9-ДИЕН-3-ОНА

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Publication number
EA200802385A1
EA200802385A1 EA200802385A EA200802385A EA200802385A1 EA 200802385 A1 EA200802385 A1 EA 200802385A1 EA 200802385 A EA200802385 A EA 200802385A EA 200802385 A EA200802385 A EA 200802385A EA 200802385 A1 EA200802385 A1 EA 200802385A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pregna
acetylphenyl
dien
hydroxy
pentafluoro
Prior art date
Application number
EA200802385A
Other languages
English (en)
Inventor
Вольфганг Бекманн
Габриела Винтер
Эдда Крэмер
Томас Гинко
Эвелин Амоулонг
Арвед Клеве
Original Assignee
Байер Шеринг Фарма Акциенгезельшафт
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Байер Шеринг Фарма Акциенгезельшафт filed Critical Байер Шеринг Фарма Акциенгезельшафт
Publication of EA200802385A1 publication Critical patent/EA200802385A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36—Antigestagens

Abstract

Настоящее изобретение относится к кристаллическим формам 11β-(4-ацетилфенил)-20,20,21,21,21-пентафтор-17-гидрокси-19-нор-17α-прегна-4,9-диен-3-она. Изобретение относится в особенности к двум кристаллическим несольватным/негидратным формам этого соединения, полиморфам I и II. Кроме этого, настоящее изобретение также относится к кристаллическим сольватам, например метанольному и этанольному сольватам 11β-(4-ацетилфенил)-20,20,21,21,21-пентафтор-17-гидрокси-19-нор-17α-прегна-4,9-диен-3-она в качестве прекурсора для получения этих двух полиморфов I и II. Описаны способ получения полиморфа I путем заместительной кристаллизации или путем порошкования. Выбор растворителя для последнего перед формированием несольватной формы может быть основан на различиях в поведении очистки индивидуальных сольватов 11β-(4-ацетилфенил)-20,20,21,21,21-пентафтор-17-гидрокси-19-нор-17α-прегна-4,9-диен-3-она. Полиморф I согласно изобретению является особенно подходящим для изготовления медицинских продуктов.
EA200802385A 2006-06-02 2007-05-31 КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 11β-(4-АЦЕТИЛФЕНИЛ)-20,20,21,21,21-ПЕНТАФТОР-17-ГИДРОКСИ-19-НОР-17A-ПРЕГНА-4,9-ДИЕН-3-ОНА EA200802385A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US81012706P 2006-06-02 2006-06-02
EP06090095A EP1862468A1 (de) 2006-06-02 2006-06-02 Kristallines 11beta-(4-Acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17alpha-pregna-4,9-dien-3-on
PCT/EP2007/004805 WO2007140917A2 (de) 2006-06-02 2007-05-31 KRISTALLINE FORMEN VON 11 ß-(4-ACETYLPHENYL)-20, 20, 21,21, 21-PENTAFLUOR-17- HYDROXY-19-NOR-17α-PREGNA-4,9-DIEN-3-ON

Publications (1)

Publication Number Publication Date
EA200802385A1 true EA200802385A1 (ru) 2009-06-30

Family

ID=37562153

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200802385A EA200802385A1 (ru) 2006-06-02 2007-05-31 КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 11β-(4-АЦЕТИЛФЕНИЛ)-20,20,21,21,21-ПЕНТАФТОР-17-ГИДРОКСИ-19-НОР-17A-ПРЕГНА-4,9-ДИЕН-3-ОНА

Country Status (15)

Country Link
US (1) US7910573B2 (ru)
EP (2) EP1862468A1 (ru)
JP (1) JP2009538855A (ru)
KR (1) KR20090016008A (ru)
AR (1) AR061151A1 (ru)
AU (1) AU2007256432A1 (ru)
BR (1) BRPI0713093A2 (ru)
CA (1) CA2654126A1 (ru)
EA (1) EA200802385A1 (ru)
EC (1) ECSP088934A (ru)
MX (1) MX2008015348A (ru)
NO (1) NO20085417L (ru)
TN (1) TNSN08499A1 (ru)
UY (1) UY30384A1 (ru)
WO (1) WO2007140917A2 (ru)

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DE102006054535A1 (de) * 2006-11-15 2008-05-21 Bayer Schering Pharma Aktiengesellschaft Progesteronrezeptorantagonisten
US8486926B2 (en) * 2006-11-17 2013-07-16 Harbor Therapeutics, Inc. Steroid tetrol solid state forms
DE102009034366A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-methylenoxyalkylenaryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034367A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-benzyliden-Derivate, Verfahren zu deren Herstellung und deren Verwendung zur Behandlung von Krankheiten
DE102009034368A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-acyloxyalkylenphenyl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034362A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034526A1 (de) 2009-07-21 2011-02-10 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-ethinylphenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung zur Behandlung von Krankheiten
DE102009034525A1 (de) 2009-07-21 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102010007719A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten
DE102010007722A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten
US9290293B2 (en) 2013-01-03 2016-03-22 Samuel A. Tilton Storage systems and related methods
CN111225671A (zh) * 2017-10-26 2020-06-02 苏州科睿思制药有限公司 一种选择性孕酮受体调节剂的晶体及其制备方法

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Also Published As

Publication number Publication date
JP2009538855A (ja) 2009-11-12
US7910573B2 (en) 2011-03-22
AU2007256432A1 (en) 2007-12-13
MX2008015348A (es) 2008-12-17
AR061151A1 (es) 2008-08-06
NO20085417L (no) 2008-12-30
CA2654126A1 (en) 2007-12-13
ECSP088934A (es) 2009-01-30
WO2007140917A3 (de) 2008-04-10
WO2007140917A2 (de) 2007-12-13
EP2024383A2 (de) 2009-02-18
UY30384A1 (es) 2008-03-31
TNSN08499A1 (en) 2010-04-14
BRPI0713093A2 (pt) 2012-10-16
EP1862468A1 (de) 2007-12-05
US20080085875A1 (en) 2008-04-10
KR20090016008A (ko) 2009-02-12

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