AU2003287076C1 - Heterocyclic selective androgen receptor modulators and methods of use thereof - Google Patents

Heterocyclic selective androgen receptor modulators and methods of use thereof Download PDF

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Publication number
AU2003287076C1
AU2003287076C1 AU2003287076A AU2003287076A AU2003287076C1 AU 2003287076 C1 AU2003287076 C1 AU 2003287076C1 AU 2003287076 A AU2003287076 A AU 2003287076A AU 2003287076 A AU2003287076 A AU 2003287076A AU 2003287076 C1 AU2003287076 C1 AU 2003287076C1
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Prior art keywords
androgen receptor
receptor modulator
selective androgen
subject
modulator compound
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AU2003287076A
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AU2003287076B2 (en
AU2003287076A2 (en
AU2003287076A1 (en
Inventor
James T. Dalton
Duane D. Miller
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University of Tennessee Research Foundation
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University of Tennessee Research Foundation
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Publication of AU2003287076A1 publication Critical patent/AU2003287076A1/en
Publication of AU2003287076B2 publication Critical patent/AU2003287076B2/en
Priority to AU2009202683A priority Critical patent/AU2009202683A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • A61P15/16—Masculine contraceptives
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/72—Receptors; Cell surface antigens; Cell surface determinants for hormones
    • C07K14/721—Steroid/thyroid hormone superfamily, e.g. GR, EcR, androgen receptor, oestrogen receptor

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Cell Biology (AREA)
  • Immunology (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
AU2003287076A 2002-10-15 2003-10-14 Heterocyclic selective androgen receptor modulators and methods of use thereof Ceased AU2003287076C1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2009202683A AU2009202683A1 (en) 2002-10-15 2009-07-02 Heterocyclic selective androgen receptor modulators and methods of use thereof

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41817302P 2002-10-15 2002-10-15
US60/418,173 2002-10-15
PCT/US2003/032510 WO2004035737A2 (en) 2002-10-15 2003-10-14 Heterocyclic selective androgen receptor modulators and methods of use thereof

Related Child Applications (1)

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AU2009202683A Division AU2009202683A1 (en) 2002-10-15 2009-07-02 Heterocyclic selective androgen receptor modulators and methods of use thereof

Publications (4)

Publication Number Publication Date
AU2003287076A2 AU2003287076A2 (en) 2004-05-04
AU2003287076A1 AU2003287076A1 (en) 2004-05-04
AU2003287076B2 AU2003287076B2 (en) 2009-04-02
AU2003287076C1 true AU2003287076C1 (en) 2010-03-04

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AU2003287076A Ceased AU2003287076C1 (en) 2002-10-15 2003-10-14 Heterocyclic selective androgen receptor modulators and methods of use thereof
AU2009202683A Abandoned AU2009202683A1 (en) 2002-10-15 2009-07-02 Heterocyclic selective androgen receptor modulators and methods of use thereof

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US (2) US7214693B2 (enExample)
EP (1) EP1562906A4 (enExample)
JP (1) JP2006518328A (enExample)
CN (1) CN1726193A (enExample)
AU (2) AU2003287076C1 (enExample)
CA (1) CA2501867A1 (enExample)
TW (1) TW200502249A (enExample)
WO (1) WO2004035737A2 (enExample)

