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EA200000896A1 - S-ЗАМЕЩЕННЫЕ ТИОЛОВЫЕ ЭФИРЫ 11b-БЕНЗАЛЬДОКСИМЭСТРА-4,9-ДИЕНУГОЛЬНОЙ КИСЛОТЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ЭТИ СОЕДИНЕНИЯ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ - Google Patents

S-ЗАМЕЩЕННЫЕ ТИОЛОВЫЕ ЭФИРЫ 11b-БЕНЗАЛЬДОКСИМЭСТРА-4,9-ДИЕНУГОЛЬНОЙ КИСЛОТЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ЭТИ СОЕДИНЕНИЯ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Info

Publication number
EA200000896A1
EA200000896A1 EA200000896A EA200000896A EA200000896A1 EA 200000896 A1 EA200000896 A1 EA 200000896A1 EA 200000896 A EA200000896 A EA 200000896A EA 200000896 A EA200000896 A EA 200000896A EA 200000896 A1 EA200000896 A1 EA 200000896A1
Authority
EA
Eurasian Patent Office
Prior art keywords
benzaldoximestra
acid
substituted
dienugolic
compops
Prior art date
Application number
EA200000896A
Other languages
English (en)
Other versions
EA002766B1 (ru
Inventor
Герд Шуберт
Свен Ринг
Гюнтер Кауфманн
Вальтер Элгер
Биргит Шнайдер
Original Assignee
Йенафарм Гмбх Унд Ко. Кг
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 Йенафарм Гмбх Унд Ко. Кг filed Critical Йенафарм Гмбх Унд Ко. Кг
Publication of EA200000896A1 publication Critical patent/EA200000896A1/ru
Publication of EA002766B1 publication Critical patent/EA002766B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/006Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton spiro-condensed

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

В заявке описываются S-замещенные тиоловые эфиры 11β-бензальдоксимэстра-4,9-диенугольной кислоты общей формулы (I)и их фармацевтически приемлемые соли, а также способ получения этих соединений и содержащие их фармацевтические композиции. Предлагаемые соединения связываются на рецепторе прогестерона и обладают заметно сниженным антиглюкокортикоидным действием.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200000896A 1998-03-03 1999-02-10 S-ЗАМЕЩЕННЫЕ ТИОЛОВЫЕ ЭФИРЫ 11β-БЕНЗАЛЬДОКСИМЭСТРА-4,9-ДИЕНУГОЛЬНОЙ КИСЛОТЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ЭТИ СОЕДИНЕНИЯ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ EA002766B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19809845A DE19809845A1 (de) 1998-03-03 1998-03-03 S-substituierte 11beta-Benzaldoxim-estra-4,9-dien-kohlensäurethiolester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zubereitungen
PCT/DE1999/000408 WO1999045023A1 (de) 1998-03-03 1999-02-10 S-SUBSTITUIERTE 11β-BENZALDOXIM-ESTRA-4,9-DIEN-KOHLENSÄURETHIOLESTER, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENE PHARMAZEUTISCHE ZUBEREITUNGEN

Publications (2)

Publication Number Publication Date
EA200000896A1 true EA200000896A1 (ru) 2001-04-23
EA002766B1 EA002766B1 (ru) 2002-08-29

Family

ID=7860080

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000896A EA002766B1 (ru) 1998-03-03 1999-02-10 S-ЗАМЕЩЕННЫЕ ТИОЛОВЫЕ ЭФИРЫ 11β-БЕНЗАЛЬДОКСИМЭСТРА-4,9-ДИЕНУГОЛЬНОЙ КИСЛОТЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ЭТИ СОЕДИНЕНИЯ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Country Status (28)

