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 (enExample) | 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 (enExample) |
| EP (1) | EP1480634B1 (enExample) |
| JP (3) | JP4677516B2 (enExample) |
| KR (2) | KR101032661B1 (enExample) |
| CN (2) | CN101732298B (enExample) |
| AT (1) | ATE518537T1 (enExample) |
| AU (2) | AU2003216174C1 (enExample) |
| BR (1) | BRPI0307699A2 (enExample) |
| CA (2) | CA2689080C (enExample) |
| CY (1) | CY1111917T1 (enExample) |
| DK (1) | DK1480634T3 (enExample) |
| EA (2) | EA200901492A1 (enExample) |
| GE (1) | GEP20074122B (enExample) |
| HR (2) | HRP20040793A2 (enExample) |
| IL (2) | IL163380A (enExample) |
| MX (1) | MXPA04007639A (enExample) |
| PT (1) | PT1480634E (enExample) |
| RS (1) | RS69704A (enExample) |
| TW (2) | TW200918043A (enExample) |
| WO (1) | WO2003065992A2 (enExample) |
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 |
| US7645898B2 (en) | 2000-08-24 | 2010-01-12 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and method of use thereof |
| US7622503B2 (en) | 2000-08-24 | 2009-11-24 | 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 |
| 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 |
| 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 |
| 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 |
| EP1673376A4 (en) * | 2003-10-14 | 2010-06-23 | Gtx Inc | TREATMENT OF BONE DISEASES WITH SELECTIVE ANDROGEN RECEPTOR MODULATORS |
| EA009902B1 (ru) | 2004-02-13 | 2008-04-28 | УОРНЕР-ЛАМБЕРТ КОМПАНИ Эл-Эл-Си | Модуляторы рецепторов андрогенов |
| WO2005100305A1 (en) * | 2004-04-13 | 2005-10-27 | Warner-Lambert Company Llc | Androgen modulators |
| WO2005102990A1 (en) | 2004-04-22 | 2005-11-03 | Warner-Lambert Company Llc | Androgen modulators |
| US20110237664A1 (en) * | 2004-06-07 | 2011-09-29 | Dalton James T | Selective androgen receptor modulators for treating diabetes |
| AU2005251781C1 (en) * | 2004-06-07 | 2008-02-21 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| DK1753417T3 (da) * | 2004-06-07 | 2012-07-23 | Univ Tennessee Res Foundation | Selektiv androgenreceptormodulator og medicinske anvendelser deraf |
| 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 |
| US9884038B2 (en) | 2004-06-07 | 2018-02-06 | University Of Tennessee Research Foundation | Selective androgen receptor modulator and methods of use thereof |
| WO2006006065A1 (en) | 2004-07-08 | 2006-01-19 | Warner-Lambert Company Llc | Androgen modulators |
| BRPI0513405A (pt) | 2004-07-16 | 2008-05-06 | Sunesis Pharmaceuticals Inc | tienopirimidinas úteis como inibidores de aurora quinase |
| TW200724139A (en) | 2005-05-05 | 2007-07-01 | Warner Lambert Co | Androgen modulators |
| WO2007123682A2 (en) * | 2006-04-03 | 2007-11-01 | Medexis S.A. | Detection of membrane androgen receptor (mar) agents |
| US9730908B2 (en) | 2006-08-24 | 2017-08-15 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| KR101264820B1 (ko) | 2006-08-24 | 2013-05-22 | 유니버시티 오브 테네시 리서치 파운데이션 | 치환된 아실아닐리드 및 그의 사용 방법 |
| 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 |
| JP2015509538A (ja) * | 2012-03-07 | 2015-03-30 | リガンド・ファーマシューティカルズ・インコーポレイテッド | １つに統合された恒常性システムとしてのステロイドホルモン経路およびコレステロール経路 |
| AU2013203784A1 (en) * | 2012-04-06 | 2013-10-24 | Kaushik J. Dave | Needle assisted jet injection administration of testosterone compositions |
| 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) |
| 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) |
| 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) |
| 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) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| JP6226978B2 (ja) | 2012-07-13 | 2017-11-08 | ジーティーエックス・インコーポレイテッド | 選択的アンドロゲン受容体モジュレーター（ｓａｒｍ）によりアンドロゲン受容体（ａｒ）陽性乳癌を処置する方法 |
