JP2007538094A5 - - Google Patents
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- Publication number
- JP2007538094A5 JP2007538094A5 JP2007527445A JP2007527445A JP2007538094A5 JP 2007538094 A5 JP2007538094 A5 JP 2007538094A5 JP 2007527445 A JP2007527445 A JP 2007527445A JP 2007527445 A JP2007527445 A JP 2007527445A JP 2007538094 A5 JP2007538094 A5 JP 2007538094A5
- Authority
- JP
- Japan
- Prior art keywords
- metabolite
- sarm compound
- compound according
- represented
- structural formula
- 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
- 229940083324 Selective androgen receptor modulator Drugs 0.000 claims 128
- 239000000849 selective androgen receptor modulator Substances 0.000 claims 128
- 150000001875 compounds Chemical class 0.000 claims 126
- 239000002207 metabolite Substances 0.000 claims 102
- 239000000126 substance Substances 0.000 claims 49
- 239000003814 drug Substances 0.000 claims 35
- 238000004519 manufacturing process Methods 0.000 claims 28
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 20
- NRKYWOKHZRQRJR-UHFFFAOYSA-N 2,2,2-trifluoroacetamide Chemical compound NC(=O)C(F)(F)F NRKYWOKHZRQRJR-UHFFFAOYSA-N 0.000 claims 10
- 206010060862 Prostate cancer Diseases 0.000 claims 10
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 8
- 239000003098 androgen Substances 0.000 claims 6
- 230000001419 dependent effect Effects 0.000 claims 6
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 4
- 206010013774 Dry eye Diseases 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 229910052740 iodine Inorganic materials 0.000 claims 3
- 230000021595 spermatogenesis Effects 0.000 claims 3
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 2
- 229940124011 Androgen receptor agonist Drugs 0.000 claims 2
- 229940123407 Androgen receptor antagonist Drugs 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 239000003936 androgen receptor antagonist Substances 0.000 claims 2
- 102000001307 androgen receptors Human genes 0.000 claims 2
- 108010080146 androgen receptors Proteins 0.000 claims 2
- 230000006907 apoptotic process Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000001934 delay Effects 0.000 claims 2
- 125000004982 dihaloalkyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 230000003054 hormonal effect Effects 0.000 claims 2
- 238000002657 hormone replacement therapy Methods 0.000 claims 2
- 238000001794 hormone therapy Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004385 trihaloalkyl group Chemical group 0.000 claims 2
- WSNMPAVSZJSIMT-UHFFFAOYSA-N COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 Chemical compound COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 WSNMPAVSZJSIMT-UHFFFAOYSA-N 0.000 claims 1
- -1 alkyl aldehyde Chemical class 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 0 CCN(*)CC(NC([C@@](*)(C*C1=CC=CC(C)(*)C=C1)N)=*)=C/C=S/* Chemical compound CCN(*)CC(NC([C@@](*)(C*C1=CC=CC(C)(*)C=C1)N)=*)=C/C=S/* 0.000 description 3
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/849,039 US20040260108A1 (en) | 2001-06-25 | 2004-05-20 | Metabolites of selective androgen receptor modulators and methods of use thereof |
| PCT/US2005/017588 WO2005113565A2 (en) | 2004-05-20 | 2005-03-19 | Metabolites of selective androgen receptor modulators and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007538094A JP2007538094A (ja) | 2007-12-27 |
| JP2007538094A5 true JP2007538094A5 (https=) | 2008-03-27 |
Family
ID=35428908
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007527445A Pending JP2007538094A (ja) | 2004-05-20 | 2005-03-19 | 選択的アンドロゲン受容体調節剤化合物の代謝物及びその使用方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20040260108A1 (https=) |
| EP (1) | EP1750694A4 (https=) |
