WO2003074473A3 - Modulateurs irreversibles selectifs de recepteur d'androgene et procede d'utilisation associes - Google Patents

Modulateurs irreversibles selectifs de recepteur d'androgene et procede d'utilisation associes Download PDF

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Publication number
WO2003074473A3
WO2003074473A3 PCT/US2003/003121 US0303121W WO03074473A3 WO 2003074473 A3 WO2003074473 A3 WO 2003074473A3 US 0303121 W US0303121 W US 0303121W WO 03074473 A3 WO03074473 A3 WO 03074473A3
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WO
WIPO (PCT)
Prior art keywords
androgen receptor
androgen
cancer
sarm compounds
sarm
Prior art date
Application number
PCT/US2003/003121
Other languages
English (en)
Other versions
WO2003074473A2 (fr
Inventor
James Dalton
Duane D Miller
Kiwon Chung
Yali He
Mitchell S Steiner
Karen A Veverka
Original Assignee
Univ Tennessee Res Corp
James Dalton
Duane D Miller
Kiwon Chung
Yali He
Mitchell S Steiner
Karen A Veverka
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
Priority to JP2003572945A priority Critical patent/JP2005519111A/ja
Priority to CA002476651A priority patent/CA2476651A1/fr
Priority to EP03710820A priority patent/EP1487783A4/fr
Priority to AU2003214971A priority patent/AU2003214971A1/en
Priority to KR10-2004-7013473A priority patent/KR20040104463A/ko
Priority to MXPA04008412A priority patent/MXPA04008412A/es
Application filed by Univ Tennessee Res Corp, James Dalton, Duane D Miller, Kiwon Chung, Yali He, Mitchell S Steiner, Karen A Veverka filed Critical Univ Tennessee Res Corp
Priority to EA200401121A priority patent/EA200401121A1/ru
Priority to BR0308076-5A priority patent/BR0308076A/pt
Priority to IL16374203A priority patent/IL163742A0/xx
Publication of WO2003074473A2 publication Critical patent/WO2003074473A2/fr
Publication of WO2003074473A3 publication Critical patent/WO2003074473A3/fr
Priority to HR20040851A priority patent/HRP20040851A2/hr

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    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C233/04—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C233/05—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/26—Cyanate or isocyanate esters; Thiocyanate or isothiocyanate esters
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • 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
    • 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
    • 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
    • A61P5/28—Antiandrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/50—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C261/00—Derivatives of cyanic acid
    • C07C261/02—Cyanates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C265/00—Derivatives of isocyanic acid
    • C07C265/12—Derivatives of isocyanic acid having isocyanate groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C331/00—Derivatives of thiocyanic acid or of isothiocyanic acid
    • C07C331/02—Thiocyanates
    • C07C331/10—Thiocyanates having sulfur atoms of thiocyanate groups bound to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C331/00—Derivatives of thiocyanic acid or of isothiocyanic acid
    • C07C331/16—Isothiocyanates
    • C07C331/28—Isothiocyanates having isothiocyanate groups bound to carbon atoms of six-membered aromatic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

