CA2334577A1 - Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors - Google Patents

Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors Download PDF

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Publication number
CA2334577A1
CA2334577A1 CA002334577A CA2334577A CA2334577A1 CA 2334577 A1 CA2334577 A1 CA 2334577A1 CA 002334577 A CA002334577 A CA 002334577A CA 2334577 A CA2334577 A CA 2334577A CA 2334577 A1 CA2334577 A1 CA 2334577A1
Authority
CA
Canada
Prior art keywords
estrogen receptor
selective estrogen
sex steroid
combination
receptor modulator
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.)
Granted
Application number
CA002334577A
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French (fr)
Other versions
CA2334577C (en
Inventor
Fernand Labrie
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.)
Endorecherche Inc
Original Assignee
Endorecherche, Inc.
Fernand Labrie
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 Endorecherche, Inc., Fernand Labrie filed Critical Endorecherche, Inc.
Priority to CA2632567A priority Critical patent/CA2632567C/en
Publication of CA2334577A1 publication Critical patent/CA2334577A1/en
Application granted granted Critical
Publication of CA2334577C publication Critical patent/CA2334577C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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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-3.beta.,17.beta.-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.
CA002334577A 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors Expired - Lifetime CA2334577C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2632567A CA2632567C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US09/096,284 1998-06-11
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
PCT/CA1999/000538 WO1999063974A2 (en) 1998-06-11 1999-06-10 Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2632567A Division CA2632567C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors

Publications (2)

Publication Number Publication Date
CA2334577A1 true CA2334577A1 (en) 1999-12-16
CA2334577C CA2334577C (en) 2008-08-05

Family

ID=22256661

Family Applications (7)

Application Number Title Priority Date Filing Date
CA2632567A Expired - Lifetime CA2632567C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768828A Expired - Lifetime CA2768828C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768841A Expired - Lifetime CA2768841C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768773A Expired - Lifetime CA2768773C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA002334577A Expired - Lifetime CA2334577C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768682A Expired - Lifetime CA2768682C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768882A Expired - Lifetime CA2768882C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors

Family Applications Before (4)

Application Number Title Priority Date Filing Date
CA2632567A Expired - Lifetime CA2632567C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768828A Expired - Lifetime CA2768828C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768841A Expired - Lifetime CA2768841C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768773A Expired - Lifetime CA2768773C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors

Family Applications After (2)

Application Number Title Priority Date Filing Date
CA2768682A Expired - Lifetime CA2768682C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors
CA2768882A Expired - Lifetime CA2768882C (en) 1998-06-11 1999-06-10 Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors

Country Status (29)

Country Link
US (6) US6465445B1 (en)
EP (5) EP2386304B9 (en)
JP (3) JP2002517433A (en)
KR (6) KR100944261B1 (en)
CN (2) CN1240388C (en)
AR (1) AR043075A1 (en)
AT (1) ATE308326T1 (en)
AU (1) AU4253099A (en)
BR (1) BR9911116A (en)
CA (7) CA2632567C (en)
CY (4) CY1113712T1 (en)
DE (1) DE69928104T2 (en)
DK (5) DK1623712T3 (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) MY151187A (en)
NO (2) NO331022B1 (en)
NZ (1) NZ508801A (en)
PL (4) PL203343B1 (en)
PT (4) PT2386305E (en)
RU (1) RU2246947C2 (en)
TR (5) TR200103455T2 (en)
TW (2) TWI371279B (en)
WO (1) WO1999063974A2 (en)
ZA (1) ZA200007297B (en)

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US8835413B2 (en) 2004-10-20 2014-09-16 Endorecherche, Inc. Sex steroid precursors alone or in combination with a selective estrogen receptor modulator and/or with estrogens and/or a type 5 cGMP phosphodiesterase inhibitor for the prevention and treatment of vaginal dryness and sexual dysfunction in postmenopausal women
WO2015135061A1 (en) * 2014-03-10 2015-09-17 Endorecherche, Inc. Treatment of male androgen deficiency symptoms or diseases with sex steroid precursor combined with serm

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