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US20040260108A1 (en) * 2001-06-25 2004-12-23 Dalton James T. Metabolites of selective androgen receptor modulators and methods of use thereof
US8853266B2 (en) * 2001-12-06 2014-10-07 University Of Tennessee Research Foundation Selective androgen receptor modulators for treating diabetes
US20070161608A1 (en) * 2001-12-06 2007-07-12 Dalton James T Selective androgen receptor modulators for treating muscle wasting
UA87854C2 (en) * 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
US9889110B2 (en) 2004-06-07 2018-02-13 University Of Tennessee Research Foundation Selective androgen receptor modulator for treating hormone-related conditions
US9884038B2 (en) 2004-06-07 2018-02-06 University Of Tennessee Research Foundation Selective androgen receptor modulator and methods of use thereof
US20110237664A1 (en) * 2004-06-07 2011-09-29 Dalton James T Selective androgen receptor modulators for treating diabetes
US8288366B2 (en) 2006-06-20 2012-10-16 Chochinov Ronald H Formulation for hair growth
KR101638035B1 (ko) * 2007-01-22 2016-07-11 지티엑스, 인코포레이티드 핵 수용체에 결합하는 물질
US9604931B2 (en) 2007-01-22 2017-03-28 Gtx, Inc. Nuclear receptor binding agents
US9623021B2 (en) * 2007-01-22 2017-04-18 Gtx, Inc. Nuclear receptor binding agents
US7968603B2 (en) 2007-09-11 2011-06-28 University Of Tennessee Research Foundation Solid forms of selective androgen receptor modulators
CN101945853B (zh) 2007-12-21 2014-08-20 配体药物公司 选择性雄激素受体调节剂(sarm)及其应用
US8791158B2 (en) * 2010-01-11 2014-07-29 Gtx, Inc. Methods of treating meibomian gland dysfunction
US8395552B2 (en) 2010-11-23 2013-03-12 Metamagnetics, Inc. Antenna module having reduced size, high gain, and increased power efficiency
FR2982261B1 (fr) * 2011-11-04 2014-06-13 Galderma Res & Dev Nouveaux amides, et leur utilisation pharmaceutique ou cosmetique
US10987334B2 (en) 2012-07-13 2021-04-27 University Of Tennessee Research Foundation Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs)
US9744149B2 (en) 2012-07-13 2017-08-29 Gtx, Inc. Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
US12685719B2 (en) 2012-07-13 2026-07-21 University Of Tennessee Research Foundation Treatment of breast cancer with selective androgen receptor modulators and cyclin-dependent kinase 4/6 inhibitors
US10314807B2 (en) 2012-07-13 2019-06-11 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
US9622992B2 (en) 2012-07-13 2017-04-18 Gtx, Inc. Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
EP3733170A1 (en) 2012-07-13 2020-11-04 Oncternal Therapeutics, Inc. A method of treating androgen receptor (ar) -positive breast cancers with selective androgen receptor modulator (sarms)
US10258596B2 (en) 2012-07-13 2019-04-16 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
US9969683B2 (en) 2012-07-13 2018-05-15 Gtx, Inc. Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS)
GB201321601D0 (en) 2013-12-06 2014-01-22 Canbex Therapeutics Ltd Modulator
EP3613418A1 (en) 2014-01-17 2020-02-26 Ligand Pharmaceuticals, Inc. Methods and compositions for modulating hormone levels
CN103772238B (zh) * 2014-01-24 2017-03-22 苏州伊莱特新药研发有限公司 一类新的含酯基芳香丙酰胺化合物及其制备方法和用途
US10093613B2 (en) 2015-04-21 2018-10-09 Gtx, Inc. Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10441570B2 (en) 2015-04-21 2019-10-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) Ligands and methods of use thereof
US10806720B2 (en) 2015-04-21 2020-10-20 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10654809B2 (en) 2016-06-10 2020-05-19 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10865184B2 (en) 2015-04-21 2020-12-15 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
AU2017278314B2 (en) * 2016-06-10 2022-06-30 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US10806719B2 (en) 2016-06-10 2020-10-20 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US11230523B2 (en) 2016-06-10 2022-01-25 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
US12202815B2 (en) 2018-09-05 2025-01-21 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
AU2020257397B2 (en) 2019-04-19 2026-02-26 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
CN122228246A (zh) * 2023-11-16 2026-06-16 恩多凯医药科技（北京）有限公司 神经活性雄激素受体调节剂及其用途

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US6569896B2 (en) * 2000-08-24 2003-05-27 The University Of Tennessee Research Corporation Selective androgen receptor modulators and methods of use thereof
AU7604798A (en) * 1997-05-30 1998-12-30 University Of Tennessee Research Corporation, The Non-steroidal agonist compounds and their use in male hormone therapy
DE19723722A1 (de) * 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
WO2003074473A2 (en) * 2002-02-28 2003-09-12 University Of Tennessee Research Foundation Irreversible selective androgen receptor modulators and methods of use thereof
AU2003241583B2 (en) * 2002-06-17 2009-05-21 University Of Tennessee Research Foundation N-bridged selective androgen receptor modulators and methods of use thereof

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Publication number Publication date
AU2003287076B2 (en) 2009-04-02
US20040138244A1 (en) 2004-07-15
US20070265290A1 (en) 2007-11-15
AU2003287076A2 (en) 2004-05-04
TW200502249A (en) 2005-01-16
JP2006518328A (ja) 2006-08-10
WO2004035737A2 (en) 2004-04-29
EP1562906A2 (en) 2005-08-17
CN1726193A (zh) 2006-01-25
EP1562906A4 (en) 2009-12-02
WO2004035737A3 (en) 2004-09-10
CA2501867A1 (en) 2004-04-29
AU2003287076A1 (en) 2004-05-04
US7214693B2 (en) 2007-05-08
AU2009202683A1 (en) 2009-07-23

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