JP5130453B2 - 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性 - Google Patents

新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性 Download PDF

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JP5130453B2
JP5130453B2 JP2007558143A JP2007558143A JP5130453B2 JP 5130453 B2 JP5130453 B2 JP 5130453B2 JP 2007558143 A JP2007558143 A JP 2007558143A JP 2007558143 A JP2007558143 A JP 2007558143A JP 5130453 B2 JP5130453 B2 JP 5130453B2
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compound
compounds
diene
cyp17
mice
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JP2008536807A5 (enExample
JP2008536807A (ja
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ブローディー，アンジェラ
ヌジャー，ビンセント
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ユニバーシティ オブ メリーランド，ボルティモア
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    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2007558143A 2005-03-02 2006-03-02 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性 Active JP5130453B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US65739005P 2005-03-02 2005-03-02
US60/657,390 2005-03-02
PCT/US2006/007143 WO2006093993A1 (en) 2005-03-02 2006-03-02 Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity

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JP2012196525A Division JP5613206B2 (ja) 2005-03-02 2012-09-06 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性

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JP2008536807A JP2008536807A (ja) 2008-09-11
JP2008536807A5 JP2008536807A5 (enExample) 2012-10-25
JP5130453B2 true JP5130453B2 (ja) 2013-01-30

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JP2012196525A Active JP5613206B2 (ja) 2005-03-02 2012-09-06 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性

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US (1) US7875599B2 (enExample)
EP (2) EP2206719B1 (enExample)
JP (2) JP5130453B2 (enExample)
KR (1) KR101380959B1 (enExample)
CN (2) CN101155823A (enExample)
AT (1) ATE482969T1 (enExample)
AU (1) AU2006218711B2 (enExample)
BR (1) BRPI0607523A2 (enExample)
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EA (1) EA019560B1 (enExample)
ES (2) ES2528055T3 (enExample)
IL (3) IL185608A (enExample)
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NZ (1) NZ561571A (enExample)
PL (2) PL2206719T3 (enExample)
PT (2) PT1853619E (enExample)
SI (2) SI2206719T1 (enExample)
WO (1) WO2006093993A1 (enExample)
ZA (1) ZA200708106B (enExample)

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JP2012255026A (ja) * 2005-03-02 2012-12-27 Univ Of Maryland Baltimore 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性

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GB2454118B (en) 2007-06-06 2010-06-02 Univ Maryland Hdac inhibitors and hormone targeted drugs for the treatment of cancer
GB2470873A (en) * 2008-03-12 2010-12-08 Univ Maryland Androgen receptor inactivation contributes to antitumor efficacy of CYP17 inhibitors in prostrate cancer
US20100048913A1 (en) * 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
GB2470700B (en) * 2008-03-25 2012-08-08 Univ Maryland C-17 heteroaryl steroidal CYP17 inhibitors
US8785423B2 (en) * 2008-04-14 2014-07-22 University Of Maryland, Baltimore Compositions and methods of inducing endoplasmic reticulum stress response for the treatment of cell proliferative diseases
US20110190323A1 (en) 2008-08-28 2011-08-04 President And Fellows Of Harvard College Cortistatin analogues and syntheses thereof
CN102282133A (zh) * 2008-10-28 2011-12-14 生物马林药物股份有限公司 十氢-1h-茚并喹啉酮和十氢-3h-环戊并菲啶酮cyp17抑制剂
GB2479337A (en) * 2009-02-05 2011-10-05 Tokai Pharmaceuticals Inc Combination of a 17 alpha-hydroxylase/c17, 20-lyase inhibitor with an additional therapeutic agent
US8791095B2 (en) 2009-02-05 2014-07-29 Tokai Pharmaceuticals, Inc. Steroidal CYP17 inhibitors/antiandrogens
US20110312916A1 (en) * 2009-02-05 2011-12-22 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
SG176105A1 (en) 2009-06-26 2011-12-29 Novartis Ag 1, 3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17
US8791094B2 (en) * 2009-08-07 2014-07-29 Tokai Pharmaceuticals, Inc. Treatment of prostate cancer
BR112012012167A2 (pt) * 2009-11-13 2017-10-03 Tokai Pharmaceuticals Inc Metabólitos mamíferos de esteróides
US20110129423A1 (en) * 2009-11-30 2011-06-02 Frincke James M Anticancer compounds and screening method
CN103108871B (zh) 2010-09-16 2014-09-10 诺华股份有限公司 17α-羟化酶/C17,20-裂合酶抑制剂
RU2013132766A (ru) * 2010-12-16 2015-01-27 Байомарин Фармасьютикал Инк. Ингибиторы cyp11b, cyp17 и/или cyp21
US9029399B2 (en) 2011-04-28 2015-05-12 Novartis Ag 17α-hydroxylase/C17,20-lyase inhibitors
JP2014523445A (ja) * 2011-07-18 2014-09-11 トーカイ ファーマシューティカルズ，インク． 前立腺癌を処置するための新規な組成物及び方法
WO2013096907A1 (en) * 2011-12-22 2013-06-27 Tokai Pharmaceuticals, Inc. Methods and compositions for combination therapy using p13k/mtor inhibitors
KR20150127720A (ko) 2013-03-14 2015-11-17 유니버시티 오브 매릴랜드, 발티모어 안드로겐 수용체 하향 조절제 및 그의 용도
EP3514147B1 (en) * 2013-04-04 2022-08-03 University of Maryland, Baltimore Steroidal compounds with potent androgen receptor down-regulation and anti prostate cancer activity
EP3033088A4 (en) 2013-08-12 2017-03-08 Tokai Pharmaceuticals, Inc. Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
AU2014369834B2 (en) 2013-12-24 2018-12-20 President And Fellows Of Harvard College Cortistatin analogues and syntheses and uses thereof
CN103694299A (zh) * 2014-01-13 2014-04-02 中国药科大学 甾体类雄激素受体抑制剂、其制备方法及其医药用途
CN105732759A (zh) * 2015-01-29 2016-07-06 苏州晶云药物科技有限公司 (3β)-17-(1H-苯并咪唑-1-基)雄甾-5，16-二烯-3-醇的盐及其制备方法
WO2016182932A1 (en) 2015-05-08 2016-11-17 President And Fellows Of Harvard College Cortistatin analogues, syntheses, and uses thereof
EP3316889A4 (en) 2015-07-01 2018-11-14 President and Fellows of Harvard College Cortistatin analogues and syntheses and uses thereof
WO2017066697A1 (en) 2015-10-14 2017-04-20 Dou Qingping Treatments and diagnostics for cancers
IT201600121375A1 (it) * 2016-11-30 2018-05-30 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI 3ß-IDROSSI-17-(1H-BENZIMIDAZOL-1-IL)ANDROSTA-5,16-DIENE
RU2749134C1 (ru) * 2016-08-08 2021-06-04 Индустриале Кимика С.Р.Л. СПОСОБ ПОЛУЧЕНИЯ 3β-ГИДРОКСИ-17-(1Н-БЕНЗИМИДАЗОЛ-1-ИЛ)АНДРОСТА-5,16-ДИЕНА
IT201600083406A1 (it) * 2016-08-08 2018-02-08 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI 3β-IDROSSI-17-(1H-BENZIMIDAZOL-1-IL)ANDROSTA-5,16-DIENE
CA3087286C (en) 2018-02-13 2023-06-27 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase degraders and methods of use
EP3752518B1 (en) * 2018-02-13 2024-12-04 Dana-Farber Cancer Institute, Inc. Cyclin-dependent kinase inhibitors and methods of use
WO2021108581A1 (en) 2019-11-26 2021-06-03 Dana-Farber Cancer Institute, Inc. Potent and selective azaindole inhibitors of cdk8 and cdk19

