CA2477737C - Modulateurs de recepteur selectif d'androgene a substitutions multiples et procedes et utilisations associes - Google Patents

Modulateurs de recepteur selectif d'androgene a substitutions multiples et procedes et utilisations associes Download PDF

Info

Publication number
CA2477737C
CA2477737C CA2477737A CA2477737A CA2477737C CA 2477737 C CA2477737 C CA 2477737C CA 2477737 A CA2477737 A CA 2477737A CA 2477737 A CA2477737 A CA 2477737A CA 2477737 C CA2477737 C CA 2477737C
Authority
CA
Canada
Prior art keywords
compound
another embodiment
androgen receptor
sarm
present
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CA2477737A
Other languages
English (en)
Other versions
CA2477737A1 (fr
Inventor
James T. Dalton
Duane D. Miller
Mitchell S. Steiner
Karen A. Veverka
Dong Jin Hwang
Jiyun Chen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Tennessee Research Foundation
Original Assignee
University of Tennessee Research Foundation
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 University of Tennessee Research Foundation filed Critical University of Tennessee Research Foundation
Publication of CA2477737A1 publication Critical patent/CA2477737A1/fr
Application granted granted Critical
Publication of CA2477737C publication Critical patent/CA2477737C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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

L'invention concerne des 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). Parmi les composés SARM plusieurs ont démontré des activités androgène et anabolique inattendue de ligand non stéroïde pour le récepteur d'androgène. D'autres composés SARM ont démontré un activité anti-androgène inattendue de ligand non stéroïde pour le récepteur d'androgène. Ces 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.
CA2477737A 2002-02-28 2003-02-24 Modulateurs de recepteur selectif d'androgene a substitutions multiples et procedes et utilisations associes Expired - Fee Related CA2477737C (fr)

Applications Claiming Priority (5)

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
US10/084,680 2002-02-28
US42338102P 2002-11-04 2002-11-04
US60/423,381 2002-11-04
PCT/US2003/003123 WO2003074449A2 (fr) 2002-02-28 2003-02-24 Modulateurs de recepteur selectif d'androgene a substitutions multiples et procedes et utilisations associes

Publications (2)

Publication Number Publication Date
CA2477737A1 CA2477737A1 (fr) 2003-09-12
CA2477737C true CA2477737C (fr) 2012-08-07

Family

ID=27791169

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2477737A Expired - Fee Related CA2477737C (fr) 2002-02-28 2003-02-24 Modulateurs de recepteur selectif d'androgene a substitutions multiples et procedes et utilisations associes

Country Status (10)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9150501B2 (en) 2007-09-11 2015-10-06 Gtx, Inc. Solid forms of selective androgen receptor modulators

Families Citing this family (26)

* 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 (fr) * 2005-08-31 2009-07-29 Univ Tennessee Res Foundation Traitement de maladie renale, de brulures, de blessures ou de lesions de la moelle epiniere au moyen de modulateurs selectifs du recepteur d'androgenes
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
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 (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
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.

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9150501B2 (en) 2007-09-11 2015-10-06 Gtx, Inc. Solid forms of selective androgen receptor modulators

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 (fr) 2003-09-12
IL163744A (en) 2013-03-24
TW200307661A (en) 2003-12-16
MXPA04009460A (es) 2006-04-27
TWI338678B (en) 2011-03-11
WO2003074449A3 (fr) 2003-12-18
BR0308176A (pt) 2005-01-04
EA013818B1 (ru) 2010-08-30
EA200401122A1 (ru) 2005-06-30
WO2003074449A2 (fr) 2003-09-12

Similar Documents

Publication Publication Date Title
EP1487458B1 (fr) Modulateurs de recepteur selectif d'androgene a substitutions multiples et procedes et utilisations associes
US7803970B2 (en) Multi-substitued selective androgen receptor modulators and methods of use thereof
CA2477737C (fr) Modulateurs de recepteur selectif d'androgene a substitutions multiples et procedes et utilisations associes
US7026500B2 (en) Halogenated selective androgen receptor modulators and methods of use thereof
US7022870B2 (en) N-bridged selective androgen receptor modulators and methods of use thereof
US7518013B2 (en) Selective androgen receptor modulators
US20040147489A1 (en) Haloacetamide and azide substituted compounds and methods of use thereof
US20040087810A1 (en) Irreversible selective androgen receptor modulators and methods of use thereof
US20060287547A1 (en) Selective androgen receptor modulators
US20030232792A1 (en) Selective androgen receptor modulators and methods of use thereof
US20030225040A1 (en) Selective androgen receptor modulators and methods of use thereof
US20090264534A1 (en) Selective androgen receptor modulators
US20050038110A1 (en) Selective androgen receptor modulators and methods of use thereof
US20040167103A1 (en) Haloacetamide and azide substituted compounds and methods of use thereof
US20040138244A1 (en) Heterocyclic selective androgen receptor modulators and methods of use thereof
EP1562594A2 (fr) Modulateurs selectifs du recepteur des androgenes a liaison methylene et procedes d'utilisation associes
CA2476651A1 (fr) Modulateurs irreversibles selectifs de recepteur d'androgene et procede d'utilisation associes
AU2008201811B2 (en) Multi-substituted selective androgen receptor modulators and methods of use thereof
EP2266577B1 (fr) Modulateurs de récepteur sélectif d'androgène à substitutions multiples et procédé d'utilisation associés

Legal Events

Date Code Title Description
EEER Examination request
MKLA Lapsed

Effective date: 20210224