| JP (1) | JP2007538094A (https=) |
| CN (1) | CN1972682A (https=) |
| AU (1) | AU2005245941A1 (https=) |
| BR (1) | BRPI0510822A (https=) |
| CA (1) | CA2563908A1 (https=) |
| EA (1) | EA200602151A1 (https=) |
| GE (1) | GEP20094850B (https=) |
| IL (1) | IL178717A0 (https=) |
| MX (1) | MXPA06013296A (https=) |
| TW (1) | TW200613252A (https=) |
| WO (1) | WO2005113565A2 (https=) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US20070161608A1 (en) * | 2001-12-06 | 2007-07-12 | Dalton James T | Selective androgen receptor modulators for treating muscle wasting |
| 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 |
| WO2007001448A2 (en) | 2004-11-04 | 2007-01-04 | Massachusetts Institute Of Technology | Coated controlled release polymer particles as efficient oral delivery vehicles for biopharmaceuticals |
| WO2007070682A2 (en) | 2005-12-15 | 2007-06-21 | Massachusetts Institute Of Technology | System for screening particles |
| CA2648099C (en) | 2006-03-31 | 2012-05-29 | The Brigham And Women's Hospital, Inc | System for targeted delivery of therapeutic agents |
| CA2649788A1 (en) * | 2006-04-20 | 2007-11-01 | Technion Research And Development Foundation Ltd. | Casein micelles for nanoencapsulation of hydrophobic compounds |
| 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 |
| EP2134830A2 (en) | 2007-02-09 | 2009-12-23 | Massachusetts Institute of Technology | Oscillating cell culture bioreactor |
| WO2008124634A1 (en) | 2007-04-04 | 2008-10-16 | Massachusetts Institute Of Technology | Polymer-encapsulated reverse micelles |
| JP2010523595A (ja) | 2007-04-04 | 2010-07-15 | 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 | ポリ（アミノ酸）ターゲッティング部分 |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| EP2436376B1 (en) | 2007-09-28 | 2014-07-09 | BIND Therapeutics, Inc. | Cancer cell targeting using nanoparticles |
| JP2011500569A (ja) | 2007-10-12 | 2011-01-06 | 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 | ワクチンナノテクノロジー |
| US8003689B2 (en) | 2008-06-20 | 2011-08-23 | Gtx, Inc. | Metabolites of selective androgen receptor modulators and methods of use thereof |
| US8277812B2 (en) | 2008-10-12 | 2012-10-02 | Massachusetts Institute Of Technology | Immunonanotherapeutics that provide IgG humoral response without T-cell antigen |
| 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 |
| US8343498B2 (en) | 2008-10-12 | 2013-01-01 | Massachusetts Institute Of Technology | Adjuvant incorporation in 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 |
| 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) |
| 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) |
| LT2872482T (lt) | 2012-07-13 | 2020-12-28 | Oncternal Therapeutics, Inc. | Krūties vėžių gydymo būdas selektyviu androgeno receptoriaus moduliatoriumi |
| 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) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive 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) |
| 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 |
| KR20230084476A (ko) | 2020-10-08 | 2023-06-13 | 타르그이뮨 테라퓨틱스 아게 | 암의 치료를 위한 면역요법 |
| WO2023079142A2 (en) | 2021-11-05 | 2023-05-11 | Targimmune Therapeutics Ag | Targeted linear conjugates comprising polyethyleneimine and polyethylene glycol and polyplexes comprising the same |
| US20260000700A1 (en) | 2022-11-07 | 2026-01-01 | Targimmune Therapeutics Ag | Targeted linear conjugates comprising polyethyleneimine and polyethylene glycol and polyplexes comprising the same |
| IL320615A (en) | 2022-11-07 | 2025-07-01 | Targimmune Therapeutics Ag | PSMA-targeting linear conjugates containing polyethyleneimine and polyethylene glycol and polyplexes containing the same materials |
