EA201390598A1 - Антагонист мутантного андрогенного рецептора - Google Patents

Антагонист мутантного андрогенного рецептора

Info

Publication number
EA201390598A1
EA201390598A1 EA201390598A EA201390598A EA201390598A1 EA 201390598 A1 EA201390598 A1 EA 201390598A1 EA 201390598 A EA201390598 A EA 201390598A EA 201390598 A EA201390598 A EA 201390598A EA 201390598 A1 EA201390598 A1 EA 201390598A1
Authority
EA
Eurasian Patent Office
Prior art keywords
androgen receptor
present
prostate cancer
pharmaceutical composition
active ingredient
Prior art date
Application number
EA201390598A
Other languages
English (en)
Inventor
Юкитака Идеяма
Садао Куромицу
Такаси Фурутани
Масаеси Такеда
Сатоси Конагаи
Томохиро Ямада
Нобуаки Танигути
Ютака Кондох
Масааки Хирано
Казуси Ватанабе
Такаси Сугане
Акио Какефуда
Original Assignee
Астеллас Фарма Инк.
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 Астеллас Фарма Инк. filed Critical Астеллас Фарма Инк.
Publication of EA201390598A1 publication Critical patent/EA201390598A1/ru

Links

Classifications

    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Цель настоящего изобретения состоит в разработке нового противоракового средства, полезного для лечения рака предстательной железы, сопровождающего мутацию андрогенного рецептора. Заявителями проведено всестороннее исследование связанных с мутантными андрогенами заболеваний, при которых традиционные антиандрогенные лекарственные средства становятся неэффективными. В результате заявителями обнаружено, что соединение, являющееся активным ингредиентом фармацевтической композиции по настоящему изобретению, обладает ингибирующим действием против активации транскрипции в мутантном андрогенном рецепторе (AR) человека и оказывает исключительное противораковое действие на мышей с раковой опухолью предстательной железы человека, в результате чего оформлено настоящее изобретение. Таким образом, соединение, являющееся активным ингредиентом фармацевтической композиции по настоящему изобретению, полезно при ряде зависимых от андрогенного рецептора заболеваний, включая рак предстательной железы.
EA201390598A 2010-10-22 2011-10-21 Антагонист мутантного андрогенного рецептора EA201390598A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2010237242 2010-10-22
PCT/JP2011/074261 WO2012053630A1 (ja) 2010-10-22 2011-10-21 変異アンドロゲン受容体拮抗薬

Publications (1)

Publication Number Publication Date
EA201390598A1 true EA201390598A1 (ru) 2013-08-30

Family

ID=45975338

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201390598A EA201390598A1 (ru) 2010-10-22 2011-10-21 Антагонист мутантного андрогенного рецептора

Country Status (13)

Country Link
US (1) US20130197009A1 (ru)
EP (1) EP2631233A4 (ru)
JP (1) JPWO2012053630A1 (ru)
KR (1) KR20130139979A (ru)
CN (1) CN103180309A (ru)
AU (1) AU2011318875A1 (ru)
BR (1) BR112013009274A2 (ru)
CA (1) CA2813063A1 (ru)
EA (1) EA201390598A1 (ru)
IL (1) IL225395A0 (ru)
MX (1) MX2013004517A (ru)
TW (1) TW201305130A (ru)
WO (1) WO2012053630A1 (ru)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2772491A1 (en) * 2011-10-21 2014-09-03 Astellas Pharma Inc. Crystals of androgen receptor antagonist compound
US10206911B2 (en) 2012-10-26 2019-02-19 Memorial Sloan-Kettering Cancer Center Androgen receptor variants and methods for making and using
EP3696276A1 (en) * 2013-02-25 2020-08-19 Novartis AG Novel androgen receptor mutation
US9682960B2 (en) 2013-12-19 2017-06-20 Endorecherche, Inc. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety
WO2021061642A1 (en) * 2019-09-23 2021-04-01 Accutar Biotechnology Inc. Novel ureas having androgen receptor degradation activity and uses thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU754529B2 (en) * 1998-09-22 2002-11-21 Yamanouchi Pharmaceutical Co., Ltd. Cyanophenyl derivatives
JP2001328938A (ja) * 2000-03-17 2001-11-27 Yamanouchi Pharmaceut Co Ltd シアノフェニル誘導体を有効成分とする医薬
SI1557411T1 (ru) * 2002-07-12 2013-01-31 Astellas Pharma Inc
DE10322108B4 (de) 2003-05-09 2008-12-11 Bayer Schering Pharma Aktiengesellschaft Antiandrogene Pyrrolidine mit tumorhemmender Wirksamkeit
US20050124625A1 (en) * 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
TW200628446A (en) 2004-12-14 2006-08-16 Takeda Pharmaceuticals Co Substituted pyrrole derivative
WO2009003077A1 (en) 2007-06-27 2008-12-31 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as modulators of nuclear hormone receptor function
MX2010002266A (es) 2007-08-30 2010-03-25 Takeda Pharmaceutical Derivados de pirazol sustituidos.
US8466171B2 (en) 2007-11-01 2013-06-18 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as modulators of nuclear hormone receptor function

Also Published As

Publication number Publication date
CA2813063A1 (en) 2012-04-26
EP2631233A4 (en) 2014-03-19
IL225395A0 (en) 2013-06-27
JPWO2012053630A1 (ja) 2014-02-24
AU2011318875A1 (en) 2013-05-02
BR112013009274A2 (pt) 2018-05-02
CN103180309A (zh) 2013-06-26
WO2012053630A1 (ja) 2012-04-26
TW201305130A (zh) 2013-02-01
EP2631233A1 (en) 2013-08-28
KR20130139979A (ko) 2013-12-23
MX2013004517A (es) 2013-06-03
US20130197009A1 (en) 2013-08-01

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