EA010572B1 - 7α,17α-ЗАМЕЩЕННЫЕ 11β-ГАЛОГЕНОСТЕРОИДЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ПРИМЕНЕНИЕ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ НА ИХ ОСНОВЕ - Google Patents

7α,17α-ЗАМЕЩЕННЫЕ 11β-ГАЛОГЕНОСТЕРОИДЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ПРИМЕНЕНИЕ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ НА ИХ ОСНОВЕ Download PDF

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Publication number
EA010572B1
EA010572B1 EA200601030A EA200601030A EA010572B1 EA 010572 B1 EA010572 B1 EA 010572B1 EA 200601030 A EA200601030 A EA 200601030A EA 200601030 A EA200601030 A EA 200601030A EA 010572 B1 EA010572 B1 EA 010572B1
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EA
Eurasian Patent Office
Prior art keywords
substituted
general formula
halogen
steroids
group
Prior art date
Application number
EA200601030A
Other languages
English (en)
Russian (ru)
Other versions
EA200601030A1 (ru
Inventor
Людвиг Цорн
Рольф Больманн
Норберт Галлус
Германн Кюнцер
Ханс-Петер Мун
Райнхард Нуббемейер
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
Priority claimed from DE10233723A external-priority patent/DE10233723A1/de
Application filed by Шеринг Акциенгезельшафт filed Critical Шеринг Акциенгезельшафт
Publication of EA200601030A1 publication Critical patent/EA200601030A1/ru
Publication of EA010572B1 publication Critical patent/EA010572B1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J5/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J11/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00Preparation of steroids
    • C12P33/06Hydroxylating
    • C12P33/08Hydroxylating at 11 position
    • C12P33/10Hydroxylating at 11 position at 11 alpha-position
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P33/00Preparation of steroids
    • C12P33/12Acting on D ring
    • C12P33/16Acting at 17 position

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Reproductive Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
EA200601030A 2002-07-24 2003-07-24 7α,17α-ЗАМЕЩЕННЫЕ 11β-ГАЛОГЕНОСТЕРОИДЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ПРИМЕНЕНИЕ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ НА ИХ ОСНОВЕ EA010572B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10233723A DE10233723A1 (de) 2002-07-24 2002-07-24 Mikrobiologische Verfahren zur Herstellung von 7α-substituierten 11α-Hydroxysteroiden, daraus herstellbare 7α,17α-substituierte 11β-Halogensteroide, deren Herstellungsverfahren und Verwendung sowie pharmazeutische Präparate, die diese Verbindungen enthalten, sowie daraus herstellbare 7α-substituierte Estra-1,3,5(10)-triene
US40295302P 2002-08-14 2002-08-14

Publications (2)

Publication Number Publication Date
EA200601030A1 EA200601030A1 (ru) 2006-10-27
EA010572B1 true EA010572B1 (ru) 2008-10-30

Family

ID=31189296

Family Applications (2)

Application Number Title Priority Date Filing Date
EA200601030A EA010572B1 (ru) 2002-07-24 2003-07-24 7α,17α-ЗАМЕЩЕННЫЕ 11β-ГАЛОГЕНОСТЕРОИДЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ПРИМЕНЕНИЕ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ НА ИХ ОСНОВЕ
EA200500224A EA008147B1 (ru) 2002-07-24 2003-07-24 МИКРОБИОЛОГИЧЕСКИЕ СПОСОБЫ ПОЛУЧЕНИЯ 7α-ЗАМЕЩЁННЫХ 11α-ГИДРОКСИСТЕРОИДОВ

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA200500224A EA008147B1 (ru) 2002-07-24 2003-07-24 МИКРОБИОЛОГИЧЕСКИЕ СПОСОБЫ ПОЛУЧЕНИЯ 7α-ЗАМЕЩЁННЫХ 11α-ГИДРОКСИСТЕРОИДОВ

Country Status (20)

Country Link
EP (1) EP1523568A2 (xx)
JP (1) JP4417838B2 (xx)
KR (1) KR101041328B1 (xx)
CN (1) CN100339486C (xx)
BR (1) BR0313210A (xx)
CA (1) CA2492079C (xx)
CO (1) CO5690563A2 (xx)
CR (1) CR7672A (xx)
EA (2) EA010572B1 (xx)
EC (1) ECSP055630A (xx)
HK (1) HK1081999A1 (xx)
HR (1) HRP20050172A2 (xx)
IL (1) IL166358A0 (xx)
MX (1) MXPA05001024A (xx)
NO (1) NO20050980L (xx)
NZ (2) NZ549529A (xx)
PH (1) PH12005500143B1 (xx)
PL (1) PL373808A1 (xx)
RS (1) RS51855B (xx)
WO (1) WO2004011663A2 (xx)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101296936B (zh) * 2005-10-27 2011-06-22 大鹏药品工业株式会社 生产甾族化合物的方法
CN103834712B (zh) * 2012-11-26 2016-03-30 复旦大学 去氧孕烯中间体纳米脂质体生物转化的优化方法
CN103214543B (zh) * 2012-12-25 2015-09-02 中国人民解放军海军医学研究所 新山楂酸衍生物、其制备方法及其在抗肿瘤药物中的应用
CN104862323B (zh) * 2015-06-02 2018-01-16 中国农业科学院生物技术研究所 修饰苯二酚类化合物的羟化酶基因

