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WO2003057669A1 - Antagonistes du recepteur androgene - Google Patents

Antagonistes du recepteur androgene Download PDF

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Publication number
WO2003057669A1
WO2003057669A1 PCT/JP2002/013652 JP0213652W WO03057669A1 WO 2003057669 A1 WO2003057669 A1 WO 2003057669A1 JP 0213652 W JP0213652 W JP 0213652W WO 03057669 A1 WO03057669 A1 WO 03057669A1
Authority
WO
WIPO (PCT)
Prior art keywords
hydrogen
nitrogen
oxygen
group
carbon
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.)
Ceased
Application number
PCT/JP2002/013652
Other languages
English (en)
French (fr)
Inventor
Shuichi Furuya
Nobuyuki Matsunaga
Masami Kusaka
Takahito Hara
Junichi Miyazaki
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Takeda Pharmaceutical Co Ltd
Original Assignee
Takeda Chemical Industries Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Takeda Chemical Industries Ltd filed Critical Takeda Chemical Industries Ltd
Priority to EP02790889A priority Critical patent/EP1466902A4/en
Priority to US10/499,300 priority patent/US20050101657A1/en
Priority to CA002471754A priority patent/CA2471754A1/en
Priority to AU2002367424A priority patent/AU2002367424A1/en
Publication of WO2003057669A1 publication Critical patent/WO2003057669A1/ja
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/333Radicals substituted by oxygen or sulfur atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D207/46Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
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    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
PCT/JP2002/013652 2001-12-28 2002-12-26 Antagonistes du recepteur androgene Ceased WO2003057669A1 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP02790889A EP1466902A4 (en) 2001-12-28 2002-12-26 ANTAGONISTS OF THE ANDROGEN RECEPTOR
US10/499,300 US20050101657A1 (en) 2001-12-28 2002-12-26 Androgen receptor antagonists
CA002471754A CA2471754A1 (en) 2001-12-28 2002-12-26 Androgen receptor antagonist
AU2002367424A AU2002367424A1 (en) 2001-12-28 2002-12-26 Androgen receptor antagonists

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2001-399143 2001-12-28
JP2001399143 2001-12-28

Publications (1)

Publication Number Publication Date
WO2003057669A1 true WO2003057669A1 (fr) 2003-07-17

Family

ID=19189431

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2002/013652 Ceased WO2003057669A1 (fr) 2001-12-28 2002-12-26 Antagonistes du recepteur androgene

Country Status (5)

Country Link
US (1) US20050101657A1 (ja)
EP (1) EP1466902A4 (ja)
AU (1) AU2002367424A1 (ja)
CA (1) CA2471754A1 (ja)
WO (1) WO2003057669A1 (ja)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7323490B2 (en) 2003-05-16 2008-01-29 Ambit Biosciences Corporation Pyrrole compounds and uses thereof
WO2008153091A1 (ja) 2007-06-13 2008-12-18 Takeda Pharmaceutical Company Limited スクリーニング方法
WO2009028543A1 (ja) * 2007-08-30 2009-03-05 Takeda Pharmaceutical Company Limited 置換ピラゾール誘導体
WO2011051540A1 (en) 2009-10-27 2011-05-05 Orion Corporation Androgen receptor modulating compounds
WO2012143599A1 (en) 2011-04-21 2012-10-26 Orion Corporation Androgen receptor modulating carboxamides
JP2015526488A (ja) * 2012-08-29 2015-09-10 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング フルオロメチル置換ピロールカルボキサミド類
US9944597B2 (en) 2013-09-16 2018-04-17 The Board Of Regents Of The University Of Texas System Polysubstituted pyrroles having microtubule-disrupting, cytotoxic and antitumor activities and methods of use thereof
US20180265491A1 (en) * 2014-07-03 2018-09-20 Celgene Quanticel Research, Inc. Inhibitors of lysine specific demethylase-1

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US8026263B2 (en) 2000-01-06 2011-09-27 The Regents Of The University Of California Methods for inhibiting neoproliferative changes in blood vessel walls
JP4447826B2 (ja) * 2002-06-03 2010-04-07 武田薬品工業株式会社 変異アンドロゲン受容体、それを発現する癌細胞、それらの作出方法およびそれらの用途
CA2495383A1 (en) 2002-08-12 2004-02-26 Takeda Pharmaceutical Company Limited Fused benzene derivative and use
US7795280B2 (en) 2002-11-07 2010-09-14 N.V. Organon Indoles useful in the treatment of androgen-receptor related diseases
TW200602317A (en) * 2004-04-23 2006-01-16 Akzo Nobel Nv Novel androgens
ES2402362T3 (es) 2004-09-30 2013-05-03 Takeda Pharmaceutical Company Limited Inhibidores de la bomba de protones
TW200628446A (en) * 2004-12-14 2006-08-16 Takeda Pharmaceuticals Co Substituted pyrrole derivative
GB0427381D0 (en) * 2004-12-14 2005-01-19 Novartis Ag Organic compounds
JP5070054B2 (ja) * 2005-08-01 2012-11-07 武田薬品工業株式会社 環状アミン化合物
HRP20110473T1 (hr) 2005-08-30 2011-07-31 Takeda Pharmaceutical Company Limited Supstituirani derivati 1-heterociklilsulfonil, 2-aminometil, 5-(hetero)-aril 1-h-pirola kao inhibitori kiselinske sekrecije
KR20080080373A (ko) * 2005-12-19 2008-09-03 신젠타 리미티드 살진균제로서 치환된 방향족 헤테로사이클 화합물
CA2642619A1 (en) 2006-02-20 2007-08-30 Astellas Pharma Inc. Pyrrole derivative or salt thereof
WO2007145349A2 (en) * 2006-06-13 2007-12-21 Takeda Pharmaceutical Company Limited Substituted pyrrole derivatives
US8933105B2 (en) 2007-02-28 2015-01-13 Takeda Pharmaceutical Company Limited Pyrrole compounds
CA2688136A1 (en) * 2007-06-08 2008-12-11 Advinus Therapeutics Private Limited Pyrrole-2-carboxamide derivatives as glucokinase activators, their process and pharmaceutical application
AU2008284662B2 (en) * 2007-08-07 2013-07-25 Takeda Pharmaceutical Company Limited Pyrrolidin-2 -one derivatives as androgen receptor modulator
PE20091653A1 (es) * 2008-03-26 2009-11-14 Takeda Pharmaceutical Derivados sustituidos de pirazol y su uso
PE20141174A1 (es) 2008-08-27 2014-09-19 Takeda Pharmaceutical Compuestos de pirrol como inhibidores de la bomba de protones
CA2800936A1 (en) * 2010-07-02 2012-01-05 Ventana Medical Systems, Inc. Hapten conjugates for target detection
JP2013542918A (ja) * 2010-09-13 2013-11-28 ビーエーエスエフ ソシエタス・ヨーロピア 無脊椎有害生物を防除するためのピリジン化合物i
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
US10806720B2 (en) 2015-04-21 2020-10-20 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
US10441570B2 (en) 2015-04-21 2019-10-15 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
US10806719B2 (en) 2016-06-10 2020-10-20 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
MX393924B (es) 2016-06-10 2025-03-24 Univ Tennessee Res Found Ligandos degradadores selectivos del receptor de andrógenos (sard) y métodos de uso de los mismos.
US12202815B2 (en) 2018-09-05 2025-01-21 University Of Tennessee Research Foundation Selective androgen receptor degrader (SARD) ligands and methods of use thereof
WO2020051260A1 (en) * 2018-09-05 2020-03-12 University Of Tennessee Research Foundation Selective androgen receptor degrader (sard) ligands and methods of use thereof
IL302137A (en) 2020-10-21 2023-06-01 Arvinas Operations Inc Compounds and methods for targeted degradation of androgen receptor protein
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CA2471754A1 (en) 2003-07-17
EP1466902A4 (en) 2005-11-09
EP1466902A1 (en) 2004-10-13
AU2002367424A1 (en) 2003-07-24
US20050101657A1 (en) 2005-05-12

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