EA200201192A1 - НОВЫЕ ТВЕРДЫЕ ФОРМЫ МЕЗОПРОГЕСТИНА-11β-[4Е-(ГИДРОКСИИМИНОМЕТИЛ)ФЕНИЛ]-17α-МЕТОКСИМЕТИЛ-17β-МЕТОКСИЭСТРА-4,9-ДИЕН-3-ОНА - Google Patents

НОВЫЕ ТВЕРДЫЕ ФОРМЫ МЕЗОПРОГЕСТИНА-11β-[4Е-(ГИДРОКСИИМИНОМЕТИЛ)ФЕНИЛ]-17α-МЕТОКСИМЕТИЛ-17β-МЕТОКСИЭСТРА-4,9-ДИЕН-3-ОНА

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Publication number
EA200201192A1
EA200201192A1 EA200201192A EA200201192A EA200201192A1 EA 200201192 A1 EA200201192 A1 EA 200201192A1 EA 200201192 A EA200201192 A EA 200201192A EA 200201192 A EA200201192 A EA 200201192A EA 200201192 A1 EA200201192 A1 EA 200201192A1
Authority
EA
Eurasian Patent Office
Prior art keywords
solid forms
methoxyestra
hydroxyiminomethyl
methoxymethyl
new solid
Prior art date
Application number
EA200201192A
Other languages
English (en)
Other versions
EA005623B1 (ru
Inventor
Детлеф Граве
Петер Хёзель
Уве Мюллер
Габриеле Винтер
Original Assignee
Шеринг 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 Шеринг Акциенгезельшафт filed Critical Шеринг Акциенгезельшафт
Publication of EA200201192A1 publication Critical patent/EA200201192A1/ru
Publication of EA005623B1 publication Critical patent/EA005623B1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36Antigestagens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Reproductive Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

В заявке описаны новые твердые формы мезопрогестина - 11β-[4Е-(гидроксииминометил)фенил]-17α-метоксиметил-17β-метоксиэстра-4,9-диен-3-она (оксим J 867), прежде всего высокочистая и стабильная аморфная, соответственно высококристаллическая форма (в виде ансольвата/ангидрата) соединения J 867, способ получения таких форм, а также их применение в фармацевтических композициях. Такие новые твердые формы отличаются прежде всего высокой стабильностью. Твердые формы оксима J 867 можно применять прежде всего для контроля репродуктивной способности у женщин и для гормонзаместительной терапии.Отчет о международном поиске был опубликован 2002.04.04.
EA200201192A 2000-05-23 2001-05-09 НОВЫЕ ТВЕРДЫЕ ФОРМЫ МЕЗОПРОГЕСТИНА-11β-[4E-(ГИДРОКСИИМИНОМЕТИЛ)ФЕНИЛ]-17α-МЕТОКСИМЕТИЛ-17β-МЕТОКСИЭСТРА-4,9-ДИЕН-3-ОНА EA005623B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00110887A EP1157996A1 (de) 2000-05-23 2000-05-23 Neue Festkörperformen des Mesoprogestins 11Beta-[4E-(Hydroxyiminomethyl)-phenyl]-17Alpha-methoxymethyl-17Beta-methoxy-estra-4,9-dien-3-on
PCT/EP2001/005237 WO2001090137A2 (de) 2000-05-23 2001-05-09 NEUE FESTKÖRPERFORMEN DES MESOPROGESTINS 11β-[4E-(HYDROXYIMINOMETHYL)-PHENYL]-17α-METHOXYMETHYL-17β-METHOXY-ESTRA-4,9-DIEN-3-ON

Publications (2)

Publication Number Publication Date
EA200201192A1 true EA200201192A1 (ru) 2003-06-26
EA005623B1 EA005623B1 (ru) 2005-04-28

Family

ID=8168805

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200201192A EA005623B1 (ru) 2000-05-23 2001-05-09 НОВЫЕ ТВЕРДЫЕ ФОРМЫ МЕЗОПРОГЕСТИНА-11β-[4E-(ГИДРОКСИИМИНОМЕТИЛ)ФЕНИЛ]-17α-МЕТОКСИМЕТИЛ-17β-МЕТОКСИЭСТРА-4,9-ДИЕН-3-ОНА

Country Status (30)

