WO1999063974A3 - Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues - Google Patents

Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues Download PDF

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Publication number
WO1999063974A3
WO1999063974A3 PCT/CA1999/000538 CA9900538W WO9963974A3 WO 1999063974 A3 WO1999063974 A3 WO 1999063974A3 CA 9900538 W CA9900538 W CA 9900538W WO 9963974 A3 WO9963974 A3 WO 9963974A3
Authority
WO
WIPO (PCT)
Prior art keywords
estrogen receptor
selective estrogen
combination
receptor modulator
denydroepiandrosterone
Prior art date
Application number
PCT/CA1999/000538
Other languages
French (fr)
Other versions
WO1999063974A2 (en
Inventor
Fernand Labrie
Original Assignee
Endorecherche Inc
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
Priority to KR1020007014056A priority Critical patent/KR100944261B1/en
Priority to PL345887A priority patent/PL199798B1/en
Priority to AU42530/99A priority patent/AU4253099A/en
Priority to PL99379648A priority patent/PL195772B1/en
Priority to NZ508801A priority patent/NZ508801A/en
Priority to JP2000553043A priority patent/JP2002517433A/en
Priority to CA002334577A priority patent/CA2334577C/en
Priority to HU0103345A priority patent/HU230495B1/en
Priority to EP99955419A priority patent/EP1083905B1/en
Priority to MXPA00012306A priority patent/MXPA00012306A/en
Application filed by Endorecherche Inc filed Critical Endorecherche Inc
Priority to DE69928104T priority patent/DE69928104T2/en
Priority to AT99955419T priority patent/ATE308326T1/en
Priority to IL14017899A priority patent/IL140178A0/en
Priority to BR9911116-0A priority patent/BR9911116A/en
Publication of WO1999063974A2 publication Critical patent/WO1999063974A2/en
Publication of WO1999063974A3 publication Critical patent/WO1999063974A3/en
Priority to IL140178A priority patent/IL140178A/en
Priority to NO20006254A priority patent/NO331022B1/en
Priority to HK02101755.1A priority patent/HK1040367B/en
Priority to IL185087A priority patent/IL185087A0/en
Priority to NO20092730A priority patent/NO332187B1/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
    • A61K31/56—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
    • 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
    • A61K31/568—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • 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
    • A61K31/568—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 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • 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
    • A61K31/57—Compounds 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
    • 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
    • A61K31/66—Phosphorus compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P5/26—Androgens
    • 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
    • A61P9/10—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

Abstract

Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having general structure (I) and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3β,17β-diol and compounds converted in vivo to one of the foregoing precursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
PCT/CA1999/000538 1998-06-11 1999-06-10 Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues WO1999063974A2 (en)

Priority Applications (19)

Application Number Priority Date Filing Date Title
DE69928104T DE69928104T2 (en) 1998-06-11 1999-06-10 MEDICAL APPLICATION OF A SELECTIVE ESTROGEN RECEPTOR MODULATOR IN COMBINATION WITH A SEXUAL STEROID PREPARATION
PL345887A PL199798B1 (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
PL99379648A PL195772B1 (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
NZ508801A NZ508801A (en) 1998-06-11 1999-06-10 Selective estrogen receptor modulator in combination with dehydroepiandrosterone (DHEA) or analogues
JP2000553043A JP2002517433A (en) 1998-06-11 1999-06-10 Medical use of combinations of selective estrogen receptor modulators and sex steroid precursors
CA002334577A CA2334577C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
HU0103345A HU230495B1 (en) 1998-06-11 1999-06-10 Seelective estrogen receptors in combination with sexual steroid precursors for pharmaceutical compositions
AT99955419T ATE308326T1 (en) 1998-06-11 1999-06-10 MEDICAL USE OF A SELECTIVE ESTROGEN RECEPTOR MODULATOR IN COMBINATION WITH A SEXUAL STEROID PREDICT
MXPA00012306A MXPA00012306A (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors.
KR1020007014056A KR100944261B1 (en) 1998-06-11 1999-06-10 Selective estrogen receptor modulator in combination with denydroepiandrosterone dhea or analogues
AU42530/99A AU4253099A (en) 1998-06-11 1999-06-10 Selective estrogen receptor modulator in combination with denydroepiandrosterone (DHEA) or analogues
EP99955419A EP1083905B1 (en) 1998-06-11 1999-06-10 Medical use of a selective estrogen receptor modulator in combination with a sex steroide precursor
IL14017899A IL140178A0 (en) 1998-06-11 1999-06-10 Selective estrogen receptor modulator in combination with a sex steroid precursor
BR9911116-0A BR9911116A (en) 1998-06-11 1999-06-10 Process to treat or reduce the risk of acquiring a condition selected from the group consisting of atherosclerosis, endometrial cancer, uterine cancer, ovarian cancer, lack of vaginal lubrication, and loss of muscle mass, pharmaceutical composition, and, kit.
IL140178A IL140178A (en) 1998-06-11 2000-12-07 Use of a selective estrogen receptor modulator in combination with a sex steroid precursor to manufacture a pharmaceutical composition for treating or preventing osteoporosis
NO20006254A NO331022B1 (en) 1998-06-11 2000-12-08 Selective estrogen receptor modulator in combination with dehydroepiandrosterone (DHEA) or analogues
HK02101755.1A HK1040367B (en) 1998-06-11 2002-03-07 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
IL185087A IL185087A0 (en) 1998-06-11 2007-08-07 Selective estrogen receptor modulator in combination with a sex steroid precursor
NO20092730A NO332187B1 (en) 1998-06-11 2009-07-20 Estrogen receptor modulator EM-1538 and pharmaceutical composition containing it

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/096,284 US6465445B1 (en) 1998-06-11 1998-06-11 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
US09/096,284 1998-06-11

Publications (2)

Publication Number Publication Date
WO1999063974A2 WO1999063974A2 (en) 1999-12-16
WO1999063974A3 true WO1999063974A3 (en) 2000-06-29

Family

ID=22256661

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CA1999/000538 WO1999063974A2 (en) 1998-06-11 1999-06-10 Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues

Country Status (29)

Country Link
US (6) US6465445B1 (en)
EP (5) EP1083905B1 (en)
JP (3) JP2002517433A (en)
KR (6) KR20090018870A (en)
CN (2) CN1240388C (en)
AR (1) AR043075A1 (en)
AT (1) ATE308326T1 (en)
AU (1) AU4253099A (en)
BR (1) BR9911116A (en)
CA (7) CA2768882C (en)
CY (4) CY1113712T1 (en)
DE (1) DE69928104T2 (en)
DK (5) DK2386304T3 (en)
ES (5) ES2253922T3 (en)
HK (1) HK1040367B (en)
HU (2) HU230495B1 (en)
ID (1) ID28696A (en)
IL (3) IL140178A0 (en)
MX (1) MXPA00012306A (en)
MY (3) MY157030A (en)
NO (2) NO331022B1 (en)
NZ (1) NZ508801A (en)
PL (4) PL203704B1 (en)
PT (4) PT1623712E (en)
RU (1) RU2246947C2 (en)
TR (5) TR200103454T2 (en)
TW (2) TWI371279B (en)
WO (1) WO1999063974A2 (en)
ZA (1) ZA200007297B (en)

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