WO2005005606A3 - 17-acetamido-4-azasteroid derivatives as androgen receptor modulators - Google Patents

17-acetamido-4-azasteroid derivatives as androgen receptor modulators Download PDF

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Publication number
WO2005005606A3
WO2005005606A3 PCT/US2004/020539 US2004020539W WO2005005606A3 WO 2005005606 A3 WO2005005606 A3 WO 2005005606A3 US 2004020539 W US2004020539 W US 2004020539W WO 2005005606 A3 WO2005005606 A3 WO 2005005606A3
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WO
WIPO (PCT)
Prior art keywords
androgen
disease
compounds
androgen receptor
bone
Prior art date
Application number
PCT/US2004/020539
Other languages
French (fr)
Other versions
WO2005005606A2 (en
Inventor
William P Dankulich
Mildred L Kaufman
Robert S Meissner
Helen J Mitchell
Original Assignee
Merck & Co Inc
William P Dankulich
Mildred L Kaufman
Robert S Meissner
Helen J Mitchell
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 Merck & Co Inc, William P Dankulich, Mildred L Kaufman, Robert S Meissner, Helen J Mitchell filed Critical Merck & Co Inc
Priority to EP04777129A priority Critical patent/EP1660184A4/en
Priority to AU2004255749A priority patent/AU2004255749B2/en
Priority to JP2006518687A priority patent/JP2007521292A/en
Priority to US10/557,171 priority patent/US7482357B2/en
Priority to CA002530182A priority patent/CA2530182A1/en
Publication of WO2005005606A2 publication Critical patent/WO2005005606A2/en
Publication of WO2005005606A3 publication Critical patent/WO2005005606A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
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    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
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    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
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    • 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
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
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  • Transplantation (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
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Abstract

Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer’s disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
PCT/US2004/020539 2003-06-30 2004-06-25 17-acetamido-4-azasteroid derivatives as androgen receptor modulators WO2005005606A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
EP04777129A EP1660184A4 (en) 2003-06-30 2004-06-25 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
AU2004255749A AU2004255749B2 (en) 2003-06-30 2004-06-25 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
JP2006518687A JP2007521292A (en) 2003-06-30 2004-06-25 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
US10/557,171 US7482357B2 (en) 2003-06-30 2004-06-25 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
CA002530182A CA2530182A1 (en) 2003-06-30 2004-06-25 17-acetamido-4-azasteroid derivatives as androgen receptor modulators

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US48367503P 2003-06-30 2003-06-30
US60/483,675 2003-06-30

Publications (2)

Publication Number Publication Date
WO2005005606A2 WO2005005606A2 (en) 2005-01-20
WO2005005606A3 true WO2005005606A3 (en) 2005-06-02

Family

ID=34061972

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/020539 WO2005005606A2 (en) 2003-06-30 2004-06-25 17-acetamido-4-azasteroid derivatives as androgen receptor modulators

Country Status (7)

Country Link
US (1) US7482357B2 (en)
EP (1) EP1660184A4 (en)
JP (1) JP2007521292A (en)
CN (1) CN1812824A (en)
AU (1) AU2004255749B2 (en)
CA (1) CA2530182A1 (en)
WO (1) WO2005005606A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9187460B2 (en) 2011-12-14 2015-11-17 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof

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Publication number Priority date Publication date Assignee Title
CN100528168C (en) * 2003-06-30 2009-08-19 麦克公司 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
US7301026B2 (en) * 2005-05-05 2007-11-27 Merck & Co., Inc Process for making fluorinated 4-azasteroid derivatives
CN100488979C (en) * 2005-10-14 2009-05-20 天津药物研究院 Glycyrrhetinic acid-30-acylamide derivatives and its use
WO2007091107A1 (en) * 2006-02-10 2007-08-16 Summit Corporation Plc Treatment of duchenne muscular dystrophy
PT2038252T (en) * 2006-07-12 2016-12-16 Univ Tennessee Res Found Substituted acylanilides and methods of use thereof
US9844528B2 (en) 2006-08-24 2017-12-19 University Of Tennessee Research Foundation SARMs and method of use thereof
US10010521B2 (en) 2006-08-24 2018-07-03 University Of Tennessee Research Foundation SARMs and method of use thereof
US9730908B2 (en) 2006-08-24 2017-08-15 University Of Tennessee Research Foundation SARMs and method of use thereof
GB0715087D0 (en) * 2007-08-03 2007-09-12 Summit Corp Plc Drug combinations for the treatment of duchenne muscular dystrophy
CA2800673A1 (en) 2010-06-10 2011-12-15 Aragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
CN102207101B (en) * 2011-05-18 2013-04-10 大连理工大学 CFD (Computational Fluid Dynamics)-based modeling design method for nuclear main pump and designed million-kilowatt-grade nuclear main pump impeller
PL3929196T3 (en) 2013-09-24 2023-12-11 Fujifilm Corporation Pharmaceutical composition of a nitrogen-containing compound or salt thereof, or metal complex thereof
LT3691620T (en) 2017-10-05 2022-09-26 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD

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Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
US5510485A (en) * 1992-05-20 1996-04-23 Merck & Co., Inc. 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5A-reductase inhibitors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9187460B2 (en) 2011-12-14 2015-11-17 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
US9193714B2 (en) 2011-12-14 2015-11-24 Seragon Pharmaceuticals, Inc. Fluorinated estrogen receptor modulators and uses thereof

Also Published As

Publication number Publication date
AU2004255749B2 (en) 2008-12-18
AU2004255749A1 (en) 2005-01-20
WO2005005606A2 (en) 2005-01-20
CA2530182A1 (en) 2005-01-20
EP1660184A4 (en) 2008-05-14
CN1812824A (en) 2006-08-02
US7482357B2 (en) 2009-01-27
EP1660184A2 (en) 2006-05-31
JP2007521292A (en) 2007-08-02
US20060258661A1 (en) 2006-11-16

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