WO2005051401A3 - Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol - Google Patents

Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol Download PDF

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Publication number
WO2005051401A3
WO2005051401A3 PCT/EP2004/013121 EP2004013121W WO2005051401A3 WO 2005051401 A3 WO2005051401 A3 WO 2005051401A3 EP 2004013121 W EP2004013121 W EP 2004013121W WO 2005051401 A3 WO2005051401 A3 WO 2005051401A3
Authority
WO
WIPO (PCT)
Prior art keywords
estra
trien
diol
vinyl
17beta
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/EP2004/013121
Other languages
French (fr)
Other versions
WO2005051401A2 (en
Inventor
Christa Hegele-Hartung
Karl-Heinrich Fritzemeier
Olaf Peters
Theo Pelzer
Ludwig Neyses
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.)
Bayer Pharma AG
Original Assignee
Schering AG
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 Schering AG filed Critical Schering AG
Priority to JP2006540330A priority Critical patent/JP2007512279A/en
Priority to PL04803177T priority patent/PL1689410T3/en
Priority to DE602004014020T priority patent/DE602004014020D1/en
Priority to EP04803177A priority patent/EP1689410B1/en
Priority to DK04803177T priority patent/DK1689410T3/en
Publication of WO2005051401A2 publication Critical patent/WO2005051401A2/en
Publication of WO2005051401A3 publication Critical patent/WO2005051401A3/en
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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

The present invention relates to the use of the ERb agonists 8b-Vinyl-estra-1,3,5(10)-trien-3,17b-diol and 17b-Fluor- 9a-vinyl-estra-1,3,5(10)-trien-3,16a-diol for production of medicaments for the prevention and/or treatment of hypertensive heart disease, especially for the prevention and/or treatment of one or more of the conditions selected from the group of (1) hypertension, (2) cardiac hypertrophy and (3) heart failure.
PCT/EP2004/013121 2003-11-26 2004-11-16 Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol Ceased WO2005051401A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
JP2006540330A JP2007512279A (en) 2003-11-26 2004-11-16 Selective estrogens 8β-vinyl-estradi-1,3,5 (10) -triene-3,17β-diol, and 17β-fluor-9α-vinyl-estradi-1,3,5 (10) -triene-3, Prevention and treatment of hypertensive heart disease with 16α-diol
PL04803177T PL1689410T3 (en) 2003-11-26 2004-11-16 Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol
DE602004014020T DE602004014020D1 (en) 2003-11-26 2004-11-16 PREVENTION AND TREATMENT OF HYPERTONE DISEASES WITH THE SELECTIVE ESTROGENIC 8BETA-VINYL-ESTRA-1,3,5 (10) -TRIEN-3,17BETA-DIOL AND 17BETA-FLUOR-9ALPHA-VINYL-ESTRA-1,3,5 (10 ) -triene-3,16ALPHA-dIOL
EP04803177A EP1689410B1 (en) 2003-11-26 2004-11-16 Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol
DK04803177T DK1689410T3 (en) 2003-11-26 2004-11-16 Prevention and treatment of hypertensive heart disease by the selective estrogens 8beta-vinyl-estra-1,3,5 (10) -triene-3,17beta-diol and 17beta-fluoro-9alpha-vinyl-estra-1,3,5 (10 ) -triene-3,16alpha-diol

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03090406.4 2003-11-26
EP03090406 2003-11-26

Publications (2)

Publication Number Publication Date
WO2005051401A2 WO2005051401A2 (en) 2005-06-09
WO2005051401A3 true WO2005051401A3 (en) 2005-09-01

Family

ID=34626396

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2004/013121 Ceased WO2005051401A2 (en) 2003-11-26 2004-11-16 Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol

Country Status (16)