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JP2012255026A (ja) * 2005-03-02 2012-12-27 Univ Of Maryland Baltimore 新規なｃ−１７−ヘテロアリールステロイドｃｙｐ１７阻害剤／抗アンドロゲン：合成、インビトロ生物活性、薬物動態および抗腫瘍活性

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DK1853619T3 (da) 2011-01-10
EA019560B1 (ru) 2014-04-30
EP1853619A1 (en) 2007-11-14
ES2528055T3 (es) 2015-02-03
US7875599B2 (en) 2011-01-25
KR101380959B1 (ko) 2014-04-04
EP2206719A2 (en) 2010-07-14
SI2206719T1 (sl) 2015-03-31
AU2006218711A1 (en) 2006-09-08
JP2012255026A (ja) 2012-12-27
PL1853619T3 (pl) 2011-03-31
ZA200708106B (en) 2008-12-31
IL185608A0 (en) 2008-01-06
HK1115387A1 (en) 2008-11-28
DE602006017175D1 (de) 2010-11-11
PT2206719E (pt) 2015-02-05
NZ561571A (en) 2009-09-25
BRPI0607523A2 (pt) 2009-09-08
CA2599953A1 (en) 2006-09-08
MX2007010593A (es) 2008-02-20
WO2006093993A1 (en) 2006-09-08
ATE482969T1 (de) 2010-10-15
CN101155823A (zh) 2008-04-02
ES2353413T3 (es) 2011-03-01
AU2006218711B2 (en) 2010-11-11
US20080280864A1 (en) 2008-11-13
EP1853619B1 (en) 2010-09-29
CN103349664A (zh) 2013-10-16
IL210478A0 (en) 2011-03-31
CA2599953C (en) 2013-08-13
AU2006218711A2 (en) 2006-09-08
IL210480A (en) 2015-06-30
IL185608A (en) 2016-06-30
DK2206719T3 (en) 2015-01-26
JP2008536807A (ja) 2008-09-11
PT1853619E (pt) 2011-01-03
EP1853619A4 (en) 2009-08-26
JP5613206B2 (ja) 2014-10-22
IL210480A0 (en) 2011-03-31
PL2206719T3 (pl) 2015-03-31
EP2206719A3 (en) 2011-01-05
SI1853619T1 (sl) 2011-01-31
KR20070120119A (ko) 2007-12-21
EP2206719B1 (en) 2014-10-22
EA200701872A1 (ru) 2008-06-30

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