EA200100828A1 - 16-гидроксиэстратриены в качестве эстрогенов избирательного действия - Google Patents

16-гидроксиэстратриены в качестве эстрогенов избирательного действия

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Publication number
EA200100828A1
EA200100828A1 EA200100828A EA200100828A EA200100828A1 EA 200100828 A1 EA200100828 A1 EA 200100828A1 EA 200100828 A EA200100828 A EA 200100828A EA 200100828 A EA200100828 A EA 200100828A EA 200100828 A1 EA200100828 A1 EA 200100828A1
Authority
EA
Eurasian Patent Office
Prior art keywords
new compounds
estrogen receptor
preparations
rat
describes
Prior art date
Application number
EA200100828A
Other languages
English (en)
Inventor
Герман Кюнцер
Рудольф Кнауте
Моника Лессль
Карл-Генрих Фрицемайер
Криста Хегеле-Хартунг
Ульф Бёмер
Герд Мюллер
Дирк Коземунд
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 EA200100828A1 publication Critical patent/EA200100828A1/ru

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    • 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
    • C07J41/0094Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07J1/0055Estrane derivatives not substituted in position 17
    • 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
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J15/00Stereochemically pure steroids containing carbon, hydrogen, halogen or oxygen having a partially or totally inverted skeleton, e.g. retrosteroids, L-isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J33/00Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J33/002Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J53/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002Carbocyclic rings fused
    • C07J53/0043 membered carbocyclic rings

Abstract

В заявке описываются новые соединения в качестве фармацевтически активных веществ, характеризующиеся более высокой степенью аффиности in vitro на препаратах эстрогенного рецептора простаты крысы в сравнении с этим показателем на препаратах эстрогенного рецептора матки крысы и предпочтительно проявляющих in vivo преимущественную эффективность по отношению к костной ткани в сравнении с воздействием на матку и/или оказывающих четко выраженное воздействие на стимуляцию экспрессии 5НТ2а-рецептора и переносчика. В заявке описываются также получение предлагаемых соединений, их применение в терапии и фармацевтические лекарственные формы, содержащие эти новые соединения. Новые соединения представляют собой 16α- и 16β-гидроксиэстра-1,3,5(10)-эстратриены, которые в стероидном скелете могут нести другие заместители, а в кольцах В, С и D могут иметь одну или несколько дополнительных двойных связей.Отчет о международном поиске был опубликован 2001.08.02.
EA200100828A 1999-02-09 2000-02-09 16-гидроксиэстратриены в качестве эстрогенов избирательного действия EA200100828A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19906159A DE19906159A1 (de) 1999-02-09 1999-02-09 16-Hydroxyestratriene als selektiv wirksame Estrogene
PCT/EP2000/001073 WO2000047603A2 (de) 1999-02-09 2000-02-09 16-hydroxyestratriene als selektiv wirksame estrogene

Publications (1)

Publication Number Publication Date
EA200100828A1 true EA200100828A1 (ru) 2002-04-25

Family

ID=7897485

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200100828A EA200100828A1 (ru) 1999-02-09 2000-02-09 16-гидроксиэстратриены в качестве эстрогенов избирательного действия

Country Status (30)

Country Link
EP (2) EP1144431B1 (ru)
JP (1) JP2002536455A (ru)
KR (1) KR20010101822A (ru)
CN (1) CN1346364A (ru)
AR (1) AR034392A1 (ru)
AT (1) ATE313553T1 (ru)
AU (1) AU2909500A (ru)
BG (1) BG105804A (ru)
BR (1) BR0008076A (ru)
CA (1) CA2359660A1 (ru)
CO (1) CO5150223A1 (ru)
CZ (1) CZ20012843A3 (ru)
DE (2) DE19906159A1 (ru)
DK (1) DK1144431T3 (ru)
EA (1) EA200100828A1 (ru)
EE (1) EE200100412A (ru)
ES (1) ES2255983T3 (ru)
HK (1) HK1046145A1 (ru)
HU (1) HUP0200055A3 (ru)
IL (1) IL144455A0 (ru)
MX (1) MXPA01008065A (ru)
NO (1) NO20013860L (ru)
NZ (1) NZ513409A (ru)
PE (1) PE20001461A1 (ru)
PL (1) PL350360A1 (ru)
PT (1) PT1144431E (ru)
SK (1) SK11302001A3 (ru)
WO (1) WO2000047603A2 (ru)
YU (1) YU57201A (ru)
ZA (1) ZA200107388B (ru)

