EA200401121A1 - Необратимые селективные модуляторы андрогенового рецептора и способы их применения - Google Patents

Необратимые селективные модуляторы андрогенового рецептора и способы их применения

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Publication number
EA200401121A1
EA200401121A1 EA200401121A EA200401121A EA200401121A1 EA 200401121 A1 EA200401121 A1 EA 200401121A1 EA 200401121 A EA200401121 A EA 200401121A EA 200401121 A EA200401121 A EA 200401121A EA 200401121 A1 EA200401121 A1 EA 200401121A1
Authority
EA
Eurasian Patent Office
Prior art keywords
androgen receptor
androgen
treatment
sarm compounds
sarm
Prior art date
Application number
EA200401121A
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English (en)
Inventor
Джеймс Долтон
Дуэйн Д. Миллер
Митчелл С. Стейнер
Карен А. Веверка
Леонид И. Кирковский
Арнаб Мухерджее
Донг Дзин Хванг
Хюйпинг Ксю
Original Assignee
Юниверсити Оф Теннесси Рисерч Фаундейшн
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.)
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Publication date
Application filed by Юниверсити Оф Теннесси Рисерч Фаундейшн filed Critical Юниверсити Оф Теннесси Рисерч Фаундейшн
Publication of EA200401121A1 publication Critical patent/EA200401121A1/ru

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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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

В одном из воплощений настоящее изобретение обеспечивает класс агентов, нацеленных на андрогеновый рецептор (ARTA). Агенты образуют новый подкласс соединений, которые являются селективными модуляторами андрогенового рецептора (SARM). Соединения SARM имеют неожиданную антиандрогеновую активность нестероидного лиганда для андрогенового рецептора. В одном из воплощений соединения SARM связаны необратимо с андрогеновым рецептором. В другом воплощении соединения SARM представляют собой антагонист андрогенового рецептора, который связывается необратимо с андрогеновым рецептором. В другом воплощении соединения SARM представляют собой алкилирующий агент. Соединения SARM, или сами по себе, или в виде композиций, являются полезными для а) мужской контрацепции; б) лечения различных гормональнозависимых состояний, например состояний, связанных с уменьшением андрогена у пожилых мужчин (ADAM), таких как усталость, депрессия, понижение либидо, сексуальная дисфункция, эректильная дисфункция, гипогонадизм, остеопороз, выпадение волос, анемия, ожирение, саркопения, остеопения, остеопороз, мягкая гиперплазия простаты, изменения в настроении и узнавании и рак простаты; в) лечения состояний, связанных с уменьшением андрогена у женщин (ADIF), таких как сексуальная дисфункция, пониженное половое либидо, гипогонадизм, саркопения, остеопения, остеопороз, изменения в способности узнавания и настроении, депрессия, анемия, выпадение волос, ожирение, эндометриоз, рак груди, рак матки и рак яичника; г) лечения и/или профилактика острых и/или хронических состояний, связанных с атрофией мышц; д) профилактики и/или лечения состояний сухого глаза; е) оральной андрогенной заместительной
EA200401121A 2002-02-28 2003-02-24 Необратимые селективные модуляторы андрогенового рецептора и способы их применения EA200401121A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US8467902A 2002-02-28 2002-02-28
US42024802P 2002-10-23 2002-10-23
PCT/US2003/003121 WO2003074473A2 (en) 2002-02-28 2003-02-24 Irreversible selective androgen receptor modulators and methods of use thereof

Publications (1)

Publication Number Publication Date
EA200401121A1 true EA200401121A1 (ru) 2005-10-27

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA200401121A EA200401121A1 (ru) 2002-02-28 2003-02-24 Необратимые селективные модуляторы андрогенового рецептора и способы их применения

Country Status (12)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113137836A (zh) * 2021-04-23 2021-07-20 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

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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
AU2003287077B2 (en) 2002-10-15 2007-09-20 University Of Tennessee Research Foundation Methylene-bridged selective androgen receptor modulators and methods of use thereof
CN1726193A (zh) * 2002-10-15 2006-01-25 田纳西大学研究基金会 杂环选择性雄激素受体调节剂及其使用方法
CA2513242C (en) * 2003-01-13 2013-07-09 Gtx Inc. Large-scale synthesis of selective androgen receptor modulators
EP1594490A4 (en) * 2003-01-22 2006-03-22 Gtx Inc TREATMENT OF WOMEN ANDROGEN DISEASE ASSOCIATED DISORDERS (ADIF) USING ANDROGENIC RECEPTOR MODULATORS (SARM)
EP1631540A4 (en) * 2003-12-16 2006-10-04 Gtx Inc PRODRUGS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHOD OF USE THEREOF
JP3997255B2 (ja) 2004-02-13 2007-10-24 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー アンドロゲンレセプターモジュレーター
US7507860B2 (en) 2004-04-13 2009-03-24 Pfizer Inc. Androgen modulators
WO2005102990A1 (en) * 2004-04-22 2005-11-03 Warner-Lambert Company Llc Androgen modulators
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
BRPI0513020A (pt) 2004-07-08 2008-04-22 Warner Lambert Co moduladores de andrÈgenio, seus usos, composição farmacêutica, formulação farmacêutica tópica e artigo de fabricação
WO2006018732A1 (en) * 2004-08-18 2006-02-23 Warner-Lambert Company Llc Androgen modulators
TW200724139A (en) 2005-05-05 2007-07-01 Warner Lambert Co Androgen modulators
CA2934772C (en) * 2013-12-23 2021-04-27 Bcn Peptides, S.A. Bicalutamide analogs or (s)-bicalutamide as exocytosis activating compounds for use in the treatment of a lysosomal storage disorder or glycogenosis
US10093613B2 (en) 2015-04-21 2018-10-09 Gtx, Inc. 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
US10806720B2 (en) 2015-04-21 2020-10-20 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
US11230523B2 (en) 2016-06-10 2022-01-25 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof

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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
WO1998053826A1 (en) * 1997-05-30 1998-12-03 The University Of Tennessee Research Corporation Non-steroidal agonist compounds and their use in male hormone therapy
EP1401801B1 (en) * 2000-08-24 2006-11-02 The University Of Tennessee Research Corporation Selective androgen receptor modulators and methods of use thereof

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113137836A (zh) * 2021-04-23 2021-07-20 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
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

Also Published As

Publication number Publication date
AU2003214971A1 (en) 2003-09-16
CA2476651A1 (en) 2003-09-12
KR20040104463A (ko) 2004-12-10
CN1646479A (zh) 2005-07-27
JP2005519111A (ja) 2005-06-30
IL163742A0 (en) 2005-12-18
EP1487783A2 (en) 2004-12-22
WO2003074473A3 (en) 2003-12-18
WO2003074473A2 (en) 2003-09-12
TW200304806A (en) 2003-10-16
HRP20040851A2 (en) 2005-02-28
MXPA04008412A (es) 2005-05-17
EP1487783A4 (en) 2006-09-27

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