[go: up one dir, main page]

EA200300474A1 - ESTROGEN RECEPTOR MODULATORS - Google Patents

ESTROGEN RECEPTOR MODULATORS

Info

Publication number
EA200300474A1
EA200300474A1 EA200300474A EA200300474A EA200300474A1 EA 200300474 A1 EA200300474 A1 EA 200300474A1 EA 200300474 A EA200300474 A EA 200300474A EA 200300474 A EA200300474 A EA 200300474A EA 200300474 A1 EA200300474 A1 EA 200300474A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
estrogen
present
estrogen receptors
estrogen receptor
Prior art date
Application number
EA200300474A
Other languages
Russian (ru)
Inventor
Фрэнк П. Дининно
Хелен Й. Чен
Сеонгкон Ким
Джейн Й. Ву
Original Assignee
Мерк Энд Ко., Инк.
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 Мерк Энд Ко., Инк. filed Critical Мерк Энд Ко., Инк.
Publication of EA200300474A1 publication Critical patent/EA200300474A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D411/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D411/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P19/00Drugs for skeletal disorders
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D327/00Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D327/02Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
    • C07D327/06Six-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D339/00Heterocyclic compounds containing rings having two sulfur atoms as the only ring hetero atoms
    • C07D339/08Six-membered rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям и их производным, способам их получения и их использованию в качестве модуляторов рецепторов эстрогена. Соединения настоящего изобретения являются лигандами для рецепторов эстрогена и как таковые могут быть полезными для лечения или профилактики различных состояний, относящихся к функционированию эстрогена, включающих: потерю костной массы, переломы костей, остеопороз, дегенерацию хрящей, эндометриоз, фиброидное заболевание матки, приступообразное ощущение жара, повышенные уровни холестерина LDL, сердечно-сосудистое заболевание, недостаточность когнитивной деятельности, церебральные дегенеративные нарушения, рестеноз, гинекомастию, пролиферацию клеток гладких мышц сосудов, ожирение, недержание и рак, особенно молочной железы, матки и простаты.Отчет о международном поиске был опубликован 2002.08.22.The present invention relates to compounds and their derivatives, methods for their preparation and their use as modulators of estrogen receptors. The compounds of the present invention are ligands for estrogen receptors and, as such, may be useful for treating or preventing various conditions relating to the functioning of estrogen, including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, elevated LDL cholesterol levels, cardiovascular disease, cognitive insufficiency, cerebral degenerative disorders, restenosis, gynecomastia, n the role of the vascular smooth muscle cell carriage, obesity, incontinence, and cancer, especially of the mammary gland, uterus, and prostate. The international search report was published on 2002.08.22.

EA200300474A 2000-10-19 2001-10-15 ESTROGEN RECEPTOR MODULATORS EA200300474A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24158200P 2000-10-19 2000-10-19
PCT/US2001/042735 WO2002032377A2 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators

Publications (1)

Publication Number Publication Date
EA200300474A1 true EA200300474A1 (en) 2003-10-30

Family

ID=22911282

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200300474A EA200300474A1 (en) 2000-10-19 2001-10-15 ESTROGEN RECEPTOR MODULATORS

Country Status (20)

