EA200401122A1 - Полизамещённые селективные модуляторы рецептора андрогенов и способы их применения - Google Patents

Полизамещённые селективные модуляторы рецептора андрогенов и способы их применения

Info

Publication number
EA200401122A1
EA200401122A1 EA200401122A EA200401122A EA200401122A1 EA 200401122 A1 EA200401122 A1 EA 200401122A1 EA 200401122 A EA200401122 A EA 200401122A EA 200401122 A EA200401122 A EA 200401122A EA 200401122 A1 EA200401122 A1 EA 200401122A1
Authority
EA
Eurasian Patent Office
Prior art keywords
androgen receptor
androgen
conditions
osteoporosis
sarm
Prior art date
Application number
EA200401122A
Other languages
English (en)
Other versions
EA013818B1 (ru
Inventor
Джеймс Т. Долтон
Дуэйн Д. Миллер
Митчелл С. Стейнер
Карен А. Веверка
Донг Дзин Хванг
Дзюн Чен
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.)
Filing date
Publication date
Priority claimed from US10/084,680 external-priority patent/US20030022868A1/en
Application filed by Юниверсити Оф Теннесси Рисерч Фаундейшн filed Critical Юниверсити Оф Теннесси Рисерч Фаундейшн
Publication of EA200401122A1 publication Critical patent/EA200401122A1/ru
Publication of EA013818B1 publication Critical patent/EA013818B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
    • C07C235/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • 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
    • 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
    • A61P27/04—Artificial tears; Irrigation solutions
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Настоящее изобретение обеспечивает агенты, направленные на рецептор андрогенов (ARTA). Агенты образуют новый подкласс соединений, которые являются селективными модуляторами рецептора андрогенов (SARM). Было обнаружено, что некоторые из соединений SARM имеют неожиданную андрогенную и анаболическую активность нестероидного лиганда для рецептора андрогенов. Было обнаружено, что другие соединения SARM имеют неожиданную антиандрогенную активность нестероидного лиганда для рецептора андрогенов. Соединения SARM сами по себе или в виде композиций являются полезными для а) мужской контрацепции; б) лечения различных гормональнозависимых состояний, например состояний, связанных со снижением андрогенов у пожилых мужчин (ADAM), таких как усталость, депрессия, понижение либидо, сексуальная дисфункция, эректильная дисфункция, гипогонадизм, остеопороз, выпадение волос, анемия, ожирение, саркопения, остеопения, остеопороз, доброкачественная гиперплазия простаты, изменения в настроении и узнавании и рак простаты, в) лечения состояний, связанных со снижением андрогенов у женщин (ADIF), таких как сексуальная дисфункция, пониженное половое либидо, гипогонадизм, саркопения, остеопения, остеопороз, изменения в узнавании и настроении, депрессия, анемия, выпадение волос, ожирение, эндометриоз, рак груди, рак матки и рак яичника; г) лечения и/или предупреждения острых и/или хронических состояний, потери мышечной массы; д) предупреждения и/или лечения состояний сухого глаза; е) оральной андрогенной заместительной терапии и/или ж) уменьшения частоты возникновения, прекращения или вызывания регрессии рака простаты.Отчет о международном поиске был опубликован 2003.12.18.
EA200401122A 2002-02-28 2003-02-24 Полизамещённые селективные модуляторы рецептора андрогенов и способы их применения EA013818B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10/084,680 US20030022868A1 (en) 2001-06-25 2002-02-28 Selective androgen receptor modulators and methods of use thereof
US42338102P 2002-11-04 2002-11-04
PCT/US2003/003123 WO2003074449A2 (en) 2002-02-28 2003-02-24 Multi-substitued selective androgen receptor modulators and methods of use thereof

Publications (2)

Publication Number Publication Date
EA200401122A1 true EA200401122A1 (ru) 2005-06-30
EA013818B1 EA013818B1 (ru) 2010-08-30