L'invention concerne, dans un mode de réalisation une classe d'agents de ciblage de récepteur d'androgène (ARTA). Ces agents définissent une nouvelle sous-classe de composés qui sont des modulateurs sélectifs de récepteur d'androgène (SARM). Les composés SARM possèdent l'activité anti-androgène inattendue d'un ligand non stéroïde pour le récepteur d'androgène. Dans un mode de réalisation suivant, les composés SARM se lient irréversiblement au récepteur d'androgène. Dans une autre mode de réalisation, les composés SARM constituent des antagonistes de récepteur d'androgène qui se lient irréversiblement au récepteur d'androgène. Dans un dernier mode de réalisation, les composés SARM sont des agents alkylants. Les composés SARM, seuls ou dans une composition, sont utiles dans a) la contraception masculine, b) le traitement de différents troubles associés à des hormones, par exemple des troubles associés au déclin d'androgènes chez le mâle vieillissant (ADAM), tels que fatigue, dépression, diminution de la libido, dysfonctionnement sexuel, dysfonctionnement érectile, hypogonadisme, ostéoporose, perte de cheveux, anémie, obésité, sarcopénie, ostéopénie, hyperplasie bénigne de la prostate, altérations d'humeur et de compréhension et cancer de la prostate, c) le traitement de troubles associés au déclin d'androgènes chez la femme (ADIF), tels que dysfonctionnement sexuel, libido sexuelle en régression, hypogonadisme, sarcopénie, ostéopénie, ostéoporose, altérations de l'humeur et de la compréhension, dépression, anémie, perte de cheveux, obésité, endométriose, cancer du sein, cancer de l'utérus et des ovaires, d) le traitement et/ou la prévention de troubles d'atrophie musculaire aiguë et/ou chronique, e) la prévention et/ou le traitement de troubles de l'oeil sec, f) la thérapie orale de remplacement d'androgène, g) la réduction de l'incidence de l'arrêt ou de la provocation d'une régression du cancer de la prostate, et/ou h) l'induction d'apoptose dans une cellule cancéreuse.
PCT/US2003/003121 2002-02-28 2003-02-24 Modulateurs irreversibles selectifs de recepteur d'androgene et procede d'utilisation associes WO2003074473A2 (fr)

Priority Applications (10)

Application Number Priority Date Filing Date Title
CA002476651A CA2476651A1 (fr) 2002-02-28 2003-02-24 Modulateurs irreversibles selectifs de recepteur d'androgene et procede d'utilisation associes
EP03710820A EP1487783A4 (fr) 2002-02-28 2003-02-24 Modulateurs irreversibles selectifs de recepteur d'androgene et procede d'utilisation associes
AU2003214971A AU2003214971A1 (en) 2002-02-28 2003-02-24 Irreversible selective androgen receptor modulators and methods of use thereof
KR10-2004-7013473A KR20040104463A (ko) 2002-02-28 2003-02-24 비가역적 선택적 안드로겐 수용체 모듈레이터 및 이를사용하는 방법
MXPA04008412A MXPA04008412A (es) 2002-02-28 2003-02-24 Moduladores irreversibles del receptor de androgeno selectivo y metodos para utilizar los mismos.
JP2003572945A JP2005519111A (ja) 2002-02-28 2003-02-24 不可逆型選択的アンドロゲンレセプタ修飾因子及びその使用方法
EA200401121A EA200401121A1 (ru) 2002-02-28 2003-02-24 Необратимые селективные модуляторы андрогенового рецептора и способы их применения
BR0308076-5A BR0308076A (pt) 2002-02-28 2003-02-24 Modulares seletivos receptores de androgênio irreversìveis e seus métodos de uso
IL16374203A IL163742A0 (en) 2002-02-28 2003-02-24 Irreversible selective androgen receptor modulators and methods of use thereof
HR20040851A HRP20040851A2 (en) 2002-02-28 2004-09-16 Irreversible selective androgen receptor modulators and methods of use thereof

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US8467902A 2002-02-28 2002-02-28
US60/453,704 2002-02-28
US42024802P 2002-10-23 2002-10-23
US60/420,248 2002-10-23

Publications (2)

Publication Number Publication Date
WO2003074473A2 WO2003074473A2 (fr) 2003-09-12
WO2003074473A3 true WO2003074473A3 (fr) 2003-12-18

Family

ID=27791168

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/003121 WO2003074473A2 (fr) 2002-02-28 2003-02-24 Modulateurs irreversibles selectifs de recepteur d'androgene et procede d'utilisation associes

Country Status (12)