| 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 |
| EP0748220A4 (en) | 1994-01-21 | 1997-09-10 | Sepracor Inc | METHOD 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 |
| US6492554B2 (en) | 2000-08-24 | 2002-12-10 | The University Of Tennessee Research Corporation | Selective androgen receptor modulators and methods of use thereof |
| US7205437B2 (en) * | 1996-11-27 | 2007-04-17 | University Of Tennessee Research Foundation | Selective androgen receptor modulators |
| US6995284B2 (en) | 2000-08-24 | 2006-02-07 | The University Of Tennessee Research Foundation | Synthesis of 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 |
| 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 |
| US6795776B1 (en) | 1999-10-14 | 2004-09-21 | Bristol-Myers Squibb Company | Crystallographic structure of the androgen receptor ligand binding domain |
| IL149056A0 (en) | 1999-10-19 | 2002-11-10 | Nobex Corp | Methods of asymmetrically synthesizing enantiomers of casodex, its derivatives and intermediates thereof |
| CA2389100A1 (en) | 1999-10-27 | 2001-05-17 | Nobex Corporation | Resolution of intermediates in the synthesis of substantially pure bicalutamide |
| UA74826C2 (en) * | 2000-05-17 | 2006-02-15 | Ortho Mcneil Pharm Inc | ?-carboline derivatives as phosphodiesterase inhibitors |
| AU2001288213B2 (en) | 2000-06-28 | 2005-04-14 | Bristol-Myers Squibb Company | Selective androgen receptor modulators and methods for their identification, design and use |
| 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 |
| US6998500B2 (en) | 2000-08-24 | 2006-02-14 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| ES2321933T3 (es) | 2000-08-24 | 2009-06-15 | University Of Tennessee Research Foundation | Moduladores selectivos del receptor de androgeno y metodos de uso de los mismos. |
| 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 |
| PT1463497E (pt) | 2001-12-06 | 2011-12-20 | Gtx Inc | Tratamento do desgaste muscular com moduladores selectivos do receptor de androgénios |
-
2003
- 2003-02-06 JP JP2003565418A patent/JP4677516B2/ja not_active Expired - Fee Related
- 2003-02-06 HR HR20040793A patent/HRP20040793A2/xx not_active Application Discontinuation
- 2003-02-06 PT PT03737647T patent/PT1480634E/pt unknown
- 2003-02-06 DK DK03737647.2T patent/DK1480634T3/da active
- 2003-02-06 MX MXPA04007639A patent/MXPA04007639A/es active IP Right Grant
- 2003-02-06 AU AU2003216174A patent/AU2003216174C1/en not_active Ceased
- 2003-02-06 CN CN2009101619003A patent/CN101732298B/zh not_active Expired - Fee Related
- 2003-02-06 CA CA2689080A patent/CA2689080C/en not_active Expired - Fee Related
- 2003-02-06 BR BRPI0307699-7A patent/BRPI0307699A2/pt not_active IP Right Cessation
- 2003-02-06 CA CA002475108A patent/CA2475108A1/en not_active Abandoned
- 2003-02-06 EA EA200901492A patent/EA200901492A1/ru unknown
- 2003-02-06 CN CN038078007A patent/CN1646115B/zh not_active Expired - Fee Related
- 2003-02-06 AT AT03737647T patent/ATE518537T1/de active
- 2003-02-06 US US10/359,270 patent/US7776921B2/en 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 EA EA200401043A patent/EA013399B1/ru not_active IP Right Cessation
- 2003-02-06 KR KR1020047012236A patent/KR101032661B1/ko not_active Expired - Fee Related
- 2003-02-06 RS YU69704A patent/RS69704A/sr unknown
- 2003-02-06 KR KR1020107021280A patent/KR20100112659A/ko not_active Ceased
- 2003-02-06 HR HR20100067A patent/HRP20100067A2/hr not_active Application Discontinuation
- 2003-02-06 WO PCT/US2003/003447 patent/WO2003065992A2/en not_active Ceased
- 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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