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DE10151365A1 (de) 2001-10-17 2003-04-30 Schering Ag 17-Chlor-D-Homosteroide als selektive Estrogenrezeptorantagonisten
DK1365768T3 (da) * 2001-02-27 2008-08-18 Bayer Schering Pharma Ag Anvendelse af ER-beta-selektive antagonister som contraception.
DE10151114A1 (de) * 2001-10-15 2003-04-17 Schering Ag 8ß-Substituierte-11ß-aryl-estra-2,3,5(10)-trienderivate
DE10151363A1 (de) * 2001-10-17 2003-05-08 Schering Ag Somatotrope Therapie
DE10226326A1 (de) * 2002-06-11 2004-01-15 Schering Ag 9-alpha-substiuierte Estratriene als selektiv wirksame Estrogene
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TWI389917B (zh) * 2006-04-13 2013-03-21 Sigma Tau Ind Farmaceuti 作為心血管疾病治療藥物的雄甾烷與雄甾烯之氮雜環烷基衍生物
SE536263C2 (sv) * 2011-12-21 2013-07-23 Airqone Building Scandinavia Ab Reningsanordning för gasmedium innefattande medel för kontrollerad tillförsel av joniserad luft
PL3500265T3 (pl) * 2016-08-22 2024-03-11 Or-Genix Therapeutics, Inc. Selektywne ligandy receptora estrogenowego beta
WO2019041078A1 (en) * 2017-08-28 2019-03-07 Zhejiang Jiachi Pharmaceutical Development Ltd. ASYMMETRIC SYNTHESIS AND USES OF COMPOUNDS IN TREATMENT OF DISEASES
JP2021535183A (ja) * 2018-09-07 2021-12-16 トラスティーズ・オヴ・ダートマス・カレッジ C19骨格およびステロイドならびにそれらの使用および製造方法
CN115154474A (zh) * 2021-04-01 2022-10-11 中国人民解放军总医院 一种环菠萝蜜烷型三萜皂苷化合物在制备t细胞免疫抑制剂中的应用

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Also Published As

Publication number Publication date
NZ513409A (en) 2004-02-27
AU2909500A (en) 2000-08-29
ES2255983T3 (es) 2006-07-16
CZ20012843A3 (cs) 2002-01-16
WO2000047603A9 (de) 2001-09-07
ZA200107388B (en) 2005-01-25
KR20010101822A (ko) 2001-11-14
PL350360A1 (en) 2002-12-02
HUP0200055A2 (hu) 2002-05-29
EE200100412A (et) 2002-12-16
NO20013860D0 (no) 2001-08-08
PT1144431E (pt) 2006-05-31
HK1046145A1 (zh) 2002-12-27
YU57201A (sh) 2005-06-10
PE20001461A1 (es) 2000-12-18
CN1346364A (zh) 2002-04-24
WO2000047603A2 (de) 2000-08-17
JP2002536455A (ja) 2002-10-29
NO20013860L (no) 2001-10-08
DE19906159A1 (de) 2000-08-10
WO2000047603A3 (de) 2001-08-02
IL144455A0 (en) 2002-05-23
DK1144431T3 (da) 2006-05-08
HUP0200055A3 (en) 2002-10-28
EP1144431A2 (de) 2001-10-17
EP1144431A3 (de) 2002-06-12
SK11302001A3 (sk) 2002-01-07
ATE313553T1 (de) 2006-01-15
AR034392A1 (es) 2004-02-25
BR0008076A (pt) 2002-02-05
CO5150223A1 (es) 2002-04-29
EP1144431B1 (de) 2005-12-21
EP1580192A2 (de) 2005-09-28
CA2359660A1 (en) 2000-08-17
BG105804A (en) 2002-03-29
MXPA01008065A (es) 2002-04-24
DE50011908D1 (de) 2006-01-26

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