WO2005005606A2 - 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
WO2005005606A2
WO2005005606A2 PCT/US2004/020539 US2004020539W WO2005005606A2 WO 2005005606 A2 WO2005005606 A2 WO 2005005606A2 US 2004020539 W US2004020539 W US 2004020539W WO 2005005606 A2 WO2005005606 A2 WO 2005005606A2
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WO
WIPO (PCT)
Prior art keywords
alkyl
methyl
oxo
aza
androst
Prior art date
Application number
PCT/US2004/020539
Other languages
English (en)
French (fr)
Other versions
WO2005005606A3 (en
Inventor
William P. Dankulich
Mildred L. Kaufman
Robert S. Meissner
Helen J. Mitchell
Original Assignee
Merck & Co., 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
Application filed by Merck & Co., Inc. filed Critical Merck & Co., Inc.
Priority to US10/557,171 priority Critical patent/US7482357B2/en
Priority to EP04777129A priority patent/EP1660184A4/en
Priority to JP2006518687A priority patent/JP2007521292A/ja
Priority to AU2004255749A priority patent/AU2004255749B2/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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
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    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
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
US10/557,171 US7482357B2 (en) 2003-06-30 2004-06-25 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
EP04777129A EP1660184A4 (en) 2003-06-30 2004-06-25 17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS MODULATORS OF THE ANDROGEN RECEPTOR
JP2006518687A JP2007521292A (ja) 2003-06-30 2004-06-25 アンドロゲン受容体モジュレータとしての１７−アセトアミド−４−アザステロイド誘導体
AU2004255749A AU2004255749B2 (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 true WO2005005606A2 (en) 2005-01-20
WO2005005606A3 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)

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US (1) US7482357B2 (US07482357-20090127-C00085.png)
EP (1) EP1660184A4 (US07482357-20090127-C00085.png)
JP (1) JP2007521292A (US07482357-20090127-C00085.png)
CN (1) CN1812824A (US07482357-20090127-C00085.png)
AU (1) AU2004255749B2 (US07482357-20090127-C00085.png)
CA (1) CA2530182A1 (US07482357-20090127-C00085.png)
WO (1) WO2005005606A2 (US07482357-20090127-C00085.png)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006121655A1 (en) * 2005-05-05 2006-11-16 Merck & Co., Inc. Process for making fluorinated 4-azasteroid derivatives and intermediate thereof
WO2007091107A1 (en) * 2006-02-10 2007-08-16 Summit Corporation Plc Treatment of duchenne muscular dystrophy
JP2009511511A (ja) * 2005-10-14 2009-03-19 天津▲ヤオ▼物研究院 新規グリチルレチン酸−３０−アミド誘導体及びその用途
WO2009019505A3 (en) * 2007-08-03 2009-05-22 Summit Corp Plc Drug combinations for the treatment of duchenne muscular dystrophy
CN102207101A (zh) * 2011-05-18 2011-10-05 大连理工大学 一种基于cfd的核主泵模化设计方法及设计百万千瓦级核主泵叶轮
US8703810B2 (en) 2010-06-10 2014-04-22 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
US9730908B2 (en) 2006-08-24 2017-08-15 University Of Tennessee Research Foundation SARMs and method 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
EA031888B1 (ru) * 2006-07-12 2019-03-29 Юниверсити Оф Теннесси Рисерч Фаундейшн Способы применения замещенных ациланилидов
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
US11291659B2 (en) 2017-10-05 2022-04-05 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1641464A4 (en) * 2003-06-30 2008-05-14 Merck & Co Inc 17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS MODULATORS OF THE ANDROGEN RECEPTOR
US9193714B2 (en) 2011-12-14 2015-11-24 Seragon Pharmaceuticals, Inc. Fluorinated estrogen receptor modulators and uses thereof
HUE063437T2 (hu) 2013-09-24 2024-01-28 Fujifilm Corp Nitrogént tartalmazó vegyületet vagy sóját vagy fémkomplexét tartalmazó gyógyászati készítmény

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Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006121655A1 (en) * 2005-05-05 2006-11-16 Merck & Co., Inc. Process for making fluorinated 4-azasteroid derivatives and intermediate thereof
JP2009511511A (ja) * 2005-10-14 2009-03-19 天津▲ヤオ▼物研究院 新規グリチルレチン酸−３０−アミド誘導体及びその用途
WO2007091107A1 (en) * 2006-02-10 2007-08-16 Summit Corporation Plc Treatment of duchenne muscular dystrophy
EA031888B1 (ru) * 2006-07-12 2019-03-29 Юниверсити Оф Теннесси Рисерч Фаундейшн Способы применения замещенных ациланилидов
US10300037B2 (en) 2006-08-24 2019-05-28 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
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
WO2009019505A3 (en) * 2007-08-03 2009-05-22 Summit Corp Plc Drug combinations for the treatment of duchenne muscular dystrophy
US8703810B2 (en) 2010-06-10 2014-04-22 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
US9078871B2 (en) 2010-06-10 2015-07-14 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
CN102207101A (zh) * 2011-05-18 2011-10-05 大连理工大学 一种基于cfd的核主泵模化设计方法及设计百万千瓦级核主泵叶轮
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
US10537560B2 (en) 2017-10-05 2020-01-21 Fulcrum Therapeutics. Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
US11291659B2 (en) 2017-10-05 2022-04-05 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
US11479770B2 (en) 2017-10-05 2022-10-25 Fulcrum Therapeutics, Inc. Use of p38 inhibitors to reduce expression of DUX4

Also Published As

Publication number Publication date
WO2005005606A3 (en) 2005-06-02
JP2007521292A (ja) 2007-08-02
CA2530182A1 (en) 2005-01-20
CN1812824A (zh) 2006-08-02
AU2004255749B2 (en) 2008-12-18
US20060258661A1 (en) 2006-11-16
EP1660184A2 (en) 2006-05-31
AU2004255749A1 (en) 2005-01-20
US7482357B2 (en) 2009-01-27
EP1660184A4 (en) 2008-05-14

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