Country Link
US (1) US20050148560A1 (en)
EP (1) EP1689410B1 (en)
JP (1) JP2007512279A (en)
AR (1) AR046672A1 (en)
AT (1) ATE395919T1 (en)
DE (1) DE602004014020D1 (en)
DK (1) DK1689410T3 (en)
ES (1) ES2307064T3 (en)
GT (1) GT200400241A (en)
PA (1) PA8618401A1 (en)
PE (1) PE20050665A1 (en)
PL (1) PL1689410T3 (en)
PT (1) PT1689410E (en)
TW (1) TW200530263A (en)
UY (1) UY28630A1 (en)
WO (1) WO2005051401A2 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10027887A1 (en) 2000-05-31 2001-12-13 Jenapharm Gmbh Compounds with a sulfonamide group and pharmaceutical compositions containing these compounds
US7534780B2 (en) 2004-05-21 2009-05-19 Bayer Schering Pharma Aktiengesellschaft Estradiol prodrugs
DE102005057224A1 (en) * 2005-11-29 2007-05-31 Bayer Schering Pharma Ag New 9-alpha substituted estratriene derivatives esterified with a sulfamoylphenyl-substituted acid residue, are prodrugs useful as carboanhydrase inhibitors for treating estrogen deficiency disorders
TWI392682B (en) * 2006-04-13 2013-04-11 Sigma Tau Ind Farmaceuti Amino derivatives of androstanes and androstenes as medicaments for cardiovascular disorders
TWI389917B (en) * 2006-04-13 2013-03-21 Sigma Tau Ind Farmaceuti Azaheterocyclyl derivatives of androstanes and androstenes as medicaments for cardiovascular disorders
US9623021B2 (en) * 2007-01-22 2017-04-18 Gtx, Inc. Nuclear receptor binding agents
US9604931B2 (en) 2007-01-22 2017-03-28 Gtx, Inc. Nuclear receptor binding agents
KR101638035B1 (en) 2007-01-22 2016-07-11 지티엑스, 인코포레이티드 Nuclear receptor binding agents
EP2143432A1 (en) * 2008-07-11 2010-01-13 Bayer Schering Pharma AG 9-alpha estratriene derivatives as ER-beta selective ligands for the prevention and treatment of intestinal cancer
US20110152840A1 (en) * 2009-12-23 2011-06-23 Drugtech Corporation Methods for reducing the occurrence of preterm delivery and other pregnancy-related conditions
US9844558B1 (en) 2015-04-30 2017-12-19 Amag Pharmaceuticals, Inc. Methods of reducing risk of preterm birth
US10556922B2 (en) 2015-09-29 2020-02-11 Amag Pharmaceuticals, Inc. Crystalline and amorphous forms of 17-alpha-hydroxyprogesterone caproate

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10019167A1 (en) * 2000-04-12 2001-10-18 Schering Ag New 8 beta-substituted 11 beta-(pentyl or hexyl)-estra-1,3,5(10)-triene derivatives, are ovary-selective estrogen receptor ligands useful e.g. as female or male contraceptives or for treating ovarian carcinoma
GB2374412A (en) * 2001-04-11 2002-10-16 Karobio Ab Hypertension treatment and assay
WO2003104253A2 (en) * 2002-06-11 2003-12-18 Schering Aktiengesellschaft 9-alpha-substituted estratrienes as selectively active estrogen

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001077139A1 (en) * 2000-04-12 2001-10-18 Schering Aktiengesellschaft 8ss-HYDROCARBYL-SUBSTITUTED ESTRATRIENES FOR USE AS SELECTIVE ESTROGENS
US7414043B2 (en) * 2002-06-11 2008-08-19 Schering Ag 9-α-substituted estratrienes as selectively active estrogens

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10019167A1 (en) * 2000-04-12 2001-10-18 Schering Ag New 8 beta-substituted 11 beta-(pentyl or hexyl)-estra-1,3,5(10)-triene derivatives, are ovary-selective estrogen receptor ligands useful e.g. as female or male contraceptives or for treating ovarian carcinoma
GB2374412A (en) * 2001-04-11 2002-10-16 Karobio Ab Hypertension treatment and assay
WO2003104253A2 (en) * 2002-06-11 2003-12-18 Schering Aktiengesellschaft 9-alpha-substituted estratrienes as selectively active estrogen

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CATALANO M; LIBRETTI A: "Captopril for the treatment of patients with hypertension and peripheral vascular disease", ANGIOLOGY, vol. 36, no. 5, 1985, pages 293 - 296, XP009049918 *
MOERS A; SCHREZENMEIR J: "Palmitic acid but not stearic acid inhibits NO-production in endothelial cells", EXPERIMENTAL AND CLINICAL ENDOCRINOLOGY AND DIABETES, vol. 105, no. 2, 1997, pages 78 - 80, XP009049890 *

Also Published As

Publication number Publication date
TW200530263A (en) 2005-09-16
AR046672A1 (en) 2005-12-14
PT1689410E (en) 2008-08-18
GT200400241A (en) 2005-10-31
ES2307064T3 (en) 2008-11-16
DE602004014020D1 (en) 2008-07-03
WO2005051401A2 (en) 2005-06-09
UY28630A1 (en) 2005-06-30
PL1689410T3 (en) 2008-10-31
JP2007512279A (en) 2007-05-17
PA8618401A1 (en) 2005-08-04
US20050148560A1 (en) 2005-07-07
PE20050665A1 (en) 2005-11-02
EP1689410B1 (en) 2008-05-21
EP1689410A2 (en) 2006-08-16
DK1689410T3 (en) 2008-09-08
ATE395919T1 (en) 2008-06-15

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