TW200503711A - Methylene-bridged selective androgen receptor modulators and methods of use thereof - Google Patents
Methylene-bridged selective androgen receptor modulators and methods of use thereofInfo
- Publication number
- TW200503711A TW200503711A TW092128551A TW92128551A TW200503711A TW 200503711 A TW200503711 A TW 200503711A TW 092128551 A TW092128551 A TW 092128551A TW 92128551 A TW92128551 A TW 92128551A TW 200503711 A TW200503711 A TW 200503711A
- Authority
- TW
- Taiwan
- Prior art keywords
- androgen receptor
- cancer
- androgen
- osteoporosis
- treatment
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/16—Masculine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
- C07C235/38—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
- C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Child & Adolescent Psychology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41816602P | 2002-10-15 | 2002-10-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW200503711A true TW200503711A (en) | 2005-02-01 |
Family
ID=32107896
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW092128551A TW200503711A (en) | 2002-10-15 | 2003-10-15 | Methylene-bridged selective androgen receptor modulators and methods of use thereof |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7253210B2 (https=) |
| EP (1) | EP1562594A4 (https=) |
| JP (1) | JP2006506369A (https=) |
| CN (1) | CN1726034A (https=) |
| AU (1) | AU2003287077B2 (https=) |
| CA (1) | CA2502209A1 (https=) |
| TW (1) | TW200503711A (https=) |
| WO (1) | WO2004035738A2 (https=) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7855229B2 (en) | 2000-08-24 | 2010-12-21 | University Of Tennessee Research Foundation | Treating wasting disorders with selective androgen receptor modulators |
| 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 |
| US7919647B2 (en) | 2000-08-24 | 2011-04-05 | University Of Tennessee Research Foundation | 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 |
| AU2006200749A1 (en) * | 2000-08-24 | 2006-03-16 | University Of Tennessee Research Foundation | Halogenated 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 |
| AU2003287075A1 (en) * | 2002-10-15 | 2004-05-04 | Gtx, Inc. | Treating obesity with selective androgen receptor modulators |
| JP2006516286A (ja) * | 2003-01-22 | 2006-06-29 | ジーティーエックス・インコーポレイテッド | Sarmによる女性のアンドロゲン減少に関連する病気の治療 |
| 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 |
| ES2776100T3 (es) | 2006-03-31 | 2020-07-29 | Massachusetts Inst Technology | Sistema para el suministro dirigido de agentes terapéuticos |
| US8367113B2 (en) | 2006-05-15 | 2013-02-05 | Massachusetts Institute Of Technology | Polymers for functional particles |
| 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 |
| WO2008012845A1 (en) * | 2006-07-26 | 2008-01-31 | Stmicroelectronics S.R.L. | 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 |
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| WO2008124632A1 (en) | 2007-04-04 | 2008-10-16 | Massachusetts Institute Of Technology | Amphiphilic compound assisted nanoparticles for targeted delivery |
| HRP20180500T1 (hr) * | 2007-09-11 | 2018-06-01 | Gtx, Inc. | Kristalni polimorf selektivnih modulatora androgena (r) ili (s)-n-(4-cijano-3-(trifluorometil)fenil)-3-(4-cijanofenoksi)-2-hidroksi-2-metilpropanamida |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| EP2630966B1 (en) | 2007-10-12 | 2017-04-19 | Massachusetts Institute of Technology | Vaccine nanotechnology |
| PL2500062T3 (pl) * | 2007-11-13 | 2015-12-31 | Curadis Gmbh | Steroidy C-19 do określonych zastosowań terapeutycznych |
| KR101595238B1 (ko) | 2007-12-21 | 2016-02-18 | 리간드 파마슈티칼스 인코포레이티드 | 선택적 안드로겐 수용체 조절제(sarm) 및 이의 용도 |