Country Link
EP (1) EP1487783A4 (fr)
JP (1) JP2005519111A (fr)
KR (1) KR20040104463A (fr)
CN (1) CN1646479A (fr)
AU (1) AU2003214971A1 (fr)
CA (1) CA2476651A1 (fr)
EA (1) EA200401121A1 (fr)
HR (1) HRP20040851A2 (fr)
IL (1) IL163742A0 (fr)
MX (1) MXPA04008412A (fr)
TW (1) TW200304806A (fr)
WO (1) WO2003074473A2 (fr)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040260108A1 (en) * 2001-06-25 2004-12-23 Dalton James T. Metabolites of selective androgen receptor modulators and methods of use thereof
US7253210B2 (en) * 2002-10-15 2007-08-07 University Of Tennessee Research Foundation Methylene-bridged selective androgen receptor modulators and methods of use thereof
EP1562906A4 (fr) * 2002-10-15 2009-12-02 Univ Tennessee Res Foundation Modulateurs heterocycliques selectifs du recepteur des androgenes et procedes d'utilisation associes
EP1592658B1 (fr) * 2003-01-13 2013-04-24 University of Tennessee Research Foundation Synthèse a grande échelle de modulateurs sélectifs de récepteur d'androgène
AU2004206909A1 (en) * 2003-01-22 2004-08-05 Gtx Inc. Treating androgen deficiency in female (ADIF)-associated conditions with sarms
EP1631540A4 (fr) * 2003-12-16 2006-10-04 Gtx Inc Promedicaments de modulateurs selectifs des recepteurs aux androgenes et leurs methodes d'utilisation
CA2554696C (fr) 2004-02-13 2009-06-30 Warner-Lambert Company Llc Modulateurs du recepteur d'androgene
EP1737813A1 (fr) 2004-04-13 2007-01-03 Warner-Lambert Company LLC Modulateurs d'androgenes
CA2562672C (fr) * 2004-04-22 2009-09-29 Warner-Lambert Company Llc Derives du type 4-cyano-phenoxy utilises comme modulateurs d'androgenes
UA87854C2 (en) * 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
WO2006006065A1 (fr) 2004-07-08 2006-01-19 Warner-Lambert Company Llc Modulateurs d'androgenes
MX2007001248A (es) * 2004-08-18 2007-03-23 Warner Lambert Co Moduladores de androgenos.
TW200724139A (en) 2005-05-05 2007-07-01 Warner Lambert Co Androgen modulators
DK3086784T3 (da) * 2013-12-23 2019-06-17 Bcn Peptides Sa Bicalutamid analoger eller (s)-bicalutamid som exocytose aktiverende forbindelser til brug i behandling af lysosomal lagringssygdom eller glycogenose
US10093613B2 (en) 2015-04-21 2018-10-09 Gtx, Inc. 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
US10865184B2 (en) 2015-04-21 2020-12-15 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
US11230523B2 (en) 2016-06-10 2022-01-25 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
KR102481319B1 (ko) * 2016-06-10 2022-12-26 유니버시티 오브 테네시 리서치 파운데이션 선택적 안드로겐 수용체 분해제(sard) 리간드 및 이의 사용 방법
CN113137836B (zh) * 2021-04-23 2023-04-07 柳州东风容泰化工股份有限公司 一种制备邻氯苯腈的干燥方法及系统

Citations (1)

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Publication number Priority date Publication date Assignee Title
US6071957A (en) * 1996-11-27 2000-06-06 The University Of Tennessee Research Corporation Irreversible non-steroidal antagonist compound and its use in the treatment of prostate cancer

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998053826A1 (fr) * 1997-05-30 1998-12-03 The University Of Tennessee Research Corporation Composes agonistes non steroidiens et leur utilisation dans le cadre de therapies a base d'hormones males
EA014224B1 (ru) * 2000-08-24 2010-10-29 Юниверсити Оф Теннесси Рисерч Фаундейшн Селективные модуляторы андрогенового рецептора и способы их применения

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6071957A (en) * 1996-11-27 2000-06-06 The University Of Tennessee Research Corporation Irreversible non-steroidal antagonist compound and its use in the treatment of prostate cancer

Also Published As

Publication number Publication date
CN1646479A (zh) 2005-07-27
EP1487783A2 (fr) 2004-12-22
MXPA04008412A (es) 2005-05-17
JP2005519111A (ja) 2005-06-30
TW200304806A (en) 2003-10-16
CA2476651A1 (fr) 2003-09-12
WO2003074473A2 (fr) 2003-09-12
EA200401121A1 (ru) 2005-10-27
IL163742A0 (en) 2005-12-18
EP1487783A4 (fr) 2006-09-27
AU2003214971A1 (en) 2003-09-16
KR20040104463A (ko) 2004-12-10
HRP20040851A2 (en) 2005-02-28

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