JP2006506369A5 - - Google Patents
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- Publication number
- JP2006506369A5 JP2006506369A5 JP2004544890A JP2004544890A JP2006506369A5 JP 2006506369 A5 JP2006506369 A5 JP 2006506369A5 JP 2004544890 A JP2004544890 A JP 2004544890A JP 2004544890 A JP2004544890 A JP 2004544890A JP 2006506369 A5 JP2006506369 A5 JP 2006506369A5
- 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 73
- 229940083324 Selective androgen receptor modulator Drugs 0.000 claims 72
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 72
- 239000003814 drug Substances 0.000 claims 45
- 239000013078 crystal Substances 0.000 claims 34
- 239000002207 metabolite Substances 0.000 claims 34
- 229940002612 prodrug Drugs 0.000 claims 34
- 239000000651 prodrug Substances 0.000 claims 34
- 150000003839 salts Chemical class 0.000 claims 34
- 150000001204 N-oxides Chemical class 0.000 claims 30
- 150000004677 hydrates Chemical class 0.000 claims 21
- 206010060862 Prostate cancer Diseases 0.000 claims 20
- 238000004519 manufacturing process Methods 0.000 claims 20
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 18
- 239000000126 substance Substances 0.000 claims 16
- 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 9
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 8
- 206010013774 Dry eye Diseases 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 239000003098 androgen Substances 0.000 claims 6
- 102000001307 androgen receptors Human genes 0.000 claims 6
- 108010080146 androgen receptors Proteins 0.000 claims 6
- 230000021595 spermatogenesis Effects 0.000 claims 6
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 4
- 101100149678 Caenorhabditis elegans snr-3 gene Proteins 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 230000006907 apoptotic process Effects 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 125000004982 dihaloalkyl group Chemical group 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 4
- -1 polymorph Substances 0.000 claims 4
- 125000004385 trihaloalkyl group Chemical group 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 3
- 229940124011 Androgen receptor agonist Drugs 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000005556 hormone Substances 0.000 claims 2
- 229940088597 hormone Drugs 0.000 claims 2
- 238000002657 hormone replacement therapy Methods 0.000 claims 2
- 238000001794 hormone therapy Methods 0.000 claims 2
- 239000002583 male contraceptive agent Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 1
- 0 *[C@](C*c1ccc(*)cc1)(C(Nc1cc(*)c(*)cc1)=O)O Chemical compound *[C@](C*c1ccc(*)cc1)(C(Nc1cc(*)c(*)cc1)=O)O 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41816602P | 2002-10-15 | 2002-10-15 | |
| PCT/US2003/032511 WO2004035738A2 (en) | 2002-10-15 | 2003-10-14 | Methylene-bridged selective androgen receptor modulators and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006506369A JP2006506369A (ja) | 2006-02-23 |
| JP2006506369A5 true JP2006506369A5 (enExample) | 2006-08-17 |
Family
ID=32107896
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004544890A Pending JP2006506369A (ja) | 2002-10-15 | 2003-10-14 | メチレン架橋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) | US7253210B2 (enExample) |
| EP (1) | EP1562594A4 (enExample) |
| JP (1) | JP2006506369A (enExample) |
| CN (1) | CN1726034A (enExample) |
| AU (1) | AU2003287077B2 (enExample) |
| CA (1) | CA2502209A1 (enExample) |
| TW (1) | TW200503711A (enExample) |
| WO (1) | WO2004035738A2 (enExample) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU2006200749A1 (en) * | 2000-08-24 | 2006-03-16 | 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 |
| US7855229B2 (en) | 2000-08-24 | 2010-12-21 | University Of Tennessee Research Foundation | Treating wasting disorders with 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 |
| US8853266B2 (en) | 2001-12-06 | 2014-10-07 | University Of Tennessee Research Foundation | Selective androgen receptor modulators for treating diabetes |
| WO2004034978A2 (en) * | 2002-10-15 | 2004-04-29 | Gtx, Inc. | Treating obesity with selective androgen receptor modulators |