Family

ID=27791169

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200401122A EA013818B1 (ru) 2002-02-28 2003-02-24 Полизамещённые селективные модуляторы рецептора андрогенов и способы их применения

Country Status (10)

Country Link
AU (1) AU2003216153B2 (ru)
BR (1) BR0308176A (ru)
CA (1) CA2477737C (ru)
EA (1) EA013818B1 (ru)
GE (1) GEP20074209B (ru)
HR (1) HRP20040830A2 (ru)
IL (2) IL163744A0 (ru)
MX (1) MXPA04009460A (ru)
TW (1) TWI338678B (ru)
WO (1) WO2003074449A2 (ru)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7759520B2 (en) 1996-11-27 2010-07-20 University Of Tennessee Research Foundation Synthesis of selective androgen receptor modulators
US7622503B2 (en) 2000-08-24 2009-11-24 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
US7645898B2 (en) 2000-08-24 2010-01-12 University Of Tennessee Research Foundation Selective androgen receptor modulators and method of use thereof
US7855229B2 (en) 2000-08-24 2010-12-21 University Of Tennessee Research Foundation Treating wasting disorders with selective androgen receptor modulators
US8445534B2 (en) 2000-08-24 2013-05-21 University Of Tennessee Research Foundation Treating androgen decline in aging male (ADAM)-associated conditions with SARMs
US20040260108A1 (en) * 2001-06-25 2004-12-23 Dalton James T. Metabolites of selective androgen receptor modulators and methods of use thereof
US7919647B2 (en) 2000-08-24 2011-04-05 University Of Tennessee Research Foundation 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
US8309603B2 (en) 2004-06-07 2012-11-13 University Of Tennessee Research Foundation SARMs and method of use thereof
AU2004206909A1 (en) * 2003-01-22 2004-08-05 Gtx Inc. Treating androgen deficiency in female (ADIF)-associated conditions with sarms
CN102976973B (zh) * 2004-06-07 2015-10-21 田纳西大学研究基金会 选择性雄激素受体调节剂及其使用方法
US9884038B2 (en) 2004-06-07 2018-02-06 University Of Tennessee Research Foundation Selective androgen receptor modulator and methods of use thereof
US9889110B2 (en) 2004-06-07 2018-02-13 University Of Tennessee Research Foundation Selective androgen receptor modulator for treating hormone-related conditions
AU2005251781C1 (en) * 2004-06-07 2008-02-21 University Of Tennessee Research Foundation Selective androgen receptor modulators and methods of use thereof
EP1931199A4 (en) * 2005-08-31 2009-07-29 Univ Tennessee Res Foundation TREATMENT OF RENAL DISEASE, BURNS, INJURIES OR SPINAL CORD INJURY USING ANDROGEN RECEPTOR SELECTIVE MODULATORS
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
US10010521B2 (en) 2006-08-24 2018-07-03 University Of Tennessee Research Foundation SARMs and method of use thereof
US7968603B2 (en) 2007-09-11 2011-06-28 University Of Tennessee Research Foundation Solid forms of selective androgen receptor modulators
RU2012134351A (ru) 2010-01-11 2014-02-20 ДЖиТиЭкс, ИНК. Способы лечения дисфункции мейбомиевых желез
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)
US10314807B2 (en) 2012-07-13 2019-06-11 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)
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)
US10258596B2 (en) 2012-07-13 2019-04-16 Gtx, Inc. Method of treating HER2-positive 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)
KR102238970B1 (ko) 2012-07-13 2021-04-09 지티엑스, 인코포레이티드 선택적 안드로겐 수용체 조절자(sarms)를 이용한 안드로겐 수용체(ar) 양성 유방암의 치료 방법

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8617653D0 (en) * 1986-07-18 1986-08-28 Ici Plc Amide derivatives
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
AU7723198A (en) * 1997-06-04 1998-12-21 University Of Tennessee Research Corporation, The Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging
PT1401801E (pt) * 2000-08-24 2007-02-28 Univ Tennessee Res Foundation Modulares selectivos de receptor de androgénio e métodos para a sua utilização
MXPA04005519A (es) * 2001-12-06 2005-06-20 Gtx Inc Tratamiento del desgaste muscular con moduladores receptores de androgeno selectivos.