Country Link
EP (1) EP1333827A2 (en)
JP (1) JP2004511502A (en)
KR (1) KR20030042020A (en)
CN (1) CN1469743A (en)
AU (2) AU2002232381B2 (en)
BG (1) BG107676A (en)
BR (1) BR0114689A (en)
CA (1) CA2424729A1 (en)
EA (1) EA200300474A1 (en)
EC (1) ECSP034558A (en)
EE (1) EE200300153A (en)
HU (1) HUP0303563A2 (en)
IL (1) IL154984A0 (en)
IS (1) IS6761A (en)
MX (1) MXPA03003485A (en)
NO (1) NO20031737L (en)
PE (1) PE20021083A1 (en)
PL (1) PL361053A1 (en)
SK (1) SK4772003A3 (en)
WO (1) WO2002032377A2 (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030225132A1 (en) * 2002-04-11 2003-12-04 Dininno Frank P. Estrogen receptor modulators
EP1501819B1 (en) 2002-04-24 2010-09-15 Merck Sharp & Dohme Corp. Estrogen receptor modulators
DE60317061T2 (en) 2002-05-10 2008-07-24 F. Hoffmann-La Roche Ag IBANDRONIC ACID FOR THE TREATMENT AND PREVENTION OF OSTEOPOROSIS
AU2003292625B2 (en) * 2002-12-26 2008-07-24 Eisai R & D Management Co., Ltd. Selective estrogen receptor modulators
US8410109B2 (en) 2005-07-29 2013-04-02 Resverlogix Corp. Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
CA2627139A1 (en) * 2005-10-27 2007-05-03 Banyu Pharmaceutical Co., Ltd. Novel benzoxathiin derivative
AU2007345526B2 (en) 2007-02-01 2013-02-28 Resverlogix Corp. Compounds for the prevention and treatment of cardiovascular diseases
AU2010204106B2 (en) 2009-01-08 2014-05-08 Resverlogix Corp. Compounds for the prevention and treatment of cardiovascular disease
MX392179B (en) 2009-03-18 2025-03-21 Resverlogix Corp NEW ANTI-INFLAMMATORY AGENTS.
TR201818390T4 (en) 2009-04-22 2019-01-21 Resverlogix Corp NEW ANTI-INFLAMMATORY AGENTS
MX2012014431A (en) 2010-06-10 2013-02-26 Aragon Pharmaceuticals Inc MODULAR RECEPTOR OF STROGENS AND USES OF THE SAME.
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
ES2745471T3 (en) 2011-11-01 2020-03-02 Resverlogix Corp Oral immediate-release formulations for substituted quinazolinones
JP2015500346A (en) 2011-12-14 2015-01-05 セラゴン ファーマシューティカルズ,インク. Estrogen receptor modulators and uses thereof
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
EP2935253B1 (en) 2012-12-21 2018-08-01 Zenith Epigenetics Ltd. Novel heterocyclic compounds as bromodomain inhibitors
KR102662814B1 (en) 2015-03-13 2024-05-03 리스버로직스 코퍼레이션 Compositions and treatment methods for treating complement-related diseases

Also Published As

Publication number Publication date
IS6761A (en) 2003-03-27
BR0114689A (en) 2003-07-01
HUP0303563A2 (en) 2004-03-01
SK4772003A3 (en) 2003-08-05
MXPA03003485A (en) 2003-07-14
CN1469743A (en) 2004-01-21
PE20021083A1 (en) 2002-12-16
ECSP034558A (en) 2003-06-25
PL361053A1 (en) 2004-09-20
EP1333827A2 (en) 2003-08-13
AU3238102A (en) 2002-04-29
WO2002032377A3 (en) 2002-08-22
WO2002032377A2 (en) 2002-04-25
KR20030042020A (en) 2003-05-27
NO20031737L (en) 2003-06-19
EE200300153A (en) 2003-06-16
IL154984A0 (en) 2003-10-31
BG107676A (en) 2003-11-28
CA2424729A1 (en) 2002-04-25
AU2002232381B2 (en) 2004-11-18
JP2004511502A (en) 2004-04-15
NO20031737D0 (en) 2003-04-15

Similar Documents

Publication Publication Date Title
EA200300474A1 (en) ESTROGEN RECEPTOR MODULATORS
EP1501819A4 (en) OESTROGENE RECEPTOR MODULATORS
ATE524170T1 (en) ESTROGEN RECEPTOR MODULATORS
WO2002091993A3 (en) Estrogen receptor modulators
ATE329904T1 (en) ESTROGEN RECEPTOR MODULATORS
NO20072771L (en) estrogen
MX2007006878A (en) Estrogen receptor modulators.
DE69935335D1 (en) PYRAZOLE AS MODULATORS OF THE ESTROGEN RECEPTOR
WO2004073612A3 (en) Estrogen receptor modulators
PT1140889E (en) COMPOUNDS AND METHODS FOR MODULATION OF ESTROGEN RECEPTORS
PT1246814E (en) COMPOUNDS AND METHODS FOR THE MODULATION OF ESTRGEN RECEPTORS
WO2004091488A3 (en) Estrogen receptor modulators
WO2002032373A3 (en) Estrogen receptor modulators
AR039282A1 (en) STROGEN RECEIVERS MODULATORS
DE60112624D1 (en) ESTROGEN RECEPTOR LIGANDS AND METHOD
WO2006081152A3 (en) Estrogen receptor modulators
ATE517871T1 (en) ESTROGEN RECEPTOR MODULATORS
WO2002058639A3 (en) Pyranoflavonoid compounds and their use as estrogen receptor modulators
WO2004073610A3 (en) Estrogen receptor modulators
WO2004026887A3 (en) Estrogen receptor modulators
WO2008057309A3 (en) Estrogen receptor modulators
DOP2002000384A (en) MODULATORS OF ESTROGEN RECEPTORS.
DOP2005000224A (en) MODULATORS OF STROGEN RECEIVERS