EA201390598A1 - Антагонист мутантного андрогенного рецептора - Google Patents
Антагонист мутантного андрогенного рецептораInfo
- 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
Links
- 102000001307 androgen receptors Human genes 0.000 title abstract 5
- 108010080146 androgen receptors Proteins 0.000 title abstract 5
- 239000005557 antagonist Substances 0.000 title 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 3
- 239000004480 active ingredient Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 241000699670 Mus sp. Species 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 239000003098 androgen Substances 0.000 abstract 1
- 229940030486 androgens Drugs 0.000 abstract 1
- 230000002280 anti-androgenic effect Effects 0.000 abstract 1
- 230000001093 anti-cancer Effects 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000035772 mutation Effects 0.000 abstract 1
- 230000035897 transcription Effects 0.000 abstract 1
- 238000013518 transcription Methods 0.000 abstract 1
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 or sparfloxacin
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
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.
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20140275105A1 (en) * | 2011-10-21 | 2014-09-18 | Astellas Pharma Inc. | Crystal of androgen receptor antagonistic compound |
EP2912194B1 (en) * | 2012-10-26 | 2019-05-08 | Memorial Sloan-Kettering Cancer Center | Androgen receptor variants and methods for making and using |
ES2798899T3 (es) * | 2013-02-25 | 2020-12-14 | Novartis Ag | Mutación novedosa del receptor de andrógenos |
US9682960B2 (en) | 2013-12-19 | 2017-06-20 | Endorecherche, Inc. | Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety |
JP2022549222A (ja) * | 2019-09-23 | 2022-11-24 | アキュター バイオテクノロジー インコーポレイテッド | アンドロゲン受容体分解活性を有する新規尿素およびその使用 |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2345146C (en) * | 1998-09-22 | 2010-02-23 | Yamanouchi Pharmaceutical Co., Ltd. | Cyanophenyl derivative |
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 |
WO2004007471A1 (ja) * | 2002-07-12 | 2004-01-22 | Yamanouchi Pharmaceutical Co., Ltd. | N−フェニル−(2r,5s)ジメチルピペラジン誘導体 |
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 |
CN101687881A (zh) | 2007-06-27 | 2010-03-31 | 百时美施贵宝公司 | 可用作核激素受体功能调节剂的稠合杂环化合物 |
KR20100046275A (ko) | 2007-08-30 | 2010-05-06 | 다케다 야쿠힌 고교 가부시키가이샤 | 치환 피라졸 유도체 |
WO2009059077A1 (en) | 2007-11-01 | 2009-05-07 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as modulators of nuclear hormone receptor function |
-
2011
- 2011-10-21 WO PCT/JP2011/074261 patent/WO2012053630A1/ja active Application Filing
- 2011-10-21 TW TW100138310A patent/TW201305130A/zh unknown
- 2011-10-21 EP EP11834469.6A patent/EP2631233A4/en not_active Withdrawn
- 2011-10-21 MX MX2013004517A patent/MX2013004517A/es unknown
- 2011-10-21 CN CN2011800505477A patent/CN103180309A/zh active Pending
- 2011-10-21 US US13/877,358 patent/US20130197009A1/en not_active Abandoned
- 2011-10-21 JP JP2012539778A patent/JPWO2012053630A1/ja active Pending
- 2011-10-21 EA EA201390598A patent/EA201390598A1/ru unknown
- 2011-10-21 CA CA2813063A patent/CA2813063A1/en not_active Abandoned
- 2011-10-21 AU AU2011318875A patent/AU2011318875A1/en not_active Abandoned
- 2011-10-21 BR BR112013009274-2A patent/BR112013009274A2/pt not_active IP Right Cessation
- 2011-10-21 KR KR1020137011626A patent/KR20130139979A/ko not_active Application Discontinuation
-
2013
- 2013-03-21 IL IL225395A patent/IL225395A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
EP2631233A4 (en) | 2014-03-19 |
US20130197009A1 (en) | 2013-08-01 |
MX2013004517A (es) | 2013-06-03 |
BR112013009274A2 (pt) | 2018-05-02 |
IL225395A0 (en) | 2013-06-27 |
KR20130139979A (ko) | 2013-12-23 |
WO2012053630A1 (ja) | 2012-04-26 |
CN103180309A (zh) | 2013-06-26 |
JPWO2012053630A1 (ja) | 2014-02-24 |
CA2813063A1 (en) | 2012-04-26 |
EP2631233A1 (en) | 2013-08-28 |
TW201305130A (zh) | 2013-02-01 |
AU2011318875A1 (en) | 2013-05-02 |
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