| CA2514024A1 (en) * | 2003-01-22 | 2004-08-05 | Gtx Inc. | Treating androgen deficiency in female (adif)-associated conditions with sarms |
| US9884038B2 (en) | 2004-06-07 | 2018-02-06 | University Of Tennessee Research Foundation | Selective androgen receptor modulator and methods of use thereof |
| US9889110B2 (en) | 2004-06-07 | 2018-02-13 | University Of Tennessee Research Foundation | Selective androgen receptor modulator for treating hormone-related conditions |
| US9492400B2 (en) | 2004-11-04 | 2016-11-15 | Massachusetts Institute Of Technology | Coated controlled release polymer particles as efficient oral delivery vehicles for biopharmaceuticals |
| CN101146535A (zh) * | 2005-03-25 | 2008-03-19 | 默克公司 | 用睾酮补充剂和5α-还原酶抑制剂治疗男性病人的方法 |
| US9267937B2 (en) | 2005-12-15 | 2016-02-23 | Massachusetts Institute Of Technology | System for screening particles |
| WO2008105773A2 (en) | 2006-03-31 | 2008-09-04 | Massachusetts Institute Of Technology | System for targeted delivery of therapeutic agents |
| JP5630998B2 (ja) | 2006-05-15 | 2014-11-26 | マサチューセッツ インスティテュート オブ テクノロジー | 機能的粒子のためのポリマー |
| US8288366B2 (en) | 2006-06-20 | 2012-10-16 | Chochinov Ronald H | Formulation for hair growth |
| WO2007150030A2 (en) | 2006-06-23 | 2007-12-27 | Massachusetts Institute Of Technology | Microfluidic synthesis of organic nanoparticles |
| EP2051935B1 (en) | 2006-07-26 | 2016-09-07 | STMicroelectronics Srl | Use of nitroaniline derivatives for the production of nitric oxide |
| US9217129B2 (en) | 2007-02-09 | 2015-12-22 | Massachusetts Institute Of Technology | Oscillating cell culture bioreactor |
| WO2008124634A1 (en) | 2007-04-04 | 2008-10-16 | Massachusetts Institute Of Technology | Polymer-encapsulated reverse micelles |
| WO2008124639A2 (en) | 2007-04-04 | 2008-10-16 | Massachusetts Institute Of Technology | Poly (amino acid) targeting moieties |
| EP2205552B1 (en) * | 2007-09-11 | 2018-02-28 | GTx, Inc. | Crystalline polymorph of the selective androgen modulators (r) or (s)-n-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| ES2376175T3 (es) | 2007-09-28 | 2012-03-09 | Bind Biosciences, Inc. | Direccionamiento a células de c�?ncer usando nanopart�?culas. |
| BRPI0817664A2 (pt) | 2007-10-12 | 2015-03-24 | Massachusetts Inst Technology | Nanopartículas, método para preparar nanopartículas e método para tratar terapeuticamente ou profilaticamente um indivíduo |
| EP2060300B1 (en) * | 2007-11-13 | 2015-04-15 | Curadis GmbH | C-19 steroids for therapeutic uses |
| ES2413504T3 (es) | 2007-12-21 | 2013-07-16 | Ligand Pharmaceuticals Inc. | Moduladores selectivos del receptor de andrógeno (SARM) y usos de los mismos |
| US8277812B2 (en) | 2008-10-12 | 2012-10-02 | Massachusetts Institute Of Technology | Immunonanotherapeutics that provide IgG humoral response without T-cell antigen |
| US8343498B2 (en) | 2008-10-12 | 2013-01-01 | Massachusetts Institute Of Technology | Adjuvant incorporation in immunonanotherapeutics |
| US8343497B2 (en) | 2008-10-12 | 2013-01-01 | The Brigham And Women's Hospital, Inc. | Targeting of antigen presenting cells with immunonanotherapeutics |
| US8591905B2 (en) | 2008-10-12 | 2013-11-26 | The Brigham And Women's Hospital, Inc. | Nicotine immunonanotherapeutics |
| US8791158B2 (en) | 2010-01-11 | 2014-07-29 | Gtx, Inc. | Methods of treating meibomian gland dysfunction |
| 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 |
| 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) |
| 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) |
| 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) |
| IN2015DN01046A (enExample) | 2012-07-13 | 2015-06-26 | Gtx Inc | |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| EP3613418A1 (en) | 2014-01-17 | 2020-02-26 | Ligand Pharmaceuticals, Inc. | Methods and compositions for modulating hormone levels |
| DE102014210587A1 (de) | 2014-06-04 | 2015-12-17 | Siemens Aktiengesellschaft | Verfahren zur Herstellung eines feststoffisolierten Schalterpols und feststoffisolierter Schalterpol |
| 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 |
