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WO2002072003A3 - Use of steroid derivatives for the treatment of a benighn and/or malignant tumour - Google Patents

Use of steroid derivatives for the treatment of a benighn and/or malignant tumour Download PDF

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Publication number
WO2002072003A3
WO2002072003A3 PCT/SE2002/000443 SE0200443W WO02072003A3 WO 2002072003 A3 WO2002072003 A3 WO 2002072003A3 SE 0200443 W SE0200443 W SE 0200443W WO 02072003 A3 WO02072003 A3 WO 02072003A3
Authority
WO
WIPO (PCT)
Prior art keywords
androstane
medicament
treatment
derivatives
malignant tumour
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/SE2002/000443
Other languages
French (fr)
Other versions
WO2002072003A2 (en
Inventor
Tomas Hagstroem
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to CA002440973A priority Critical patent/CA2440973A1/en
Priority to EP02704017A priority patent/EP1379542A2/en
Priority to AU2002237613A priority patent/AU2002237613B2/en
Priority to JP2002570963A priority patent/JP2004524325A/en
Publication of WO2002072003A2 publication Critical patent/WO2002072003A2/en
Publication of WO2002072003A3 publication Critical patent/WO2002072003A3/en
Priority to US10/658,125 priority patent/US20050192262A1/en
Anticipated expiration legal-status Critical
Priority to US11/609,643 priority patent/US20070111973A1/en
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/366Lactones having six-membered rings, e.g. delta-lactones
    • A61K31/37Coumarins, e.g. psoralen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/568Compounds 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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • A61K31/568Compounds 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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/569Compounds 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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0014Androstane derivatives substituted in position 17 alfa, not substituted in position 17 beta

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention relates to steroid derivatives for use as medicaments. More specifically, the invention also relates to the use of a steroid derivative of 5-androstene-, 5-pregnenolone or corresponding saturated derivatives (androstane- or pregnane-) in the manufacture of a medicament for the treatment of a benign and/or malignant tumour, which medicament is capable of interrupting disturbances in Wnt-signaling, such as cell-cycle arrest in G1-phase, and/or providing an angiostatic effect. Examples of such steroid derivatives are Δ-5-androstene-17α-ol, androstane-17α-ol-pregnane-17α-ol or pregnane-17α-ol derivatives. In a further aspect, the invention relates to a method of producing a medicament for the treatment of a benign and/or malignant tumour and/or an inflammatory condition comprising the steps of contacting 5-androstane-3ß,17α-diol or androstane-3ßα-diol, an enzyme and a sulfotransferase to provide 5-androstene-17α-ol-3ß-sulfate or corresponding androstane derivative (17α-AEDS or 17-AADS); and mixing the 17α-AEDS or 17α-AADS so produced with a suitable carrier; whereby a medicament which is capable of acting as a ligand to perox-isome proliferator-activated receptor-η (PPARη) is produced.
PCT/SE2002/000443 2001-03-13 2002-03-11 Use of steroid derivatives for the treatment of a benighn and/or malignant tumour Ceased WO2002072003A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CA002440973A CA2440973A1 (en) 2001-03-13 2002-03-11 Use of steroid derivatives for the treatment of a benighn and/or malignant tumour
EP02704017A EP1379542A2 (en) 2001-03-13 2002-03-11 Treatment of tumours
AU2002237613A AU2002237613B2 (en) 2001-03-13 2002-03-11 Use of steroid derivatives for the treatment of a benighn and/or malignant tumour
JP2002570963A JP2004524325A (en) 2001-03-13 2002-03-11 Use of steroid derivatives for the treatment of benign and / or malignant tumors
US10/658,125 US20050192262A1 (en) 2001-03-13 2003-09-09 Treatment of tumours
US11/609,643 US20070111973A1 (en) 2001-03-13 2006-12-12 Treatment of tumours

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE0100857-2 2001-03-13
SE0100857A SE0100857D0 (en) 2001-03-13 2001-03-13 Treatment of tumors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US10/658,125 Continuation US20050192262A1 (en) 2001-03-13 2003-09-09 Treatment of tumours

