WO2008052709A3 - Monoesters of estrogens with conjugated linoleic acid and uses thereof - Google Patents

Monoesters of estrogens with conjugated linoleic acid and uses thereof Download PDF

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Publication number
WO2008052709A3
WO2008052709A3 PCT/EP2007/009309 EP2007009309W WO2008052709A3 WO 2008052709 A3 WO2008052709 A3 WO 2008052709A3 EP 2007009309 W EP2007009309 W EP 2007009309W WO 2008052709 A3 WO2008052709 A3 WO 2008052709A3
Authority
WO
WIPO (PCT)
Prior art keywords
conjugated linoleic
linoleic acid
monoester
fatty acid
estrogens
Prior art date
Application number
PCT/EP2007/009309
Other languages
French (fr)
Other versions
WO2008052709A2 (en
Inventor
Lamana Maria Alemany
Original Assignee
Oleoyl Estrone Developments S
Lamana Maria Alemany
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 Oleoyl Estrone Developments S, Lamana Maria Alemany filed Critical Oleoyl Estrone Developments S
Priority to EP07846512A priority Critical patent/EP2078031A2/en
Publication of WO2008052709A2 publication Critical patent/WO2008052709A2/en
Publication of WO2008052709A3 publication Critical patent/WO2008052709A3/en

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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • 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
    • A61K31/566—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 having an oxo group in position 17, e.g. estrone
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/52—Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
    • C07C69/587—Monocarboxylic acid esters having at least two carbon-to-carbon double bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A substantially pure fatty acid monoester of an estrogen, where the fatty acid is a conjugated linoleic acid or a fatty acid of at least eighteen carbons with at least two double bonds arranged in a conjugated system. It also discloses compositions which contain the monoester and use thereof for the treatment and/or prophylaxis of diabetes mellitus type 2, hyperlipidemia, metabolic syndrome, obesity and excess weight. The substantially pure monoester of conjugated linoleic acid of an estrogen allows treating the indicated diseases due to their capacity to decrease insulin resistance. The oral administration of said compound facilitates the treatment thereof.
PCT/EP2007/009309 2006-10-30 2007-10-26 Monoesters of estrogens with conjugated linoleic acid and uses thereof WO2008052709A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP07846512A EP2078031A2 (en) 2006-10-30 2007-10-26 Monoesters of estrogens with conjugated linoleic acid and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ES200602751A ES2302449B1 (en) 2006-10-30 2006-10-30 MONOESTERS OF STROGENS WITH CONJUGATED LINOLEIC ACID AND USES OF THE SAME.
ESP200602751 2006-10-30

Publications (2)

Publication Number Publication Date
WO2008052709A2 WO2008052709A2 (en) 2008-05-08
WO2008052709A3 true WO2008052709A3 (en) 2008-07-03

Family

ID=39325862

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2007/009309 WO2008052709A2 (en) 2006-10-30 2007-10-26 Monoesters of estrogens with conjugated linoleic acid and uses thereof

Country Status (3)

Country Link
EP (1) EP2078031A2 (en)
ES (1) ES2302449B1 (en)
WO (1) WO2008052709A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8809560B2 (en) 2011-05-17 2014-08-19 Board Of Trustees Of The University Of Arkansas Trans-, trans-conjugated linoleic acid compositions and use thereof
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
US9062276B2 (en) 2012-12-03 2015-06-23 Board Of Trustees Of The University Of Arkansas Conjugated linoleic acid rich vegetable oil production from linoleic rich oils by heterogeneous catalysis

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003018529A1 (en) * 2001-08-24 2003-03-06 Girouard Michael P Monounsaturated fatty acids of at least 20 carbon atoms and perhydrocyclopentanophenanthrene nucleus combination molecules and their use as weight-loss agents
WO2004045560A2 (en) * 2002-11-20 2004-06-03 Girouard Michael P Combination of monounsaturated fatty acids and estogen, and their use

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT771817E (en) * 1995-10-30 2003-06-30 Oleoyl Estrone Developments S OLEATE ESTERS OF ESTROGEN FOR THE TREATMENT OF OBESITY AND / OR EXCESS OF WEIGHT
US20060084637A1 (en) * 2004-10-18 2006-04-20 Maria Alemany Methods of using fatty-acid esters of estrogens and thermogenic compounds for reducing the body weight of a mammal and compositions containing the same
US20060084636A1 (en) * 2004-10-18 2006-04-20 Maria Alemany Methods of using fatty-acid esters of estrogens and serotonin reuptake inhibiting compounds for reducing the body weight of a mammal and compositions containing the same

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003018529A1 (en) * 2001-08-24 2003-03-06 Girouard Michael P Monounsaturated fatty acids of at least 20 carbon atoms and perhydrocyclopentanophenanthrene nucleus combination molecules and their use as weight-loss agents
WO2004045560A2 (en) * 2002-11-20 2004-06-03 Girouard Michael P Combination of monounsaturated fatty acids and estogen, and their use

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
ALEMANY M ET AL: "Oral oleoyl-estrone effects on insulin resistance of Zucker obese rats", INTERNATIONAL JOURNAL OF OBESITY, NEWMAN PUBLISHING, LONDON, GB, vol. 24, no. SUPPL. 1, 1 May 2000 (2000-05-01), pages 232, XP002958357, ISSN: 0307-0565 *
ROMERO M M ET AL: "The conjugated linoleic acid ester of estrone induces the mobilisation of fat in male Wistar rats", NAUNYN-SCHMIEDEBERG'S ARCHIVES OF PHARMACOLOGY, SPRINGER-VERLAG, BE, vol. 375, no. 4, 27 March 2007 (2007-03-27), pages 283 - 290, XP019512050, ISSN: 1432-1912 *
SANCHIS D ET AL: "Structural determinants of oleoyl-estrone slimming effects", LIFE SCIENCES, PERGAMON PRESS, OXFORD, GB, vol. 62, no. 15, 6 March 1998 (1998-03-06), pages 1349 - 1359, XP002361948, ISSN: 0024-3205 *

Also Published As

Publication number Publication date
ES2302449B1 (en) 2009-06-12
ES2302449A1 (en) 2008-07-01
EP2078031A2 (en) 2009-07-15
WO2008052709A2 (en) 2008-05-08

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