EA200401544A1 - 9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ - Google Patents

9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ

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Publication number
EA200401544A1
EA200401544A1 EA200401544A EA200401544A EA200401544A1 EA 200401544 A1 EA200401544 A1 EA 200401544A1 EA 200401544 A EA200401544 A EA 200401544A EA 200401544 A EA200401544 A EA 200401544A EA 200401544 A1 EA200401544 A1 EA 200401544A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
uterus
estrogen
application describes
rat
Prior art date
Application number
EA200401544A
Other languages
English (en)
Other versions
EA008442B1 (ru
Inventor
Дирк Коземунд
Герд Мюллер
Александер Хиллиш
Карл-Генрих Фритцемайер
Петер Мун
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 EA200401544A1 publication Critical patent/EA200401544A1/ru
Publication of EA008442B1 publication Critical patent/EA008442B1/ru

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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
    • C07J1/0051—Estrane derivatives
    • C07J1/0055—Estrane derivatives not substituted in position 17
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

В заявке описываются новые 9α-замещенные эстратриены общей формулы (I)в которой остатки R, R, R, R, R, R, Rи Rимеют указанные в описании значения, а Rобозначает прямоцепочечный или разветвленный, необязательно частично либо полностью галогенированный алкенильный остаток с 2-6 атомами углерода, этинильный или проп-1-инильный остаток, в качестве фармацевтических действующих веществ, которые in vitro обладают более высокой аффинностью к эстрогенным рецепторам в препаратах из предстательной железы крысы по сравнению с аффинностью к эстрогенным рецепторам в препаратах из матки крысы и действие которых in vivo преимущественно направлено на яичник, а не на матку. В заявке описываются получение предлагаемых соединений, их терапевтическое применение, а также фармацевтические лекарственные формы, содержащие новые соединения. Далее описывается применение этих соединений для лечения обусловленных недостатком эстрогенов заболеваний и болезненных состояний.Отчет о международном поиске был опубликован 2004.09.16.
EA200401544A 2002-06-11 2003-06-11 9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ EA008442B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10226326A DE10226326A1 (de) 2002-06-11 2002-06-11 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene
PCT/EP2003/006172 WO2003104253A2 (de) 2002-06-11 2003-06-11 9-alpha-substituierte estratriene als selektiv wirksame estrogene

Publications (2)

Publication Number Publication Date
EA200401544A1 true EA200401544A1 (ru) 2005-06-30
EA008442B1 EA008442B1 (ru) 2007-06-29

Family

ID=29723144

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200401544A EA008442B1 (ru) 2002-06-11 2003-06-11 9α-ЗАМЕЩЁННЫЕ ЭСТРАТРИЕНЫ В КАЧЕСТВЕ ЭСТРОГЕНОВ ИЗБИРАТЕЛЬНОГО ДЕЙСТВИЯ

Country Status (29)