Also Published As

Publication number Publication date
AU2003216153A1 (en) 2003-09-16
GEP20074209B (en) 2007-10-10
HRP20040830A2 (en) 2005-06-30
AU2003216153B2 (en) 2008-01-24
IL163744A0 (en) 2005-12-18
CA2477737A1 (en) 2003-09-12
IL163744A (en) 2013-03-24
CA2477737C (en) 2012-08-07
TW200307661A (en) 2003-12-16
MXPA04009460A (es) 2006-04-27
TWI338678B (en) 2011-03-11
WO2003074449A3 (en) 2003-12-18
BR0308176A (pt) 2005-01-04
EA013818B1 (ru) 2010-08-30
WO2003074449A2 (en) 2003-09-12

Similar Documents

Publication Publication Date Title
EA200401122A1 (ru) Полизамещённые селективные модуляторы рецептора андрогенов и способы их применения
EA200500022A1 (ru) N- мостиковые селективные модуляторы андрогенных рецепторов и способы их применения
ATE533494T1 (de) Mehrfach substituierte selektive androgen- rezeptor-modulatoren und anwendungsverfahren dafür
TW200503711A (en) Methylene-bridged selective androgen receptor modulators and methods of use thereof
TW200420571A (en) Halogenated selective androgen receptor modulators and methods of use thereof
TW200502249A (en) Heterocyclic selective androgen receptor modulators and methods of use thereof
EA200401121A1 (ru) Необратимые селективные модуляторы андрогенового рецептора и способы их применения
CY1114156T1 (el) Μεγαλης κλιμακας συνθεση επιλεκτικων ρυθμιστων υποδοχεων ανδρογονων
EA200602151A1 (ru) Метаболиты селективных модуляторов андрогеновых рецепторов и способы их применения
EA200300283A1 (ru) Селективные модуляторы андрогенового рецептора и способы их применения
BR0307981A (pt) Compostos substituìdos de haloacetamida e azida e seus métodos de uso
EA200501761A1 (ru) Пролекарственные формы селективных модуляторов андрогеновых рецепторов и способы их применения
EP1606264A4 (en) ANTAGONISTS OF MONOCYCLIC SPIROHYDANTOIN ANILIDE CGRP RECEPTORS
ATE418972T1 (de) Verhinderung und behandlung von durch androgenmangel induzierter osteoporose
ATE439845T1 (de) Kombination von einem ístrogen und einem androgen zur behandlung von hormonmangel in der ístrogenersatztherapie für frauen
MX2021008094A (es) Metodos y composiciones para el tratamiento del cancer.
CY1107816T1 (el) Η χρηση ενος συνδυασμου ενος αναστολεα αρωματασης, μιας προγεστερονης και ενος οιστρογονου για τη θεραπεια της ενδομητριωσης
TW200502250A (en) Treating androgen decline in aging male (ADAM)-associated conditions with SARMS
NZ762312A (en) Anti-pacap antibody
EA202092861A1 (ru) Специфичные в отношении злокачественной опухоли t-клеточные рецепторы
EA200401123A1 (ru) Галогенацетамидные и азидзамещённые соединения и способы их применения
TW200716662A (en) Process for making fluorinated 4-azasteroid derivatives
WO2007081696A3 (en) Treating androgen decline in aging male (adam)-associated conditions with sarms
ECSP067024A (es) Nuevos derivados de indazol e indolona y su uso como productos farmaceuticos
BR0308076A (pt) Modulares seletivos receptores de androgênio irreversìveis e seus métodos de uso

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU