JP2005522431A5 - - Google Patents
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- Publication number
- JP2005522431A5 JP2005522431A5 JP2003565418A JP2003565418A JP2005522431A5 JP 2005522431 A5 JP2005522431 A5 JP 2005522431A5 JP 2003565418 A JP2003565418 A JP 2003565418A JP 2003565418 A JP2003565418 A JP 2003565418A JP 2005522431 A5 JP2005522431 A5 JP 2005522431A5
- Authority
- JP
- Japan
- Prior art keywords
- sarm compound
- sarm
- compound according
- represented
- alpha
- 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.)
- Granted
Links
- 229940083324 Selective androgen receptor modulator Drugs 0.000 claims 122
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 122
- 150000001875 compounds Chemical class 0.000 claims 102
- 108010066551 Cholestenone 5 alpha-Reductase Proteins 0.000 claims 22
- 239000003814 drug Substances 0.000 claims 19
- 239000000126 substance Substances 0.000 claims 13
- 238000004519 manufacturing process Methods 0.000 claims 7
- 239000003112 inhibitor Substances 0.000 claims 5
- 230000002401 inhibitory effect Effects 0.000 claims 5
- 150000001204 N-oxides Chemical class 0.000 claims 4
- 239000002207 metabolite Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 108010029908 3-oxo-5-alpha-steroid 4-dehydrogenase Proteins 0.000 claims 3
- 102000001779 3-oxo-5-alpha-steroid 4-dehydrogenase Human genes 0.000 claims 3
- 229940123407 Androgen receptor antagonist Drugs 0.000 claims 3
- 239000003936 androgen receptor antagonist Substances 0.000 claims 3
- 102000001307 androgen receptors Human genes 0.000 claims 3
- 108010080146 androgen receptors Proteins 0.000 claims 3
- 230000002860 competitive effect Effects 0.000 claims 3
- 229940124011 Androgen receptor agonist Drugs 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 2
- MUMGGOZAMZWBJJ-DYKIIFRCSA-N Testostosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 MUMGGOZAMZWBJJ-DYKIIFRCSA-N 0.000 claims 2
- 239000008188 pellet Substances 0.000 claims 2
- 229940113178 5 Alpha reductase inhibitor Drugs 0.000 claims 1
- 239000002677 5-alpha reductase inhibitor Substances 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 108020004414 DNA Proteins 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 206010020880 Hypertrophy Diseases 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- 239000003098 androgen Substances 0.000 claims 1
- 230000000903 blocking effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000002297 mitogenic effect Effects 0.000 claims 1
- 230000007115 recruitment Effects 0.000 claims 1
- 229960003604 testosterone Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35430002P | 2002-02-07 | 2002-02-07 | |
| US36299702P | 2002-03-11 | 2002-03-11 | |
| PCT/US2003/003447 WO2003065992A2 (en) | 2002-02-07 | 2003-02-06 | Treating benign prostate hyperplasia with sarms |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010108498A Division JP2010209102A (ja) | 2002-02-07 | 2010-05-10 | Ｓａｒｍを用いた前立腺肥大症治療 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005522431A JP2005522431A (ja) | 2005-07-28 |
| JP2005522431A5 true JP2005522431A5 (https=) | 2006-01-05 |
| JP4677516B2 JP4677516B2 (ja) | 2011-04-27 |
Family
ID=27737453
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003565418A Expired - Fee Related JP4677516B2 (ja) | 2002-02-07 | 2003-02-06 | Ｓａｒｍを用いた前立腺肥大症治療 |
| JP2010108498A Ceased JP2010209102A (ja) | 2002-02-07 | 2010-05-10 | Ｓａｒｍを用いた前立腺肥大症治療 |
| JP2013082815A Pending JP2013144713A (ja) | 2002-02-07 | 2013-04-11 | 選択的アンドロゲンレセプタ修飾因子（ｓａｒｍ）化合物の使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010108498A Ceased JP2010209102A (ja) | 2002-02-07 | 2010-05-10 | Ｓａｒｍを用いた前立腺肥大症治療 |
| JP2013082815A Pending JP2013144713A (ja) | 2002-02-07 | 2013-04-11 | 選択的アンドロゲンレセプタ修飾因子（ｓａｒｍ）化合物の使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US7776921B2 (https=) |
| EP (1) | EP1480634B1 (https=) |
| JP (3) | JP4677516B2 (https=) |
| KR (2) | KR101032661B1 (https=) |
| CN (2) | CN101732298B (https=) |
| AT (1) | ATE518537T1 (https=) |
| AU (2) | AU2003216174C1 (https=) |
| BR (1) | BRPI0307699A2 (https=) |
| CA (2) | CA2475108A1 (https=) |
| CY (1) | CY1111917T1 (https=) |
| DK (1) | DK1480634T3 (https=) |
| EA (2) | EA013399B1 (https=) |
| GE (1) | GEP20074122B (https=) |
| HR (2) | HRP20100067A2 (https=) |
| IL (2) | IL163380A (https=) |
| MX (1) | MXPA04007639A (https=) |
| PT (1) | PT1480634E (https=) |
| RS (1) | RS69704A (https=) |
| TW (2) | TW200918043A (https=) |
| WO (1) | WO2003065992A2 (https=) |
Families Citing this family (47)
| 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 |
| US7518013B2 (en) | 2000-08-24 | 2009-04-14 | University Of Tennessee Research Foundation | Selective androgen receptor modulators |
| US7855229B2 (en) | 2000-08-24 | 2010-12-21 | University Of Tennessee Research Foundation | Treating wasting disorders with selective androgen receptor modulators |
| US7026500B2 (en) * | 2000-08-24 | 2006-04-11 | University Of Tennessee Research Foundation | Halogenated 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 |
| 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 |
| US8445534B2 (en) | 2000-08-24 | 2013-05-21 | University Of Tennessee Research Foundation | Treating androgen decline in aging male (ADAM)-associated conditions with SARMs |
| US7622503B2 (en) | 2000-08-24 | 2009-11-24 | 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 |
| US20070161608A1 (en) * | 2001-12-06 | 2007-07-12 | Dalton James T | Selective androgen receptor modulators for treating muscle wasting |
| WO2004035739A2 (en) * | 2002-10-16 | 2004-04-29 | Gtx, Inc. | 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 |
| US8309603B2 (en) | 2004-06-07 | 2012-11-13 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| DE602004026583D1 (de) * | 2003-06-27 | 2010-05-27 | Orion Corp | Als androgenrezeptormodulatoren geeignete propionamidderivate |
| 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 |
| KR100783255B1 (ko) | 2004-02-13 | 2007-12-06 | 워너-램버트 캄파니 엘엘씨 | 안드로젠 수용체 조절제 |
| JP2007532621A (ja) | 2004-04-13 | 2007-11-15 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | アンドロゲンモジュレータ |
| WO2005102990A1 (en) | 2004-04-22 | 2005-11-03 | Warner-Lambert Company Llc | Androgen modulators |
| HUE034317T2 (en) * | 2004-06-07 | 2018-02-28 | Univ Tennessee Res Found | Medical application of a selective androgen receptor modulator |
| UA87854C2 (en) * | 2004-06-07 | 2009-08-25 | Мерк Энд Ко., Инк. | N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators |
| US9889110B2 (en) | 2004-06-07 | 2018-02-13 | University Of Tennessee Research Foundation | Selective androgen receptor modulator for treating hormone-related conditions |
| ATE552235T1 (de) * | 2004-06-07 | 2012-04-15 | Univ Tennessee Res Foundation | Selektive androgen-rezeptor-modulator und anwendungsverfahren dafür |
| US20110237664A1 (en) * | 2004-06-07 | 2011-09-29 | Dalton James T | Selective androgen receptor modulators for treating diabetes |
| US9884038B2 (en) | 2004-06-07 | 2018-02-06 | University Of Tennessee Research Foundation | Selective androgen receptor modulator and methods of use thereof |
| EP1781598A1 (en) | 2004-07-08 | 2007-05-09 | Warner-Lambert Company LLC | Androgen modulators |
| EP1768984B1 (en) | 2004-07-16 | 2010-10-20 | Sunesis Pharmaceuticals, Inc. | Thienopyrimidines useful as aurora kinase inhibitors |
| TW200724139A (en) | 2005-05-05 | 2007-07-01 | Warner Lambert Co | Androgen modulators |
| EP2008099A4 (en) * | 2006-04-03 | 2009-12-23 | Medexis S A | DETECTION OF MEMBRANE ANDROGEN RECEPTOR (MAR) ACTIVE SUBSTANCES |
| 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 |
| 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 |
| US9730908B2 (en) | 2006-08-24 | 2017-08-15 | 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 |
| US20150071857A1 (en) * | 2012-03-07 | 2015-03-12 | Ligand Pharmaceuticals, Inc. | Steroid hormone and cholesterol pathways as one unified homeostatic system |
| KR20150011346A (ko) * | 2012-04-06 | 2015-01-30 | 안타레스 팔마, 인코퍼레이티드 | 테스토스테론 조성물의 바늘-보조식 젯 주입 투여 장치 및 방법 |
| 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) |
