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BR0308176A - Selective multi-substituted androgen receptor modulators and their methods of use - Google Patents

Selective multi-substituted androgen receptor modulators and their methods of use

Info

Publication number
BR0308176A
BR0308176A BR0308176-1A BR0308176A BR0308176A BR 0308176 A BR0308176 A BR 0308176A BR 0308176 A BR0308176 A BR 0308176A BR 0308176 A BR0308176 A BR 0308176A
Authority
BR
Brazil
Prior art keywords
androgen
androgen receptor
msra
compounds
cancer
Prior art date
Application number
BR0308176-1A
Other languages
Portuguese (pt)
Inventor
James Dalton
Duane D Miller
Mitchell S Steiner
Karen A Veverka
Dong Jin Hwang
Jiyun Chen
Original Assignee
Univ Tennessee Res 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 Univ Tennessee Res Foundation filed Critical Univ Tennessee Res Foundation
Publication of BR0308176A publication Critical patent/BR0308176A/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

Landscapes

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

Abstract

"MODULADORES SELETIVOS RECEPTORES DE ANDROGêNIO MULTI-SUBSTITUìDOS E SEUS MéTODOS DE USO". Esta invenção provê uma nova classe de agentes direcionantes receptores de androgênio (ADRA). Estes agentes que definem uma nova sub-classe de compostos, que são moduladores seletivos receptores de androgênio (MSRA). Vários compostos MSRA têm uma inesperada atividade androgênica e anabólica de um ligante não-esteroidal para o receptor de androgênio. Outros compostos MSRA têm uma inesperada atividade anti-androgênica de um ligante não-esteroidal para o receptor de androgênio. Os compostos de MSRA, tanto sozinhos como em uma composição, servem para a) contracepção masculina; b) tratamento de uma variedade de estados relacionados com os hormónios, por exemplo estados associados com o Declínio Androgênico no Envelhecimento Masculino (DAEM), tais como fadiga, depressão, libido diminuída, disfunção sexual, disfunção erétil, hipogonadismo, osteoporose, perda de cabelo, anemia, obesidade, sarcopenia, osteopenia, osteoporose, hiperplasia benigna de próstata, alterações em humor e cognição e câncer de próstata; c) tratamento de estados associados ao Declínio Androgênico Feminino (DAF), tais como disfunção sexual, libido sexual diminuída, hipogonadismo, sarcopenia, osteopenia, osteoporose, alterações em cognição e humor, depressão, anemia, perda de cabelo, obesidade, endometriose, câncer de mama, câncer uterino e câncer ovariano; d) tratamento e/ou prevenção de estados de degeneração muscular aguda ou crónica; e) prevenção e/ou tratamento de estados de "olho seco"; f) terapia de reposição androgênica oral; e/ou g) diminuição da incidência, interrompendo, ou causando uma regressão de câncer de próstata."SELECTIVE MULTI-REPLACED ANDROGEN RECEIVER MODULATORS AND THEIR METHODS OF USE". This invention provides a new class of androgen receptor targeting agents (ADRA). These agents define a new subclass of compounds, which are selective androgen receptor modulators (MSRA). Several MSRA compounds have an unexpected androgenic and anabolic activity of a non-steroidal androgen receptor ligand. Other MSRA compounds have an unexpected anti-androgenic activity of a non-steroidal androgen receptor ligand. The MSRA compounds, either alone or in a composition, serve for a) male contraception; b) treating a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Male Aging (DAEM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss , anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, changes in mood and cognition, and prostate cancer; c) treatment of conditions associated with Female Androgen Decline (DAF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, changes in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, cancer. breast, uterine cancer and ovarian cancer; d) treatment and / or prevention of acute or chronic muscle degeneration states; e) prevention and / or treatment of "dry eye" conditions; f) oral androgen replacement therapy; and / or g) decreased incidence by stopping or causing a regression of prostate cancer.

BR0308176-1A 2002-02-28 2003-02-24 Selective multi-substituted androgen receptor modulators and their methods of use BR0308176A (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 (1)

Publication Number Publication Date
BR0308176A true BR0308176A (en) 2005-01-04

Family

ID=27791169

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0308176-1A BR0308176A (en) 2002-02-28 2003-02-24 Selective multi-substituted androgen receptor modulators and their methods of use

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)

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
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
US7855229B2 (en) 2000-08-24 2010-12-21 University Of Tennessee Research Foundation Treating wasting disorders with selective androgen receptor modulators
US7919647B2 (en) 2000-08-24 2011-04-05 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
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
US20050032750A1 (en) * 2003-01-22 2005-02-10 Steiner Mitchell S. Treating androgen deficiency in female (ADIF)-associated conditions with SARMS
US9889110B2 (en) 2004-06-07 2018-02-13 University Of Tennessee Research Foundation Selective androgen receptor modulator for treating hormone-related conditions
ATE552235T1 (en) * 2004-06-07 2012-04-15 Univ Tennessee Res Foundation SELECTIVE ANDROGEN RECEPTOR MODULATOR AND METHOD OF USE THEREOF
US9884038B2 (en) 2004-06-07 2018-02-06 University Of Tennessee Research Foundation Selective androgen receptor modulator and methods of use thereof
PT1753417E (en) * 2004-06-07 2012-07-05 Univ Tennessee Res Foundation A selective androgen receptor modulator and medical uses thereof
BRPI0617117A2 (en) * 2005-08-31 2011-07-12 Univ Tennessee Res Foundation treatment of kidney disease, burns, injuries and spinal cord damage with selective androgen receptor modulators
US10010521B2 (en) 2006-08-24 2018-07-03 University Of Tennessee Research Foundation SARMs and method of use thereof
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
US7968603B2 (en) 2007-09-11 2011-06-28 University Of Tennessee Research Foundation Solid forms of selective androgen receptor modulators
JP2013516501A (en) 2010-01-11 2013-05-13 ジーティーエックス・インコーポレイテッド How to treat meibomian gland dysfunction
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)
CN108143728A (en) 2012-07-13 2018-06-12 Gtx公司 Purposes of the selective androgen receptor modulators in breast cancer is treated
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)
US10258596B2 (en) 2012-07-13 2019-04-16 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)

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
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
WO1998055153A1 (en) * 1997-06-04 1998-12-10 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
HRP20040588A2 (en) * 2001-12-06 2004-10-31 Gtx Inc Treating muscle wasting with selective androgen receptor modulators

Also Published As

Publication number Publication date
TW200307661A (en) 2003-12-16
EA013818B1 (en) 2010-08-30
GEP20074209B (en) 2007-10-10
MXPA04009460A (en) 2006-04-27
AU2003216153B2 (en) 2008-01-24
CA2477737A1 (en) 2003-09-12
HRP20040830A2 (en) 2005-06-30
AU2003216153A1 (en) 2003-09-16
IL163744A0 (en) 2005-12-18
IL163744A (en) 2013-03-24
CA2477737C (en) 2012-08-07
TWI338678B (en) 2011-03-11
WO2003074449A2 (en) 2003-09-12
EA200401122A1 (en) 2005-06-30
WO2003074449A3 (en) 2003-12-18

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: PARA: INT. CL. A61K 31/655, 31/275, 31/165; C07C 247/16, 331/08, 255/49, 233/05; A61P 5/28

Ipc: A61K 31/655 (2011.01), A61K 31/275 (2011.01), A61K

B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 9A ANUIDADE(S).

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: NAO APRESENTADA A GUIA DE CUMPRIMENTO DE EXIGENCIA. REFERENTE A 9A ANUIDADE.