EA201100226A1 - Производные эстратриена, содержащие гетероциклические биоизостеры для фенольного а-кольца - Google Patents

Производные эстратриена, содержащие гетероциклические биоизостеры для фенольного а-кольца

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Publication number
EA201100226A1
EA201100226A1 EA201100226A EA201100226A EA201100226A1 EA 201100226 A1 EA201100226 A1 EA 201100226A1 EA 201100226 A EA201100226 A EA 201100226A EA 201100226 A EA201100226 A EA 201100226A EA 201100226 A1 EA201100226 A1 EA 201100226A1
Authority
EA
Eurasian Patent Office
Prior art keywords
derivatives
bioisolas
estratrien
containing heterocyclic
estrogen receptor
Prior art date
Application number
EA201100226A
Other languages
English (en)
Inventor
Торстен Блуме
Дитер Хельдманн
Норберт Шмес
Кристиане Отто
Тим Винтермантель
Йоахим Кунке
Original Assignee
Байер Шеринг Фарма 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 Байер Шеринг Фарма Акциенгезельшафт filed Critical Байер Шеринг Фарма Акциенгезельшафт
Publication of EA201100226A1 publication Critical patent/EA201100226A1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0047—Nitrogen only at position 2(3)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P15/18—Feminine contraceptives
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P9/10—Drugs 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pregnancy & Childbirth (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)

Abstract

Изобретение относится к новым производным пиразолоэстриена и триазолоэстриена, фармацевтическим композициям, которые их содержат, и к их применению для лечения или предотвращения нарушений и заболеваний, опосредуемых рецептором эстрогена, таких как приливы, вагинальная сухость, остеопения, остеопороз, гиперлипидемия, потеря познавательной функции, дегенеративные заболевания головного мозга, сердечно-сосудистые заболевания, нарушения мозгового кровообращения, гормонально-чувствительные злокачественные новообразования и гиперплазия (в тканях, включая молочную железу, эндометрий и шейку матки у женщин и предстательную железу у мужчин), эндометриоз, фиброз матки, остеоартрит; и в качестве противозачаточных средств либо отдельно или в комбинации с прогестогеном или антагонистом прогестогена. Соединения в соответствии с изобретением являются селективными модуляторами рецептора эстрогена.
EA201100226A 2008-07-24 2009-07-14 Производные эстратриена, содержащие гетероциклические биоизостеры для фенольного а-кольца EA201100226A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08161108A EP2147924A1 (en) 2008-07-24 2008-07-24 Estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring
PCT/EP2009/005086 WO2010009828A1 (en) 2008-07-24 2009-07-14 Estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring

Publications (1)

Publication Number Publication Date
EA201100226A1 true EA201100226A1 (ru) 2011-08-30

Family

ID=40329347

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201100226A EA201100226A1 (ru) 2008-07-24 2009-07-14 Производные эстратриена, содержащие гетероциклические биоизостеры для фенольного а-кольца

Country Status (24)

Country Link
US (1) US20110190246A1 (ru)
EP (2) EP2147924A1 (ru)
JP (1) JP2011528675A (ru)
KR (1) KR20110036739A (ru)
CN (1) CN102105484A (ru)
AR (1) AR072533A1 (ru)
AU (1) AU2009273494A1 (ru)
BR (1) BRPI0915987A2 (ru)
CA (1) CA2731634A1 (ru)
CL (1) CL2011000153A1 (ru)
CO (1) CO6351799A2 (ru)
CR (1) CR20110045A (ru)
DO (1) DOP2011000024A (ru)
EA (1) EA201100226A1 (ru)
EC (1) ECSP11010780A (ru)
IL (1) IL210314A0 (ru)
MA (1) MA32477B1 (ru)
MX (1) MX2011000939A (ru)
PE (1) PE20110402A1 (ru)
SV (1) SV2011003817A (ru)
TW (1) TW201008570A (ru)
UY (1) UY32005A (ru)
WO (1) WO2010009828A1 (ru)
ZA (1) ZA201101445B (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011092127A1 (en) * 2010-01-26 2011-08-04 Bayer Schering Pharma Aktiengesellschaft 14,17-bridged estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring
CN115836068A (zh) * 2020-05-15 2023-03-21 先声药业有限公司 吡咯烷类化合物及其应用
DE102022109556A1 (de) 2022-04-20 2023-10-26 Eberspächer Catem Gmbh & Co. Kg Elektrische Heizvorrichtung
DE102022109544A1 (de) 2022-04-20 2023-10-26 Eberspächer Catem Gmbh & Co. Kg Elektrische Heizvorrichtung

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3458504A (en) * 1966-10-24 1969-07-29 Sterling Drug Inc Steroido(3,4-c)pyrazoles of the 5alpha- and 5beta-androstane series
CA2491132A1 (en) * 2002-07-03 2004-01-15 Ortho-Mcneil Pharmaceutical, Inc. Estrieno[3,2-b]/[3,4-c]pyrrole derivatives useful as modulators of the estrogen receptors

Also Published As

Publication number Publication date
CO6351799A2 (es) 2011-12-20
ZA201101445B (en) 2012-07-25
KR20110036739A (ko) 2011-04-08
AU2009273494A1 (en) 2010-01-28
CN102105484A (zh) 2011-06-22
PE20110402A1 (es) 2011-06-19
AR072533A1 (es) 2010-09-01
IL210314A0 (en) 2011-03-31
SV2011003817A (es) 2011-05-20
UY32005A (es) 2010-02-26
TW201008570A (en) 2010-03-01
CL2011000153A1 (es) 2011-07-08
BRPI0915987A2 (pt) 2019-09-24
CA2731634A1 (en) 2010-01-28
MX2011000939A (es) 2011-03-04
EP2147924A1 (en) 2010-01-27
JP2011528675A (ja) 2011-11-24
EP2307439A1 (en) 2011-04-13
MA32477B1 (fr) 2011-07-03
WO2010009828A1 (en) 2010-01-28
US20110190246A1 (en) 2011-08-04
DOP2011000024A (es) 2011-02-28
ECSP11010780A (es) 2011-02-28
CR20110045A (es) 2012-05-28

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