| RU2019115778A (ru) * | 2015-04-21 | 2019-06-24 | Джи Ти Икс, ИНК. | Селективные лиганды - разрушители андрогенных рецепторов (sard) и способы их применения |
| US10314797B2 (en) * | 2016-06-10 | 2019-06-11 | University Of Tennessee Research Foundation | 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 |
| US10093613B2 (en) | 2015-04-21 | 2018-10-09 | Gtx, Inc. | 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 |
| US11230523B2 (en) | 2016-06-10 | 2022-01-25 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| JP2021523151A (ja) | 2018-05-11 | 2021-09-02 | ホスホレックス、インコーポレイテッド | 負の表面電荷を有するマイクロ粒子及びナノ粒子 |
| US12202815B2 (en) | 2018-09-05 | 2025-01-21 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
| BR112021020864A2 (pt) | 2019-04-19 | 2021-12-14 | Ligand Pharm Inc | Formas cristalinas e métodos de produção de formas cristalinas de um composto |
| JP2023514455A (ja) * | 2020-02-25 | 2023-04-05 | ユニバーシティ オブ テネシー リサーチ ファウンデーション | 選択的アンドロゲン受容体共有結合性アンタゴニスト（ｓａｒｃａ）およびその使用方法 |
| AU2021357354A1 (en) | 2020-10-08 | 2023-04-20 | Targimmune Therapeutics Ag | Immunotherapy for the treatment of cancer |
| WO2023079142A2 (en) | 2021-11-05 | 2023-05-11 | Targimmune Therapeutics Ag | Targeted linear conjugates comprising polyethyleneimine and polyethylene glycol and polyplexes comprising the same |
| KR20250106292A (ko) | 2022-11-07 | 2025-07-09 | 타르그이뮨 테라퓨틱스 아게 | 폴리에틸렌이민 및 폴리에틸렌 글리콜을 포함하는 psma 표적화 선형 컨쥬게이트 및 이들을 포함하는 다중복합체 |
| IL320618A (en) | 2022-11-07 | 2025-07-01 | Targimmune Therapeutics Ag | Polyplexes of nucleic acids and targeted pairs containing polyethyleneimine and polyethylene glycol |
| WO2024100046A1 (en) | 2022-11-07 | 2024-05-16 | Targimmune Therapeutics Ag | Targeted linear conjugates comprising polyethyleneimine and polyethylene glycol and polyplexes comprising the same |
| WO2025238236A1 (en) | 2024-05-16 | 2025-11-20 | Targimmune Therapeutics Ag | Polyplexes of nucleic acids and targeted conjugates comprising polyethyleneimine and polyethylene glycol |
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| US616011A (en) * | 1898-12-13 | Pipe joint | ||
| US565651A (en) * | 1896-08-11 | Relief trip-lever for binding-machines | ||
| 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 |
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| JPS57171904A (en) | 1981-04-15 | 1982-10-22 | Mitsubishi Petrochem Co Ltd | Tri- or tetra-substituted phenoxycarboxylic acid anilide type herbicide |
| LU88769I2 (fr) | 1982-07-23 | 1996-11-05 | Zeneca Ltd | Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R)) |
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| 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 |
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| US7205437B2 (en) * | 1996-11-27 | 2007-04-17 | University Of Tennessee Research Foundation | Selective androgen receptor modulators |
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| 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 |
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| US8853266B2 (en) * | 2001-12-06 | 2014-10-07 | University Of Tennessee Research Foundation | Selective androgen receptor modulators for treating diabetes |
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| PT1592658E (pt) | 2003-01-13 | 2013-06-25 | Univ Tennessee Res Foundation | Síntese em larga escala de modulador selectivo de receptor de androgénio |
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-
2003
- 2003-10-14 AU AU2003287077A patent/AU2003287077B2/en not_active Ceased
- 2003-10-14 JP JP2004544890A patent/JP2006506369A/ja active Pending
- 2003-10-14 CN CNA2003801061426A patent/CN1726034A/zh active Pending
- 2003-10-14 US US10/683,157 patent/US7253210B2/en not_active Expired - Lifetime
- 2003-10-14 WO PCT/US2003/032511 patent/WO2004035738A2/en not_active Ceased
- 2003-10-14 CA CA002502209A patent/CA2502209A1/en not_active Abandoned
- 2003-10-14 EP EP03777598A patent/EP1562594A4/en not_active Withdrawn
- 2003-10-15 TW TW092128551A patent/TW200503711A/zh unknown
-
2007
- 2007-07-30 US US11/882,073 patent/US20080319009A1/en not_active Abandoned