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| 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) |
| 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) |
| 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) |
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| US10441570B2 (en) | 2015-04-21 | 2019-10-15 | 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 |
| MX2017013563A (es) * | 2015-04-21 | 2018-07-06 | Gtx Inc | LIGANDOS DEGRADADORES SELECTIVOS DEL RECEPTOR ANDROGíNICO (SARD) Y SUS MíTODOS DE USO. |
| US10865184B2 (en) | 2015-04-21 | 2020-12-15 | 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 |
| 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 |
| 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 |
| 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 |
| KR20220146532A (ko) * | 2020-02-25 | 2022-11-01 | 유니버시티 오브 테네시 리서치 파운데이션 | 선택적 안드로겐 수용체 공유 길항제(SARCAs) 및 이의 사용 방법 |
| JP2023544201A (ja) | 2020-10-08 | 2023-10-20 | ターグイミューン セラピューティクス アクチエンゲゼルシャフト | がんを処置するための免疫療法 |
| CA3237153A1 (en) | 2021-11-05 | 2023-05-11 | Targimmune Therapeutics Ag | Targeted linear conjugates comprising polyethyleneimine and polyethylene glycol and polyplexes comprising the same |
| KR20250105420A (ko) | 2022-11-07 | 2025-07-08 | 타르그이뮨 테라퓨틱스 아게 | 핵산 및 폴리에틸렌이민 및 폴리에틸렌 글리콜을 포함하는 표적화된 컨쥬게이트의 다중복합체 |
| EP4615511A1 (en) | 2022-11-07 | 2025-09-17 | 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 |
| 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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| 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. |
| CA2476657A1 (en) * | 2002-02-28 | 2003-09-12 | The University Of Tennessee Research Corporation | Haloacetamide and azide substituted compounds and methods of use thereof |
| US7344700B2 (en) * | 2002-02-28 | 2008-03-18 | University Of Tennessee Research Corporation | Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy |
| GEP20074191B (en) * | 2002-06-17 | 2007-09-10 | Univ Tennessee Res Foundation | N-bridged selective androgen receptor modulators and methods of use thereof |
| EP2457892A1 (en) * | 2003-01-13 | 2012-05-30 | University of Tennessee Research Foundation | Large-scale synthesis of selective androgen receptor modulators |
| DE602004017609D1 (de) * | 2003-06-20 | 2008-12-18 | Ucb Pharma Sa | Verfahren zur herstellung von 3-aminothienopyridon-derivaten |
| FI20030958A0 (fi) | 2003-06-27 | 2003-06-27 | Orion Corp | Uusia yhdisteitä |
| US20050137172A1 (en) * | 2003-10-15 | 2005-06-23 | Dalton James T. | Haloacetamide and azide substituted compounds and methods of use thereof |
| JP2009506119A (ja) * | 2005-08-31 | 2009-02-12 | 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モジュレーターを用いる腎疾患、熱傷、創傷および脊髄損傷の処置 |
-
2003
- 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 CN CNA2003801061426A patent/CN1726034A/zh active Pending
- 2003-10-14 CA CA002502209A patent/CA2502209A1/en not_active Abandoned
- 2003-10-14 AU AU2003287077A patent/AU2003287077B2/en not_active Ceased
- 2003-10-14 JP JP2004544890A patent/JP2006506369A/ja active Pending
- 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
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003287077A1 (en) | 2004-05-04 |
| US20080319009A1 (en) | 2008-12-25 |
| WO2004035738A3 (en) | 2004-07-15 |
| CA2502209A1 (en) | 2004-04-29 |
| US7253210B2 (en) | 2007-08-07 |
| EP1562594A2 (en) | 2005-08-17 |
| EP1562594A4 (en) | 2008-12-17 |
| US20040147550A1 (en) | 2004-07-29 |
| WO2004035738A2 (en) | 2004-04-29 |
| JP2006506369A (ja) | 2006-02-23 |
| CN1726034A (zh) | 2006-01-25 |
| AU2003287077B2 (en) | 2007-09-20 |
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