AU2004206909A1 - Treating androgen deficiency in female (ADIF)-associated conditions with sarms - Google Patents
Treating androgen deficiency in female (ADIF)-associated conditions with sarms Download PDFInfo
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- AU2004206909A1 AU2004206909A1 AU2004206909A AU2004206909A AU2004206909A1 AU 2004206909 A1 AU2004206909 A1 AU 2004206909A1 AU 2004206909 A AU2004206909 A AU 2004206909A AU 2004206909 A AU2004206909 A AU 2004206909A AU 2004206909 A1 AU2004206909 A1 AU 2004206909A1
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- sarm
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| US44130803P | 2003-01-22 | 2003-01-22 | |
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| PCT/US2004/001359 WO2004064747A2 (en) | 2003-01-22 | 2004-01-20 | Treating androgen deficiency in female (adif)-associated conditions with sarms |
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| AU2004206909A1 true AU2004206909A1 (en) | 2004-08-05 |
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| US (1) | US20050032750A1 (https=) |
| EP (1) | EP1594490A4 (https=) |
| JP (1) | JP2006516286A (https=) |
| CN (1) | CN1771031A (https=) |
| AU (1) | AU2004206909A1 (https=) |
| CA (1) | CA2514024A1 (https=) |
| TW (1) | TW200503729A (https=) |
| WO (1) | WO2004064747A2 (https=) |
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| CN106405064A (zh) * | 2016-08-30 | 2017-02-15 | 嘉兴行健生物科技有限公司 | 一种40岁以上女性骨转换率的评估方法 |
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| US7759520B2 (en) | 1996-11-27 | 2010-07-20 | University Of Tennessee Research Foundation | Synthesis of selective androgen receptor modulators |
| 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 |
| US20060276539A1 (en) * | 2002-10-16 | 2006-12-07 | Dalton James T | Treating Androgen Decline in Aging Male (ADAM)- associated conditions with SARMS |
| WO2004035739A2 (en) * | 2002-10-16 | 2004-04-29 | Gtx, Inc. | Treating androgen decline in aging male (adam)-associated conditions with sarms |
| US8309603B2 (en) | 2004-06-07 | 2012-11-13 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| FI20030958A0 (fi) * | 2003-06-27 | 2003-06-27 | Orion Corp | Uusia yhdisteitä |
| CA2535953C (en) * | 2003-10-14 | 2012-07-03 | Gtx, Inc. | Treating bone-related disorders with selective androgen receptor modulators |
| US9884038B2 (en) | 2004-06-07 | 2018-02-06 | University Of Tennessee Research Foundation | Selective androgen receptor modulator and methods of use thereof |
| JP5449775B2 (ja) | 2005-10-19 | 2014-03-19 | チャバフ ピーティーワイ エルティーディー | 乳癌の治療に使用されるアロマターゼ阻害薬による副作用の低減 |
| KR100785038B1 (ko) * | 2006-04-17 | 2007-12-12 | 삼성전자주식회사 | 비정질 ＺｎＯ계 ＴＦＴ |
| PT2038252T (pt) * | 2006-07-12 | 2016-12-16 | Univ Tennessee Res Found | Acilanilidos substituidos e métodos de utilização dos mesmos |
| 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 |
| CN101528214B (zh) * | 2006-08-24 | 2013-06-05 | 田纳西大学研究基金会 | 取代的n-酰基苯胺及其使用方法 |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| CN103002737A (zh) | 2010-01-11 | 2013-03-27 | Gtx公司 | 治疗睑板腺功能障碍的方法 |
| FR2982261B1 (fr) * | 2011-11-04 | 2014-06-13 | Galderma Res & Dev | Nouveaux amides, et leur utilisation pharmaceutique ou cosmetique |
| PT2872482T (pt) * | 2012-07-13 | 2020-09-22 | Oncternal Therapeutics Inc | Método de tratamento de cancro de mama com modulador seletivo do recetor de andrógeno (sarm) |
| 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) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| 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) |