Country Link
US (1) US6365582B1 (ru)
EP (1) EP1060187B1 (ru)
JP (1) JP3796405B2 (ru)
KR (1) KR100488823B1 (ru)
CN (1) CN1208341C (ru)
AT (1) ATE237627T1 (ru)
AU (1) AU749163B2 (ru)
BG (1) BG64735B1 (ru)
BR (1) BR9908458A (ru)
CA (1) CA2322471C (ru)
CZ (1) CZ20003125A3 (ru)
DE (2) DE19809845A1 (ru)
DK (1) DK1060187T3 (ru)
EA (1) EA002766B1 (ru)
EE (1) EE04242B1 (ru)
ES (1) ES2197634T3 (ru)
HU (1) HUP0100962A3 (ru)
ID (1) ID26972A (ru)
IL (1) IL137851A (ru)
IS (1) IS5579A (ru)
NO (1) NO316977B1 (ru)
NZ (1) NZ506048A (ru)
PL (1) PL193687B1 (ru)
PT (1) PT1060187E (ru)
SK (1) SK284177B6 (ru)
TR (1) TR200002506T2 (ru)
UA (1) UA59437C2 (ru)
WO (1) WO1999045023A1 (ru)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19906152B4 (de) 1999-02-10 2005-02-10 Jenapharm Gmbh & Co. Kg Wirkstoffhaltige Laminate für Transdermalsysteme
US8193252B1 (en) 1999-08-31 2012-06-05 Bayer Pharma AG Mesoprogestins (progesterone receptor modulators) for the treatment and prevention of benign hormone dependent gynecological disorders
HUP0202460A3 (en) * 1999-08-31 2004-04-28 Schering Ag Mesoprogestins (progesterone receptor modulators) as a component of compositions for hormone replacement therapy (hrt)
YU13902A (sh) * 1999-08-31 2006-01-16 Schering Ag. Mezoprogestini (progesteron receptor modulatori) kao komponente kontraceptivnih sredstava za žene
US7629334B1 (en) * 1999-08-31 2009-12-08 Bayer Schering Pharma Aktiengesellschaft Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT)
PT1229906E (pt) * 1999-08-31 2008-01-18 Bayer Schering Pharma Ag Mesoprogestinas para o tratamento e prevenção de distúrbios ginecológicos hormonodependentes benignos
EP1285927A3 (de) * 2001-08-16 2005-06-29 Schering Aktiengesellschaft Verwendung von Glucocorticoid-Rezeptorantagonisten zur Vorbeugung und Behandlung von Erkrankungen des männlichen Reproduktionssystems
DE10221034A1 (de) * 2002-05-03 2003-11-20 Schering Ag 17alpha-Fluoralkyl-11ß-benzaldoxim-Steroide, Verfahren zu deren Herstellung, diese Steroide enthaltende pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
AU2003255355A1 (en) * 2002-08-02 2004-02-25 Schering Aktiengesellschaft Progesterone receptor modulators having an increased antigonadotropic activity for use in female fertility testing and hormone replacement therapy
DE10236405A1 (de) * 2002-08-02 2004-02-19 Schering Ag Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie
DE102005059222B4 (de) * 2005-12-08 2007-10-11 Bayer Schering Pharma Ag 11ß-Benzaldoximderivate von D-Homoestra-4,9-dien-3-onen
ES2643318T3 (es) 2006-10-24 2017-11-22 Repros Therapeutics Inc. Composiciones y métodos para suprimir la proliferación endometrial
US7981927B2 (en) 2007-03-07 2011-07-19 Janssen Pharmaceutica N.V. Steroids derivatives as selective progesterone receptor modulators
TWI539953B (zh) 2008-04-28 2016-07-01 瑞波若斯治療學公司 用於治療乳癌之組成物和方法
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
CN107260745A (zh) 2010-03-22 2017-10-20 利普生物药剂公司 用于抗孕酮的非毒性递送的组合物和方法
EP2664325A1 (en) * 2012-05-16 2013-11-20 PregLem S.A. Methods for preventing or treating androgen mediated diseases

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4039677A (en) * 1976-03-01 1977-08-02 Syntex (U.S.A.) Inc. Novel 1-phenethylimidazoles
ZA8231B (en) * 1981-01-09 1982-11-24 Roussel Uclaf New 11 -substituted steroid derivatives, their preparation, their use as medicaments, the compositions containing them and the new intermediates thus obtained
DE3504421A1 (de) * 1985-02-07 1986-08-07 Schering AG, 1000 Berlin und 4709 Bergkamen Neue 11ss-phenyl-gonane, deren herstellung und diese enthaltende pharmazeutische praeparate
DE4332283A1 (de) * 1993-09-20 1995-04-13 Jenapharm Gmbh Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
DE4332284C2 (de) * 1993-09-20 1997-05-28 Jenapharm Gmbh 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
US5576310A (en) * 1994-09-20 1996-11-19 Jenapharm Gmbh 11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds
IL115738A (en) 1994-10-24 2002-05-23 Schering Ag Competitive progesterone antagonists for regulating female fertility as required
ZA9510926B (en) * 1994-12-23 1996-07-03 Schering Ag Compounds with progesterone-antagonistic and antiestrogenic action to be used together for female contraception
WO1996028145A1 (en) 1995-03-14 1996-09-19 Schering Aktiengesellschaft Use of nitric oxide donors or nitric oxide inhibitors for regulating cervical dilatation and extensibility

Also Published As

Publication number Publication date
WO1999045023A1 (de) 1999-09-10
DK1060187T3 (da) 2003-08-11
DE19809845A1 (de) 1999-09-09
EP1060187A1 (de) 2000-12-20
AU3406799A (en) 1999-09-20
PL193687B1 (pl) 2007-03-30
CN1208341C (zh) 2005-06-29
NO20004362L (no) 2000-10-31
NO20004362D0 (no) 2000-09-01
PT1060187E (pt) 2003-09-30
CZ20003125A3 (cs) 2002-01-16
SK13052000A3 (sk) 2001-11-06
JP2002505335A (ja) 2002-02-19
CA2322471A1 (en) 1999-09-10
HUP0100962A2 (hu) 2001-09-28
ATE237627T1 (de) 2003-05-15
BG64735B1 (bg) 2006-01-31
US6365582B1 (en) 2002-04-02
KR100488823B1 (ko) 2005-05-12
NO316977B1 (no) 2004-07-12
NZ506048A (en) 2003-05-30
SK284177B6 (sk) 2004-10-05
ES2197634T3 (es) 2004-01-01
KR20010041536A (ko) 2001-05-25
UA59437C2 (ru) 2003-09-15
AU749163B2 (en) 2002-06-20
EP1060187B1 (de) 2003-04-16
ID26972A (id) 2001-02-22
TR200002506T2 (tr) 2000-12-21
BR9908458A (pt) 2000-11-14
IL137851A0 (en) 2001-10-31
BG104712A (en) 2001-02-28
IL137851A (en) 2005-06-19
PL342449A1 (en) 2001-06-04
EE04242B1 (et) 2004-02-16
CA2322471C (en) 2007-04-24
DE59905075D1 (de) 2003-05-22
EE200000500A (et) 2002-02-15
EA002766B1 (ru) 2002-08-29
CN1291990A (zh) 2001-04-18
IS5579A (is) 2000-07-28
HUP0100962A3 (en) 2002-07-29
JP3796405B2 (ja) 2006-07-12

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PC4A Registration of transfer of a eurasian patent by assignment