| 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) |
| US10258596B2 (en) | 2012-07-13 | 2019-04-16 | 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) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (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) |
| 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) |
| WO2015122858A1 (en) | 2014-02-15 | 2015-08-20 | Erdal Can Alkoçlar | A composition containing synthetic components formed for suppressing ribonucleotide reductase |
| HUP1400294A2 (hu) | 2014-06-13 | 2015-12-28 | Skillpharm Kft | Clopidogrel új alkalmazása |
| MX2017004819A (es) * | 2014-10-16 | 2018-06-12 | Gtx Inc | Metodos de tratamiento de transtornos urológicos usando sarm. |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US644970A (en) * | 1899-02-06 | 1900-03-06 | Thomas Graham Donaldson | Dental flask. |
| US935044A (en) * | 1909-01-12 | 1909-09-28 | Lenn G Mccorry | Valve. |
| US935045A (en) * | 1909-06-19 | 1909-09-28 | Robert J Mckelvey | Turn-table. |
| GB1360001A (en) | 1971-06-16 | 1974-07-17 | Scherico Ltd | Pharmaceutical compositions comprising substituted anilides |
| US3875229A (en) | 1972-11-24 | 1975-04-01 | Schering Corp | Substituted carboxanilides |
| JPS6044294B2 (ja) | 1976-04-15 | 1985-10-02 | 帝国臓器製薬株式会社 | アニリド誘導体 |
| US4139638A (en) | 1976-09-23 | 1979-02-13 | Schering Corporation | Methods for the treatment of hirsutism |
| EP0002309B1 (en) | 1977-10-12 | 1982-12-01 | Imperial Chemical Industries Plc | Acylanilides, process for their manufacture and pharmaceutical and veterinary compositions containing them |
| US4191775A (en) | 1977-12-15 | 1980-03-04 | Imperial Chemical Industries Limited | Amide derivatives |
| NZ197008A (en) | 1980-05-22 | 1984-10-19 | Ici Ltd | Acylanilide derivatives and pharmaceutical compositions |
| JPS57171904A (en) | 1981-04-15 | 1982-10-22 | Mitsubishi Petrochem Co Ltd | Tri- or tetra-substituted phenoxycarboxylic acid anilide type herbicide |
| EP0100172B1 (en) * | 1982-07-23 | 1987-08-12 | Imperial Chemical Industries Plc | Amide derivatives |
| GB8617653D0 (en) * | 1986-07-18 | 1986-08-28 | Ici Plc | Amide derivatives |
| GB8617652D0 (en) | 1986-07-18 | 1986-08-28 | Ici Plc | Acylanilide derivatives |
| US5162504A (en) | 1988-06-03 | 1992-11-10 | Cytogen Corporation | Monoclonal antibodies to a new antigenic marker in epithelial prostatic cells and serum of prostatic cancer patients |
| CA2181358A1 (en) | 1994-01-21 | 1995-07-27 | Nancy M. Gray | Methods and compositions for treating androgen-dependent diseases using optically pure r-(-)-casodex |
| US5609849A (en) | 1994-03-11 | 1997-03-11 | The Trustees Of The University Of Pennsylvania | Serotonin (5-HT1A) receptor ligands and imaging agents |
| US5656651A (en) | 1995-06-16 | 1997-08-12 | Biophysica Inc. | Androgenic directed compositions |
| WO1998005962A1 (en) | 1996-08-02 | 1998-02-12 | Panvera Corporation | A method for quantitating competitive binding of molecules to proteins utilizing fluorescence polarization |
| US20090264534A1 (en) * | 1996-11-27 | 2009-10-22 | Dalton James T | Selective androgen receptor modulators |
| 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 |
| US6995284B2 (en) | 2000-08-24 | 2006-02-07 | The University Of Tennessee Research Foundation | Synthesis of selective androgen receptor modulators |
| US7205437B2 (en) * | 1996-11-27 | 2007-04-17 | University Of Tennessee Research Foundation | Selective androgen receptor modulators |
| JPH10182457A (ja) * | 1996-12-25 | 1998-07-07 | Yuichi Hashimoto | 抗アンドロゲン剤 |
| US6160011A (en) | 1997-05-30 | 2000-12-12 | The University Of Tennessee Research Corporation | 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 |
| JPH1135558A (ja) * | 1997-07-18 | 1999-02-09 | Zeria Pharmaceut Co Ltd | ３−ベンゾイルインドール誘導体及びそれらを含有する医薬 |
| GB9919778D0 (en) * | 1999-08-21 | 1999-10-27 | Zeneca Ltd | Chemical compounds |
| AU775928B2 (en) | 1999-10-14 | 2004-08-19 | Bristol-Myers Squibb Company | Crystallographic structure of the androgen receptor ligand binding domain |
