EA200401122A1 - POLISHMISSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF THEIR APPLICATION - Google Patents

POLISHMISSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF THEIR APPLICATION

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
Russian (ru)
Other versions
EA013818B1 (en
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/en
Publication of EA013818B1 publication Critical patent/EA013818B1/en

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

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.The present invention provides agents directed to the androgen receptor (ARTA). Agents form a new subclass of compounds that are selective androgen receptor modulators (SARM). Some of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of the nonsteroidal ligand for the androgen receptor. It has been found that other SARM compounds have an unexpected anti-androgenic activity of the nonsteroidal ligand for the androgen receptor. SARM compounds alone or in the form of compositions are useful for a) male contraception; b) treatment of various hormone-dependent conditions, such as conditions associated with androgen decline in elderly men (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia , osteoporosis, benign prostatic hyperplasia, changes in mood and recognition, and prostate cancer, c) treatment of conditions associated with androgen reduction in women (ADIF), such as sexual dysfunction, decreased sexual libi before, hypogonadism, sarcopenia, osteopenia, osteoporosis, changes in recognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treating and / or preventing acute and / or chronic conditions, loss of muscle mass; e) preventing and / or treating dry eye conditions; f) oral androgen replacement therapy and / or g) reduce the incidence, cessation or induction of regression of prostate cancer. The international search report was published 2003.12.18.

EA200401122A 2002-02-28 2003-02-24 Multi-substituted selective androgen receptor modulators and methods of use thereof EA013818B1 (en)

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 (en) 2005-06-30
EA013818B1 EA013818B1 (en) 2010-08-30

Family

ID=27791169

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200401122A EA013818B1 (en) 2002-02-28 2003-02-24 Multi-substituted selective androgen receptor modulators and methods of use thereof

Country Status (10)

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

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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
US7855229B2 (en) 2000-08-24 2010-12-21 University Of Tennessee Research Foundation Treating wasting disorders with selective androgen receptor modulators
US7645898B2 (en) 2000-08-24 2010-01-12 University Of Tennessee Research Foundation Selective androgen receptor modulators and method 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
US20040260108A1 (en) * 2001-06-25 2004-12-23 Dalton James T. Metabolites of selective androgen receptor modulators and methods of use thereof
US8445534B2 (en) 2000-08-24 2013-05-21 University Of Tennessee Research Foundation Treating androgen decline in aging male (ADAM)-associated conditions with SARMs
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
JP2006516286A (en) * 2003-01-22 2006-06-29 ジーティーエックス・インコーポレイテッド Treatment of diseases related to androgen depletion in women by SARM
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
PT1753417E (en) * 2004-06-07 2012-07-05 Univ Tennessee Res Foundation A selective androgen receptor modulator and medical uses thereof
DK2289872T3 (en) * 2004-06-07 2017-10-09 Univ Tennessee Res Found Medical use of a selective androgen receptor modulator
EP1931199A4 (en) * 2005-08-31 2009-07-29 Univ Tennessee Res Foundation Treating renal disease, burns, wounds and spinal cord injury with selective androgen receptor modulators
US9730908B2 (en) 2006-08-24 2017-08-15 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
US9844528B2 (en) 2006-08-24 2017-12-19 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
EP2523556A4 (en) 2010-01-11 2013-08-28 Gtx Inc Methods of treating meibomian gland dysfunction
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)
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)
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)
US10314807B2 (en) 2012-07-13 2019-06-11 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
US10258596B2 (en) 2012-07-13 2019-04-16 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
RU2717835C2 (en) 2012-07-13 2020-03-26 Джи Ти Икс, ИНК. Method of treating androgen receptor (ar)-positive forms of breast cancer using selective androgen receptor modulators (sarm)

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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
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
US6019957A (en) * 1997-06-04 2000-02-01 The University Of Tennessee Research Corporation Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging
DE60124322T2 (en) * 2000-08-24 2007-05-31 University Of Tennessee Research Foundation, Knoxville SELECTIVE MODULATORS OF THE ANDROGEN RECEPTOR AND METHODS OF THEIR USE
DK1463497T3 (en) * 2001-12-06 2012-01-30 Gtx Inc Treatment of muscle wasting with selective androgen receptor modulators

Also Published As

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

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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