WO2002032377A3 - Estrogen receptor modulators - Google Patents

Estrogen receptor modulators Download PDF

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Publication number
WO2002032377A3
WO2002032377A3 PCT/US2001/042735 US0142735W WO0232377A3 WO 2002032377 A3 WO2002032377 A3 WO 2002032377A3 US 0142735 W US0142735 W US 0142735W WO 0232377 A3 WO0232377 A3 WO 0232377A3
Authority
WO
WIPO (PCT)
Prior art keywords
estrogen
receptor modulators
compounds
estrogen receptor
functioning
Prior art date
Application number
PCT/US2001/042735
Other languages
French (fr)
Other versions
WO2002032377A2 (en
Inventor
Frank P Dininno
Helen Y Chen
Seongkon Kim
Jane Y Wu
Original Assignee
Merck & Co Inc
Frank P Dininno
Helen Y Chen
Seongkon Kim
Jane Y Wu
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 to BR0114689-0A priority Critical patent/BR0114689A/en
Priority to JP2002535616A priority patent/JP2004511502A/en
Priority to AU2002232381A priority patent/AU2002232381B2/en
Priority to PL01361053A priority patent/PL361053A1/en
Priority to KR10-2003-7005518A priority patent/KR20030042020A/en
Priority to AU3238102A priority patent/AU3238102A/en
Priority to SK477-2003A priority patent/SK4772003A3/en
Priority to EP01987654A priority patent/EP1333827A2/en
Priority to EEP200300153A priority patent/EE200300153A/en
Priority to CA002424729A priority patent/CA2424729A1/en
Application filed by Merck & Co Inc, Frank P Dininno, Helen Y Chen, Seongkon Kim, Jane Y Wu filed Critical Merck & Co Inc
Priority to IL15498401A priority patent/IL154984A0/en
Priority to EA200300474A priority patent/EA200300474A1/en
Priority to HU0303563A priority patent/HUP0303563A2/en
Priority to MXPA03003485A priority patent/MXPA03003485A/en
Priority to US10/120,723 priority patent/US6750213B2/en
Priority to PE2002000308A priority patent/PE20021083A1/en
Publication of WO2002032377A2 publication Critical patent/WO2002032377A2/en
Publication of WO2002032377A3 publication Critical patent/WO2002032377A3/en
Priority to BG107676A priority patent/BG107676A/en
Priority to IS6761A priority patent/IS6761A/en
Priority to NO20031737A priority patent/NO20031737L/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic 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
    • C07D411/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D411/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02—Heterocyclic 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
    • C07D411/12—Heterocyclic 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
    • 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
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D327/00—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D327/02—Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms one oxygen atom and one sulfur atom
    • C07D327/06—Six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D339/00—Heterocyclic compounds containing rings having two sulfur atoms as the only ring hetero atoms
    • C07D339/08—Six-membered rings

Landscapes

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

Abstract

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
PCT/US2001/042735 2000-10-19 2001-10-15 Estrogen receptor modulators WO2002032377A2 (en)

Priority Applications (19)

Application Number Priority Date Filing Date Title
IL15498401A IL154984A0 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
JP2002535616A JP2004511502A (en) 2000-10-19 2001-10-15 Estrogen receptor modulator
PL01361053A PL361053A1 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
KR10-2003-7005518A KR20030042020A (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
AU3238102A AU3238102A (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
SK477-2003A SK4772003A3 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
EP01987654A EP1333827A2 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
EA200300474A EA200300474A1 (en) 2000-10-19 2001-10-15 ESTROGEN RECEPTOR MODULATORS
CA002424729A CA2424729A1 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
BR0114689-0A BR0114689A (en) 2000-10-19 2001-10-15 Compound, pharmaceutical composition, process for producing a pharmaceutical composition, methods for eliciting an estrogen receptor modulation effect in a mammal, for the treatment or prevention of osteoporosis, postmenopause in a female, and for the treatment or prevention of a disorder
AU2002232381A AU2002232381B2 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
EEP200300153A EE200300153A (en) 2000-10-19 2001-10-15 Estrogen Receptor Modulators, Pharmaceutical Composition and Method of Preparation
HU0303563A HUP0303563A2 (en) 2000-10-19 2001-10-15 Estrogen receptor modulators
MXPA03003485A MXPA03003485A (en) 2000-10-19 2001-10-15 Estrogen receptor modulators.
US10/120,723 US6750213B2 (en) 2000-10-19 2002-04-11 Estrogen receptor modulators
PE2002000308A PE20021083A1 (en) 2000-10-19 2002-04-15 MODULATORS OF THE ESTROGEN RECEPTORS
BG107676A BG107676A (en) 2000-10-19 2003-03-26 Estrogen receptor modulators
IS6761A IS6761A (en) 2000-10-19 2003-03-27 Estrogen receptor regulators
NO20031737A NO20031737L (en) 2000-10-19 2003-04-15 estrogen