| PL354620A1 (en) | 1999-10-19 | 2004-02-09 | Nobex Corporation | Methods of asymmetrically synthesizing enantiomers of casodex, its derivatives and intermediates thereof |
| CN1413188A (zh) | 1999-10-27 | 2003-04-23 | 诺贝克斯公司 | 基本纯的比卡鲁胺合成中中间体的拆分 |
| UA74826C2 (en) * | 2000-05-17 | 2006-02-15 | Ortho Mcneil Pharm Inc | ?-carboline derivatives as phosphodiesterase inhibitors |
| BR0111298A (pt) | 2000-06-28 | 2005-05-10 | Bristol Myers Squibb Co | Moduladores seletivos dos receptores de andrógenos e métodos para identificação, projeto e uso dos mesmos |
| GB0016877D0 (en) * | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| US20030232792A1 (en) | 2000-08-24 | 2003-12-18 | Dalton James T. | Selective androgen receptor modulators and methods of use thereof |
| US7547728B2 (en) | 2001-12-06 | 2009-06-16 | University Of Tennessee Research Foundation | Treating muscle wasting with selective androgen receptor modulators |
| EP1401801B1 (en) * | 2000-08-24 | 2006-11-02 | The University Of Tennessee Research Corporation | Selective androgen receptor modulators and methods of use thereof |
| US6998500B2 (en) | 2000-08-24 | 2006-02-14 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| IL154425A0 (en) | 2000-08-24 | 2003-09-17 | Univ Tennessee Res H Corp | Selective androgen receptor modulators and methods of use thereof |
| US6838484B2 (en) | 2000-08-24 | 2005-01-04 | University Of Tennessee Research Foundation | Formulations comprising selective androgen receptor modulators |
| US20070161608A1 (en) * | 2001-12-06 | 2007-07-12 | Dalton James T | Selective androgen receptor modulators for treating muscle wasting |
-
2003
- 2003-02-06 PT PT03737647T patent/PT1480634E/pt unknown
- 2003-02-06 WO PCT/US2003/003447 patent/WO2003065992A2/en not_active Ceased
- 2003-02-06 HR HR20100067A patent/HRP20100067A2/hr not_active Application Discontinuation
- 2003-02-06 JP JP2003565418A patent/JP4677516B2/ja not_active Expired - Fee Related
- 2003-02-06 DK DK03737647.2T patent/DK1480634T3/da active
- 2003-02-06 CN CN2009101619003A patent/CN101732298B/zh not_active Expired - Fee Related
- 2003-02-06 CA CA002475108A patent/CA2475108A1/en not_active Abandoned
- 2003-02-06 KR KR1020047012236A patent/KR101032661B1/ko not_active Expired - Fee Related
- 2003-02-06 EP EP03737647A patent/EP1480634B1/en not_active Expired - Lifetime
- 2003-02-06 GE GEAP8396A patent/GEP20074122B/en unknown
- 2003-02-06 KR KR1020107021280A patent/KR20100112659A/ko not_active Ceased
- 2003-02-06 CA CA2689080A patent/CA2689080C/en not_active Expired - Fee Related
- 2003-02-06 CN CN038078007A patent/CN1646115B/zh not_active Expired - Fee Related
- 2003-02-06 BR BRPI0307699-7A patent/BRPI0307699A2/pt not_active IP Right Cessation
- 2003-02-06 EA EA200401043A patent/EA013399B1/ru not_active IP Right Cessation
- 2003-02-06 HR HR20040793A patent/HRP20040793A2/xx not_active Application Discontinuation
- 2003-02-06 AT AT03737647T patent/ATE518537T1/de active
- 2003-02-06 AU AU2003216174A patent/AU2003216174C1/en not_active Ceased
- 2003-02-06 EA EA200901492A patent/EA200901492A1/ru unknown
- 2003-02-06 US US10/359,270 patent/US7776921B2/en not_active Expired - Fee Related
- 2003-02-06 MX MXPA04007639A patent/MXPA04007639A/es active IP Right Grant
- 2003-02-06 RS YU69704A patent/RS69704A/sr unknown
- 2003-02-07 TW TW097147185A patent/TW200918043A/zh unknown
- 2003-02-07 TW TW092102512A patent/TWI374737B/zh not_active IP Right Cessation
-
2004
- 2004-08-05 IL IL163380A patent/IL163380A/en not_active IP Right Cessation
-
2009
- 2009-03-18 AU AU2009201084A patent/AU2009201084A1/en not_active Abandoned
- 2009-12-10 IL IL202675A patent/IL202675A/en not_active IP Right Cessation
-
2010
- 2010-05-10 JP JP2010108498A patent/JP2010209102A/ja not_active Ceased
- 2010-06-30 US US12/826,842 patent/US8088828B2/en not_active Expired - Fee Related
-
2011
- 2011-10-31 CY CY20111101039T patent/CY1111917T1/el unknown
-
2013
- 2013-04-11 JP JP2013082815A patent/JP2013144713A/ja active Pending
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