AU2003219656B2 - 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators - Google Patents

17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators Download PDF

Info

Publication number
AU2003219656B2
AU2003219656B2 AU2003219656A AU2003219656A AU2003219656B2 AU 2003219656 B2 AU2003219656 B2 AU 2003219656B2 AU 2003219656 A AU2003219656 A AU 2003219656A AU 2003219656 A AU2003219656 A AU 2003219656A AU 2003219656 B2 AU2003219656 B2 AU 2003219656B2
Authority
AU
Australia
Prior art keywords
hydroxy
aza
methyl
aryl
androst
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.)
Ceased
Application number
AU2003219656A
Other languages
English (en)
Other versions
AU2003219656A1 (en
Inventor
William P. Dankulich
Robert S. Meissner
Helen J. Mitchell
James J. Perkins
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.)
Merck Sharp & Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp & Dohme LLC
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 Sharp and Dohme Ltd, Merck Sharp & Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Publication of AU2003219656A1 publication Critical patent/AU2003219656A1/en
Application granted granted Critical
Publication of AU2003219656B2 publication Critical patent/AU2003219656B2/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Toxicology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2003219656A 2002-01-15 2003-01-10 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators Ceased AU2003219656B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34880802P 2002-01-15 2002-01-15
US60/348,808 2002-01-15
PCT/US2003/000874 WO2003059293A2 (en) 2002-01-15 2003-01-10 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators

Publications (2)

Publication Number Publication Date
AU2003219656A1 AU2003219656A1 (en) 2003-07-30
AU2003219656B2 true AU2003219656B2 (en) 2007-05-17

Family

ID=23369629

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2003219656A Ceased AU2003219656B2 (en) 2002-01-15 2003-01-10 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators

Country Status (6)

Country Link
US (1) US7605152B2 (enExample)
EP (1) EP1467739A4 (enExample)
JP (1) JP4563032B2 (enExample)
AU (1) AU2003219656B2 (enExample)
CA (1) CA2472475C (enExample)
WO (1) WO2003059293A2 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
EP2160187B1 (en) * 2007-05-16 2013-05-22 Merck Sharp & Dohme Corp. Spiroindalones
WO2009136629A1 (ja) * 2008-05-09 2009-11-12 あすか製薬株式会社 生活習慣病予防・治療剤
US8461102B2 (en) 2010-03-02 2013-06-11 George E. Royster, JR. Methods and compositions for treating and preventing symptoms of hormonal variations
ES2927715T3 (es) 2017-10-05 2022-11-10 Fulcrum Therapeutics Inc Inhibidores de la quinasa p38 reducen la expresión de dux4 y de los genes que le siguen para el tratamiento de la FSHD

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5693809A (en) * 1992-05-20 1997-12-02 Merck & Co., Inc. Substituted 4-aza-5α-androstan-ones as 5α-reductase inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU527030B2 (en) * 1978-04-13 1983-02-10 Merck & Co., Inc. 4-aza-17-substituted-5a-androstan-3-ones
GB9002922D0 (en) * 1990-02-09 1990-04-04 Erba Carlo Spa 17 beta-substituted-4-aza-5 alpha-androstan-3-one derivatives and process for their preparation
WO1993023420A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. NEW 7β-SUBSTITUTED-4-AZA-5α-ANDROSTAN-3-ONES AS 5α-REDUCTASE INHIBITORS
AU680818B2 (en) * 1992-05-21 1997-08-14 Endorecherche Inc. Improved antiandrogens
KR950701527A (ko) * 1992-05-21 1995-04-28 라브리 페르낭 테스토스테론 5α 환원효소 활성 저해제(INHIBITORS OF TESTOSTERONE 5α-REDUCTASE ACTIVITY)
CZ285893B6 (cs) * 1993-05-17 1999-11-17 Endorecherche Inc. Antiandrogenní sloučenina, její prekursor a farmaceutický prostředek ji obsahující
US5550134A (en) * 1995-05-10 1996-08-27 Eli Lilly And Company Methods for inhibiting bone loss
AU5369198A (en) * 1996-12-09 1998-07-03 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
WO1998025623A1 (en) * 1996-12-09 1998-06-18 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
US5945412A (en) * 1996-12-09 1999-08-31 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
WO1998025622A1 (en) * 1996-12-09 1998-06-18 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5693809A (en) * 1992-05-20 1997-12-02 Merck & Co., Inc. Substituted 4-aza-5α-androstan-ones as 5α-reductase inhibitors

Also Published As

Publication number Publication date
EP1467739A2 (en) 2004-10-20
JP4563032B2 (ja) 2010-10-13
CA2472475A1 (en) 2003-07-24
JP2005518404A (ja) 2005-06-23
US20050107416A1 (en) 2005-05-19
WO2003059293A3 (en) 2004-07-22
US7605152B2 (en) 2009-10-20
WO2003059293A2 (en) 2003-07-24
CA2472475C (en) 2010-05-18
EP1467739A4 (en) 2008-01-09
AU2003219656A1 (en) 2003-07-30

Similar Documents

Publication Publication Date Title
AU2003218235B2 (en) Fluorinated 4-azasteroid derivatives as androgen receptor modulators
AU2003223754B2 (en) 4-azasteroid derivatives as androgen receptor modulators
AU2002330031B2 (en) Androstanes as androgen receptor modulators
AU2002330031A1 (en) Androstanes as androgen receptor modulators
US7402577B2 (en) Androstane 17-beta-carboxamides as androgen receptor modulators
AU2002331916A1 (en) Androstane 17-beta-carboxamides as androgen receptor modulators
CA2472475C (en) 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
US7625920B2 (en) Fluorinated 4-azasteroid derivatives as androgen receptor modulators
AU2002322678B2 (en) Androgens receptor modulators and methods of use thereof
AU2006275699A1 (en) N-(pyridin-4-yl)-2-phenylbutanamides as androgen receptor modulators
AU2002322678A1 (en) Androgens receptor modulators and methods of use thereof

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE PATENTEE NAME FROM MERCK & CO., INC. TO MERCK SHARP & DOHME CORP.

MK14 Patent ceased section 143(a) (annual fees not paid) or expired