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WO2000076529A3 - Recepteur d'oestrogenes - Google Patents

Recepteur d'oestrogenes Download PDF

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Publication number
WO2000076529A3
WO2000076529A3 PCT/GB2000/002283 GB0002283W WO0076529A3 WO 2000076529 A3 WO2000076529 A3 WO 2000076529A3 GB 0002283 W GB0002283 W GB 0002283W WO 0076529 A3 WO0076529 A3 WO 0076529A3
Authority
WO
WIPO (PCT)
Prior art keywords
erko
derko
estrogen
skeleton
berko
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/GB2000/002283
Other languages
English (en)
Other versions
WO2000076529A2 (fr
Inventor
Claes Ohlsson
Jan Ake Gustafsson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Karo Healthcare AB
Original Assignee
Karo Bio AB
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 Karo Bio AB filed Critical Karo Bio AB
Priority to EP00940530A priority Critical patent/EP1185287A2/fr
Priority to AU55454/00A priority patent/AU5545400A/en
Priority to CA002376441A priority patent/CA2376441A1/fr
Publication of WO2000076529A2 publication Critical patent/WO2000076529A2/fr
Publication of WO2000076529A3 publication Critical patent/WO2000076529A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Les androgènes régulent le squelette du mâle directement, par la stimulation de récepteurs d'androgènes, et indirectement, par l'aromatisation d'androgènes et par leur transformation en oestrogènes suivie de la stimulation des récepteurs d'oestrogènes (RO). Afin d'étudier dans le détail l'importance relative des sous-types de récepteurs oestrogènes dans la régulation du squelette mâle, on a comparé les phénotypes du squelette des souris de type sauvage (TS), ROα, Knock-out (ROKO), ROβ Knock-out (BROKO) et ROα/β Double Knock-out (DROKO). ROKO et DROKO ont un poids corporel réduit et une croissance longitudinale d'os moins importante. En outre, ROKO et DROKO mais pas BROKO manifestent une diminution prononcée de la teneur minérale dans les os longs et le squelette axial. Cette diminution de la teneur minérale des os est due à l'ostéopénie corticale causée par une croissance radicale des os moins importante. Des tests mécaniques ont montré que le fémur des ROKO est plus faible, ce qui est une conséquence du changement des dimensions de l'os cortical. Dans aucun groupe, on n'a remarqué aucun changement notable au niveau de la densité osseuse trabéculaire. Les ROKO ont manifesté des taux de sérum réduits en ostéocalcine et en IGF-I. En outre, les taux de sérum en IGF-I ont été corrélés avec la plupart des changements au niveau du squelette que l'on a vu chez DROKO et ROKO. On peut en conclure que les phénotypes squelettiques des DROKO et des ROKO sont similaires et peuvent être clairement distingués du TS et des BROKO. Ainsi, c'est le récepteur ROα mais non pas celui ROβ qui sert de médiateur de l'effet de l'oestrogène dans le squelette de la souris.
PCT/GB2000/002283 1999-06-11 2000-06-12 Recepteur d'oestrogenes Ceased WO2000076529A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP00940530A EP1185287A2 (fr) 1999-06-11 2000-06-12 Recepteur d'oestrogenes
AU55454/00A AU5545400A (en) 1999-06-11 2000-06-12 Estrogen receptor
CA002376441A CA2376441A1 (fr) 1999-06-11 2000-06-12 Recepteur d'oestrogenes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9913649.1A GB9913649D0 (en) 1999-06-11 1999-06-11 Estrogen receptor
GB9913649.1 1999-06-11

Publications (2)

Publication Number Publication Date
WO2000076529A2 WO2000076529A2 (fr) 2000-12-21
WO2000076529A3 true WO2000076529A3 (fr) 2001-07-12

Family

ID=10855195

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2000/002283 Ceased WO2000076529A2 (fr) 1999-06-11 2000-06-12 Recepteur d'oestrogenes

Country Status (5)

Country Link
EP (1) EP1185287A2 (fr)
AU (1) AU5545400A (fr)
CA (1) CA2376441A1 (fr)
GB (1) GB9913649D0 (fr)
WO (1) WO2000076529A2 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA83620C2 (ru) 2001-12-05 2008-08-11 Уайт Замещенные бензоксазолы и их аналоги как эстрогенные агенты
US6835745B2 (en) 2002-01-15 2004-12-28 Wyeth Phenyl substituted thiophenes as estrogenic agents
CN101052641A (zh) 2004-09-07 2007-10-10 惠氏公司 6H－[1]苯并吡喃并[4,3－b]喹啉及其作为雌激素药物的用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0629697A2 (fr) * 1993-06-21 1994-12-21 Eli Lilly And Company Matériael et méthodes de screening d'agents anti-ostéoporotiques
WO1996002565A1 (fr) * 1994-07-20 1996-02-01 Celtrix Pharmaceuticals, Inc. Complexe igf/igfbp destines a favoriser la formation osseuse et a reguler le remodelage osseux
WO1997031640A1 (fr) * 1996-02-28 1997-09-04 Pfizer Inc. Therapie combinee de l'osteoporose
WO1998025623A1 (fr) * 1996-12-09 1998-06-18 Merck & Co., Inc. Procedes et compositions destines a prevenir et a traiter la perte osseuse

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0629697A2 (fr) * 1993-06-21 1994-12-21 Eli Lilly And Company Matériael et méthodes de screening d'agents anti-ostéoporotiques
WO1996002565A1 (fr) * 1994-07-20 1996-02-01 Celtrix Pharmaceuticals, Inc. Complexe igf/igfbp destines a favoriser la formation osseuse et a reguler le remodelage osseux
WO1997031640A1 (fr) * 1996-02-28 1997-09-04 Pfizer Inc. Therapie combinee de l'osteoporose
WO1998025623A1 (fr) * 1996-12-09 1998-06-18 Merck & Co., Inc. Procedes et compositions destines a prevenir et a traiter la perte osseuse

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BARKHEM ET AL: "Differential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists", MOLECULAR PHARMACOLOGY, vol. 54, no. 1, August 1998 (1998-08-01), pages 105 - 111, XP000978331 *
EVANS, GLENDA ET AL: "The effects of raloxifene on tibia histomorphometry in ovariectomized rats", ENDOCRINOLOGY (1994), 134(5), 2283-8, XP000563692 *
EVANS, GLENDA L. ET AL: "Raloxifene inhibits bone turnover and prevents further cancellous bone loss in adult ovariectomized rats wit established osteopenia", ENDOCRINOLOGY (1996), 137(10), 4139-4144, XP002088886 *
FRITZ, P. C. ET AL: "Tamoxifen attenuates the effects of exogenous glucocorticoid on bone formation and growth in piglets", ENDOCRINOLOGY (1998), 139(8), 3399-3403, XP000979648 *
LABRIE, FERNAND ET AL: "EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium", J. STEROID BIOCHEM. MOL. BIOL. (1999), 69(1-6), 51-84, XP000978361 *
NILSSON ET AL: "ER-beta: A novel estrogen receptor offers the potential for new drug development", TRENDS ENDOCRINOL. METAB., vol. 9, no. 10, 1998, pages 387 - 395, XP000978334 *

Also Published As

Publication number Publication date
GB9913649D0 (en) 1999-08-11
WO2000076529A2 (fr) 2000-12-21
EP1185287A2 (fr) 2002-03-13
AU5545400A (en) 2001-01-02
CA2376441A1 (fr) 2000-12-21

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