CA2530182A1 - 17-acetamido-4-azasteroid derivatives as androgen receptor modulators - Google Patents
17-acetamido-4-azasteroid derivatives as androgen receptor modulators Download PDFInfo
- Publication number
- CA2530182A1 CA2530182A1 CA002530182A CA2530182A CA2530182A1 CA 2530182 A1 CA2530182 A1 CA 2530182A1 CA 002530182 A CA002530182 A CA 002530182A CA 2530182 A CA2530182 A CA 2530182A CA 2530182 A1 CA2530182 A1 CA 2530182A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- methyl
- oxo
- androst
- aza
- 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.)
- Abandoned
Links
Classifications
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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
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- 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
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- 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
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- 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
- A61P25/24—Antidepressants
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- 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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- 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]
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- 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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- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- 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
- 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
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- 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
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- 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
Landscapes
- 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)
- Hematology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Reproductive Health (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Virology (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Transplantation (AREA)
- Hospice & Palliative Care (AREA)
- Tropical Medicine & Parasitology (AREA)
- Heart & Thoracic Surgery (AREA)
- Molecular Biology (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US48367503P | 2003-06-30 | 2003-06-30 | |
US60/483,675 | 2003-06-30 | ||
PCT/US2004/020539 WO2005005606A2 (en) | 2003-06-30 | 2004-06-25 | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
Publications (1)
Publication Number | Publication Date |
---|---|
CA2530182A1 true CA2530182A1 (en) | 2005-01-20 |
Family
ID=34061972
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002530182A Abandoned CA2530182A1 (en) | 2003-06-30 | 2004-06-25 | 17-acetamido-4-azasteroid derivatives as androgen receptor modulators |
Country Status (7)
Families Citing this family (15)
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 |
US7301026B2 (en) * | 2005-05-05 | 2007-11-27 | Merck & Co., Inc | Process for making fluorinated 4-azasteroid derivatives |
CN100488979C (zh) * | 2005-10-14 | 2009-05-20 | 天津药物研究院 | 甘草次酸-30-酰胺类衍生物及其用途 |
EP1986643A1 (en) * | 2006-02-10 | 2008-11-05 | Summit Corporation Plc | Treatment of duchenne muscular dystrophy |
MX2009000385A (es) * | 2006-07-12 | 2009-04-06 | Univ Tennessee Res Foundation | Acil-anilidas sustituidas y metodos de uso de las mismas. |
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 |
US9844528B2 (en) | 2006-08-24 | 2017-12-19 | 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 |
CN102939287B (zh) | 2010-06-10 | 2016-01-27 | 塞拉根制药公司 | 雌激素受体调节剂及其用途 |
CN102207101B (zh) * | 2011-05-18 | 2013-04-10 | 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 |
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 |
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 |
CA3128468A1 (en) | 2017-10-05 | 2019-04-11 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd |
Family Cites Families (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4377584A (en) | 1978-04-13 | 1983-03-22 | Merck & Co., Inc. | 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors |
US5237065A (en) | 1987-01-28 | 1993-08-17 | Smithkline Beecham Corporation | Steroid 5-alpha-reductase inhibitors |
IE76452B1 (en) * | 1990-10-29 | 1997-10-22 | Sankyo Co | Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use |
IL101243A (en) | 1991-03-20 | 1999-12-22 | Merck & Co Inc | Pharmaceutical preparations for the treatment of benign prostatic hyperplasia containing steroid history |
WO1992018132A1 (en) | 1991-04-17 | 1992-10-29 | Merck & Co., Inc. | Pharmaceutical combination for the treatment of benign prostatic hyperplasia comtaining a 5 alpha-reductase inhibitor |
WO1993023039A1 (en) * | 1992-05-20 | 1993-11-25 | Merck & Co., Inc. | Substituted 4-aza-5a-androstan-ones as 5a-reductase inhibitors |
CA2135167A1 (en) * | 1992-05-20 | 1993-11-25 | Donald W. Graham | New 17-ester, amide, and ketone derivatives of 3-oxo-4- azasteroids as 5a-reductase inhibitors |
JPH07508032A (ja) | 1992-05-20 | 1995-09-07 | メルク エンド カンパニー インコーポレーテッド | 5α−レダクターゼ阻害剤としての新規Δ−17−及びΔ−20オレフィン性並びに飽和17β−置換4−アザ−5α−アンドロスタン−オン |
US5710275A (en) * | 1992-05-20 | 1998-01-20 | Merck & Co., Inc. | 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors |
US5620986A (en) * | 1992-05-20 | 1997-04-15 | Merck & Co., Inc. | 17 urea, thiourea, thiocarbamyl and carbamyl4-azasteroid 5-reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders |
ATE183193T1 (de) * | 1992-05-20 | 1999-08-15 | Merck & Co Inc | 17-amino-substituierte 4-azasteroide als 5-alpha- reductase inhibitoren |
KR950701527A (ko) * | 1992-05-21 | 1995-04-28 | 라브리 페르낭 | 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY) |
GB9216280D0 (en) | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | Steroids with a fluorinated acylureidic type side chain |
GB9216284D0 (en) | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | Fluorinated 17beta-substituted 4-aza-5alpha-androstane-3-one derivatives |
GB9216329D0 (en) | 1992-07-31 | 1992-09-16 | Erba Carlo Spa | 17beta-substituted 4-aza-5alpha-androstan-3-one derivatives |
WO1994022900A1 (en) | 1993-04-02 | 1994-10-13 | Ciba-Geigy Ag | AZA-ANDROSTANE-17β-CARBOXAMIDES |
GB9415178D0 (en) | 1994-07-28 | 1994-09-21 | Erba Carlo Spa | 4-azasteroids with side-chain fluoroketones |
US5595996A (en) | 1994-10-25 | 1997-01-21 | Merck & Co., Inc. | 7-substituted 4-aza cholanic acid derivatives and their use |
GB9518858D0 (en) | 1995-09-14 | 1995-11-15 | Pharmacia Spa | Phenylsubstituted 4-azasteroid fluoroderivatives |
GB9608045D0 (en) | 1996-04-18 | 1996-06-19 | Pharmacia Spa | Process for preparing steroids having a carboxamide side-chain |
GB9727522D0 (en) | 1997-12-31 | 1998-02-25 | Pharmacia & Upjohn Spa | Process for preparing carboxamido-4-azasteroids |
EP1641464A4 (en) * | 2003-06-30 | 2008-05-14 | Merck & Co Inc | 17-ACETAMIDO-4-AZASTEROID DERIVATIVES AS MODULATORS OF THE ANDROGEN RECEPTOR |
-
2004
- 2004-06-25 JP JP2006518687A patent/JP2007521292A/ja active Pending
- 2004-06-25 CA CA002530182A patent/CA2530182A1/en not_active Abandoned
- 2004-06-25 WO PCT/US2004/020539 patent/WO2005005606A2/en active Application Filing
- 2004-06-25 AU AU2004255749A patent/AU2004255749B2/en not_active Ceased
- 2004-06-25 US US10/557,171 patent/US7482357B2/en not_active Expired - Fee Related
- 2004-06-25 EP EP04777129A patent/EP1660184A4/en not_active Withdrawn
- 2004-06-25 CN CNA200480018337XA patent/CN1812824A/zh active Pending
Also Published As
Publication number | Publication date |
---|---|
WO2005005606A3 (en) | 2005-06-02 |
JP2007521292A (ja) | 2007-08-02 |
WO2005005606A2 (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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Legal Events
Date | Code | Title | Description |
---|---|---|---|
EEER | Examination request | ||
FZDE | Discontinued |