| IL320618A (en) | 2022-11-07 | 2025-07-01 | Targimmune Therapeutics Ag | Polyplexes of nucleic acids and targeted pairs containing polyethyleneimine and polyethylene glycol |
| WO2025238236A1 (en) | 2024-05-16 | 2025-11-20 | Targimmune Therapeutics Ag | Polyplexes of nucleic acids and targeted conjugates comprising polyethyleneimine and polyethylene glycol |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3875229A (en) * | 1972-11-24 | 1975-04-01 | Schering Corp | Substituted carboxanilides |
| 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 |
| ATE28864T1 (de) * | 1982-07-23 | 1987-08-15 | Ici Plc | Amide-derivate. |
| 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 |
| 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 |
| 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 |
| 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 |
| DE60137728D1 (de) * | 2000-08-24 | 2009-04-02 | Univ Tennessee Res Foundation | Selektive Modulatoren des Androgenrezeptors und Methoden zu deren Verwendung |
| US6838484B2 (en) * | 2000-08-24 | 2005-01-04 | University Of Tennessee Research Foundation | Formulations comprising selective androgen receptor modulators |
| IL154425A0 (en) * | 2000-08-24 | 2003-09-17 | Univ Tennessee Res H Corp | 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 |
| US6998500B2 (en) * | 2000-08-24 | 2006-02-14 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| US7214690B2 (en) * | 2001-02-23 | 2007-05-08 | Ligand Pharmaceuticals Incorporated | Tricyclic quinolinone and tricyclic quinoline androgen receptor modulator compounds and methods |
| WO2003033478A1 (en) * | 2001-10-12 | 2003-04-24 | Warner-Lambert Company Llc | Alkynylated fused ring pyrimidine compounds as matrix metalloprotease-13 inhibitors |
| DK1463497T3 (da) * | 2001-12-06 | 2012-01-30 | Gtx Inc | Behandling af muskelsvind med selektive androgenreceptormodulatorer |
| CA2475108A1 (en) * | 2002-02-07 | 2003-08-14 | Mitchell S. Steiner | Treating benign prostate hyperplasia with sarms |
| KR20040104463A (ko) * | 2002-02-28 | 2004-12-10 | 유니버시티 오브 테네시 리서치 파운데이션 | 비가역적 선택적 안드로겐 수용체 모듈레이터 및 이를사용하는 방법 |
| AU2003216153B2 (en) * | 2002-02-28 | 2008-01-24 | The University Of Tennessee Research Foundation | Multi-substitued selective androgen receptor modulators and methods of use thereof |
| EP1562906A4 (en) * | 2002-10-15 | 2009-12-02 | Univ Tennessee Res Foundation | HETEROCYCLIC SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHOD FOR THEIR USE |
| AU2004206909A1 (en) * | 2003-01-22 | 2004-08-05 | Gtx Inc. | Treating androgen deficiency in female (ADIF)-associated conditions with sarms |
| WO2005060647A2 (en) * | 2003-12-16 | 2005-07-07 | Gtx, Inc. | Prodrugs of selective androgen receptor modulators and methods of use thereof |
-
2004
- 2004-05-20 US US10/849,039 patent/US20040260108A1/en not_active Abandoned
-
2005
- 2005-03-19 EP EP05779984A patent/EP1750694A4/en not_active Withdrawn
- 2005-03-19 MX MXPA06013296A patent/MXPA06013296A/es not_active Application Discontinuation
- 2005-03-19 EA EA200602151A patent/EA200602151A1/ru unknown
- 2005-03-19 BR BRPI0510822-5A patent/BRPI0510822A/pt not_active IP Right Cessation
- 2005-03-19 GE GEAP20059769A patent/GEP20094850B/en unknown
- 2005-03-19 CN CNA2005800209124A patent/CN1972682A/zh active Pending
- 2005-03-19 WO PCT/US2005/017588 patent/WO2005113565A2/en not_active Ceased
- 2005-03-19 AU AU2005245941A patent/AU2005245941A1/en not_active Abandoned
- 2005-03-19 CA CA002563908A patent/CA2563908A1/en not_active Abandoned
- 2005-03-19 JP JP2007527445A patent/JP2007538094A/ja active Pending
- 2005-05-20 TW TW094116570A patent/TW200613252A/zh unknown
-
2006
- 2006-10-18 IL IL178717A patent/IL178717A0/en unknown