JP2006518328A5 - - Google Patents
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- Publication number
- JP2006518328A5 JP2006518328A5 JP2004544889A JP2004544889A JP2006518328A5 JP 2006518328 A5 JP2006518328 A5 JP 2006518328A5 JP 2004544889 A JP2004544889 A JP 2004544889A JP 2004544889 A JP2004544889 A JP 2004544889A JP 2006518328 A5 JP2006518328 A5 JP 2006518328A5
- Authority
- JP
- Japan
- Prior art keywords
- androgen receptor
- receptor modulator
- modulator compound
- selective androgen
- pharmaceutically acceptable
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 111
- 229940083324 Selective androgen receptor modulator Drugs 0.000 claims 109
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 109
- 239000003814 drug Substances 0.000 claims 78
- 239000013078 crystal Substances 0.000 claims 51
- 229940002612 prodrug Drugs 0.000 claims 51
- 239000000651 prodrug Substances 0.000 claims 51
- 150000003839 salts Chemical class 0.000 claims 51
- 239000002207 metabolite Substances 0.000 claims 49
- 150000001204 N-oxides Chemical class 0.000 claims 44
- 150000004677 hydrates Chemical class 0.000 claims 42
- 206010060862 Prostate cancer Diseases 0.000 claims 30
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 30
- 238000004519 manufacturing process Methods 0.000 claims 27
- 239000000126 substance Substances 0.000 claims 22
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 101100149678 Caenorhabditis elegans snr-3 gene Proteins 0.000 claims 12
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 12
- 206010013774 Dry eye Diseases 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 12
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 102000001307 androgen receptors Human genes 0.000 claims 11
- 108010080146 androgen receptors Proteins 0.000 claims 11
- 229910052717 sulfur Inorganic materials 0.000 claims 11
- 239000003098 androgen Substances 0.000 claims 9
- 230000021595 spermatogenesis Effects 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 230000006907 apoptotic process Effects 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000004982 dihaloalkyl group Chemical group 0.000 claims 6
- 239000003085 diluting agent Substances 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- -1 polymorph Substances 0.000 claims 6
- 125000004385 trihaloalkyl group Chemical group 0.000 claims 6
- 230000001419 dependent effect Effects 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 239000005556 hormone Substances 0.000 claims 3
- 229940088597 hormone Drugs 0.000 claims 3
- 238000002657 hormone replacement therapy Methods 0.000 claims 3
- 238000001794 hormone therapy Methods 0.000 claims 3
- 239000002583 male contraceptive agent Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 230000004060 metabolic process Effects 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 0 C**1C=N*C=CC(OC[C@@](C)([C@](Nc(cc2C(F)(F)F)ccc2C#N)O)O)=C1 Chemical compound C**1C=N*C=CC(OC[C@@](C)([C@](Nc(cc2C(F)(F)F)ccc2C#N)O)O)=C1 0.000 description 6
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41817302P | 2002-10-15 | 2002-10-15 | |
| PCT/US2003/032510 WO2004035737A2 (en) | 2002-10-15 | 2003-10-14 | Heterocyclic selective androgen receptor modulators and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006518328A JP2006518328A (ja) | 2006-08-10 |
| JP2006518328A5 true JP2006518328A5 (https=) | 2006-09-21 |
Family
ID=32107899
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004544889A Pending JP2006518328A (ja) | 2002-10-15 | 2003-10-14 | 複素環選択的アンドロゲン受容体調節剤及びその使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7214693B2 (https=) |
| EP (1) | EP1562906A4 (https=) |
| JP (1) | JP2006518328A (https=) |
| CN (1) | CN1726193A (https=) |
| AU (2) | AU2003287076C1 (https=) |
| CA (1) | CA2501867A1 (https=) |
| TW (1) | TW200502249A (https=) |
| WO (1) | WO2004035737A2 (https=) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040260108A1 (en) * | 2001-06-25 | 2004-12-23 | Dalton James T. | Metabolites of selective androgen receptor modulators and methods of use thereof |
| US20070161608A1 (en) * | 2001-12-06 | 2007-07-12 | Dalton James T | Selective androgen receptor modulators for treating muscle wasting |