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997021830A1 (en) * 1995-12-12 1997-06-19 Akzo Nobel N.V. MICROBIAL 11α-HYDROXYLATION OF STEROIDS
WO1999013812A1 (en) * 1997-09-17 1999-03-25 The Population Council, Inc. Transdermal administration of ment
WO2002059139A1 (en) * 2001-01-24 2002-08-01 Schering Aktiengesellschaft Androgenic 7-substituted 11-halogen steroids
WO2004011008A1 (de) * 2002-07-25 2004-02-05 Schering Aktiengesellschaft ZUSAMMENSETZUNG, ENTHALTEND EIN ANDROGENES 11β-HALOGENSTEROID UND EIN GESTAGEN SOWIE MÄNNLICHES KONTRAZEPTIVUM AUF BASIS DIESER ZUSAMMENSETZUNG

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL75841C (xx) 1949-06-11
US2658023A (en) * 1953-04-21 1953-11-03 Pfizer & Co C Oxygenation of steroids
US2985563A (en) * 1958-11-13 1961-05-23 Schering Corp 11alpha-hydroxylation of steroids by glomerella
US3004047A (en) * 1959-03-13 1961-10-10 Olin Mathieson 6alpha-halo-11alpha-hydroxy steroids of the pregnane series and esters thereof
US3341557A (en) * 1961-06-05 1967-09-12 Upjohn Co 7-methyltestosterones
US3203869A (en) * 1962-10-11 1965-08-31 Syntex Corp 11alpha-hydroxylation of 6-substituted-11-desoxy steroids with microorganisms of thegenus fusarium, liseola section
US5342834A (en) 1989-04-07 1994-08-30 The Population Council, Inc. Method for androgen supplementation
EP1167381A3 (en) * 1995-12-11 2004-09-29 G.D. Searle & Co. Process for preparation of 7 alpha-carboxyl 9,11-epoxy steroids and Intermediates useful therein
GB9525194D0 (en) 1995-12-12 1996-02-07 Zeneca Ltd Pharmaceutical composition
US6767902B2 (en) 1997-09-17 2004-07-27 The Population Council, Inc. Androgen as a male contraceptive and non-contraceptive androgen replacement
US5952319A (en) 1997-11-26 1999-09-14 Research Triangle Institute Androgenic steroid compounds and a method of making and using the same
SI1267885T1 (sl) 2000-02-15 2007-08-31 Bayer Schering Pharma Ag Formulacija za moško kontracepcijo, ki vsebuje noretisteron in testosteron undekanoat

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997021830A1 (en) * 1995-12-12 1997-06-19 Akzo Nobel N.V. MICROBIAL 11α-HYDROXYLATION OF STEROIDS
WO1999013812A1 (en) * 1997-09-17 1999-03-25 The Population Council, Inc. Transdermal administration of ment
WO2002059139A1 (en) * 2001-01-24 2002-08-01 Schering Aktiengesellschaft Androgenic 7-substituted 11-halogen steroids
WO2004011008A1 (de) * 2002-07-25 2004-02-05 Schering Aktiengesellschaft ZUSAMMENSETZUNG, ENTHALTEND EIN ANDROGENES 11β-HALOGENSTEROID UND EIN GESTAGEN SOWIE MÄNNLICHES KONTRAZEPTIVUM AUF BASIS DIESER ZUSAMMENSETZUNG

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
SHIBAHARA M. ET AL.: "MICROBIAL HYDROXYLATIONS V. IIALPHA-HYDROXYLATION OF PROGESTERONE BY CELL-FREE PREPARATIONS OF ASPERGILLUS OCHRACEUS", BIOCHIMICA ET BIOPHYSICA ACTA, AMSTERDAM, NL, Bd. 202, 1970, Seiten 172-179, XP009023368, ISSN: 0006-3002, das ganze Dokument *
TAN L. ET AL.: "INTERACTIONS OF STEROIDS AND FUNGI. 11 ALPHA-HYDROXYLATION AND DEGRADATION OF PROGESTERONE-4-C BY A CELL-FREE PREPARATION FROM ASPERGILLUS OCHRACEUS", JOURNAL OF STEROID BIOCHEMISTRY, PERGAMON PRESS PLC, GB, Bd. 1, Nr. 3, 1. September 1970 (1970-09-01), Seiten 221-227, XP000671122, ISSN: 0022-4731, das ganze Dokument *

Also Published As

Publication number Publication date
RS20050045A (xx) 2007-06-04
EA200601030A1 (ru) 2006-10-27
PL373808A1 (en) 2005-09-19
CO5690563A2 (es) 2006-10-31
EA200500224A1 (ru) 2005-08-25
CN100339486C (zh) 2007-09-26
CA2492079A1 (en) 2004-02-05
PH12005500143B1 (en) 2011-03-25
EA008147B1 (ru) 2007-04-27
BR0313210A (pt) 2005-06-28
NO20050980L (no) 2005-02-23
RS51855B (sr) 2012-02-29
JP2006503813A (ja) 2006-02-02
JP4417838B2 (ja) 2010-02-17
MX260952B (xx) 2008-10-01
EP1523568A2 (de) 2005-04-20
KR101041328B1 (ko) 2011-06-14
AU2003281677A1 (en) 2004-02-16
MXPA05001024A (es) 2005-05-16
HK1081999A1 (en) 2006-05-26
KR20050026507A (ko) 2005-03-15
IL166358A0 (en) 2006-01-16
NZ549529A (en) 2008-04-30
CA2492079C (en) 2012-01-10
ECSP055630A (es) 2005-04-18
CN1671858A (zh) 2005-09-21
WO2004011663A9 (de) 2004-05-06
WO2004011663A3 (de) 2004-07-15
WO2004011663A2 (de) 2004-02-05
HRP20050172A2 (en) 2005-04-30
CR7672A (es) 2006-05-29
NZ537871A (en) 2006-10-27

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): BY RU