Publications (2)

Publication Number Publication Date
WO2002072003A2 WO2002072003A2 (en) 2002-09-19
WO2002072003A3 true WO2002072003A3 (en) 2003-02-20

Family

ID=20283329

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/SE2002/000443 Ceased WO2002072003A2 (en) 2001-03-13 2002-03-11 Use of steroid derivatives for the treatment of a benighn and/or malignant tumour

Country Status (6)

Country Link
EP (1) EP1379542A2 (en)
JP (1) JP2004524325A (en)
AU (1) AU2002237613B2 (en)
CA (1) CA2440973A1 (en)
SE (1) SE0100857D0 (en)
WO (1) WO2002072003A2 (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7223761B2 (en) 2003-10-03 2007-05-29 Amgen Inc. Salts and polymorphs of a potent antidiabetic compound
US7601841B2 (en) 2000-06-28 2009-10-13 Amgen Inc. Quinolinyl and benzothiazolyl modulators
US7626033B2 (en) 1999-06-30 2009-12-01 Amgen Inc. Compounds for the modulation of PPARγ activity

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5912240A (en) 1997-04-10 1999-06-15 Loria; Roger M. 5-androstene 3β, 17α diol as an inhibitor of tumor growth
ATE411028T1 (en) * 2002-03-21 2008-10-15 Roger M Loria ALPHA-AED AND BETA-AED REGULATION OF NUCLEAR TRANSCRIPTION, GENE REGULATION AND/OR GENE EXPRESSION
CN1964706A (en) 2004-03-17 2007-05-16 拉斯·M·拉森 Preventing retinopathy by inhibiting the visual cycle
GB2421183A (en) * 2004-12-17 2006-06-21 Stegram Pharmaceuticals Ltd Topical formulations for use in the treatment or prevention of skin cancers
EP2147673A1 (en) * 2006-11-30 2010-01-27 Hunter-Fleming Limited Modulation of prostaglandin/cyclooxygenase metabolic pathways
EP2709631B9 (en) 2011-05-20 2017-07-26 INSERM - Institut National de la Santé et de la Recherche Médicale Antagonists of cb1 receptor
CA2892347C (en) 2012-11-28 2019-04-02 Inserm (Institut National De La Sante Et De La Recherche Medicale) 3-(4'-substituted)-benzyl-ether derivatives of pregnenolone
WO2023246940A1 (en) * 2022-06-24 2023-12-28 Huang Chi Ying Method of treating a cancer through suppression of growth of cancer stem cells, and downregulation of wnt pathway

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5912240A (en) * 1997-04-10 1999-06-15 Loria; Roger M. 5-androstene 3β, 17α diol as an inhibitor of tumor growth

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6667299B1 (en) * 2000-03-16 2003-12-23 Hollis-Eden Pharmaceuticals, Inc. Pharmaceutical compositions and treatment methods

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5912240A (en) * 1997-04-10 1999-06-15 Loria; Roger M. 5-androstene 3β, 17α diol as an inhibitor of tumor growth

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
D.J. WAXMAN: "Role of metabolism in the activation of dehydroepiandrosterone as a peroxisome proliferator", JOURNAL OF ENDOCRINOLOGY, vol. 150, 1996, pages S129 - S147, XP002954541 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7626033B2 (en) 1999-06-30 2009-12-01 Amgen Inc. Compounds for the modulation of PPARγ activity
US7601841B2 (en) 2000-06-28 2009-10-13 Amgen Inc. Quinolinyl and benzothiazolyl modulators
US7223761B2 (en) 2003-10-03 2007-05-29 Amgen Inc. Salts and polymorphs of a potent antidiabetic compound

Also Published As

Publication number Publication date
JP2004524325A (en) 2004-08-12
CA2440973A1 (en) 2002-09-19
SE0100857D0 (en) 2001-03-13
AU2002237613B2 (en) 2008-01-03
WO2002072003A2 (en) 2002-09-19
EP1379542A2 (en) 2004-01-14

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