| CN113633644A (zh) | 2014-10-22 | 2021-11-12 | 哈瓦赫治疗有限公司 | 降低乳房摄影乳腺密度和/或乳腺癌风险的方法 |
| JP2018534291A (ja) | 2015-10-22 | 2018-11-22 | ハバフ セラピューティクス ピーティーワイ エルティーディー | マンモグラフィ乳房密度及び／又は乳癌のリスクを低下させる方法 |
| CA3142193A1 (en) | 2019-06-03 | 2020-12-10 | Havah Therapeutics Pty Ltd | Pharmaceutical formulations and systems for delivery of an androgenic agent and an aromatase inhibitor and methods for use |
| US11701332B2 (en) | 2020-11-18 | 2023-07-18 | Bryce Nicholas Day | Methods and compositions for treating female sexual interest and arousal disorder |
| US20230172897A1 (en) * | 2021-12-02 | 2023-06-08 | Veru, Inc. | Methods of treating breast cancers with selective androgen receptor modulators and additional therapeutic agents |
| WO2025102293A1 (zh) * | 2023-11-16 | 2025-05-22 | 北京脑科学与类脑研究所 | 神经活性雄激素受体调节剂及其用途 |
Family Cites Families (8)
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|---|---|---|---|---|
| GB8617653D0 (en) * | 1986-07-18 | 1986-08-28 | Ici Plc | Amide derivatives |
| US5498626A (en) * | 1992-04-10 | 1996-03-12 | Pfizer Inc. | Acylaminoindole derivatives as 5-ht1 agonists |
| US7253210B2 (en) * | 2002-10-15 | 2007-08-07 | University Of Tennessee Research Foundation | Methylene-bridged selective androgen receptor modulators and methods of use thereof |
| EP1401801B1 (en) * | 2000-08-24 | 2006-11-02 | The University Of Tennessee Research Corporation | Selective androgen receptor modulators and methods of use thereof |
| US7026500B2 (en) * | 2000-08-24 | 2006-04-11 | University Of Tennessee Research Foundation | Halogenated selective androgen receptor modulators and methods of use thereof |
| GEP20074209B (en) * | 2002-02-28 | 2007-10-10 | , | Multi-substitued selective androgen receptor modulators and methods of use thereof |
| MXPA04008412A (es) * | 2002-02-28 | 2005-05-17 | Univ Tennessee Res Corp | Moduladores irreversibles del receptor de androgeno selectivo y metodos para utilizar los mismos. |
| GEP20074191B (en) * | 2002-06-17 | 2007-09-10 | Univ Tennessee Res Foundation | N-bridged selective androgen receptor modulators and methods of use thereof |
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2004
- 2004-01-20 JP JP2006501034A patent/JP2006516286A/ja active Pending
- 2004-01-20 AU AU2004206909A patent/AU2004206909A1/en not_active Abandoned
- 2004-01-20 CN CNA2004800077667A patent/CN1771031A/zh active Pending
- 2004-01-20 CA CA002514024A patent/CA2514024A1/en not_active Abandoned
- 2004-01-20 US US10/759,538 patent/US20050032750A1/en not_active Abandoned
- 2004-01-20 EP EP04703606A patent/EP1594490A4/en not_active Withdrawn
- 2004-01-20 WO PCT/US2004/001359 patent/WO2004064747A2/en not_active Ceased
- 2004-01-27 TW TW093101758A patent/TW200503729A/zh unknown
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106405064A (zh) * | 2016-08-30 | 2017-02-15 | 嘉兴行健生物科技有限公司 | 一种40岁以上女性骨转换率的评估方法 |
| CN106405064B (zh) * | 2016-08-30 | 2018-10-26 | 嘉兴行健生物科技有限公司 | 一种40岁以上女性骨转换率的评估方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1594490A2 (en) | 2005-11-16 |
| CN1771031A (zh) | 2006-05-10 |
| WO2004064747A2 (en) | 2004-08-05 |
| CA2514024A1 (en) | 2004-08-05 |
| TW200503729A (en) | 2005-02-01 |
| WO2004064747A3 (en) | 2005-01-27 |
| JP2006516286A (ja) | 2006-06-29 |
| EP1594490A4 (en) | 2006-03-22 |
| AU2004206909A2 (en) | 2004-08-05 |
| US20050032750A1 (en) | 2005-02-10 |
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