| US8853266B2 (en) * | 2001-12-06 | 2014-10-07 | University Of Tennessee Research Foundation | 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 |
| US20110237664A1 (en) * | 2004-06-07 | 2011-09-29 | Dalton James T | Selective androgen receptor modulators for treating diabetes |
| 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 |
| US8288366B2 (en) | 2006-06-20 | 2012-10-16 | Chochinov Ronald H | Formulation for hair growth |
| US9623021B2 (en) * | 2007-01-22 | 2017-04-18 | Gtx, Inc. | Nuclear receptor binding agents |
| ES2475193T3 (es) * | 2007-01-22 | 2014-07-10 | Gtx, Inc. | Agentes de unión al receptor nuclear |
| US9604931B2 (en) | 2007-01-22 | 2017-03-28 | Gtx, Inc. | Nuclear receptor binding agents |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| KR101595238B1 (ko) | 2007-12-21 | 2016-02-18 | 리간드 파마슈티칼스 인코포레이티드 | 선택적 안드로겐 수용체 조절제(ｓａｒｍ) 및 이의 용도 |
| CN103002737A (zh) * | 2010-01-11 | 2013-03-27 | Gtx公司 | 治疗睑板腺功能障碍的方法 |
| US8395552B2 (en) | 2010-11-23 | 2013-03-12 | Metamagnetics, Inc. | Antenna module having reduced size, high gain, and increased power efficiency |
| FR2982261B1 (fr) * | 2011-11-04 | 2014-06-13 | Galderma Res & Dev | Nouveaux amides, et leur utilisation pharmaceutique ou cosmetique |
| 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) |
| 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) |
| 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) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| GB201321601D0 (en) * | 2013-12-06 | 2014-01-22 | Canbex Therapeutics Ltd | Modulator |
| EP3094323A4 (en) | 2014-01-17 | 2017-10-11 | Ligand Pharmaceuticals Incorporated | Methods and compositions for modulating hormone levels |
| CN103772238B (zh) * | 2014-01-24 | 2017-03-22 | 苏州伊莱特新药研发有限公司 | 一类新的含酯基芳香丙酰胺化合物及其制备方法和用途 |
| US10093613B2 (en) | 2015-04-21 | 2018-10-09 | Gtx, Inc. | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10654809B2 (en) | 2016-06-10 | 2020-05-19 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10806720B2 (en) | 2015-04-21 | 2020-10-20 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10441570B2 (en) | 2015-04-21 | 2019-10-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) Ligands and methods of use thereof |
| US10865184B2 (en) | 2015-04-21 | 2020-12-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| US10806719B2 (en) | 2016-06-10 | 2020-10-20 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| EP3468552A4 (en) * | 2016-06-10 | 2020-07-08 | University of Tennessee Research Foundation | SARD LIGANDS - SELECTIVE ANDROGEN RECEPTOR DEGRADATION COMPOUNDS - AND METHODS OF USE |
| US11230523B2 (en) | 2016-06-10 | 2022-01-25 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| WO2020051344A1 (en) | 2018-09-05 | 2020-03-12 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (sard) ligands and methods of use thereof |
| AU2020257397B2 (en) | 2019-04-19 | 2026-02-26 | Ligand Pharmaceuticals Inc. | Crystalline forms and methods of producing crystalline forms of a compound |
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US6174905B1 (en) | 1996-09-30 | 2001-01-16 | Mitsui Chemicals, Inc. | Cell differentiation inducer |
| DE19723722A1 (de) * | 1997-05-30 | 1998-12-10 | Schering Ag | Nichtsteroidale Gestagene |
| 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 |
| EP1401801B1 (en) * | 2000-08-24 | 2006-11-02 | The University Of Tennessee Research Corporation | 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 |
-
2003
- 2003-10-14 JP JP2004544889A patent/JP2006518328A/ja active Pending
- 2003-10-14 WO PCT/US2003/032510 patent/WO2004035737A2/en not_active Ceased
- 2003-10-14 CA CA002501867A patent/CA2501867A1/en not_active Abandoned
- 2003-10-14 CN CNA2003801061407A patent/CN1726193A/zh active Pending
- 2003-10-14 US US10/683,125 patent/US7214693B2/en not_active Expired - Fee Related
- 2003-10-14 AU AU2003287076A patent/AU2003287076C1/en not_active Ceased
- 2003-10-14 EP EP03777597A patent/EP1562906A4/en not_active Withdrawn
- 2003-10-15 TW TW092128552A patent/TW200502249A/zh unknown
-
2007
- 2007-03-22 US US11/723,957 patent/US20070265290A1/en not_active Abandoned
-
2009
- 2009-07-02 AU AU2009202683A patent/AU2009202683A1/en not_active Abandoned