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WO2003034028A2 - Methodes d'identification et d'utilisation de modulateurs du recepteur gamma dependant des oestrogenes - Google Patents

Methodes d'identification et d'utilisation de modulateurs du recepteur gamma dependant des oestrogenes Download PDF

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Publication number
WO2003034028A2
WO2003034028A2 PCT/US2002/032917 US0232917W WO03034028A2 WO 2003034028 A2 WO2003034028 A2 WO 2003034028A2 US 0232917 W US0232917 W US 0232917W WO 03034028 A2 WO03034028 A2 WO 03034028A2
Authority
WO
WIPO (PCT)
Prior art keywords
errγ
compound
compounds
ligand
hydroxytamoxifen
Prior art date
Application number
PCT/US2002/032917
Other languages
English (en)
Other versions
WO2003034028A3 (fr
Inventor
Steven G. Blanchard
Aaron Bayne Miller
Lisa A. Orband-Miller
Original Assignee
Smithkline Beecham Corporation
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 Smithkline Beecham Corporation filed Critical Smithkline Beecham Corporation
Priority to EP02776223A priority Critical patent/EP1436395A4/fr
Priority to JP2003536715A priority patent/JP2005509628A/ja
Priority to US10/491,677 priority patent/US20050074765A1/en
Priority to AU2002342058A priority patent/AU2002342058A1/en
Publication of WO2003034028A2 publication Critical patent/WO2003034028A2/fr
Publication of WO2003034028A3 publication Critical patent/WO2003034028A3/fr

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Classifications

    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G01N33/743—Steroid hormones
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/70567—Nuclear receptors, e.g. retinoic acid receptor [RAR], RXR, nuclear orphan receptors
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/10—Musculoskeletal or connective tissue disorders
    • G01N2800/108—Osteoporosis
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/32—Cardiovascular disorders
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/36—Gynecology or obstetrics
    • G01N2800/362—Menopause

Definitions

  • Formulations suitable for topical administration in the mouth include lozenges comprising an ERR ⁇ ligand in a flavored base, usually sucrose and acacia or tragacanth; pastilles comprising the active ingredient in an inert base such as gelatin and glycerin or sucrose and acacia; and mouth washes comprising the active ingredient in a suitable liquid carrier.
  • the ERR ⁇ ligands of the present invention can be made up in solution or suspension in a suitable sterile aqueous or non-aqueous vehicle. Additives such as buffers (e.g. sodium metabisulphite or disodium edeate) and thickening agents such as hypromellose can also be included.
  • compositions of the present invention comprising an ERR ⁇ ligand can also used in combination with other therapeutic agents.
  • the amount of an ERR ⁇ ligand of the present invention required for use in treatment will of course vary not only with the particular ERR ⁇ ligand selected but also with the route of administration, the nature of the condition being treated, and the age and condition of the patients. Selection of such an amount, referred to herein as the "therapeutically effective amount or concentration" is ultimately at the discretion of the attending physician.
  • suitable doses of pharmaceutical compositions of the present invention providing a therapeutically effective amount of an ERR ⁇ ligand will be in the range of from about 0.1 to 300 mg/kg of bodyweight per day, particularly from about 1 to 100 mg/kg of bodyweight per day.
  • An appropriate dosage unit for oral administration generally contains from about 1 to about 250 mg, more preferably 25 to 250 mg of an ERR ⁇ ligand.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Food Science & Technology (AREA)
  • Rheumatology (AREA)
  • Cell Biology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne des méthodes d'identification de composés qui interagissent avec le récepteur gamma dépendant des oestrogènes (RGDO) et qui sont utiles dans le traitement des maladies induites par RGDO et par les récepteurs des oestrogènes (RO), des facteurs de risque et des affections. Cette invention se rapporte également à des compositions pharmaceutiques contenant des composés qui interagissent directement avec RGDO et des méthodes d'utilisation de ces compositions dans le traitement des maladies induites par RGDO et RO, des facteurs de risque et des affections.
PCT/US2002/032917 2001-10-16 2002-10-16 Methodes d'identification et d'utilisation de modulateurs du recepteur gamma dependant des oestrogenes WO2003034028A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP02776223A EP1436395A4 (fr) 2001-10-16 2002-10-16 Methodes d'identification et d'utilisation de modulateurs du recepteur gamma dependant des oestrogenes
JP2003536715A JP2005509628A (ja) 2001-10-16 2002-10-16 エストロゲン関連受容体γのモジュレーターの特定方法および使用方法
US10/491,677 US20050074765A1 (en) 2002-10-16 2002-10-16 Methods for identifying and using modulators of estrogen related receptor gamma
AU2002342058A AU2002342058A1 (en) 2001-10-16 2002-10-16 Methods for identifying and using modulators of estrogen related receptor gamma

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32988801P 2001-10-16 2001-10-16
US60/329,888 2001-10-16

Publications (2)

Publication Number Publication Date
WO2003034028A2 true WO2003034028A2 (fr) 2003-04-24
WO2003034028A3 WO2003034028A3 (fr) 2004-02-19

Family

ID=23287445

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/032917 WO2003034028A2 (fr) 2001-10-16 2002-10-16 Methodes d'identification et d'utilisation de modulateurs du recepteur gamma dependant des oestrogenes

Country Status (4)

Country Link
EP (1) EP1436395A4 (fr)
JP (1) JP2005509628A (fr)
AU (1) AU2002342058A1 (fr)
WO (1) WO2003034028A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006130503A2 (fr) * 2005-05-27 2006-12-07 Janssen Pharmaceutica N.V. Complexes de fragments de peptides errg et utilisation de ceux-ci dans un nouveau medicament

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101631581B1 (ko) * 2010-06-11 2016-06-17 한국생명공학연구원 나노입자가 융합된 ｆｒｅｔ 센서 및 이를 이용한 파이토에스트로겐을 고감도로 검출하는 방법
KR101579008B1 (ko) * 2013-09-25 2015-12-22 경북대학교 산학협력단 ERR-γ 저해제를 포함하는, 망막병증의 예방 또는 치료용 약학적 조성물 및 이의 용도

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6096301A (en) * 1986-10-10 2000-08-01 Industria Farmaceutica Serono Spa Combined interferon/antiestrogen therapy for treatment of breast cancer
US6218128B1 (en) * 1997-09-12 2001-04-17 Allergan Sales, Inc. Methods of identifying compounds having nuclear receptor negative hormone and/or antagonist activities

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006130503A2 (fr) * 2005-05-27 2006-12-07 Janssen Pharmaceutica N.V. Complexes de fragments de peptides errg et utilisation de ceux-ci dans un nouveau medicament
WO2006130503A3 (fr) * 2005-05-27 2007-01-25 Janssen Pharmaceutica Nv Complexes de fragments de peptides errg et utilisation de ceux-ci dans un nouveau medicament
US7655756B2 (en) 2005-05-27 2010-02-02 Johnson & Johnson Pharmaceutical Research & Development, Llc Crystallized structure of estrogen related receptor gamma in complex with bisphenol A

Also Published As

Publication number Publication date
JP2005509628A (ja) 2005-04-14
WO2003034028A3 (fr) 2004-02-19
AU2002342058A1 (en) 2003-04-28
EP1436395A4 (fr) 2006-12-13
EP1436395A2 (fr) 2004-07-14

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