Country Link
EP (1) EP1517914B1 (ru)
JP (1) JP4615998B2 (ru)
KR (1) KR101006612B1 (ru)
CN (1) CN1293090C (ru)
AR (1) AR040188A1 (ru)
AT (1) ATE303397T1 (ru)
AU (1) AU2003242683B9 (ru)
BR (1) BR0312140A (ru)
CA (1) CA2486495C (ru)
CR (1) CR10289A (ru)
CU (1) CU23414B7 (ru)
DE (2) DE10226326A1 (ru)
DK (1) DK1517914T3 (ru)
EA (1) EA008442B1 (ru)
EC (1) ECSP055530A (ru)
ES (1) ES2248770T3 (ru)
HK (1) HK1081203A1 (ru)
HR (1) HRP20050009B1 (ru)
IL (1) IL165321A (ru)
MX (1) MXPA04012491A (ru)
NO (1) NO329563B1 (ru)
PE (1) PE20040613A1 (ru)
PL (1) PL209910B1 (ru)
RS (1) RS50878B (ru)
TW (1) TWI286140B (ru)
UA (1) UA78062C2 (ru)
UY (1) UY27844A1 (ru)
WO (1) WO2003104253A2 (ru)
ZA (1) ZA200500217B (ru)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10027887A1 (de) 2000-05-31 2001-12-13 Jenapharm Gmbh Verbindungen mit einer Sulfonamidgruppe und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
EP1689410B1 (en) * 2003-11-26 2008-05-21 Bayer Schering Pharma Aktiengesellschaft Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol
US7534780B2 (en) 2004-05-21 2009-05-19 Bayer Schering Pharma Aktiengesellschaft Estradiol prodrugs
DE102005057224A1 (de) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag Prodrugs ERß-selektiver Substanzen, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
EP2252261A2 (en) * 2008-02-13 2010-11-24 Bayer Schering Pharma Aktiengesellschaft Drug delivery system with stabilising effect
EP2143432A1 (en) 2008-07-11 2010-01-13 Bayer Schering Pharma AG 9-alpha estratriene derivatives as ER-beta selective ligands for the prevention and treatment of intestinal cancer
CN102215818A (zh) * 2008-11-21 2011-10-12 拜耳先灵医药股份有限公司 药物递送系统
JP2017529388A (ja) 2014-08-26 2017-10-05 ベタニエン ホスピタル 炎症性病態の治療のための方法、薬剤および組成物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2336432A1 (de) * 1973-07-13 1975-01-30 Schering Ag 3.17.18-trihydroxy-1.3.5(10)-oestratriene
US6154158A (en) * 1998-06-30 2000-11-28 Qualcomm Incorporated Digital-to-analog converter D.C. offset correction comparing converter input and output signals
DE19906159A1 (de) * 1999-02-09 2000-08-10 Schering Ag 16-Hydroxyestratriene als selektiv wirksame Estrogene
JP2003513102A (ja) * 1999-11-02 2003-04-08 シエーリング アクチエンゲゼルシャフト 選択的な作用を有するエストロゲンとしての１８−ノル−ステロイド
NZ543724A (en) * 2000-04-12 2007-07-27 Schering Ag 8beta-hydrocarbyl-substituted estratrienes as selectively active estrogens

Also Published As

Publication number Publication date
TW200407331A (en) 2004-05-16
NO20050127L (no) 2005-03-11
CN1659181A (zh) 2005-08-24
MXPA04012491A (es) 2005-06-08
BR0312140A (pt) 2005-04-05
WO2003104253A2 (de) 2003-12-18
JP4615998B2 (ja) 2011-01-19
CA2486495A1 (en) 2003-12-18
DK1517914T3 (da) 2006-01-16
HRP20050009A2 (en) 2005-04-30
AU2003242683B9 (en) 2009-08-27
DE50301116D1 (de) 2005-10-06
AR040188A1 (es) 2005-03-16
UA78062C2 (en) 2007-02-15
DE10226326A1 (de) 2004-01-15
NO329563B1 (no) 2010-11-15
RS50878B (sr) 2010-08-31
AU2003242683A1 (en) 2003-12-22
HK1081203A1 (en) 2006-05-12
UY27844A1 (es) 2003-12-31
JP2005533053A (ja) 2005-11-04
RS107004A (en) 2006-10-27
IL165321A (en) 2009-08-03
NO20050127D0 (no) 2005-01-10
EP1517914B1 (de) 2005-08-31
ATE303397T1 (de) 2005-09-15
CA2486495C (en) 2011-04-19
KR20050009745A (ko) 2005-01-25
ES2248770T3 (es) 2006-03-16
AU2003242683B2 (en) 2009-07-02
EA008442B1 (ru) 2007-06-29
PL209910B1 (pl) 2011-11-30
HRP20050009B1 (hr) 2013-07-31
ECSP055530A (es) 2005-03-10
ZA200500217B (en) 2006-03-29
EP1517914A2 (de) 2005-03-30
KR101006612B1 (ko) 2011-01-10
CN1293090C (zh) 2007-01-03
PL373090A1 (en) 2005-08-08
WO2003104253A3 (de) 2004-09-16
TWI286140B (en) 2007-09-01
PE20040613A1 (es) 2004-12-01
CU23414B7 (es) 2009-09-08
CR10289A (es) 2008-11-26

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