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24158200P 2000-10-19 2000-10-19
US60/241,582 2000-10-19

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US10/120,723 Continuation-In-Part US6750213B2 (en) 2000-10-19 2002-04-11 Estrogen receptor modulators

Publications (2)

Publication Number Publication Date
WO2002032377A2 WO2002032377A2 (en) 2002-04-25
WO2002032377A3 true WO2002032377A3 (en) 2002-08-22

Family

ID=22911282

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/042735 WO2002032377A2 (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 (17)

* 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
ATE481397T1 (en) * 2002-04-24 2010-10-15 Merck Sharp & Dohme MODULATORS OF THE ESTROGEN RECEPTOR
WO2004058682A1 (en) * 2002-12-26 2004-07-15 Eisai Co., Ltd. Selective estrogen receptor modulators
NZ566180A (en) 2005-07-29 2011-04-29 Resverlogix Corp Pharmaceutical compositions for the prevention and treatment of complex diseases and their delivery by insertable medical devices
US8163770B2 (en) * 2005-10-27 2012-04-24 Msd. K. K. Benzoxathiin derivative
US8053440B2 (en) 2007-02-01 2011-11-08 Resverlogix Corporation 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
NZ617779A (en) 2009-03-18 2015-08-28 Resverlogix Corp Novel anti-inflammatory agents
KR20180096823A (en) 2009-04-22 2018-08-29 리스버로직스 코퍼레이션 Novel anti-inflammatory agents
LT2580210T (en) 2010-06-10 2017-07-25 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
WO2011159769A2 (en) 2010-06-17 2011-12-22 Aragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
RS58911B1 (en) 2011-11-01 2019-08-30 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
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
JP2016507496A (en) 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． Novel heterocyclic compounds as bromodomain inhibitors
US10111885B2 (en) 2015-03-13 2018-10-30 Resverlogix Corp. Compositions and therapeutic methods for the treatment of complement-associated diseases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BENDINSKAS ET AL.: "Sequence-specific photomodification of DNA by an oligonucleotide-phenanthrodihydrodioxin conjugate", BIOCONJUGATE CHEMISTRY, vol. 9, no. 5, September 1998 (1998-09-01), pages 555 - 563, XP002909731 *

Also Published As

Publication number Publication date
CN1469743A (en) 2004-01-21
MXPA03003485A (en) 2003-07-14
JP2004511502A (en) 2004-04-15
ECSP034558A (en) 2003-06-25
EA200300474A1 (en) 2003-10-30
AU2002232381B2 (en) 2004-11-18
AU3238102A (en) 2002-04-29
EE200300153A (en) 2003-06-16
HUP0303563A2 (en) 2004-03-01
WO2002032377A2 (en) 2002-04-25
CA2424729A1 (en) 2002-04-25
NO20031737L (en) 2003-06-19
IS6761A (en) 2003-03-27
IL154984A0 (en) 2003-10-31
PE20021083A1 (en) 2002-12-16
BG107676A (en) 2003-11-28
SK4772003A3 (en) 2003-08-05
PL361053A1 (en) 2004-09-20
NO20031737D0 (en) 2003-04-15
KR20030042020A (en) 2003-05-27
BR0114689A (en) 2003-07-01
EP1333827A2 (en) 2003-08-13

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