Country Link
US (1) US7799770B2 (ru)
EP (3) EP1157996A1 (ru)
JP (1) JP2003534350A (ru)
KR (1) KR100553292B1 (ru)
CN (1) CN100384867C (ru)
AT (1) ATE397617T1 (ru)
AU (2) AU2001256344B2 (ru)
BG (1) BG65968B1 (ru)
BR (1) BR0111058A (ru)
CA (1) CA2409869C (ru)
CZ (1) CZ2003620A3 (ru)
DE (1) DE50114012D1 (ru)
DK (1) DK1292607T3 (ru)
EA (1) EA005623B1 (ru)
EC (2) ECSP024358A (ru)
ES (1) ES2307613T3 (ru)
HR (2) HRP20021032B1 (ru)
HU (1) HUP0301956A3 (ru)
IL (2) IL152868A0 (ru)
ME (1) MEP15608A (ru)
MX (1) MXPA02011524A (ru)
NO (1) NO327004B1 (ru)
NZ (1) NZ522768A (ru)
PL (1) PL358789A1 (ru)
PT (1) PT1292607E (ru)
RS (1) RS50493B (ru)
SK (1) SK2922003A3 (ru)
UA (1) UA73988C2 (ru)
WO (1) WO2001090137A2 (ru)
ZA (1) ZA200209322B (ru)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10218109A1 (de) * 2002-04-23 2003-11-20 Jenapharm Gmbh Verfahren zum Herstellen von Kristallen, danach erhältliche Kristalle und deren Verwendung in pharmazeutischen Formulierungen
DE10218107A1 (de) * 2002-04-23 2003-11-20 Jenapharm Gmbh Verfahren zum Herstellen von Kristallen von Steroiden, danach erhältliche Kristalle und deren Verwendung in pharmazeutischen Formulierungen
WO2006078731A2 (en) * 2005-01-18 2006-07-27 Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag Amorphous and crystalline forms of dorzolamide hydrochloride and processes of making same
US20090054387A1 (en) 2006-04-18 2009-02-26 Detlef Grawe Method for preparing 4-[17beta-methoxy-17alpha-methoxymethyl-3-oxestra-4,9-dien-11beta-yl]benzaldehyde (E)-oxime (asoprisnil)
DE102006018888A1 (de) * 2006-04-18 2007-10-25 Bayer Schering Pharma Ag Verfahren zur Herstellung von 4-[17beta-Methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyd-(E)-oxims (Asoprisnil)
EP1862468A1 (de) * 2006-06-02 2007-12-05 Bayer Schering Pharma Aktiengesellschaft Kristallines 11beta-(4-Acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17alpha-pregna-4,9-dien-3-on
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
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
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
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
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
DE102010007722A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten
DE102010007719A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4332283A1 (de) * 1993-09-20 1995-04-13 Jenapharm Gmbh Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
DE19610667C2 (de) * 1996-03-08 1998-04-09 Schering Ag (Z)-11ß-[4-(Dimethylamino)phenyl]17ß-hydroxy-17alpha-(3-hydroxy-1-propenyl)estr-4-en-3-on als kristallines Ansolvat
EP1204656A2 (en) * 1999-07-29 2002-05-15 Eli Lilly And Company A crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy] phenoxy)-2-(4-methoxyphenyl) benzo[b]thiophene hydrochloride

Also Published As

Publication number Publication date
ZA200209322B (en) 2005-03-10
ECSP084358A (es) 2008-11-27
EP1862469A2 (de) 2007-12-05
NO20025613D0 (no) 2002-11-22
CA2409869C (en) 2009-02-03
HUP0301956A2 (hu) 2003-09-29
DK1292607T3 (da) 2008-10-13
NZ522768A (en) 2005-03-24
PL358789A1 (en) 2004-08-23
BG65968B1 (bg) 2010-07-30
JP2003534350A (ja) 2003-11-18
AU2001256344B8 (en) 2001-12-03
CA2409869A1 (en) 2002-11-20
HUP0301956A3 (en) 2010-03-29
AU5634401A (en) 2001-12-03
ECSP024358A (es) 2003-03-31
MEP15608A (en) 2010-06-10
SK2922003A3 (en) 2003-08-05
MXPA02011524A (es) 2004-09-10
US20040006241A1 (en) 2004-01-08
KR100553292B1 (ko) 2006-02-22
ATE397617T1 (de) 2008-06-15
UA73988C2 (en) 2005-10-17
YU88702A (sh) 2006-01-16
IL152868A (en) 2009-08-03
ES2307613T3 (es) 2008-12-01
CN100384867C (zh) 2008-04-30
DE50114012D1 (en) 2008-07-17
HRP20021032B1 (en) 2008-09-30
WO2001090137A2 (de) 2001-11-29
CN1430624A (zh) 2003-07-16
CZ2003620A3 (cs) 2003-08-13
EP1157996A1 (de) 2001-11-28
WO2001090137A3 (de) 2002-04-04
IL152868A0 (en) 2003-06-24
PT1292607E (pt) 2008-09-15
EP1292607B1 (de) 2008-06-04
NO20025613L (no) 2002-11-22
AU2001256344B2 (en) 2007-01-25
BG107557A (bg) 2004-01-30
RS50493B (sr) 2010-03-02
EP1292607A2 (de) 2003-03-19
BR0111058A (pt) 2003-04-15
EA005623B1 (ru) 2005-04-28
HRP20080423A2 (en) 2008-10-31
US7799770B2 (en) 2010-09-21
HRP20021032A2 (en) 2005-02-28
NO327004B1 (no) 2009-04-06
KR20030028742A (ko) 2003-04-10

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